Pine (Pinus spp.)

About the Pine Tree

The mighty pine tree is one of the most common trees on earth — making up close to 1% of the plant population of earth. They can be found thriving in both the coldest, and hottest environments on the planet.

All parts of the pine tree are used medicinally, and the wood is an importance source of lumbar for construction.

The leaves (needles) are an excellent source of vitamin A and C, the resin is a powerful antibacterial and carminative agent, the bark and pine nuts are highly nutritive, and the pollen is used as an analgesic, male tonic, and longevity-enhancement agent.

The pine tree is, and always has been an invaluable ally to humans.

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What Are Pine Trees Used For?

There are so many uses for the pine tree, it’s hard to list them all. The bark, needles, seeds, and pollen are incredibly nutritious, and the resin contains powerful antimicrobial and vulnerary compounds.

Humans have been using the pine tree as food and medicine for thousands of years in almost every Northern culture on earth. Many of the traditional medical uses for pine trees still stand today — but have become less popular over other more exotic herbs.

A common theme with herbal medicine is that it’s usually the least interesting, most common plant species that have the most to offer. Yet we’re always looking for that new exotic herb or supplement to use instead.

The most popular use of the pine tree today is in the form of topical salves made from the resin and male tonic supplements made from the pine pollen. Pine nuts are also a common source of nutrition you can pick up at any grocery store.

The needles and bark are also exceptionally nutritious and can be made into a tea or decoction (respectively) to support general health, as well as treating debility, fatigue, and nutritional deficiencies.

+ Pine Needle Uses

Pine needles make for an excellent tea. They're rich in vitamin A, Vitamin C, and a host of medicinal essential oils.

Pine needle tea is great for supporting the immune system, releasing phlegm from the lungs, easing a sore throat, curbing gas and bloating, or warming up on a cold winter hike.

An infusion of the needles can also be applied topically to the skin as an antimicrobial and vulnerary.

Fresh needles collected in the spring can be eaten raw and add a pleasant "piney" or "rosemary" flavor to the dish. You can also infuse these fresh pine sprigs with honey or butter.

A tincture can be made from the needles using a high alcohol menstrum (at least 95%). Use, sparingly.

+ Pine Resin Uses

Pine resin seeps out of cuts and scratches of the tree — it's used to seal the wounds and prevent infection. As a result, it's no surprise this pine resin has exceptional antimicrobial properties. It's insecticidal, anti-fungal, and antibacterial.

The resin makes for an excellent addition to topical salves designed to speed wound healing.

You can also make or buy tinctures of pine resin using a high-proof alcohol as the solvent. These are useful for releasing phlegm from the lungs and eliminating gas and bloating from the digestive tract. However, use it sparingly as the resin can be irritating to the GI tract in high amounts.

+ Pine Pollen Uses

Pine pollen has a long history of use in Asia for promoting strength and male virulity. High-proof extracts of the pollen are used by older men to maintain testosterone levels. There's a lot of promise for this effect in the scientific literature (more on this later) — but it's important to note that pine pollen is not an anabolic steroid and can't be used to boost testosterone in younger men. It only appears to work if testosterone levels are low to begin with.

Outside male virility, pine pollen is an excellent nutritional supplement for men and women alike. It's rich in the amino acids, minerals, and vitamins required for optimal health.

+ Pine Bark Uses

Pine bark is rich in vitamin C and A and a few unique medicinal components. The bark can be decocted to make a strong bitter tea with a host of medicinal benefits. Some herbalists use the bark for heart disease, varicose veins, clotting disorders, and cancer.

+ Pine Nut Uses

Pine nuts, like the rest of the pine tree, are very nutritious. They're rich in vitamins B1, B2, B6, E, C, D2, D3, and A.

Pine nuts are also rich in nicotinamide, folic acid, B-carotin, potassium, sodium, calcium, magnesium, phosphorus, iron, manganese, copper, zinc, and selenium — to name a few.

Traditional Uses of Pine Trees

Anybody living in proximity to these common forest plants (especially in Northern climates) have developed a set of uses for the herb — many of which are the same all over the world.

The pine tree has been used for coughs, allergies, urinary tract infections, sinus infections, skin infections, debility, joint pain, inflammatory diseases, immune deficiencies, scurvy, and much more.

Native American tribes used the pine tree as an important source of nutrition during the winter months — consuming the nuts, bark, and needles of the pine tree.

Early explorers to reach North America from Europe eventually started using pine needle tea to ward off scurvy.

There are countless uses for this impressive tree as well when you consider its nutritive benefits. Almost any medical condition can stand to benefit from optimal nutrition, which explains why the tree has been used in traditional medicines for almost any cause of debility.

The resin was also considered a valuable ingredient in topical salves for skin conditions, infections, and insect bites.

The boughs of the pine tree were used as an insect-repellant bedding to eliminate common pests like bedbugs or fleas.

Herb Details: Pine Trees

Herbal Actions:

• Analgesic
• Anti-Inflammatory
• Anticholesterolaemic
• Astringent
• Carminative
• Male Tonic
• Nutritive
• Respiratory Tonic

Relevant Species:

• Pinus edulis
• Pinus ponderosa
• Pinus aristata
• Pinus strobus
• Pinus contorta
• Pinus strobus
• Pinus sylvestris

Dosages

• Pine Pollen — 1.5 grams two-three times per day
• View Dosage Chart

Part Used

Needles, inner-bark, pollen, seeds, resin

Family Name

Pinaceae

Distribution

Temperate forests around the world

Constituents of Interest

• a-terpenol
• Linalool
• Caryophyllene
• Eugenol

Common Names

• Pine
• Scot's Pine
• Scotch Pine
• Logepole Pine
• Jack Pine

CYP450

• Unknown

Pregnancy

• Topical applications of pine resin, as well as pine needle tea is safe to use during pregnancy — however, avoid pine pollen or pine resin tinctures while pregnant.

Duration of Use

• Long-term use of all parts of this plant is acceptable

Botanical Information

The Pinus genus consist of roughly 144 different species of coniferous trees. It’s one of the oldest plants on earth — dating back at least 200 million years.

Pine trees are incredibly common, they’re found on every continent, and dominate forests in the Norther hemisphere. One report suggests the humble pine tree makes up about 1% of the entire plant population of earth.

No matter where you go in the northern Hemisphere, you’re likely to find pine trees a permanent member of the landscape. However, if you look more closely, different regions are home to a specific species of pine tree.

Harvesting & Preparation

All parts of the pine tree can be used medicinally. The leaves make a nutritious tea, the bark can be decocted into a strong tea, the resin can be made into antimicrobial salves, and the pollen can be supplemented as a male tonic.

Different parts of the tree should be harvested in different seasons:

1. Pine Pollen — the pine tree only releases its pollen in the early spring or summer. Each tree releases an ton of it. Collect it by placing bags over the catkins and giving it a shake.

2. Pine Needles — these can be harvested anytime, but spring is the best in order to get the young growth. Newer growth has a much better taste and higher terpene concentrations.

3. Pine pitch (resin) — This part can be harvested all year. I like to harvest it in the winter when it’s extra hard as I find this easier to collect in chunks rather than making a sticky mess of evertthing when the resin is still gooey.

4. Pine Bark — You can collect this part of the tree anytime of the year. I find it best in the spring, summer.

Pharmacology & Medical Research

+ Antinociceptive (Pain-Reduction)

In animal studies, an ethanol extract of pine pollen (100 and 200 mg/kg orally) produced significant inhibition of both pain transmission and inflammation compared to the control group [1]. (Species tested (Pinus densiflora).

+ Anticholesterolaemic

The needles of pine trees (Pinus morrisonicola) has been shown to inhibit copper-induced low-denisty lipoproteins (LDL) oxidation [2]. The study involved four different solvent extracts, but the ethyl acetate extract showed the greatest antioxidant activity overall.

+ Anti-Inflammatory

Several studies have shown different parts of the pine tree to have anti-inflammatory effects on various inflammatory enzymes and messenger molecules.

The needles were shown to possess COX-2 inhibitory activities in animal models [2].

+ Longevity

One of the longest-running applications of the pine pollen — dating back thousands of years in China — was for promoting long-life. This was especially true in men, where the pollen was used to delay the effects of aging, and sustain male virility long into old age. In traditional Chinese medicine, pine pollen is considered a jing tonic. Jing is a term used to describe “life essence” — it’s essentially our virility. When jing runs out, we die. Chinese medicine considers pine pollen a tonic for the lungs, kidneys, heart, spleen, and liver — all five major organs in the Chinese medical system.

The modern term for this effect is an adaptogen — something that improves our ability to resist both internal and external stresses and maintain homeostasis (balance).

In order to offer such broad benefits to the body, pine pollen must act on a central regulatory system. Some herbs, such as ginseng do this by acting on the hypothalamus — which is the region in the brain that manages homeostasis within the body. Other herbs, like cannabis achieve this by boosting the effects of a regulatory system called the endocannabinoid system.

A study published in 2012 looked at the potential anti-aging effects of pine pollen [3]. The study injected mice with D-galactose — which is a compound used to induce premature aging by increasing the formation of advanced glycation end-products (AGEs). Pine pollen extract was found to hinder the production of AGE at doses between 500 and 1500 mg/kg. This effect was noted to be comparable in effects to 100mg/kg aminoguanidine — a well-known longevity-enhancement medication through AGE pathways.

+ Testosterone

There was a study published in 2013 that showed black pine tree pollen (Pinus nigra) contained epi-testosterone, as well as a handful of other androgenic compounds (5α-androstane-3α,17β-diol, 5β-androstane-3α,17β-diol and etiocholanolone) [1]. The problem is that the testosterone levels contained in pine pollen were so insignificant it was unrealistic to expect any change in testosterone levels for those taking the supplement. It’s estimated that 10 grams of pine pollen contains about 0.8 micrograms of testosterone [4].

To put this in perspective, the usual dose of injectable testosterone is over 100 mg. This is an injectable form of testosterone too — which has 100% absorption rate. Oral ingestion of testosterone has significantly less absorption — closer to 3 –7%.

While you can’t use pine pollen as a natural source of testosterone, it does offer improvements to testosterone levels in older men through alternate mechanisms.

The improvement in male health and libido after using pine pollen is most likely a combination of its potent nutritional profile and anti-inflammatory benefits. Pine pollen is particularly rich in amino acids like nicotinic acid and pantothenic acid — both of which have been shown to play a major role in the function of the testes where testosterone is produced.

The benefits of pine pollen on testosterone levels are most notable in older men experiencing the natural drop-off of testosterone levels. There’s no evidence to suggest pine pollen can boost testosterone levels in healthy, younger men.

Phytochemistry

The entire pine tree is a rich source of nutrition. The bark, leaves, and pollen are all high in vitamins and minerals, while the resin is particularly rich in terpenes and other volatile compounds.

+ Pine Pollen Constituents:

Amino acids, riboflavin, nicotinic acid, pantothenic acid, pyridoxine, biotin, inositol, folic acid, vitamin D2, vitamin D3. Some species (Scot’s pine — Pinus sylvestrus) has been found to contain testosterone, epitestosterone, and androstenedione — however, the concentrations are too low to reasonably offer any direct benefits through supplementation. The male tonic effects of pine pollen are primarily the result of other compounds, rather than from the androgens themselves.

+ Pine Resin Constituents

Abietic acid, dehydroabietic acid, elliotic acid, isopimaric acid, levopimaric acid, palustric acid, pimaric acid, sandaracopimaric acid, strobinic acid, volatile oils.

+ Pine Needle Constituents

Leucocyanidin, neoabietinic acid, pinosylvin monomethyl ester, strobic acid, antioxidants, volatile oils including α-terpineol (30.2%), linalool (24.47%), limonene (17.01%), anethole (14.57%), caryophyllene (3.14%), and eugenol (2.14%).

+ Pine Bark Constituents

Abietic acid, cis-abienol, leucocyanidin, neoabietinic acid, pinosylvin, monomethyl ester, strobic acid, volatile oils.

Cautions & Safety Information:

All pine species are considered safe. There is one species of tree that resembles the pine tree — the yew tree — which is toxic. The yew tree can be differentiated by the smaller, flat needles and little red berries.

The pollen of the pine tree is a common cause for allergy — take with caution when using pine pollen for the first time to ensure there are no allergic reactions.

Be careful when using tinctures of the pine resin to avoid causing gastrointestinal irritation. Start with a very low dose before increasing gradually once you get a feel for how it affects you directly.

Author:

Justin Cooke, BHSc

The Sunlight Experiment

(Updated March 2020)

Recent Blog Posts:

Popular Herbal Monographs

References:

[1] — Choi, E. M. (2007). Antinociceptive and antiinflammatory activities of pine (Pinus densiflora) pollen extract. Phytotherapy Research, 21(5), 471-475.

[2] — Yen, G. C., Duh, P. D., Huang, D. W., Hsu, C. L., & Fu, T. Y. C. (2008). Protective effect of pine (Pinus morrisonicola Hay.) needle on LDL oxidation and its anti-inflammatory action by modulation of iNOS and COX-2 expression in LPS-stimulated RAW 264.7 macrophages. Food and chemical toxicology, 46(1), 175-185.

[3] — Mao, G. X., Zheng, L. D., Cao, Y. B., Chen, Z. M., Lv, Y. D., Wang, Y. Z., ... & Yan, J (2012). Antiaging effect of pine pollen in human diploid fibroblasts and in a mouse model induced by D-galactose. Oxidative medicine and cellular longevity, 2012.

[4] — Chamawan, P., Thisayakorn, K., & Phornchirasilp, S. (2017). Effects of Pine Pollen Extract in Relieving Hot Flushes in Sex Hormone-Deficienct Rats. Thai Journal of Pharmacology, 39(1), 19-37.

Black Horehound (Ballota nigra)

What is Black Horehound?

Black horehound is best known for its offensive odour — which resembles stale sweat.

Despite the unfortunate smell of this mint-relative, it has a lot to offer therapeutically.

Black horehound is one of the oldest medicinal herb species from Europe. It has a long history of use for infectious diseases including rabies and parasites, as well as for nausea and vomiting caused by neurological disorders.

This herb is a bit of a jack of all trades — but master of none. It offer reliable nervine, antispasmodic, antimicrobial, and anticholesterolaemic effects — all thanks to five unique phenylpropanoid glycosides contained in the leaves, stems, and roots of the herb.

What is Black Horehound Used For?

Many of the tradition uses of the herb have yet to be validated. The primary traditional uses for the herb that still stand today are for treating motion sickness or other causes of nausea or vomiting of neurological origin.

This herb is also still used as an antimicrobial for the digestive tract and topically on the skin.

Newer applications for the herb are aimed towards high cholesterol levels and diabetes.

Traditional Uses of Black Horehound

Black horehound was used for a lot of different applications. It was also a common remedy for motion sickness or any vomiting caused by neurological origins (rather than digestive).

Topically, the leaves were used to treat wounds, burns, and infection. Some herbalists even gave the herb as an enema for parasitic worms.

In Europe, where the herb originated from, the flowering tops were used to treat rabies after getting bitten by a rabid dog.

Herb Details: Black Horehound

Herbal Actions:

• Antibacterial
• Anticholesterolaemic
• Antiemetic
• Antifungal
• Antioxidant
• Antiprotozoal
• Antispasmodic
• Expectorant
• Hypoglycaemic
• Nervine
• Sedative

Weekly Dose

• (1:2 Liquid Extract)
  10 20 mL
• View Dosage Chart

Part Used

Flowering Tops

Family Name

Lamiaceae

Distribution

Europe & North America

Constituents of Interest

• Verbascoside
• Forsythoside B
• Arenarioside
• Ballotetroside
• Malic Acid

Common Names

• Black Horehound
• Black Stinking Horehound
• Fetid Horehound
• Stinking Roger

CYP450

• Unknown

Pregnancy

• Avoid black horehound if pregnant or breastfeeding

Duration of Use

• insert

Botanical Information

Black horehound originated from Europe but is now widespread across North America as well. The herb can grow over 1 meter tall and tends to grow on the side of the road in rural areas.

What this plant is best known for is its disagreeable odor — which can be described as stale sweat. The Greek name, ballo translates to “getting rid of”, or “throwing away”. This smell protects the herb by repelling both animals and humans.

Pharmacology & Medical Research

+ Anticholesterolaemic

One of the major causes of atherosclerosis is the result of oxidization of low-density lipoproteins LDL) [1].

Some of the phenolic compounds in black horehound (verbascoside, forsythoside B, arenarioside, and ballotetroside) were found to inhibit LDL oxidation through Cu2+ pathway [2].

+ Antimicrobial

Five phenolic compounds from black horehound were investigated to explore their antimicrobial potential. Of these five, three (verbascoside, forsythoside B, arenarioside) were found to have moderate activity against Proteus mirabilis, Salmonella typhi, and Staphylococcus aureus [3, 4].

Another study looked at the antimicrobial effects of each part of the plant (leaves, roots, and stems). The results suggested the crude extract of the roots had the best inhibitory activity on the strains tested (Enterococcus faecalis, Escherichia coli, Klensiella pneumonia, Proteus miribalis, Salmonella typhi, and Staphylococcus aureus, Aspergillus fumigates, Aspergillus niger, Fusarium solani, and Leishmania) [5]. The leaf and stem chloroform extracts had similar antimicrobial action.

+ Sedative

Phenylpropanoid compounds from black horehound were found to bind to benzodiazepine, dopaminergic, and morphinic receptors in animals [6, 4]. This provides a mechanism of action for the traditional sedative uses of the herb — but more research is needed to further elucidate these findings.

Phytochemistry

The flowering tops (the part used medicinally) are rich in diterpenoid lactones (labdane type) — such as ballotenol, ballotinone, 7alpha-acetoxymarrubiin, hispanolone, and preleosibirin.

The tops are also rich in phenolic compounds (luteolin-7-lactate, luteolin-7-glucosyl-lactate), phenylpropanoid glycosides (verbascoside, forsythoside B, arenarioside, ballotetroside), organic acids (quinic acid), and volatile oils.

Cautions & Safety Information:

Black horehound is considered a safe herb, with little chances of experiencing any side effects.

Allergies to the herb have been noted, so caution is advised if using the herb for the first time. Always start with a small amount first to see how you react before using a full dose.

Black horehound may interact with the following medication classes:

• Antipsychotic medications (overlap in receptor activation)

• Anti-Parkinson’s disease medications (overlap in dopaminergic action)

• Sedatives (overlap in sedative effects and benzodiazepine receptor activation)

• Iron supplements (black horehound has been suggested to prevent the absorption of iron)

Author:

Justin Cooke, BHSc

The Sunlight Experiment

(Updated March 2020)

Recent Blog Posts:

Featured Herb Monographs

References:

[1] — Steinberg, D. (1997). Low density lipoprotein oxidation and its pathobiological significance.

[2] — Seidel, V., Verholle, M., Malard, Y., Tillequin, F., Fruchart, J. C., Duriez, P., ... & Teissier, E. (2000). Phenylpropanoids from Ballota nigra L. inhibit in vitro LDL peroxidation.

[3] — Didry, N., Seidel, V., Dubreuil, L., Tillequin, F., & Bailleul, F. (1999). Isolation and antibacterial activity of phenylpropanoid derivatives from Ballota nigra.

[4] — Al-Snafi, A. E. (2015). The Pharmacological Importance of Ballota nigra–A review.

[5] — Ullah, N., Ahmad, I., & Ayaz, S. (2014). In vitro antimicrobial and antiprotozoal activities, phytochemical screening and heavy metals toxicity of different parts of Ballota nigra.

[6] — Daels-Rakotoarison, D. A., Seidel, V., Gressier, B., Brunet, C., Tillequin, F., Bailleul, F., ... & Cazin, J. C. (2000). Neurosedative and antioxidant activities of phenylpropanoids from Ballota nigra.

Astragalus (Astragalus membranaceus)

What is Astragalus?

Astragalus (aka milkvetch) is a member of the legume family — which makes it a relative of peanuts, peas, and soy.

This medicinal herb is common in both Western and Eastern herbal medicine. It has a long history of use for immune-related conditions for conditions of immune-excess (such as autoimmunity) as well as deficiency (during infection or immunodeficiencies).

Today, the most common use of the herb if for its benefits on immunity and cardiotonic. Astragalus supplements are used as a prophylaxis for infection (especially of the respiratory tract), and as a daily tonic for promoting overall vitality and stamina.

What is Astragalus Used For?

Astragalus has many uses as a respiratory tonic, but the most common application of the herb in modern herbal medicine is for boosting or modulating the immune system.

It’s popular for use with various forms of immunodeficiency, including viral and bacterial infection (prophylaxis), and as an adjunctive cancer treatment.

The immune-boosting effects of this herb isn’t one-directional — astragalus is also useful for immune excess, such as with autoimmunity or allergic reaction.

Many people use astragalus as a general health supplement for preventing cold or flu, or to enhance cardiovascular function, vitality, and overall stamina.

Other uses include, hepatitis, diarrhea, hypertension, diabetes, and Lyme Disease (not late stage).

Herb Details: Astragalus

Herbal Actions:

• Adaptogen
• Antioxidant
• Antiviral
• Cardiotonic
• Diuretic
• Hepatoprotective
• Hypotensive
• Immunomodulator
• Immune Stimulant

Dosage

• (1:1 Liquid Extract)
  20 – 40 mL
• View Dosage Chart

Part Used

• Root

Family Name

• Leguminosae

Distribution

• Eastern Asia

Constituents of Interest

• b-Glucans
• Astragalosides
• Formononetin
• Gamma-aminobutyric acid

Common Names

• Astragalus
• Milk-Vetch Root
• Huang Qi (China)
• Hwanggi (Korea)
• Ogi (Japan)

CYP450

• Unknown

Quality

• Warm and moist

Pregnancy

• No reported side effects during pregnancy — but not proven safe either.

Taste

• Sweet

Duration of Use

• Long-term use is acceptable with periodic breaks.

Botanical Information

Astragalus is a large genus containing over 3000 individual species. All species within this genus are either small, herbaceous plants, or mid to large shrubs.

The astragalus genus is a member of the legume family — making it a close relative of peas, peanuts, and soy bean.

The primary species used as medicine is Astragalus membranaceus, which originated from Eastern Asia in mountainous regions of China and Mongolia, but have since spread all over the world.

Pharmacology & Medical Research

Longevity

An extract of a closely-related species, Astragalus membranaceus (synonym A. propinquus), called TA-65 was shown to activate telomerase [3] — which is one of the primary targets for longevity-enhancement medications.

Phytochemistry

Astragalus is rich in saponins (such as cycloastragenol and astragalosides), polysaccharides (astroglucans A-C), flavonoids, phytosterols, volatile oils, asparagine, choline, betaine, gluconic acid, beta-sitosterols, amino acids (including GABA), trace elements (zinc, copper, magnesium, manganese, calcium, potassium, sodium, cobalt, rubidium, molybdenum, chromium, vanadium, tin, and silver).

Cautions & Safety

Astragalus is widely considered a safe herb, even over long periods of time or in high doses.

Traditional medical systems (such as TCM) suggest you should avoid using the herb at the acute onset stage of respiratory or sinus infection — focusing instead on using the herb before or after infection takes place. TCM also suggests avoiding the use of astragalus with signs of heat or yin deficiency.

This herb is contraindicated during the later stages of lyme disease.

Astragalus should be avoided in combination with immunosuppressive medications and after organ transplant.

Author:

Justin Cooke, BHSc

The Sunlight Experiment

Recent Blog Posts:

Popular Herbal Monographs

References

Cryptolepis (Cryptolepis sanguinolenta)

What is Cryptolepis?

Cryptolepis is a potent antibmicrobial herb originating from Africa and Southeast Asia. It’s become one of the go-to herbal species for treating resistant bacteria and malaria.

The active constituents of the plant are a group of alkaloids, each of which have been proven effective against a wide variety of bacterial, mycobacterial, fungal, and parasitic organisms (specific strains listed below).

The roots also contain a rich yellow pigment that makes the herb useful for dying fabrics and leather a deep yellow color.

What is Cryptolepis Used For?

Cryptolepis is almost exclusively used as an antimicrobial against parasitic, bacterial, amoebic, and fungal infections. This herb is very useful for infections of all kinds. It’s a popular herb for digestive disorders and infection, topically for skin infections, or orally for urinary tract infections.

Outside of medicine cryptolepis is used as a source of yellow dye — lending to one of its common names, yellow dye root.

Brewing a Decoction of Cryptolepis

Traditional Uses of Cryptolepis

+ Africa

Cryptolepis originates from Africa, where it was primarily used to treat malaria, amoebic dysentery, and both urinary and respiratory infection.

The herb’s success with malaria patients is what made the plant so popular today, and there is now large plots of land dedicated to its cultivation to meet the demand for the herb within Africa, as well as elsewhere in the world.

+ Asia & Indonesia

A closely related species — Cryptolepis buchanii — grows throughout Indonesia, Thailand, China, India, and Nepal.

This species was used in Thailand for treating systemic inflammation, arthritis, and muscle pain.

In India, this species was used to treat diarrhea, bacterial infection, ulcers, and for treating rickets in children.

Herb Details: Cryptolepis

Herbal Actions:

• Antiamoebic
• Antibacterial
• Anticancer
• Antifungal
• Anti-inflammatory
• Antiparasitic
• Antipyretic
• Antiviral (Mild)

Weekly Dose

• (1:2 Liquid Extract)
  30 100 mL
• View Dosage Chart

Part Used

Roots

Family Name

Apocynaceae

Distribution

Africa & Southeast Asia

Constituents of Interest

• Cryptolpine
• Norcyptolepine
• Cryptospirolepine
• Isocryptolepine

Common Names

• Cryptolepis
• Yellow Dye Root
• Delboi
• Gangamau
• Ghanian Quinine
• Kadze
• Koli Mekari
• Kpokpo-Yangolei
• Nibima
• Nombon
• Nurubima
• Ouidoukoi
• Paran Pupa

CYP450

• Unknown

Pregnancy

• Avoid cryptolepis if pregnant or breastfeeding

Duration of Use

• High-dose use of cryptolepis (4-6mL per day) should be limited to 60 days. Low-doses (1-2 mL per day) is considered safe for long-term use.

Botanical Information

Cryptolepis is a member of the Apocynaceae (dogbane) family — which contains roughly 348 genera of trees, shrubs, vines, and herb succulents. members of this family can be found throughout the tropics.

Another notable species in this family is Vinca major (periwinkle)

Most of the species in this family grow in dense tropical rainforests, but a select few prefer harsh, dry environments — including cryptolepis, which prefers dry savanah forests. You’re more likely to find the herb growing near a source of water, however.

You can find cryptolepis wild in dry grassy or forested regions from Senegal east to Nigeria. The plant can also be found sporatically in Camaroon and the Congo.

Some related species grow in Australia as well.

Within the cryptolepis genus there are roughly 42 species — with the primary studied species being Cryptolepis sanguinolenta.

Cultivation, Harvesting & Preparation

Both the roots and stems of the plant have been used as medicine, but the roots contain nearly twice as much of the active alkaloids than the stem — so most people tend to just use the roots instead.

Pharmacology & Medical Research

+ Antibacterial

Cryptolepis is well-known for its antibacterial activity — and is considered by many herbalists to be one of the most reliable systemic antimicrobial herbs available.

Cryptolepis has been tested agains many different strains of bacteria, amoeba, fungi, parasites, and virus.

The most active inhibitory effects of the herb are towards bacteria and parasites, with mild anti-fungal and antiviral activity.

These alkaloids work by inhibiting growth, breaking down cell membranes (lysis), causing morphological changes to the cell, and direct bactericidal activities [1, 2, 3].

One study in particular tested the effects of various cryptolepis extracts (water, ethanol, petroleum ether, chloroform, and ethyl acetate extracts) agains antibiotic-resistant bacteria [1]. The herb was effective agains 75% of the strains tested.

The study found cryptolepis extracts to be effective against the following bacteria:

• Staphylococcus saprophyticus

• Staphylococcus aureus

• Salmonella typhi

• Proteus mirabilis

• Excherichia coli

• Proteus mirabilis

• Pseudomonas aeruginosa

• Klebsiella pneumoniae

Cryptolepis has also been shown to inhibit other organisms, including:

• Neisseria gonorrhoeae [4]

• Shigella dysenteriae [2]

• Salmonella typhimurium [2]

• Vibrio cholerae [2]

• Enterococcus faecalis [2]

• Campylobacter jejuni (65 strains) [5]

• Campylobacter coli (41 strains) [5]

• Bacillus cerues [7]

• Streptococcus pyogenes [7]

• Enterobacter cloacae [7]

• Klebsiella pneumonia [7]

• Proteus vulgaris [7]

• Mycobacterium fortuitum [6]

• Mycobacterium phlei [6]

• Mycobacteriumaurum [6]

• Mycobacterium smegmatis [6]

• Mycobacterium bovis [6]

• Mycobacterium abcessus [6]

The herbs effectiveness agains Escherichia coli, Proteus miribalis, and Staphylococcus saprophyticus provide a mechanism of action for the herbs traditional uses for urinary tract infection.

it should be noted that in most of the studies cited above, the ethanolic extract was by far the most effective. Water extracts were the least effective overall unless decocted for several hours.

+ Antifungal

Many of the same alkaloids active agains bacterial strains are also effective agains fungal infection.

Cryptolepine and neocryptolepine have both been shown to have antifungal activity against the following species:

• Candida albicans [7]

• Aspergillus niger [4]

• Microsporum canis [7]

• Epidermophyton floccosum [7]

• Trichopyton rubrum [7]

• Trichopyton mentagrophytes [7]

• Saccharomyces cerevisiae [7]

+ Anti-Parasitic

This herb has a long history of use for malaria and other parasitic infections. As a result, there’s ben a lot of study to elucidate these effects further.

A preclinical trial using an aqueous extract of the root found the herb, as well as isolated fractions of cryptolepine and isocryptoleopine had direct antiplasmoidial activity [8]. I’s important to note that all strains of plasmodium falciparum used in this study were already resistant to chloroquine — suggesting alternate mechanisms for cryptolepine and isocryptolepines antimalarial effects.

These results have been replicated at least four more times using different alkaloid fractions of the plant, different administration methods (injection), and different strains of plasmodium — all showed varying levels of improvement from the application of cryptolepis [8, 9, 10].

One study noted a synergistic effect against plasmodium falciparum and Plasmodium berghei with artimisinins — which is a compound found in the Artemesia annua (Qing Hao). These same results were noted from a semi-synthetic analog of artemisinin called artesunate without producing any toxic side effects. [11].

Clinical Trials

In one trial [12], 44 patients with uncomplicated malaria were given cryptolepis root tea (2.5 gram equivalent) three times per day for five days. The effects were considered positive if the parasites were undetectable in the blood by day seven, and remained undetectable at a 28 day followup.

By the end of the study, 50% of patients were considered cleared of malaria after 2 days of treatment. Chills, vomiting, and nausea were cleared in all patients by day three. By the end of the trial, 93.5% of patients had undetectable levels of plasmodium in the blood, and no symptoms. These improvements are consistent with the pharmaceutical application chloroquine.

Phytochemistry

The primary group of medicinal compounds in cryptolepis are the alkaloids. The primary active alkaloids in the herb include:

• Cryptolepine (the primary bioactive compound)

• Norcryptolepine

• Cryptospirolepine

• Isocryptolepine

• Hydroxycryptolepine

• Cryptoheptine

• Biscryptolepine

• Neocryptolepine

• Cryptoquindoline

The primary active ingredient is cryptolepine — which is also the primary ingredient in another well-known systemic antimicrobial plant, Sida (Sida acuta).

Cryptolepine is an indoloquinoline alkaloid with significant antimicrobial activity. This compound has been shown to have direct antimalarial, antibacterial, anticancer, antipyretic, and anti-inflammatory activities [2, 13, 14, 15].

A separate alkaloid, cryptohepine, has also been shown to posess significant antibacterial activity against both gram-negative and gram-positive bacteria [5, 20]. Other alkaloids including neocryptolepine and biscryptolepine have also shown activity agains gram-positive bacteria, but aren’t as well studied as cryptohepine or cryptolepine. Neocryptine is reported to provide more bacteriostatic activity than bacteriocidal [7].

Cautions & Safety Information:

Cryptolepis has been used for thousands of years without any evidence of toxic side effects. One clinical trial gave patients 80 mL of cryptolepis extract for six days (a very high dose), with no side effects reported [16].

in rats, the LD50 of cryptolepis was over 5000 mg/kg — an incredibly potent dose [17, 18].

Some mild side effects have been noted when using isolated cryptolepis alkaloids that aren’t noted in whole-plant extracts. Side effects from this may include a rise in ALP and uric acid [12].

One animal study found cryptolepis leaf extract resulted in a decreased sperm count in rats [19].

Avoid using cryptolepis in combination with antidiabetic medications and central nervous system depressants (such as phenobarbitone).

Author:

Justin Cooke, BHSc

The Sunlight Experiment

(Updated March 2020)

Recent Blog Posts:

Featured Herb Monographs

References:

[1] — Mills-Robertson, F. C., Tay, S. C., Duker-Eshun, G., Walana, W., & Badu, K. (2012). In vitro antimicrobial activity of ethanolic fractions of Cryptolepis sanguinolenta. Annals of clinical microbiology and antimicrobials, 11(1), 16.

[2] — Paulo, A., Duarte, A., & Gomes, E. T. (1994). In vitro antibacterial screening of Cryptolepis sanguinolenta alkaloids. Journal of ethnopharmacology, 44(2), 127-130.

[3] — Sawer, I. K., Berry, M. I., & Ford, J. L. (2005). The killing effect of cryptolepine on Staphylococcus aureus. Letters in applied microbiology, 40(1), 24-29.

[4] — Boakye-Yiadom, K. (1979). Antimicrobial properties of some West African medicinal plants II. Antimicrobial activity of aqueous extracts of Cryptolepis sanguinolenta (Lindl.) Schlechter. Quarterly Journal of Crude Drug Research, 17(2), 78-80.

[5] — Paulo, A., Pimentel, M., Viegas, S., Pires, I., Duarte, A., Cabrita, J., & Gomes, E. T. (1994). Cryptolepis sanguinolenta activity against diarrhoeal bacteria. Journal of ethnopharmacology, 44(2), 73-77.

[6] — Gibbons, S., Fallah, F., & Wright, C. W. (2003). Cryptolepine hydrochloride: a potent antimycobacterial alkaloid derived from Cryptolepis sanguinolenta. Phytotherapy Research, 17(4), 434-436.

[7] — Cimanga, K., De Bruyne, T., Pieters, L., Totte, J., Tona, L., Kambu, K., ... & Vlietinck, A. J. (1998). Antibacterial and antifungal activities of neocryptolepine, biscryptolepine and cryptoquindoline, alkaloids isolated from Cryptolepis sanguinolenta. Phytomedicine, 5(3), 209-214.

[8] — Grellier, P., Ramiaramanana, L., Millerioux, V., Deharo, E., Schrével, J., Frappier, F., ... & Pousset, J. L. (1996). Antimalarial activity of cryptolepine and isocryptolepine, alkaloids isolated from Cryptolepis sanguinolenta. Phytotherapy Research, 10(4), 317-321.

[9] — Cimanga, K., De Bruyne, T., Pieters, L., Vlietinck, A. J., & Turger, C. A. (1997). In vitro and in vivo antiplasmodial activity of cryptolepine and related alkaloids from Cryptolepis sanguinolenta. Journal of natural products, 60(7), 688-691.

[10] — Whittell, L. R., Batty, K. T., Wong, R. P., Bolitho, E. M., Fox, S. A., Davis, T. M., & Murray, P. E. (2011). Synthesis and antimalarial evaluation of novel isocryptolepine derivatives. Bioorganic & medicinal chemistry, 19(24), 7519-7525.

[11] — Forkuo, A. D., Ansah, C., Boadu, K. M., Boampong, J. N., Ameyaw, E. O., Gyan, B. A., ... & Ofori, M. F. (2016). Synergistic anti-malarial action of cryptolepine and artemisinins. Malaria journal, 15(1), 89.

[12] — Bugyei, K. A., Boye, G. L., & Addy, M. E. (2010). Clinical efficacy of a tea-bag formulation of Cryptolepis sanguinolenta root in the treatment of acute uncomplicated falciparum malaria. Ghana medical journal, 44(1).

[13] — Ntie-Kang, F., Lifongo, L. L., Simoben, C. V., Babiaka, S. B., Sippl, W., & Mbaze, L. M. A. (2014). The uniqueness and therapeutic value of natural products from West African medicinal plants. Part I: uniqueness and chemotaxonomy. RSC Advances, 4(54), 28728-28755.

[14] — Bierer, D. E., Fort, D. M., Mendez, C. D., Luo, J., Imbach, P. A., Dubenko, L. G., ... & Zhang, P. (1998). Ethnobotanical-directed discovery of the antihyperglycemic properties of cryptolepine: its isolation from Cryptolepis sanguinolenta, synthesis, and in vitro and in vivo activities. Journal of medicinal chemistry, 41(6), 894-901.

[15] — Paulo, A., Gomes, E. T., & Houghton, P. J. (1995). New alkaloids from Cryptolepis sanguinolenta. Journal of Natural Products, 58(10), 1485-1491.

[16] — Luo, J., Fort, D. M., Carlson, T. J., Noamesi, B. K., nii‐Amon‐Kotei, D., King, S. R., ... & Waldeck, N. (1998). Cryptolepis sanguinolenta: an ethnobotanical approach to drug discovery and the isolation of a potentially useful new antihyperglycaemic agent. Diabetic medicine, 15(5), 367-374.

[17] — Ansha, C., & Mensah, K. B. (2013). A review of the anticancer potential of the antimalarial herbal Cryptolepis sanguinolenta and its major alkaloid cryptolepine. Ghana medical journal, 47(3), 137-147.

[18] — Ansah, C., Mfoafo, E. A., Woode, E., Opoku-Okrah, C., Owiredu, W. K. B. A., & Duwiejua, M. (2008). Toxicological evaluation of the anti-malarial herb Cryptolepis sanguinolenta in rodents. J Pharmacol Toxicol, 3, 335-43.

[19] — Ajayi, A. F., & Akhigbe, R. E. (2012). Antifertility activity of Cryptolepis sanguinolenta leaf ethanolic extract in male rats. Journal of human Reproductive sciences, 5(1), 43.

[20] — Paulo, A., Gomes, E. T., Steele, J., Warhurst, D. C., & Houghton, P. J. (2000). Antiplasmodial activity of Cryptolepis sanguinolenta alkaloids from leaves and roots. Planta medica, 66(01), 30-34.

Lion's Mane (Hericium erinaceus)

What is Lion's Mane?

Lion's mane is a medicinal wood-rotting fungus with a characteristic growth pattern that resembles the shaggy mane of a lion.

The fungus prefers temperate forests in North America, Europe, and Asia where it thrives on living oak, beech, or conifer trees.

The medicinal benefit of lions mane primarily involve the nervous system. Modern applications use the mushroom for general cognitive health and as a natural nootropic substance.

This mushroom is also eaten as a delicacy — with a flavor similar to lobster when cooked with butter.

In recent years lion's mane has caught the eye of the nootropic community for its ability to up-regulate nerve growth factor.

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How Is Lion's Mane Used?

Lion's mane is mainly used for neurodegenerative disorders like dementia and multiple sclerosis. It's also popular as a nootropic agent for supporting optimal cognitive function long term.

Most of the people using this fungus take it in the form of a powdered capsule or tincture on a daily basis. Like most medicinal mushrooms, the biggest benefit comes from using the herb on a regular basis over long periods of time — rather than short bursts for quick impact of effects.

Traditional Use of Lion’s Mane

Lion’s mane mushrooms have a long history of use in Eastern Asia — including China, Korea, and Japan. Each of these regions used the mushroom for treating neurological disorders, including neurasthenia, and age-related cognitive decline, as well as for general health.

Herb Details: Lion's Mane

Herbal Actions:

• Antibacterial
• Anticancer
• Antidiabetic
• Antioxidant
• Cardioprotective
• Hepatoprotective
• Nervine
• Immunomodulator

Weekly Dose

• (1:2 Liquid Extract)
  20-60 mL
• View Dosage Chart

Part Used

• Fruiting Body

Family Name

• Hericiaceae

Distribution

• North America, Europe, Russia, Mountainous regions of Asia

Constituents of Interest

• Hericnones
• Erinacines
• Lactones
• Polysaccharides

Common Names

• Lion's Mane
• Monkey's Head
• Hedgehog Fungus
• Pom Pom
• Houtou (China)
• Shishigashira (China)
• Yamabushitake (Japan)

Pregnancy

• Safe during pregnancy.

Duration of Use

• Long term use acceptable and recommended.

Mycological Information

The Hericiaceae family of fungi are saprophytic (consumes dead wood), yet can be found growing on living trees as well. Many experts believe the mushroom has a mutualistic relationship with the tree for some time — helping it resist disease and infection, but will eventually consume the tree after it dies.

Hericium mushrooms normally grow in cooler, mountainous regions across the globe. It contains a number of species used medicinally and nutritionally.

Hericium spp. has characteristic "tooth" structures on its fruiting body, giving it a hair-like appearance.

Pharmacology & Medical Research

+ Neuroprotective

Lion’s mane offers several different mechanisms to produce its overall neuroprotective benefits:

1. Antioxidant and free-radical scavenging activity [6]
2. Anti-inflammatory activity
3. Nerve-growth factor stimulation (hericium and erinacenes)
4. Reduction of endoplasmic reticulum stress-dependant cell death (dilinoleolyl-phosphatidylethanolamine (DLPE) [7]
5. Attenuation of beta-amyloid-related cognitive decline in animals (dementia model) [8]
6. Enhance mylenation of neurons [9, 10, 11]

In animal studies, lion’s mane has been shown to reduce the severity of damage after a stroke — effectively protecting the sensitive neurons from ischemic damage [6].

Clinical Trials:

Study: Mori et al., 2009 — Improving effects of the mushroom Yamabushitake (Hericium erinaceus) on mild cognitive impairment: a double‐blind placebo‐controlled clinical trial. [5]

This randomized, double-blind, placebo-controlled clinical trial involving 30 Japanese men and women with mil cognitive impairment found that after 16 weeks, the lion’s mane group had significantly increased cognitive scores. These improvements were noted as early as the 8 week checkup, and continued to improve compared to placebo over the rest of the 16-week trial.

The dose of lion’s mane used in this study was 1 gram of dried lion’s mane taken three times per day.

Unfortunately, 4 weeks after the trial concluded, the scores had significantly decreased — indicating that these effects are not permanent and the mushroom needs to be continued to remain effective.

+ Nootropic

A nootropic is a substance that improves cognition without causing harm. There are a lot of nootropic substances that range from herbs like lion’s mane or rhodiola, to synthetic or prescription drugs like Modafinil or Noopept.

Lion’s mane is thought to be a nootropic through its ability to promote nerve-growth factor (NGF) in the brain. NGF is the most potent growth factor for the cholinergic neurons. it influences everything from the proliferation, differentiation, and survival of neuronal cells in the brain [8, 12].

Reductions in NGF has been considered a major implication in conditions such as depression, substance abuse, Alzheimer’s disease, and Huntington’s disease [12].

There have been a lot of studies looking at the role of lion’s mane and nerve growth factor — most of which have concluded that lion’s mane applications directly lead to an increase in NGF. This research has been done both in vivo and in vitro [13, 14, 15, 16].

This effect is very important. We can give peptides like NGF to people to treat these neurodegeneration, but these peptides rarely cross the blood brain barrier [9]. Therefore, finding alternative ways to boost NGF or other peptides in the brain are of the utmost importance in the treatment, prevention, and management of neurodegenerative disorders.

+ Immunomodulation

Like many other medicinal mushrooms, lion’s mane contains a high concentration of polysaccharides with immunomodulatory effects.

A lot of this study has been done in vitro with dendritic immune cells. These cells serve as the antigen-presenting cells that act as central mediators for the immune response as a whole. They’re responsible for a lot of the tolerance formed by the immune system to help maintain homeostasis.

Studies involving lions mane extracts have shown the fungus can stimulate the maturation of dendritic cells, induce dendritic cell activation, and modulate key T-helper (Th1) immune responses [17].

+ Anti-Inflammatory

Lion’s mane has been shown to influence a variety of inflammatory mediators, including:

Induces IL-1β expression through Nf-kB, NF-IL6, and activator protein 1 (AP-1) [18]

Induces iNOS gene expression to increase nitric oxide (NO) production in macrophages

Inhibits toll-like receptor 4 (TLR4)-JNK signalling on macrophages [19]

Phytochemistry of Lion’s Mane Mushrooms

Lion’s mane fruiting body and myclelia contain an exceptionally diverse range of unique bioactive substances — including polysaccharides, meroterpenoids (hericinones), cyathane diterpenoids (erinacines), steroids, alkaloids, and lactones.

The most significant constituents in terms of the mushrooms medicinal action are the hericenones and erinacines. Both of these substances have been shown to stimulate nerve growth factor in the central nervous system. This is thought to be the primary mechanism for which the fungus an improve the health and function of the nervous system.

Clinical Applications Of Lion's Mane:

Lion's mane has many uses, but the most well-known is as a neuroprotective, and nootropic benefits. It's useful for neurodegenerative disorders including multipple sclerosis, Alzheimer's disease, and Parkinson's disease.

Other uses include depression and anxiety, cancer, diabetes, gastrointestinal infection, and fatigue.

Cautions & Safety

Lion’s mane is a culinary mushroom that’s been used for both food and medicine by countless individuals over several hundreds of years. There are no expected short-term or long-term side effects from using the fungus.

Throughout the clinical research there have been no reports of serious side effects from using the fungus — including very high-potency extracts and long-term durations of use.

Caution advised with any blood clotting conditions or medications due to possible agonistic interactions — including haemophilia or other bleeding disorder, thrombocytopenia, or post-surgery. Lion’s mane may interact with blood thinners or anti-platelet medications.

Author:

Justin Cooke, BHSc

The Sunlight Experiment

(Updated April 2020)

Recent Blog Posts:

References

[1] — Friedman, M. (2015). Chemistry, nutrition, and health-promoting properties of Hericium erinaceus (lion’s mane) mushroom fruiting bodies and mycelia and their bioactive compounds. Journal of agricultural and food chemistry, 63(32), 7108-7123.

[2] — Liu, J., Du, C., Wang, Y., & Yu, Z. (2015). Anti-fatigue activities of polysaccharides extracted from Hericium erinaceus. Experimental and therapeutic medicine, 9(2), 483-487.

[3] — Thongbai, B., Rapior, S., Hyde, K. D., Wittstein, K., & Stadler, M. (2015). Hericium erinaceus, an amazing medicinal mushroom. Mycological progress, 14(10), 91.

[4] — Wong, K. H., Naidu, M., David, R. P., Bakar, R., & Sabaratnam, V. (2012). Neuroregenerative potential of lion's mane mushroom, Hericium erinaceus (Bull.: Fr.) Pers.(higher Basidiomycetes), in the treatment of peripheral nerve injury. International journal of medicinal mushrooms, 14(5).

[5] — Mori, K., Inatomi, S., Ouchi, K., Azumi, Y., & Tuchida, T. (2009). Improving effects of the mushroom Yamabushitake (Hericium erinaceus) on mild cognitive impairment: a double‐blind placebo‐controlled clinical trial. Phytotherapy Research, 23(3), 367-372.

[6] — Lee, K. F., Chen, J. H., Teng, C. C., Shen, C. H., Hsieh, M. C., Lu, C. C., ... & Huang, W. S. (2014). Protective effects of Hericium erinaceus mycelium and its isolated erinacine A against ischemia-injury-induced neuronal cell death via the inhibition of iNOS/p38 MAPK and nitrotyrosine. International journal of molecular sciences, 15(9), 15073-15089.

[7] — Nagai, K., Chiba, A., Nishino, T., Kubota, T., & Kawagishi, H. (2006). Dilinoleoyl-phosphatidylethanolamine from Hericium erinaceum protects against ER stress-dependent Neuro2a cell death via protein kinase C pathway. The Journal of nutritional biochemistry, 17(8), 525-530.

[8] — Mori, K., Obara, Y., Moriya, T., Inatomi, S., & Nakahata, N. (2011). Effects of Hericium erinaceus on amyloid β (25-35) peptide-induced learning and memory deficits in mice. Biomedical Research, 32(1), 67-72.

[9] — Phan, C. W., David, P., Naidu, M., Wong, K. H., & Sabaratnam, V. (2015). Therapeutic potential of culinary-medicinal mushrooms for the management of neurodegenerative diseases: diversity, metabolite, and mechanism. Critical Reviews in Biotechnology, 35(3), 355-368.

[10] — Kolotushkina, E. V., Moldavan, M. G., Voronin, K. Y., & Skibo, G. G. (2003). The influence of Hericium erinaceus extract on myelination process in vitro. Fiziol Zh, 49(1), 38-45.

[11] — Moldavan, M., Grygansky, A. P., Kolotushkina, O. V., Kirchhoff, B., Skibo, G. G., & Pedarzani, P. (2007). Neurotropic and trophic action of lion's mane mushroom Hericium erinaceus (Bull.: Fr.) Pers.(Aphyllophoromycetideae) extracts on nerve cells in vitro. International Journal of Medicinal Mushrooms, 9(1).

[12] — Chao, M. V., Rajagopal, R., & Lee, F. S. (2006). Neurotrophin signalling in health and disease. Clinical science, 110(2), 167-173.

[13] — Zhang, C. C., Yin, X., Cao, C. Y., Wei, J., Zhang, Q., & Gao, J. M. (2015). Chemical constituents from Hericium erinaceus and their ability to stimulate NGF-mediated neurite outgrowth on PC12 cells. Bioorganic & medicinal chemistry letters, 25(22), 5078-5082.

[14] — Samberkar, S., Gandhi, S., Naidu, M., Wong, K. H., Raman, J., & Sabaratnam, V. (2015). Lion's Mane, Hericium erinaceus and Tiger Milk, Lignosus rhinocerotis (Higher Basidiomycetes) medicinal mushrooms stimulate neurite outgrowth in dissociated cells of brain, spinal cord, and retina: an in vitro study. International journal of medicinal mushrooms, 17(11).

[15] — Lai, P. L., Naidu, M., Sabaratnam, V., Wong, K. H., David, R. P., Kuppusamy, U. R., ... & Malek, S. N. A. (2013). Neurotrophic properties of the Lion's mane medicinal mushroom, Hericium erinaceus (Higher Basidiomycetes) from Malaysia. International Journal of Medicinal Mushrooms, 15(6).

[16] — Mori, K., Obara, Y., Hirota, M., Azumi, Y., Kinugasa, S., Inatomi, S., & Nakahata, N. (2008). Nerve growth factor-inducing activity of Hericium erinaceus in 1321N1 human astrocytoma cells. Biological and Pharmaceutical Bulletin, 31(9), 1727-1732.

[17] — Sheu, S. C., Lyu, Y., Lee, M. S., & Cheng, J. H. (2013). Immunomodulatory effects of polysaccharides isolated from Hericium erinaceus on dendritic cells. Process biochemistry, 48(9), 1402-1408.

[18] — Son, C. G., Shin, J. W., Cho, J. H., Cho, C. K., Yun, C. H., & Han, S. (2006). Induction of murine interleukin‐1 beta expression by water‐soluble components from Hericium erinaceum 1. Acta Pharmacologica Sinica, 27(8), 1058-1064.

[19] — Mori, K., Ouchi, K., & Hirasawa, N. (2015). The anti-inflammatory effects of lion's mane culinary-medicinal mushroom, hericium erinaceus (higher basidiomycetes) in a coculture system of 3t3-L1 adipocytes and raw264 macrophages. International journal of medicinal mushrooms, 17(7).

Kratom (Mitragyna speciosa)

What is Kratom?

Kratom (Mitragyna speciosa) is a medicinal plant species native to Southeast Asia with powerful stimulating, pain-relieving, and euphoric effects.

As a member of the coffee family, it’s no surprise kratom is used to combat fatigue and work longer, more productive hours. But there are some other attributes to kratom that contradict this effect. 

Kratom is stimulating in lower doses and sedative in higher doses. It acts on the opioid pain system and interacts with neurotransmitters like serotonin, dopamine, and noradrenaline.

This unique combination of relaxing, pain-killing, and stimulating effects gives kratom interesting applications. The most common use of the plant is to work longer hours, relieve joint and muscle pain, and help people with chronic pain transition away from highly addictive pain medications. 

In this ultimate guide, we’ll cover everything you need to know about kratom. 

Topics We'll Cover in This Monograph

1. What is kratom used for?
2. Kratom Technical Details
3. History of Kratom
4. Guide to Using Kratom Safely (Dosage Information
5. Kratom Strains (Red, White, Green)
6. Different Types of Kratom Products
7. Medical Research of Kratom
8. Kratom Active Constituents
9. Kratom Side Effects & Safety
10. Legality of Kratom Around the World

Let’s jump straight in. Feel free to jump around to the sections that interest you the most. 

What is Kratom Used For?

There’s a few differences between how kratom is used today compared to its traditional uses.

Let’s cover each in more detail. 

Traditional Uses of Kratom

Traditionally, the leaves of the plant were chewed raw or made into a strong tea. This delivered much lower doses of the plant than modern methods allow. 

In low doses, the effects of kratom are highly stimulating — very similar to coffee or yerba maté. Because of this, most traditional uses of this plant revolve around its stimulating effects.  

Kratom was used by laborers as a way to combat fatigue during the long, hard working hours. Some reports even suggest kratom was used to increase the body’s tolerance to the effects of the hot sun. The pain-killing effects of the herb may have contributed to this by dulling body aches and pains while working. 

Kratom was really a herb of productivity. If you took kratom while working, you could work harder, faster, and longer than normal — ultimately, getting more done in a day. 

Other uses of the herb included treatment for intestinal infections, diarrhea, and muscle pain [5]. 

Modern Uses of Kratom

Modern applications of the herb are much more extensive because it’s easier now to choose between a low dose for stimulating effects or high doses for more sedative effects. 

Kratom powders are readily available and don’t rely on chewing the leaves to release the active compounds. We also have access to high-potency tinctures, capsules, and resin extracts thanks to modern extraction technologies. 

1. Kratom For Energy

We can split the uses of kratom according to the dose. 

Lower doses of the plant (2.5 – 7 mg) are generally much more stimulating and have better mood-enhancing effects. This is the most common dosage taken traditionally by workers looking to leverage the energizing effects of the plant. 

Many of the active ingredients in kratom stimulate the adrenergic receptors in the brain — causing increased electrical activity, faster heart rate, higher blood pressure, and more energy overall. 

These effects can last anywhere from 4 to 8 hours on a single dose. 

2. Kratom for Anxiety & Sleep

Larger doses (over 8 grams) are more sedative — making these doses better for supporting sleep and anxiety. However, this effect is less reliable than the other uses of kratom because of the stimulating activity at lower doses. Some people simply can’t take higher doses of the plant without experiencing side effects — which won’t help you with your sleep. 

Some strains are better than others for sleep and anxiety, so make sure you find a strain recommended for these uses specifically. 

3. Kratom & Opiate Withdrawal

One of the most important uses of the plant comes from its opioid effects. Kratom is able to curb opioid withdrawal symptoms, making it less likely for people to relapse during this uncomfortable stage of the recovery process. 

4. Kratom for Pain Management

Kratom is a popular alternative for pain management for its opioid pain killing properties and lower likelihood of addiction. People use this plant to numb pain without having to take highly addictive opiate pain medications like morphine, vicodin, oxycontin, or others. 

5. Kratom For Mood

The opioid effects of kratom impacts mood regulation. The cascade caused by opioid receptor activation releases dopamine in the reward center of the brain, producing a mild euphoria and sense of wellbeing. 

Other alkaloids in the kratom plant target serotonin release — another neurotransmitter associated with mood. 

Because of these effects, many people report benefits to using kratom as a way to stabilize low moods during waves of depression or during stressful times. 

6. Kratom as an Immunomodulator

One of the more interesting applications of kratom currently under investigation is its ability to support the immune system. Many of the alkaloids and saponins found in kratom are also found in a plant called cat’s claw (Uncaria tomentosa) — which is well-known for its ability to boost the immune system and protect the body from cancer, viral infection, or autoimmune disease. These alkaloids stimulate parts of the immune system such as the Th1 immune response and various prostaglandins and leukotrienes. 

Research is still needed to fully understand if kratom exerts these same effects. 

Comparing the Applications of Kratom According to Dose

Low Dose Applications of Kratom	High Dose Applications of Kratom
Increase focus and concentration Immune support As a nootropic supplement Cognitive performance enhancement As a coffee replacement for combatting fatigue To support fibromyalgia or chronic fatigue symptoms Boost mood	Managing pain Alleviating arthritis symptoms Reducing diarrhea Managing overstimulation and stress Reduce coughing Support the immune system Alleviate insomnia Boost mood

 

Herb Details: Kratom

Herbal Actions:

• Sedative (High-Dose)
• Stimulant (Low-Dose)
• Analgesic
• Anxiolytic
• Nootropic (mild)
• Antimicrobial
• Antioxidant

Dose

• (Dried Powdered Herb)
  2.5 to 15 grams

Part Used

Leaves

Family Name

Methysticum speciosa

Distribution

Southeast Asia

Constituents of Interest

• 7-Hydroxymitragynine
• Akuammiline
• Mitragynine
• Epicatechin
• Quinovic Acids

Common Names

• Kratom
• Kakuam
• Ketum
• Biak-biak
• Ithang
• Thom

CYP450

• Unknown

Pregnancy

• Avoid use during pregnancy.

Duration of Use

• Long-term use should be avoided to prevent addictive tendencies

A Brief History of Kratom

Kratom comes from various regions of Southeast Asia, including Thailand, Bali, Indonesia, Malaysia, and Papua New Guinea.

Here, kratom goes by the following names: 

• Kakuam

• Ketum

• Biak-biak

• Ithang

• Thom

In these regions, the leaves of the kratom tree are chewed or smoked throughout the day, or brewed into a strong tea and mixed with honey or citrus fruits. It was popular among laborers as a way to combat fatigue as they worked long hours throughout the day. 

For centuries, kratom helped people work harder, hunt for longer hours in the day, and manage pain caused by injuries or infection. 

It wasn’t until the 1800s that the Western world caught wind of kratom. A botanist travelling through Malaysia noted the herb as a substitute for opium — which, at the time, was already heavily restricted. 

Interest in kratom began to spread throughout Europe and eventually, North America. Still, it  wasn’t nearly as popular as a stimulant as coffee and couldn’t compete as a pain medication with pharmaceuticals. Only in the last ten years has kratom really become popular in the Western world as an alternative to pain medications as the epidemic of drug addiction is at an all-time high. 

Kratom remains a popular alternative option in Europe and the United States for pain management alongside cannabidiol (CBD) — which are often taken together.

Beginner’s Guide to Using Kratom

Getting started with kratom is simple — once you have your kratom, the next step is to figure out how much you should take, and how to prepare it. 

Kratom Dose: How Much Kratom Should I Take? 

The general dosage range for kratom leaf powder is 2.5 to 15 grams. 

Note that concentrates can vary significantly, so always follow the directions on the label when using these products. 

Everybody responds to the effects of kratom a little differently — so,  play it safe if this is your first time using kratom. Start with a very low dose (2 grams), and increase gradually over time as you start to get a feel for how kratom affects your body individually. 

A good process for beginners is to start with about 2 grams, wait 30 minutes, and follow up with another 1 gram every 30 minutes until you reach the desired level of effects. 

If you start to experience side effects, like kratom wobble (more on this later), it means you’ve reached your dosage limit for that strain of kratom. 

Once you find a dosage that works well for your body with that particular strain, you can be more confident in taking that dose from the beginning the next time you take kratom. 

If you have a food scale, weigh your kratom for accuracy. 

If you don’t have a scale, you can also use measuring spoons to get approximate doses. Use the table below to find the approximate equivalent dose from grams to teaspoons and tablespoons. 

Imperial to Metric Conversions

Metric	Imperial
2.5 Grams	1 Teaspoon
7 Grams	1 Tablespoon

How Do I Take Kratom?

There are two main methods of preparing kratom powder. Let’s go through the basic process for each method. 

Method 1: Kratom Tea

This is the most common method of preparing kratom. All you need to do is mix your dose of kratom (2.5 – 15 grams) with about 500 mL or 1 L of boiling water. 

Stir until the  powder dissolves— you don’t want to end up with any clumps of undissolved kratom powder in the mix. 

Once you’ve stirred the mixture for a minute or two, leave it for another couple of minutes to let the powder  settle to the bottom of the cup. 

Once there's a layer of sediment at the bottom, you can pour the kratom tea into drinking cups, making sure to avoid the sludge of undissolved kratom powder at the bottom. 

The final step is to add honey or sugar to sweeten, and drink up! 

Method 2: Toss & Wash

This is the simplest method. It’s not the most enjoyable, but it’s quick and requires little preparation. 

All you have to do is measure out the dose of kratom you want to use (somewhere between 2.5 and 15 grams depending on personal preference).

The next step is to simply swallow the powder with a spoon and quickly rinse it down with some water, juice, milk, or other beverage.

The powder can be hard to swallow, so it’s better to try and take a few spoonfuls than to fit the entire dose in one spoon.  

What Are the Different Kratom Strains?

Kratom contains an array of alkaloids, each with its own set of effects on the human body. Some are stimulating like caffeine from coffee, others activate the opioid pain receptors (relaxing and pain-killing effects), others work through completely different receptors in the central nervous system. 

This means the effects of kratom depend highly on which alkaloids are most abundant in the leaves.

As with most plants, there are many forms of kratom — each producing their own ratio of active alkaloids — resulting in subtle changes in growth patterns such as,  leaf and or vein color, and effect profiles. 

We call these different forms of kratom strains. 

Each strain of kratom adds its own twist on the general effect profile of the plant. All kratom has stimulating effects in low doses and sedative qualities in higher doses — however, some strains place more emphasis on one effect than the other. For example, some strains are better for pain (like Red Vein Borneo), while others have stronger immune supportive activity (like White Maeng Da). 

Let’s cover the most common strains of kratom, what makes them unique, and what their effect profiles are. 

There are a few different ways to catalog kratom strains, but I’ve found the best way is to look at the vein color of the plant. This gives us a clue as to which alkaloids are most prevalent in the sample, and therefore, what the effect profile is most likely to produce. 

Let’s get into the details. 

1. Red Vein Kratom

Red vein kratom is usually the best for fast-acting sedative action. These kratom strains tend to be rich in 7-Hydroxymitragynine compared to other colors (more on this alkaloid later). 

Kratom with red leaf veins can be found all over Southeast Asia, as you’ll find from the list below — but most users report red vein kratom to have very similar effects regardless of its place of origin. 

Most Popular Red Vein Kratom Strains

Maeng Da Thai — Red Vein

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Red Vein Kali Powder

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Red Vein Borneo

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2. Green Vein Kratom

Kratom strains with green veins are widely considered to be the middle ground for kratom effects. This means they’re both stimulating and sedative, and offer good general effects towards pain, mood, and focus. 

Covering both ends of the kratom spectrum, green vein can have many different effects, so the strain really does matter with these plants. Unlike white or red vein where the effects tend to be very similar no matter where the strain originates from. 

Most Popular Green Vein Kratom Strains

Super Green Vein Malaysian

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3. White Vein Kratom

White vein kratom has a low concentration of 7-Hydroxymitragynine. 

Kratom with white veins tend to have more of a mind effect — increasing alertness and focus, as well as producing feelings of euphoria and improvements in mood. 

Many users use white vein kratom in a similar manner to coffee or tea while working or studying. The effects of white vein kratom are more subtle than both red and green vein strains, and therefore, is a better option for daily use. 

Most Popular White Vein Kratom Strains

Maeng Da Thai — White Vein

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Sumatra White Vein

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White Vein Borneo

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What Forms of Kratom are Available? 

There are a few different ways you can use kratom. The most popular method is to mix the dried, ground leaf powder with water to drink. This produces the strongest and most reliable level of effects but isn’t exactly an enjoyable beverage to drink. 

Other ways people use kratom include capsules, kratom resin extracts, pre-mixed drinks, and alcohol or glycerine-based tinctures. 

Let’s discuss the differences between each form of kratom and what the pros and cons of each are. 

1. Kratom Powder

Kratom powder is the most versatile and cost-effective way of using kratom. You can mix it with water, juice or milk, or put it in capsules or tea bags yourself. 

Traditionally, kratom leaves were chewed to get the effects of the plant. The chewing action breaks the leaves up, while enzymes in the saliva break down the cellular structure of the kratom cells — effectively releasing the active alkaloids into the body. 

Modern techniques of drying and powdering the kratom replaces the job of chewing the leaves. All you need to do is find a way to get this leaf powder into the body for the effects to take hold. 

Unfortunately, kratom has a strong bitter flavor, so it may be difficult to take the powder raw. For this reason, most people mix kratom with chocolate milk, fruit juice, or other drinks with a strong flavor to mask the bitterness of the kratom. 

Pros

• Allows you to consume the entire leaf — which is the most efficient way of using kratom
• Powder is the most cost-effective way of using kratom
• Powders are the closest method to traditional kratom consumption
• Most kratom strains are available as a powder form
  

Cons

• Kratom powders don’t taste very good
• You need a fairly large dose of powder to feel the effects
• Kratom powders require a little bit of effort to prepare
  

2. Kratom Capsules

Another popular method of using kratom is to take them as a capsule. You can make capsules yourself by using a capsule-making machine and filling it with raw kratom leaf powder.

Commercially available kratom capsules are also available and are an excellent option for novice users. 

Capsules allow you to take consistent doses of kratom and are one of the most convenient and discrete ways of using the herb. Nobody thinks twice when you take a capsule, as it looks a lot like a regular health supplement — while mixing the green, bitter powder into a drink may draw the attention of your coworkers. 

Pros

• Discrete and convenient way of using kratom
• Provides consistent doses every time
  

Cons

• Not the cheapest way of using kratom
• You may need to take several capsules to feel the effects
• Not all strains are available in capsule form, unless you make them yourself from raw powder
  

3. Kratom Tinctures & Glycetracts

All herbs can be made into a tincture. The process involves rinsing the raw herb with alcohol, vegetable glycerine, or another solvent to extract the active ingredients through diffusion. Once most of the active compounds are removed from the leaves, the remaining fiber and cell structures of the plant are filtered out — leaving behind a liquid rich in active kratom compounds. 

Tinctures allow you to take consistent doses of kratom without having to weigh the leaf powder. This method is more discrete and can be added to any beverage or taken directly in the mouth. 

For even faster onset of effects, you can hold the tincture under the tongue where the kratom alkaloids will absorb through the microcapillaries located directly under the tongue — delivering the active compounds directly into the bloodstream. 

You can make tinctures yourself from the leaf powder or buy commercially made products. 

Pros

• One of the most convenient ways of using kratom
• Alcohol or vegetable glycerine preserve the kratom — dramatically increasing the shelf life
  

Cons

• Not the most cost-effective way of using kratom
• Some of the active compounds will be lost during the extraction process
• You may need to take fairly large amounts of the tincture to feel the effects
  

4. Kratom Resin Extracts

The active alkaloids of the kratom plant are most abundant in the plant's resin — which is a highly viscous fluid produced by the plant. This is where many active alkaloids are stored. Numerous plants have resins that can be removed and concentrated. 

Kratom resin extracts are very popular and make using kratom super simple. Since this preparation has all the unnecessary plant parts removed (the fibers, cell walls, proteins, carbohydrates, etc.), you don’t need as much of this stuff to start feeling the effects. 

For this reason, be very careful when using concentrated extracts. It doesn’t take much to go overboard with this stuff. 

Pros

• Allows you to take much less kratom to experience the effects
  

Cons

• Kratom extracts are expensive
• The effect profile isn’t as robust as the raw plant material
  

How Does Kratom Work? 

Kratom works primarily through the alkaloid content of the leaves. We’ll get into the details of what alkaloids are, and what the most important alkaloids in the kratom plant do in more detail later.  

The most important thing to note here is that alkaloids tend to have powerful pharmacological effects on the human body because they have the ability to activate or inhibit various cell receptors around the body. 

The human body uses receptors as a way to control cellular functions around the body. By activating or inhibiting these receptors, we can tell our cells to behave a certain way. 

Caffeine for example, binds to the adenosine receptors which are responsible for making us sleepy. By binding to these receptors, it prevents this from happening — causing us to feel awake and alert. 

In the kratom plant, there are over 24 different alkaloids — each with their own affinity for different receptors in the body. 

The majority of effects from kratom rely on an activation of the opioid receptors (resulting in pain inhibition, sedation, and euphoria), and adrenergic receptors (causing the stimulating effects). 

Some of these alkaloids have more novel effects such as, stimulating immune cells, modulating dopamine levels, or inhibiting noradrenaline. 

Kratom is also rich in flavonoids, including epicatechin — which is one of the primary antioxidants found in green tea, chocolate, and grapes. These antioxidants provide protection from harmful free radicals and oxidative compounds we’re exposed to from the environment. 

Pharmacology & Medical Research

Over the years, there’s been a lot of interest in kratom as a therapeutic agent. In the early 1980s, there was a particularly strong interest in the potential to use kratom as an alternative to addictive pain medications or for helping drug users wean themselves off the medication. 

There’s also  a wealth of research for using kratom for increasing energy levels, addressing anxiety symptoms, and alleviating opiate withdrawal symptoms. 

Most of this research was done in the 1970s and 1980s before there was a sweeping ban of kratom in the United States and Europe. Although most of these bans have since been lifted, kratom research is not as abundant as it once was. 

Another reason why research isn’t as common for kratom as other pant medicines is due to the incredible complexity of the plants constituents. There are at least 24 known alkaloids in kratom, each with their own potent effect profile. This makes it very hard to study the plant because there are so many variables. It’s much easier to study plants with one active ingredient than a plant with 24 or more active ingredients. 

Nevertheless, I’ll break down some of the best research we have available for the most common applications of kratom.

+ Kratom For Energy

The earliest uses of kratom involve its stimulating properties. Several alkaloids in kratom activate the adrenergic receptors [5,6].

Hormones such as noradrenaline and adrenaline (catecholamines) activate the adrenergic receptors which causes several important changes in the body — namely, increased heart rate, blood pressure, and electrical activity in the brain. The result of these changes is what we commonly experience as the fight or flight response.

However, these effects are highly dose-dependent. Higher doses of kratom have much more sedative effects on the body as a result of the opioid activity of the plant [7].

+ Kratom for Opiate Addiction

The first suggestion that kratom could alleviate opiate withdrawal symptoms came from research published in the 1930s [3]. Since then, this application has gained a lot of attention.

So how does this work? What does the research suggest?

First, let’s discuss how opiate addiction works in the first place.

After frequent exposure to opioid drugs, the body begins to change its homeostatic balance as an attempt to resist the effects of the drug — resulting in what we call tolerance. Drug tolerance forces us to take larger doses of the drug to experience the same level of effects.

As soon as the drug-use stops, it’s metabolized and removed from the body. Unfortunately, the homeostatic changes the body made in response to the drug lead to a phenomenon known as withdrawal.

Withdrawal symptoms can last several days or weeks as the body struggles to readjust homeostatic mechanisms to reverse the adaptations made while taking the drug.

Opiate withdrawal can be severe — causing symptoms such as anxiety, insomnia, chills, fever, body aches, seizures, headaches, and hallucinations. These symptoms are often strong enough to force the user to seek out more of the drug to alleviate these symptoms — resulting in a relapse.

Therefore, one of the major goals of addiction treatment is to alleviate the symptoms of withdrawal while the user goes through the detox process.

The most common medications used for this stage are methadone and buprenorphine — however, both these medications can also lead to a second stage of opiate and opiate-like drug dependance.

Kratom is a strong candidate for opiate withdrawal symptoms because it has the potential to alleviate opiate withdrawal symptoms without possessing nearly the same chances of secondary addiction.

So how does this work? Is there any data to back this up?

Kratom alkaloids alleviate opioid withdrawal symptoms in zebrafish (a common model of addiction) [4].

Unfortunately, there aren’t many high-quality studies on this application of kratom. The best data we have at the moment involves anecdotal evidence of people who successfully weaned themselves off opiate drug addiction, and animal research including the study cited above.

It’s likely kratom’s effects on the opioid system are much more complicated than simply activating these receptors in place of the opioid medications. This could explain why kratom has a lower incidence of addiction compared to specific opioid agonist medications such as morphine, fentanyl, methadone, and oxycontin.

More research is needed to fully understand the role kratom might play in helping people wean off addictive opiate drugs like heroin, vicodin, morphine, fentanyl, and oxycontin.

+ Kratom For Pain

Since kratom is able to exert its effects through the opioid system, it’s not surprising the herb possesses pain-relieving benefits. The opioid system is integral to the transmission of pain from the body to the brain. Mu- and gamma-opioid receptors located in the spinal cord and brain regulate the transmission of pain signals.

By activating the opioid receptors, kratom inhibits pain signals and reduces both chronic and acute pain.

A study published in 2009, highlighted the pain-killing and anti-inflammatory effects of kratom [8]. The study gave rats a standardized extract of kratom known as MSM at doses of 100 and 200 mg/kg. A significant reduction in both inflammation and pain were noted in the rats following the treatment with kratom.

Researchers in the study suggested the anti-inflammatory effects were a result of lipoxygenase and cyclooxygenase inhibition.

The pain-relief is likely a combined result of the anti-inflammatory effects and opioid receptor activation.

+ Kratom For Focus

Kratom alkaloids possess adrenergic [5] and serotonergic [9] activity. Additionally, through the opioid system, kratom alkaloids like mitragynine are theorized to possess secondary dopaminergic and GABAergic effects in the brain [10, 11].

All of these effects are associated with cognitive performance and focus. Many of the most popular cognitive enhancing supplements and medications rely on activating one or more of these pathways in the brain.

Although there’s no research currently available that explores this interaction more closely, there's plenty of anecdotal reports that suggest kratom can boost focus and attention — especially with white veined kratom strains.

This is another area where more research is welcomed to fully elucidate the applications of kratom.

Kratom Constituents: What Are Kratom Alkaloids? 

Kratom is a rich source of indole and oxindole alkaloids similar to caffeine. It’s also rich in antioxidant flavonoids, and pharmacologically-active saponins and glycoside derivatives.  

The main constituents of kratom are mitragynine, paynantheine, speciogynine, and 7-Hydroxymitragynine — which collectively make up around 90% of the alkaloid content of the plant. 

The alkaloid content of kratom plants can vary significantly. Even within the same strain, the alkaloid content can change depending on how much rain there was during the growing season, the altitude in which the plants are grown, and how soon the leaves were harvested during the season. 

It’s thought the kratom plant produces these alkaloids as a way to defend itself from insects and animals and as a way to store excess nitrogen. 

A) Kratom Alkaloids

Alkaloids are notorious for having powerful pharmacological effects on the human body. 

Some of the most well-known alkaloids include caffeine (stimulant), cocaine (stimulant), morphine (pain-killer), nicotine (stimulant), ephedrine (stimulant), and ibogaine (psychedelic). 

Alkaloids can be beneficial to the body, but they can also be quite toxic — as with the case of strychnine, aconitine, or coniine. 

Kratom is exceptionally rich in alkaloids — most of which have been confirmed to be pharmacologically active in humans. 

By far the most abundant alkaloid in kratom is mitragynine, so most of the current research explores his compound. However, over 23 other alkaloids have also been discovered, many of which have been investigated more closely for their effects. 

Some of these alkaloids are even found in other useful plant species such as yohimbe or cat’s claw — both of which have a great deal of research highlighting their effect profiles. 

Let’s briefly explore each alkaloid in kratom and their interaction with the human body. 

1. 7-Hydroxymitragynine

This alkaloid is analgesic, antitussive (inhibits coughing), and antidiarrheal [12]. It’s also considered one of the key mu-opioid receptor agonists and one of the main alkaloids in red vein kratom strains. 

2. 9-Hydroxycorynantheidine

This alkaloid is a partial opioid agonist — which means it’s not as strong as other alkaloids in the plant at activating the opioid pain receptors. However, many experts believe this alkaloid works through a different mechanism and can amplify the pain-killing effects of other alkaloids like mitragynine or 7-hydroxymitragynine. 

3. Ajmalicine

Ajmalicine is also found in another popular stimulating herb known as yohimbe and Rauwolfia serpentina. Extracts of this same alkaloid from the yohimbe plant is referred to as δ-yohimbine. 

There’s actually a lot of information available on this alkaloid, and there are synthetic versions available used in the treatment of high blood pressure. 

Ajmalicine is an α-1 adrenergic receptor antagonist, which goes against many of the other alkaloids in the plant. It’s believed this alkaloid works as a smooth muscle relaxant, mild sedative, and helps reduce some of the side effects of other prevalent kratom alkaloids. 

4. Akuammiline

Akuammiline is in the indole class of alkaloids and is also found in abundance in the akuamma seed (Picralima nitida) — which is where the name comes from. 

This compound is structurally very similar to yohimbine and mitragynine — and likely offers a similar set of effects. 

5. Ciliaphylline

There isn’t much research available on ciliaphylline, but it’s believed to be analgesic and antitussive (cough-suppressant) from preliminary research. 

6. Corynantheidine

This alkaloid is a mu-opioid antagonist — which works against many of the other alkaloids in the plant. This compound is also found in yohimbe and acts as an α1-adrenergic and α2-adrenergic receptor antagonist (inhibitor). 

7. Corynanthine

There isn’t much research on this alkaloid currently available, but some studies observed it to provide mild calcium channel blocking activity. 

8. Corynoxine A & B

These two alkaloids have dopaminergic, neuroprotective, and mild sedative effects. Corynoxine A is also found in the medicinal herb cat’s claw (Uncaria tomentosa). 

9. Iso Mitraphylline

This compound is a potent immunostimulant — suggested to provide the marhodity of the immune supportive effects of kratom despite making up less than 1% of the total alkaloid profile of the plant. 

10. Isopteropodine

Isopteropodine is another immunostimulant and a 5-HTP modulator and mood supportive. This compound is involved in the concentration and mood-enhancing effects of some kratom strains.

11. Isorhynchophylline

Isorhynchophylline is found in Chinese cat’s claw (Uncaria rhynchophylla) and has immunostimulating and calcium channel blocking effects [13]. There isn’t much research currently available on this particular alkaloid. 

12. Mitragynine

Mitragynine is considered the primary alkaloid in the kratom plant, responsible for the majority of the plants effects. It was the first discovered, and makes up roughly 66% of the total alkaloid profile of the kratom plant. 

This alkaloid is an opioid receptor agonist, miod adrenergic receptor agonist, and 5HT2A (serotonin) receptor agonist. Its primary effects are antitussive (cough suppressant), anti-diarrheal, analgesic (pain-relieving), and central nervous stimulant and sedative. 

13. Mitraphylline

Mitraphylline is an oxindole alkaloid with vasodilating, blood pressure lowering, muscle relaxing, and diuretic activity. 

14. Mitraversine

This alkaloid is sometimes found in kratom but is more commonly found in a closely related species — Mitragyna parvifolia. 

15. Paynantheine

This alkaloid is the second most abundant alkaloid in most kratom strains (though not all). It’s a smooth muscle relaxant and has minor activity on the opioid and adrenergic receptors. There’s a synthetic version of this compound available at the moment undergoing preliminary research. 

16. Rhynchophylline

Rhynchophylline is found in both kratom and Chinese cat’s claw (Uncaria rhynchophylla). It’s been studied for its hypotensive effects — which were noted to leave blood flow in the kidneys unaffected [13]. Decreased blood flow in the kidneys is a serious side effect of modern pharmaceutical blood pressure medications — so there’s a lot of interest in this compound as a potential new blood pressure medication. 

This alkaloid is also suggested to be an anti-inflammatory, antipyretic, NMDA receptor agonist, dopaminergic, serotonergic, and antiarrhythmic through calcium channel blocking activity. All of these suggested effects need to be studied in further detail to confirm. 

17. Speciociliatine

This compound is a diastereomer of mitragynine — which means it’s very similar in structure to mitragynine.

This alkaloid is a weak opioid agonist and may inhibit acetylcholine release from presynaptic nerve terminals. 

18. Speciogynine

This alkaloid is very similar in structure to the primary kratom alkaloid mitragynine and the third most abundant alkaloid in the plant. It’s thought to have muscle relaxant properties, and is attributed for a lot of kratoms stress-reduction effects.

19. Speciophylline

Speciophylline is another alkaloid kratom that has in common with cat’s claw. There isn’t much research on this compound, but early research suggests it may have anticancer activity — specifically towards leukemia cell lines. 

B) Other Compounds in Kratom

1. Epicatechin

Epicatechin is a flavonoid with potent antioxidant effect. It’s abundant in the plant kingdom, best known for its role in providing many of the health benefits of green tea (Camellia sinensis), chocolate (Theobroma cacao), and grapes (Vitis vinifera). 

2. Daucosterol

Daucosterol is classified as a saponin — which is another class of compound that often possess pharmacologically active effects in animals. This particular saponin is thought to contribute to the anti-inflammatory activity of kratom. It’s been shown to induce Th1 immune responses in animals [15] — which is a key component of a healthy immune system. 

Daucosterol has also been shown to promote the regeneration of neural stem cells in vitro [16]. 

3. Quinovic Acids

Kratom shares a lot in common with cat’s claw — one of the world's premier immune-supportive herbs. Quinovic acids are another group of compounds the two herbs have in common. 

Quibovic acids are classified as triterpene saponins. They’ve been shown to have potent antiviral activity in vitro [17], though more research is needed to see if this effect applies in living animals as well. 

Safety & Side-Effects of Kratom

Caution is advised whenever using kratom. The effects can be very unpredictable, and the oposing effects some strains have from each other make it unreliable as a form of treatment for many conditions. If using kratom for its stimulating effects but sedation is delivered the condition can worsen. Only use kratom with the advice or observation of an experienced individual and only for minor conditions. Speak with your doctor before trying kratom is taking any medications or if you have any medical conditions.

Kratom Side Effects

Kratom doesn’t come without side effects — however, with responsible use the side effects of kratom acan be managed and mitigated.

The primary activity of kratom works through the opioid receptors and adrenergic receptors — so naturally, the most common side effects of the plant stem from the interaction with these receptors. 

Adrenergic side effects cause a similar set of side effects of stress. This is because the adrenergic system is closely associated with the stress response. 

Adrenergic side effects of kratom:

• Nausea

• Dizziness

• Anxiety

• Stimulation

• Insomnia

• Dry mouth

• Headaches

• Irritability

• Sweating

• Diarrhea

• Increased urination

• Rapid heartbeat

The opioid effects of kratom may produce a completely different set of side effects which are similar to other opioid medications. 

Opioid side effects of kratom: 

• Sedation

• Lethargy

• Nausea or vomiting

• Dizziness

• Itchy nose

• Euphoria

• Constipation

• Increased urination

Despite the fact that most of these side effects are very rare and only tend to show up if kratom is used in high doses, it’s important to consider the potential dangers of using kratom. As with any compound, you can always take too much. Be responsible when taking kratom and listen to your body. 

With that said, there’s a trio set of side effects that many users experience if they take too much. These side effects are one of the main reasons kratom doesn't tend to cause addiction. To take enough kratom to “nod out” — which is the goal for a lot of recreational users, you're more than likely to experience something called the kratom wobble before you get enough of the herb to start nodding out. 

What Is the “Kratom Wobble?” 

So-called kratom wobble is the most common side effect from high doses of kratom. It causes dizziness and loss of coordination. It can make users feel quite unwell. 

Kratom wobble has 3 main symptoms: 

1. Blurry vision

2. Dizziness

3. Nausea/Vomiting

These effects are more common in some strains of kratom than others. The likelihood a specific kratom is to cause these side effects is called the wobble threshold. 

Strains with a low wobble threshold are more likely to cause wobble side effects if you take too much. Strains with a high wobble threshold will have a much lower chance of causing these effects if you go slightly over the optimal dose for your body.

The lower the wobble threshold, the more likely that strain is of causing kratom wobble — especially in higher doses. 

What Happens if I Experience Kratom Wobble? 

The first thing you need to do when you experience wobble effects is to relax. Panicking is only going to amplify the effects. Instead, find somewhere comfortable to sit or lay down and gather yourself. The effects will usually pass within a few minutes but may last up to 3 hours. 

Many people find it helps to drink ginger tea or warm water. 

If you experienced wobble while taking kratom, make sure to reduce the dose the next time you take kratom, or find a strain that’s less likely to cause these effects. 

The most common cause for kratom wobble is taking too much. This is a sign you’ve hit your dose limit for that particular strain of kratom. 

Is Kratom Dangerous? 

Just about everything is dangerous if you take enough of it — kratom is no different. There have been some reports of people dying from kratom — however, this is over-sensationalized in media reports. In most of these cases, kratom was abused or mixed with other drugs.

Never do this. 

Kratom is a powerful medicinal plant and should be treated with respect. 

Stick within the recommended dosage limits, don’t mix kratom with other drugs or medications, and listen to what your body is telling you. 

There are plenty of safety studies on kratom — the majority of which report little to no toxicity even in very high doses. An older study (1972) investigating the safety profile of the main alkaloid in kratom — mitragynine — found that even after significantly high doses (920 mg/kg), there were no deaths [2]. 

This is an insanely high dose. In the average 150 lbs. person, this is the equivalent of over 62,000 mg of kratom (62 grams). 

That’s five times the high-end of the recommended dose and nine times the average 7 g dose. 

Is Kratom Addictive? 

The most concerning potential long-term side effect of kratom use is addiction. 

Kratom is an opioid agonist, much the same way oxycontin or heroin is — however, unlike these pharmaceuticals, kratom contains dozens of active ingredients, each acting on different pathways in the body. This gives kratom a more rounded effect profile and has a much lower chance of leading to addiction. 

In fact, kratom is often limited in its addictive qualities because the dose can only go so high before it causes the user to feel kratom wobble or other unwanted side effects. You can’t get high from kratom the same way you can with pharmaceutical opioid drugs. 

Short term, low dose, or sporadic use of the plant is highly unlikely to result in addiction and is even used to help wean people off addictive drugs. 

With that said, be careful when using opioid agonist plants or medications. Speak with your doctor before using the plant if you have a history of addiction — especially to opiate-based drugs or medications. 

Kratom Legality

Kratom has a shaky legal history. It’s been banned, unbanned, and banned again all around the world. The laws on whether or not you can order kratom can be difficult to navigate. 

Here’s a brief overview on the current legal climate around kratom. 

Is Kratom Legal in the United States?

In the United States, kratom was banned, then unbanned, then banned again. It’s a rollercoaster ride trying to keep up with the changing laws. The argument goes back and forth whether kratom is useful for avoiding or treating addiction or if it causes addiction. 

At the moment, kratom is legal on a federal level and banned in specific states or municipalities. 

+ States Where Kratom is Banned

• Alabama
• Arkansas
• Indiana
• Rhode Island
• Vermont
• Wisconsin

In some states, the laws aren't black and white. For example, kratom is legal in the state of California, but banned in the city of San Diego. There are similar examples of this in Florida, where kratom is only banned in the Sarasota county.

+ States Where Kratom is Legal

• Alaska
• Arizona
• California (Except San Diego)
• Colorado (Except Denver)
• Connecticut
• Delaware
• Florida (Except Sarasota county)
• Georgia
• Hawaii
• Idaho
• Illinois (Except Jerseyville)
• Iowa
• Kansas
• Kentucky
• Louisiana
• Maine
• Maryland
• Massachusetts
• Michigan
• Minnesota
• Mississippi (Except Union County)
• Missouri
• Montana
• Nebraska
• Nevada
• New Hampshire
• New Jersey
• New Mexico
• New York
• North Carolina
• North Dakota
• Ohio
• Oklahoma
• Pennsylvania
• South Carolina
• South Dakota
• Tennessee
• Texas
• Utah
• Virginia
• Washington
• West Virginia
• Wyoming

Is Kratom Legal In Europe? 

Kratom is very hit/miss in Europe. Some countries have decided to ban the plant because of fears of addiction, while others allow its use as a way for people to avoid addiction to prescription medications. 

+ Legal

• Austria
• Belarus
• Belgium
• Bulgaria
• Croatia
• Czech Republic
• France
• Germany
• Greece
• Holland
• Hungary
• Moldova
• Netherlands
• Norway
• Portugal

+ Illegal

• Ireland
• Italy
• Latvia
• Lithuania
• Poland
• Romania
• Russia
• Sweden
• Turkey
• United Kingdom
• Denmark
• Finland

Is Kratom Legal in Asia and Australasia? 

Starting with Thailand in 1943, and neighboring countries in the years following, kratom use and cultivation were banned. There’s a lot of conspiracy around this which we’ll get into later in the “Is Kratom Legal Where I Live” section. 

To summarize, many people believe it was the pharmaceutical companies that lobbied against kratom because it was widely used by people as a substitute for opioid medications or to wean opiate addicts off these drugs. The main argument is that kratom is significantly less addictive than these medications, and despite the potential for uncomfortable side effects, the herb is much safer than prescription pain medications. 

Nevertheless, kratom was banned in Thailand, and massive fines were given to anybody caught using, or growing the herb. Later in 2018, these laws were finally redacted and kratom is now a major economic export for the country. 

Other Southeast Asian countries have had similar bans on kratom — many of which have been overturned. 

+ Legal

• Thailand (medicinal only)
• Bali
• China (legal grey-area)

+ Illegal

• Malaysia
• South Korea
• Australia
• Japan
• New Zealand
• Myanmar
• Singapore
• Vietnam

Final Thoughts: Kratoms Usefulness & Safety index 

Kratom is an incredibly useful plant. It has stimulating effects similar to coffee or tea in lower doses and sedative effects similar to kava in higher doses. It has powerful pain-killing activity and can even be used to boost mood and our immune systems.

The contradictory set of effects kratom provides have boggled researchers for decades as they try to decipher the interaction between dozens of active alkaloids and other phytochemicals found in the plant. 

After a few decades of banishment in the United States and much of Europe, the research on these chemicals fell out of interest. Only within the last 10 years or so has interest in the plant peaked again and research resumed.

Many people are finding usefulness for the plant as an alternative to coffee in the morning, for managing chronic or tough to treat pain without having to take pharmaceutical pain medications, boost focus and concentration, or stabilize mood. 

As with any powerful medicine, it’s important you treat kratom with respect if you want to avoid side effects and stay safe.

Author:

Justin Cooke, BHSc

The Sunlight Experiment

Recent Blog Posts:

Popular Herbal Monographs

References

[1] — Jansen, K. L., & Prast, C. J. (1988). Ethnopharmacology of kratom and the Mitragyna alkaloids. Journal of Ethnopharmacology, 23(1), 115-119.

[2] — Macko, E., Weisbach, J. A., & Douglas, B. (1972). Some observations on the pharmacology of mitragynine. Archives internationales de pharmacodynamie et de thérapie, 198(1), 145.

[3] — Jansen, K. L., & Prast, C. J. (1988). Psychoactive properties of mitragynine (kratom). Journal of psychoactive drugs, 20(4), 455-457.

[4] — Khor, B. S., Jamil, M. F. A., Adenan, M. I., & Shu-Chien, A. C. (2011). Mitragynine attenuates withdrawal syndrome in morphine-withdrawn zebrafish. PLoS One, 6(12).

[5] — Hassan, Z., Muzaimi, M., Navaratnam, V., Yusoff, N. H., Suhaimi, F. W., Vadivelu, R., ... & Jayabalan, N. (2013). From Kratom to mitragynine and its derivatives: physiological and behavioural effects related to use, abuse, and addiction. Neuroscience & Biobehavioral Reviews, 37(2), 138-151.

[6] — Beckett, A. H., Shellard, E. J., & Tackie, A. N. (1965). The Mitragyna Species of Species of Asia-Part IV. The alkaloids of the leaves of Mitragyna speciosa Korth.. Isolation of Mitragynine and Speciofoline1. Isolation of Mitragynine and Speciofoline1. Planta Medica, 13(02), 241-246.

[7] — Prozialeck, W. C., Jivan, J. K., & Andurkar, S. V. (2012). Pharmacology of kratom: an emerging botanical agent with stimulant, analgesic and opioid-like effects. The Journal of the American Osteopathic Association, 112(12), 792-799.

[8] — Mossadeq, W. S., Sulaiman, M. R., Mohamad, T. T., Chiong, H. S., Zakaria, Z. A., Jabit, M. L., ... & Israf, D. A. (2009). Anti-inflammatory and antinociceptive effects of Mitragyna speciosa Korth methanolic extract. Medical Principles and Practice, 18(5), 378-384.

[9] — Matsumoto, K., Mizowaki, M., Suchitra, T., Murakami, Y., Takayama, H., Sakai, S. I., ... & Watanabe, H. (1996). Central antinociceptive effects of mitragynine in mice: contribution of descending noradrenergic and serotonergic systems. European Journal of Pharmacology, 317(1), 75-81.

[10] — Klitenick, M. A., DeWitte, P., & Kalivas, P. W. (1992). Regulation of somatodendritic dopamine release in the ventral tegmental area by opioids and GABA: an in vivo microdialysis study. Journal of Neuroscience, 12(7), 2623-2632.

[11] — Sasaki, K., Fan, L. W., Tien, L. T., Ma, T., Loh, H. H., & Ho, K. (2002). The interaction of morphine and γ-aminobutyric acid (GABA) ergic systems in anxiolytic behavior: using μ-opioid receptor knockout mice. Brain research bulletin, 57(5), 689-694.

[12] — Ponglux, D., Wongseripipatana, S., Takayama, H., Kikuchi, M., Kurihara, M., Kitajima, M., ... & Sakai, S. I. (1994). A new indole alkaloid, 7 α-hydroxy-7H-mitragynine, from Mitragyna speciosa in Thailand. Planta medica, 60(06), 580-581.

[13] — Shi, J. S., Yu, J. X., Chen, X. P., & Xu, R. X. (2003). Pharmacological actions of Uncaria alkaloids, rhynchophylline and isorhynchophylline. Acta Pharmacologica Sinica, 24(2), 97-101.

[14] — León, F., Habib, E., Adkins, J. E., Furr, E. B., McCurdy, C. R., & Cutler, S. J. (2009). Phytochemical characterization of the leaves of Mitragyna speciosa grown in the USA. Natural product communications, 4(7), 1934578X0900400705.

[15] — Lee, J. H., Lee, J. Y., Park, J. H., Jung, H. S., Kim, J. S., Kang, S. S., ... & Han, Y. (2007). Immunoregulatory activity by daucosterol, a β-sitosterol glucoside, induces protective Th1 immune response against disseminated Candidiasis in mice. Vaccine, 25(19), 3834-3840.

[16] — Jiang, L. H., Yang, N. Y., Yuan, X. L., Zou, Y. J., Zhao, F. M., Chen, J. P., ... & Lu, D. X. (2014). Daucosterol promotes the proliferation of neural stem cells. The Journal of steroid biochemistry and molecular biology, 140, 90-99.

[17] — Aquino, R., De Simone, F., Pizza, C., Conti, C., & Stein, M. L. (1989). Plant Metabolites. Structure and In Vitro Antiviral Activity of Quinovic Acid Glycosides from Uncaria tomentosa and Guettarda platypoda. Journal of natural products, 52(4), 679-685.

Horopito (Pseudowintera colorata)

What is Horopito?

Horopito is commonly known as New Zealand pepperwood for its mild spicy flavor and exclusivity to the cooler islands of the south pacific ocean — including New Zealand.

This herb has a lot of traditional uses as medicine but went largely noticed by the international herbal medicine community. Recently there’s been a surge in interest in the plant after a series of studies were done to assess the medical value of traditional New Zealand herbs.

Horopito is used for skin and digestive conditions largely due to the plant’s potent antifungal actions. This plant has been shown to kill candida, as well as a number of parasitic worms.

The mild spicy nature of the plant also brings some circulatory stimulant and analgesic activity.

This plant has a lot of practical applications, especially for infectious fungal or parasitic conditions. It’s likely this plant will become much more commonplace in western herbal medicine within the next 5 to 10 years.

What is Horopito Used For?

The primary uses of horopito in modern herbal medicine is for fungal, bacterial, and parasitic infections.

A liquid extract of the herb is the most common form used today, but you can also find capsules and topical applications of the herb. For skin infections, such as ringworm or eczema, a poultice of the leaves can be applied directly, but a liniment is more common as the plant can be difficult to grow outside New Zealand.

Traditional Uses of Horopito

The Maori of New Zealand have been using horopito for a long time and have a long list of applications for its leaves.

The Maori use horopito in the following ways:

• As a flavoring agent (spicy flavor profile)

• For sexually transmitted infection

• Ringworm

• Chaffed or damaged skin

When the early Europeans colonized New Zealand many of them began using the herb as a source of vitamin C to prevent or treat scurvy.

Herb Details: Horopito

Herbal Actions:

• Analgesic
• Anti-Allergy
• Antibacterial
• Antifungal
• Anti-Inflammatory
• Astringent
• Circulatory Stimulant
• Gastroprotective
• Insecticidal
• Nutritive
• Rubefacient

Weekly Dose

• 10 – 30 mL (1:2 Extract)
• View Dosage Chart

Part Used

Leaves & Inner Bark

Family Name

Winteraceae

Distribution

Cooler Tropical islands Around new Zealand

Constituents of Interest

• Anthocyanins
• Dialdehyde polygodial
• Sesquiterpenes
• Eugenol

Common Names

• Horopito
• New Zeland Pepper Tree
• Maori Painkiller
• Ramarama

CYP450

• Unknown

Quality

• Warm

Pregnancy

• Safety during pregnancy not well established, avoid use while pregnant or breastfeeding.

Duration of Use

• Long-term use is acceptable and common

Botanical Information

Horopito is a member of the Winteraceae family of plants — which consists of about 90 species of trees and shrubs nearly exclusive to the Southern hemisphere.

The leaves of horopito have a characteristic red color as a result of the sesquiterpene content of the leaves — which are also one of the main medicinal compounds in the plant.

Cautions & Safety Information:

There have been very few reports of side effects from using horopito — however, some reports of allergic reactions have been reported.

Horopito should be avoided by epileptics due to a possible increase in extracellular glutamate found in some animal studies.

Avoid larger doses of the herb with acute gastritis or peptic ulcers.

Author:

Justin Cooke, BHSc

The Sunlight Experiment

(Updated March 2020)

Recent Blog Posts:

References:

1. insert

Chaga (Inonotus obliquus)

What is Chaga?

Chaga is a slow-growing tree fungus found in cold climates around the world.

This fungus is thought to be one of the best immunomodulators in the natural world. It has a long history of use as medicine, has been the subject of dozens of clinical trials, and is the source product for over 40 pharmaceutical oncology medications.

The fungus itself doesn’t have an appetizing appearance, resembling burnt, diseased growth protruding from birch or alder trees. Once harvested chaga looks more like a rock than a herb.

Despite its appearance, chaga makes a delicous tea resembling the color and flavor of coffee — without the caffeine.

What is Chaga Used For?

Chaga is primarily used as an immune tonic. It’s consumed in capsules, as a strong tea, or in tincture form for supporting and stimulating several different parts of the immune system.

Medicinally, the msot common use for the herb is as an adjunctive cancer treatment, and for compromised immune systems.

Herbalists often use chaga for heart disease, high cholesterol, hypertension, hyperglycemia, and atherosclerosis. This fungus contains an array of antioxidant, immune-boosting, anti-inflammatory, and adaptogenic compounds that give it a long list of potential uses.

Traditional Uses of Chaga

Chaga was commonly used for conditions such as cancer, ulcers, infection, and heart disease. In Russia and Siberia, chaga was used for general health-promoting effects. People drank chaga tea to prevent illness and infection and promote overall vitality and health.

+ Northern Europe

A lot of the traditional knowledge we have of the fungus today comes from the Khanty people of Siberia (formerly called the Ostyaks). This group had a strong affinity for the fungus which grew abundantly in the birch forests they lived in. They used it as an anthelmintic to kill parasites, to treat tubuculosis (TB), for digestive disorders (gastritis, ulcers, etc), for liver disease, and to prevent or treat heart dissease.

The Khanty people used chaga as a tea as it’s commonly used today — but they also smoked it, or topically by burning it and using the ash to make an antiseptic soap.

In some parts of Russia where chaga consumption was common, the USSR Ministry of Health noticed dramatic reductions in cancer rates among these popularions and attributed it to the consumption of chaga. It was then added to the official Soviet Pharmacopoea in 1955.

+ Asia

Chaga can also be found in the cold regions of Korea, Japan, and China. Here, chaga was used for its benefits on metabolic function, heart function, and for its antiseptic, anti-inflammatory, and antioxidant activities.

Herb Details: Chaga

Herbal Actions:

• Adaptogen
• Anti-Ulcer
• Anticancer
• Antinflammatory
• Antioxidant
• Antiviral
• Immunomodulator

Part Used

Fruiting Body

Family Name

Hymenochaetaceae

Distribution

Northern parts of the world in cluding Canada, Siberia, and Scandanavia. It grows exclusively where birch trees are found.

Constituents of Interest

• 3β-hydroxy-lanosta-8,24-dien-21-al
• Inotodiol
• Lanosterol
• Polysaccharides/beta-glucans

Common Names

• Chaga
• Birch Mushroom
• Cinder Conk
• Champignon de l’Immortalité
• Black Mass
• Birch Canker Polypore

Pregnancy

• There are no reports of toxicity or complications using chaga while pregnant

Duration of Use

• Long-term use of chaga is acceptable

Mycological Information

Chaga grows on various hardwood tree species — including birch (Betula spp.), oaks (Quercus spp.), poplar (Populus spp.), alder (Alnus spp.), ashes (Fagus spp.), and maple (Acer spp.). The most common species of tree you’re likely to find chaga on is birch.

There’s some debate as to whether chaga is parasitic or symbiotic. While it has clear parasitic tendencies, it also offers some benefits to the host tree that detract from the parasitic hypothesis — for example, when the tree becomes wounded, chaga will often form around the injury, protecting it from infection and further damage.

With that said, most of the current literature lists chaga as a parasitic fungi.

The lifecycle of this intriguing fungus is poorly understood. The hard, dark growths we know of as chaga is completely sterile. Only after the tree dies does the chaga mushroom begin to release spores. The fruiting bodies of the chaga form in the bark of the tree. They attract insects which devour the fruiting bodies very quickly. It’s believed the insects then carry the spores to a new host tree. very few chaga fruiting bodies have ever been found in nature.

When chaga spores find a new host they germinate and begin to grow under the bark. The growth is very slow, taking place over 5 to 7 years. Eventually, a black-colored blister begins to appear on the outside of the tree which is the part we use as medicine. Inside the hard black outer layer of the fungus is a soft core with a burnt-orange color.

Cultivation, Harvesting & Preparation

Harvesting chaga is difficult, and should only be done by experienced wild crafters to avoid damaging or killing the host tree. Usually, the wild-crafter will climb up to where the chaga is located, and using a saw or chisel, they’ll cut away chunks of the chaga — being careful not to damage the host tree underneath or remove too much of the fungus.

Preparing chaga can be difficult as well unless you buy it pre-ground or chopped. This fungus is extremely tough and hard to break into smaller pieces to make a tea with.

One of the best ways to prepare chaga for tea is to cut it into smaller pieces with a ban-saw. Smaller chunks can be added to a bag and beaten with a hammer into smaller pieces.

Chaga can then be added to a pot and simmered for 10-15 minutes to produce a dark, mildly bitter tea.

Pharmacology & Medical Research

+ Inflammation

Animal studies on chaga has revealed potent anti-microbial effects on experimental models of colitis [5]. Other animal studies have tested the effects of chaga on broader inflammatory models. One such study found that chaga extracts inhibited key inflammatory messengers such as nitric oxide (NO), prostaglandin E2 (PGE2) and tumor necrosis factor-α (TNF-α) [14].

+ Cancer

One of the most well-studied aspects of chaga is its effects on cancer. None of these studies are clinical trials. The majority of research involves in vitro or animal research.

There are hundreds of medicinal compounds in chaga alone, but three in-particular stand out in the literature for their potential anti-cancer effects — betulin, betulinic acid, and inotodiol.

The tetracyclic triterpene called inotodiol has been of particular interest by the scientific community studying the effects of chaga for cancer therapy. This compound has been shown to have direct anti-proliferative activities on lung adenocarcinoma cells (A549) [8].

Chaga grown on birch trees also contain some of the medicinal compounds from the host tree — such as betulin or betulinic acid. Both of these compounds have shown promising inhibitory activity on cancer cell lines as well (cutaneous, ovarian, and pulmonary) [9,10,11].

+ Antiviral

Innonotus obliquus was found to inhibit several viruses in vitro:

• Hepatitis C [2]

• Human Immunodeficiency Virus (HIV) [3]

• Herpes simplex virus I (HSV-I) [13]

+ Immunomodulation

Chaga endo-polysaccharide extract (BELYU1102) was shown to possess powerful immuno-stimulant activity in cell cultures. The extract was shown to increase proliferation of IgM antibodies in B cells, and lead to an increase in nitrite production, IL-6, IL-1, TNF-alpha, and iNOS in macrophages [4]. The endopolysaccharide fraction used in this study did not lead to a proliferation of T cells, the IL-2 expression of Th1 cells, or the IL-4 expression of Th2 cells. This suggests that chaga doesn’t directly kill cancer cells, but may lead to indirect inhibition of cancer growth through immuno-stimulation.

+ Metabolic Disorders

Chaga has a long history of use for metabolic disorders. Animal studies involving overfed, obese mice given chaga extracts had improved insulin sensitivity and reduced adiposity [6].

One animal study found a 31% reduction in blood sugar levels of diabetic mice given a chaga extract compared to the control group after just 3-weeks [12].

The mechanism of action for this effect is thought to be through an increase peroxisome proliferator-activated receptors γ transcriptional activities — which is a common therapeutic target for metabolic disorders such as diabetes and dyslipidaemia [7].

Pharmacology & Active Ingredients

Chaga contains hundreds of different compounds — many of which are still being explored for their use as medicine. The fungus is rich in compounds including polysaccharides, triterpenes (inotodiol), polyphenols, and various minerals.

Cautions & Safety Information:

Chaga is widely considered a safe herb, with no expected side effects from high doses, or long-term use.

With that said, anybody taking anti-diabetic or blood-thinner medications should avoid using chaga due to potential antagonistic reactions.

People on immuno-suppresive medications should also avoid this fungus. Chaga has direct immunostimulant activity and could weaken or negate the effects of the medication.

Author:

Justin Cooke, BHSc

The Sunlight Experiment

(Updated March 2020)

Recent Blog Posts:

References:

[1] — Lee, S. H., Hwang, H. S., & Yun, J. W. (2009). Antitumor activity of water extract of a mushroom, Inonotus obliquus, against HT‐29 human colon cancer cells. Phytotherapy Research, 23(12), 1784-1789.

[2] — Shibnev, V. A., Mishin, D. V., Garaev, T. M., Finogenova, N. P., Botikov, A. G., & Deryabin, P. G. (2011). Antiviral activity of Inonotus obliquus fungus extract towards infection caused by hepatitis C virus in cell cultures. Bulletin of experimental biology and medicine, 151(5), 612.

[3] — Shibnev, V. A., Garaev, T. M., Finogenova, M. P., Kalnina, L. B., & Nosik, D. N. (2015). Antiviral activity of aqueous extracts of the birch fungus Inonotus obliquus on the human immunodeficiency virus. Voprosy virusologii, 60(2), 35-38.

[4] — Kim, Y. O., Han, S. B., Lee, H. W., Ahn, H. J., Yoon, Y. D., Jung, J. K., ... & Shin, C. S. (2005). Immuno-stimulating effect of the endo-polysaccharide produced by submerged culture of Inonotus obliquus. Life Sciences, 77(19), 2438-2456.

[5] — Choi, S. Y., Hur, S. J., An, C. S., Jeon, Y. H., Jeoung, Y. J., Bak, J. P., & Lim, B. O. (2010). Anti-inflammatory effects of Inonotus obliquus in colitis induced by dextran sodium sulfate. BioMed Research International, 2010.

[6] — Lee, J. H., & Hyun, C. K. (2014). Insulin‐sensitizing and beneficial lipid‐metabolic effects of the water‐soluble melanin complex extracted from Inonotus obliquus. Phytotherapy research, 28(9), 1320-1328.

[7] — Joo, J. I., Kim, D. H., & Yun, J. W. (2010). Extract of Chaga mushroom (Inonotus obliquus) stimulates 3t3‐l1 adipocyte differentiation. Phytotherapy research, 24(11), 1592-1599.

[8] — Zhong, X. H., Wang, L. B., & Sun, D. Z. (2011). Effects of inotodiol extracts from Inonotus obliquus on proliferation cycle and apoptotic gene of human lung adenocarcinoma cell line A549. Chinese journal of integrative medicine, 17(3), 218-223.

[9] — Dehelean, C. A., Şoica, C., Ledeţi, I., Aluaş, M., Zupko, I., Gǎluşcan, A., ... & Munteanu, M. (2012). Study of the betulin enriched birch bark extracts effects on human carcinoma cells and ear inflammation. Chemistry Central Journal, 6(1), 137.

[10] — Fulda, S. (2008). Betulinic acid for cancer treatment and prevention. International journal of molecular sciences, 9(6), 1096-1107.

[11] — Drag, M., Surowiak, P., Drag-Zalesinska, M., Dietel, M., Lage, H., & Oleksyszyn, J. (2009). Comparision of the cytotoxic effects of birch bark extract, betulin and betulinic acid towards human gastric carcinoma and pancreatic carcinoma drug-sensitive and drug-resistant cell lines. Molecules, 14(4), 1639-1651.

[12] — Sun, J. E., Ao, Z. H., Lu, Z. M., Xu, H. Y., Zhang, X. M., Dou, W. F., & Xu, Z. H. (2008). Antihyperglycemic and antilipidperoxidative effects of dry matter of culture broth of Inonotus obliquus in submerged culture on normal and alloxan-diabetes mice. Journal of ethnopharmacology, 118(1), 7-13.

[13] — Pan, H. H., Yu, X. T., Li, T., Wu, H. L., Jiao, C. W., Cai, M. H., ... & Peng, T. (2013). Aqueous extract from a Chaga medicinal mushroom, Inonotus obliquus (higher basidiomyetes), prevents herpes simplex virus entry through inhibition of viral-induced membrane fusion. International journal of medicinal mushrooms, 15(1).

[14] — Park, Y. M., Won, J. H., Kim, Y. H., Choi, J. W., Park, H. J., & Lee, K. T. (2005). In vivo and in vitro anti-inflammatory and anti-nociceptive effects of the methanol extract of Inonotus obliquus. Journal of Ethnopharmacology, 101(1-3), 120-128.

Fish Mint (Houttuynia cordata)

What is Houttuynia?

Houttuynia is a Southeast Asian herb that’s spread all over the world as an invasive species. It’s common name “fish mint” refers to the strong fish-like aroma of the essential oil content. This characteristic flavor makes the herb useful as a flavoring in various dishes.

The fishy roots of the herb are also eaten as a vegetable in some Asian dishes.

Houttuynia is one of the most relevant herbs at the moment in the search for potential sources of medicine against the COVID-19 virus.

This herb has potent antiviral activity — shown to be active against SARS, as well as other coronaviruses, influenza, herpes type I and II, HIV, Dengue, and Chikungunya virus.

What is Houttuynia Used For?

Houttuynia is primarily used for bacterial and viral infections of the respiratory tract. It’s considered most effective if taken prophylactically, but may provide use during infection as well to slow the spread of the disease.

Other applications of the herb are for its diuretic effects, anti-allergic effects, anti-inflammatory actions, and for diabetes.

Traditional Uses of Houttuynia

In Southeast Asia, where houttuynia thrives, the leaves are used in a lot of local culinary dishes. The leaves have a characteristic “fishy” flavor and aroma that lend itself to some dishes as a garnish or spice. In parts of China, the roots are eaten in a dish called Zhé'ěrgēn.

Medicinally, fish mint has had a long history of use in Japan, Korea, China, and Vietnam for a wide range of conditions.

The leaves of the fish mint plant were traditionally used for the following:

• Digestive issues

• Insect bites

• Hypertension

• Constipation

• Hyperglycemia

• Influenza or other viral infections

• Pneumonia

• Kidney disorders

• Inflammation of the urinary tract

• Cough

• Insect repellant

Topically, the herb was used for sores, carbuncles, and inflammation.

In traditional Chinese medicine the herb was used to reduce heat.

Herb Details: Houttuynia

Herbal Actions:

• Antiviral
• Diuretic
• Antibacterial
• Anti-Anaphylactic
• Anti-Allergy
• Antinflammatory
• Febrifuge

[1, 2]

Weekly Dose

• (1:30 Decoction)
  15 – 30 Grams
• View Dosage Chart

Part Used

Aerial Parts

Roots Are Eaten as a Vegetable

Family Name

Saururaceae

Distribution

Southeast Asia

Constituents of Interest

• β-myrcene
• 2-undecanone

Common Names

• Fish Mint
• Chameleon Plant
• Houttuynia
• Chinese Lizard Tail
• Bishop's Weed
• Diếp cá (Vietnam)
• Yu Xing Cao (China)

CYP450

• Unknown

Quality

• Cold

Pregnancy

• Avoid houttuynia if pregnant or breastfeeding

Taste

• Pungent

Duration of Use

• Long-term use should be avoided (more than 2 months)

Botanical Information

Houttuynia is a member of the Saururaceae family of plants — which is often referred to as the lizards table family because of the characteristic tail-like appearance of the flower spikes.

There are only two members of the Houttuynia genus — Houttuynia cordata and Houttuynia emeiensis.

Despite the common name “fish mint” houttuynia has no relation to the mint family of plants.

All parts of the plant posess a unique flavor and aroma — which is best described as having a raw fish aroma, with some hints of citrus, lemon, sandalwood, or coriander.

There are reportedly two varieties of fish mint:

• Japanese Fish Mint — has more of a citrus aroma & flavor

• Chinese Fish Mint — has a fishy and coriander aroma & flavor

The leaves of the fish mint plant are heart-shaped, which can range from being dark green to light pink. The underside of the leaves has a purple hue. Some of the ornamental cultivars come in a wide variety of different color combinations.

Cultivation, Harvesting & Preparation

Houttuynia prefers growing in shady, moist environments and can even grow while slightly submerged in water. You can often find this herb growing nearby streams, and in deep forests. This herb is very resourceful and can be very difficult to get rid of.

Once houttuynia finds an area it likes it will take over completely — causing many regions to classify it as a potential threat to the environment.

It’s considered an invasive weed in places such as the United States, Australia, various pacific islands, and South America. It reportedly thrives in USDA Zones 5a to 9b.

In Asia, the herb can be found growing anywhere from sea level to around 2500 meters in altitude.

Fish mint loves water, so make sure to keep this one wet at all times. As long as the leaves remain above the water-level the plant will continue to thrive.

This herb is a perennial, growing up to 1 meter in height and spreading out in a 1 meter radius. It primarily spreads with the help of adventitious roots that creep along the moist soil of the rainforest bottom.

propagating the plant is best done from cuttings. The seeds of the plant are usually sterile.

Pharmacology & Medical Research

+ SARS-CoV 1 & 2

SARS (Severe Acute Respiratory Syndrome) is a life-threatening form of pneumonia caused by the SARS-CoV-1 virus. It began spreadin in late 2002 to 2003 from patient 0 in China. The disease eventually spread to over 8000 people around the world. As the world scrambled to find treatment, houttynia was shortlisted by Chinese researchers.

During this research, houttuynia was found to increase the proportion of CD4+ and CD8+ T cells [5].

CD4+ T-helper cells play a critical role in the adaptive immune system when dealing with bacterial or viral infections. These cells then pass along information to CD8 cytotoxic cells that can use three separate mechanisms to attack and kill the infection once identified.

The same study also showed houttuynia extract increased IL-2 and IL-10 activity — both of which are critical components in the adaptive immune response necessary to fight viral infection.

This study also looked at the direct effects of houttuynia extract on the SARS virus. The study found the extract had an inhibitory effect on SARS-CoV 3C-like protease (3CLpro) and RNA-dependent RNA polymerase (RdRp).

3C-like protease and SARS-CoV are both critically important for the life-cycle of the virus. These are two areas deemed critically important target in the search for potential prevention or treatment of the virus.

Now, in 2020, another closely related virus is currently causing a pandemic around the globe — SARS-CoV-2 (AKA COVID-19). As a result, houttuynia is being re-investigated as the world seeks to find a potential cure for the new and deadly virus.

+ Other Antiviral Activity

Houttuynia has been the subject of study for dozens of human and animal viruses — many of which the herb has shown primising inhibitory effects:

• Chikungunya virus [9]
• Human Immunodeficiency virus type 1 (HIV-1) [10]
• Herpes Simplex Virus type 1 (HSV-1) [10]
• Herpes Simplex Virus Type 2 (HSV-2)
• Influenza Virus [10]
• Enterovirus-71 [11]
• Dengue Virus Type 2 [12]

+ Antibacterial Activity

Houttuynia has a long history of use for treating respiratory tract infections of both viral and bacterial causes. This has prompted a lot of researcher to look at the effects of the herb on bacterial infections — particularily those developing resistance to antibiotics such as multi-drug resistant staphylococcus aureaus (MRSA).

One study found houttuynia posessed anti-bacterial effects against MRSA through direct bacteriocidal activity (inhibition of biofilm formation) and an induction of IL-8 [6] — which is one of the first responses triggered by the body during bacterial infection.

+ Cytotoxic Effects

There are five bioactive alkaloids isolated from houttuynia that have been shown to have cytotoxic effects agains human cancer cell lines (in vitro) [1]. This was only a preliminary study but offers evidence for further investigation.

The alkaloids used in the study included:

• A-549
• SK-OV-3
• SK-MEL-2
• XF-498
• HCT-15

+ Anti-Allergic Effects

A mice study investigated the anti-allergic effects of houttuynia by exploring the potential effects of the herb to prevent anaphylaxis — a severe allergic reaction [2].

The study found hoouttuynia water extract was able to inhibit induced systemic anaphylaxis in mice, as well as local allergic reactions by reducing the degranulation of mast cells, histamine release, and calcium uptake.

The study concluded by stating that "[houttuynia] may be beneficial in the treatment of mast cell-mediated anaphylactic responses.

Another animal study showed a houttuynia water-extract had an inhibitory effect on inhibited IgE-mediated systemic passive cutaneous anaphylaxis (in mice) [4].

+ Anti-Inflammatory Effects

An animal study exploring the anti-inflammatory effects of houttuynia found the volotile oil extract of the plant had an inhibitory effect on PGE2 — a potent inflammatory cytokine produced via the COX-2 enzyme [3]. This is the main inflammatory mediator inhibited by such medications as acetyl-salycilic-acid (Aspirin).

The same study also found houttuynia volotile oil reduced other key inflammatory messengers including nitric oxide (NO) and TNF‐α.

+ Effects of Houttuynia on Diabetes

An animal study on diabetic rats given houttuynia found the herb had protective effects on the pancreatic beta-cells through an upregulation of GLUT-4 and potential antioxidant activity [7].

The beta-cells are tasked with producing the body's insulin supply. As blood glucose levels rise, the glucose can damage sensitive tissues such as the beta-cells in the pancrease — leading to a further reduction of insulin activity and worsening of hyperglycemia.

GLUT-4 is the insulin-mediated transporter on the surface of our cells. Insulin binds to GLUT-4 to pull glucose molecules inside where they're converted into energy.

Phytochemistry

+ Essential Oil Content

• 2-undecanone (methyl nonyl ketone)
• Myrcene
• Houttuynin (decanoyl acetaldehyde/3-oxo-dodecanal)
• Decanal
• (E)-caryophyllene
• Decanoic ac id
• Camphene
• β-pinene
• Lauraldehyde
• Bornyl acetate
• α-pinene
• Limonene
• 4-terpineol
• Caryophyllene oxide
• Nonanol
• linalool
  

Source: [8]

Cautions & Safety Information:

Houttuynia has been reported to cause severe allergic reactions in some people.

Avoid using this herb if pregnant or breastfeeding. There is not enough evidence to prove the herb is safe during pregnancy.

Author:

Justin Cooke, BHSc

The Sunlight Experiment

(Updated March 2020)

Recent Blog Posts:

References:

1. Kim, S. K., Ryu, S. Y., No, J., Choi, S. U., & Kim, Y. S. (2001). Cytotoxic alkaloids fromHouttuynia cordate. Archives of pharmacal research, 24(6), 518-521.

2. Li, G. Z., Chai, O. H., Lee, M. S., Han, E. H., Kim, H. T., & Song, C. H. (2005). Inhibitory effects of Houttuynia cordata water extracts on anaphylactic reaction and mast cell activation. Biological and Pharmaceutical Bulletin, 28(10), 1864-1868.

3. Li, W., Fan, T., Zhang, Y., Fan, T., Zhou, P., Niu, X., & He, L. (2013). Houttuynia cordata Thunb. Volatile Oil Exhibited Anti‐inflammatory Effects In Vivo and Inhibited Nitric Oxide and Tumor Necrosis Factor‐α Production in LPS‐stimulated Mouse Peritoneal Macrophages In Vitro. Phytotherapy Research, 27(11), 1629-1639.

4. Han, E. H., Park, J. H., Kim, J. Y., & Jeong, H. G. (2009). Houttuynia cordata water extract suppresses anaphylactic reaction and IgE-mediated allergic response by inhibiting multiple steps of FcεRI signaling in mast cells. Food and chemical toxicology, 47(7), 1659-1666.

5. Lau, K. M., Lee, K. M., Koon, C. M., Cheung, C. S. F., Lau, C. P., Ho, H. M., ... & Tsui, S. K. W. (2008). Immunomodulatory and anti-SARS activities of Houttuynia cordata. Journal of Ethnopharmacology, 118(1), 79-85.

6. Sekita, Y., Murakami, K., Yumoto, H., Mizuguchi, H., Amoh, T., Ogino, S., ... & Kashiwada, Y. (2016). Anti-bacterial and anti-inflammatory effects of ethanol extract from Houttuynia cordata poultice. Bioscience, biotechnology, and biochemistry, 80(6), 1205-1213.

7. Kumar, M., Prasad, S. K., Krishnamurthy, S., & Hemalatha, S. (2014). Antihyperglycemic activity of Houttuynia cordata Thunb. in streptozotocin-induced diabetic rats. Advances in pharmacological sciences, 2014.

8. Verma, R. S., Joshi, N., Padalia, R. C., Singh, V. R., Goswami, P., Kumar, A., ... & Saikia, D. (2017). Chemical Composition and Allelopathic, Antibacterial, Antifungal, and Antiacetylcholinesterase Activity of Fish‐mint (Houttuynia cordataThunb.) from India. Chemistry & biodiversity, 14(10), e1700189.

Rhodiola (Rhodiola rosea)

Rhodiola Summary

Rhodiola was made famous by some earlier research done by Russian scientists in the 1960's. Although a lot of this research still hasn't been released to the public, there has been a lot of new studies put forward to make up for this loss.

Rhodiola is well revered as an adaptogen for treating fatigue, cognitive decline, depression, and for athletic enhancement. It's considered to be a mild stimulant, though it doesn't produce the "wired" feeling many other stimulants produce. It increases energy levels and makes us more tolerant of stressful situations.

Although there is still a lot of research lacking, we know that Rhodiola can reduce cortisol levels in the body after exposure to stress, however, the details on how this interaction exists is still not well understood. There is also a great deal of confusion around which chemicals are active in the herb, some studies showing the rosavins, others tyrosol and the rhodiolasides.

As a result, each manufacturer tends to have a preference for one chemical group over the other in their products.

What is Rhodiola Used For?

*Rhodiola rosea* is mainly used for its adaptogenic qualities, especially those specific to lowering cortisol levels. It's reliable for improving fatigue in debilitated or chronically fatigued people, as well as those experiencing generalized adaptive disorder, depression, or acute periods of extreme stress.

Rhodiola is a popular nootropic additive for increasing focus and mental endurance and is popular among athletes for increasing physical endurance as well.

Herb Details: Rhodiola

Weekly Dose

• (1:2 Liquid Extract)
  20–40 mL
• View Dosage Chart

Part Used

• Root/Rhizome

Family Name

• Crassulaceae

Distribution

• Northern climates of North America, Asia, and Europe

Herbal Actions:

• Adaptogen
• CNS Stimulant (mild)
• Antidepressant
• Cardioprotective
• Nootropic

Constituents of Interest

• Rosavin
• Tyrosol
• Salidroside
• Rhodiolaside

Common Names

• Rhodiola
• Rose Root
• Arctic Root
• Golden Root
• King's Crown

CYP450

Unknown

Duration of Use

• Long-term use of rhodiola is acceptable.

Botanical Information

Although Rhodiola rosea is the preferred species used, there are many species used in various indigenous medical systems such as Rhodiola alterna, Rhodiola brevipetiolata, Rhodiola crenulata, Rhodiola kirilowii, Rhodiola quadrifida, Rhodiola sachalinensis, and Rhodiola sacra.

The Crassulaceae family contains 34 genera and 1400 species. Most of the plants in this family can be found in colder climates.

Another medicinal species in this family is Kalanchoe.

Habitat Ecology, & Distribution:

Rhodiola grows at high altitude, mountainous regions of Europe, Asia, the Arctic, and North America.

Pharmacology & Medical Research

+ Altitude Sickness

Salidroside and Tyrosol from Rhodiola cerrulea extracts have been shown to regulate AMPK [11], which plays a major role in energy homeostasis [10]. It was also shown to maintain sodium channel transport by preserving NA+, K+, ATPase activity. The authors concluded that this mechanism may be responsible for Rhodiolas ability to reduce the symptoms of altitude sickness, particularly HAPE [11].

+ CNS Stimulant

Numerous clinical trials have demonstrated the CNS stimulating activity of Rhodiola rosea [8] based on various cognitive and fatigue scores.

Other studies have found the use of rhodiola at varying doses inconclusive as a stimulant [7].

+ Memory & Cognitive Performance

Rhodiola extracts have been shown in animal models to improve learning capacity and short/long-term memory in animals trained to perform certain tasks [2].

Rhodiola has been shown to inhibit monoamine oxidase (both MAO-A and MAO-B) in animal studies [4].

+ Depression

MAO-A inhibitors are effective in the treatment of depression [20]. Rhodiola has been shown to inhibit MAO-A & B in animal studies [4]. Other animal studies investigating the use of rhodiola on depression has shown a non-dose dependent improvement on depression scores in mice, which is due to the tyrosin and rhodiolaside content specifically [16, 18, 19].

A randomized double-blind clinical trial using a standardized Rhodiola rosea extract showed a significant antidepressant activity in the treatment group compared to placebo. This was based on various depressive symptoms including insomnia, emotional instability, and somatization. [17].

+ Stress And Fatigue (Adaptogenic)

A group of 56 healthy physicians in a double-blind randomized clinical trial were either given Rhodiola rosea extracts or placebo control for 2 weeks. Physicians were chosen based on criteria that investigated the likelihood that these physicians would experience mental exhaustion during a normal shift. A series of tasks were then given after each night shift to investigate any changes on mental fatigue as measured by a set of complex tasks. All of the physicians treated with Rhodiola rosea were noted to show improved test scores compared to those not treated with the herb. These effects were observed to be most active after two weeks of use, and not a single adverse reaction was reported during the study. [3].

Another study investigating the mental and physical effects of a long term, low dose (SHR-5 50 mg) on students during examination periods found significant improvements on test scores among the treatment group [9]. They were looking for the presence of mental and physical fatigue indications. The only test that showed no improvement in this study was the tapping test (muscular activation).

A study investigating the effects of Rhodiola rosea on free cortisol levels in chronically fatigues patients noted a reduction in cortisol levels after just a single treatment, and significantly after a 28-day course of treatment [21]. Rhodiola was also shown to reduce serum blood levels of cortisol after a stressful event in rabbits [22].

Animal research has shown that Rhodiola rosea extracts can reduce the expression of c-Fos in the hypothalamus of rats [23]. The expression of this gene is considered to be a valuable marker for identifying the activation of cells in the central nervous system associated with the stress response [24]. This suggests the mechanism of action for Rhodiola rosea on reducing cortisol levels is the result of HPA modulation in the hypothalamus, such as increasing feedback sensitivity and therefore reducing overall CRH release rather than acting directly on the adrenal glands.

+ Withdrawal

A Rhodiola rosea extract was shown to improve withdrawal symptoms in mice, with a noted increase in 5HT activity in treated animals. [1].

Clinical Applications Of Rhodiola:

Rhodiola serves as a reliable adaptogen with little to no side effects noted in any of the studies listed. It's useful for those suffering from high-stress conditions, chronically fatigued, or depressed.

This herb is also useful for increasing athletic performance in athletes and reducing the chances of being affected by altitude sickness when traveling above 2500 meters.

Cautions:

Caution when using Rhodiola with mania as the mental stimulation may produce negative side effects.

Author:

Justin Cooke, BHSc

The Sunlight Experiment

(Updated May 2019)

Recent Blog Posts:

References

1. Mannucci, C., Navarra, M., Calzavara, E., Caputi, A. P., & Calapai, G. (2012). Serotonin involvement in Rhodiola rosea attenuation of nicotine withdrawal signs in rats. Phytomedicine, 19(12), 1117-1124. [animal studies]

2. Petkov, V. D., Yonkov, D., Mosharoff, A., Kambourova, T., Alova, L., Petkov, V. V., & Todorov, I. (1986). Effects of alcohol aqueous extract from Rhodiola rosea L. roots on learning and memory. Acta physiologica et pharmacologica Bulgarica, 12(1), 3-16. [animal studies]

3. Darbinyan, V., Kteyan, A., Panossian, A., Gabrielian, E., Wikman, G., & Wagner, H. (2000). Rhodiola rosea in stress induced fatigue—a double blind cross-over study of a standardized extract SHR-5 with a repeated low-dose regimen on the mental performance of healthy physicians during night duty. Phytomedicine, 7(5), 365-371. [RCT]

4. Van Diermen, D., Marston, A., Bravo, J., Reist, M., Carrupt, P. A., & Hostettmann, K. (2009). Monoamine oxidase inhibition by Rhodiola rosea L. roots. Journal of ethnopharmacology, 122(2), 397-401. [animal studies]

5. Ganzera, M., Yayla, Y., & Khan, I. A. (2001). Analysis of the marker compounds of Rhodiola rosea L.(golden root) by reversed phase high performance liquid chromatography. Chemical and pharmaceutical bulletin, 49(4), 465-467. [chemical analysis]

6. Panossian, A., Wikman, G., & Sarris, J. (2010). Rosenroot (Rhodiola rosea): traditional use, chemical composition, pharmacology and clinical efficacy. Phytomedicine, 17(7), 481-493. [review article]

7. Shevtsov, V. A., Zholus, B. I., Shervarly, V. I., Vol'skij, V. B., Korovin, Y. P., Khristich, M. P., ... & Wikman, G. (2003). A randomized trial of two different doses of a SHR-5 Rhodiola rosea extract versus placebo and control of capacity for mental work. Phytomedicine, 10(2), 95-105. [RCT]

8. Panossian, A., & Wagner, H. (2005). Stimulating effect of adaptogens: an overview with particular reference to their efficacy following single dose administration. Phytotherapy Research, 19(10), 819-838. [Review]

9. Spasov, A. A., Wikman, G. K., Mandrikov, V. B., Mironova, I. A., & Neumoin, V. V. (2000). A double-blind, placebo-controlled pilot study of the stimulating and adaptogenic effect of Rhodiola rosea SHR-5 extract on the fatigue of students caused by stress during an examination period with a repeated low-dose regimen. Phytomedicine, 7(2), 85-89. [RCT].

10. Lee, S. Y., Shi, L. S., Chu, H., Li, M. H., Ho, C. W., Lai, F. Y., ... & Chang, T. C. (2013). Rhodiola crenulata and its bioactive components, salidroside and tyrosol, reverse the hypoxia-induced reduction of plasma-membrane-associated Na, K-ATPase expression via inhibition of ROS-AMPK-PKCξ pathway. Evidence-Based Complementary and Alternative Medicine, 2013. [in vitro].

11. Reznick, R. M., & Shulman, G. I. (2006). The role of AMP‐activated protein kinase in mitochondrial biogenesis. The Journal of physiology, 574(1), 33-39.

12. Kerharo, J., & Adam, J. G. (1974). La pharmacopée sénégalaise traditionnelle: plantes médicinales et toxiques. (Pharmacopoeia).

13. Steinegger, E., & Hansel, R. (1992). Pharmakognosie 5 Aufl. Kap 6.2. 1. Freie Phenolcarbonsauren Springer Verlag Berlin. (Pharmacopoeia).

14. Hjaltalin, O. J. (1830). Islenzk grasafrædi. Koben havn.

15. insert

16. Kurkin, V. A., Dubishchev, A. V., Ezhkov, V. N., Titova, I. N., & Avdeeva, E. V. (2006). Antidepressant activity of some phytopharmaceuticals and phenylpropanoids. Pharmaceutical Chemistry Journal, 40(11), 614-619.

17. Darbinyan, V., Aslanyan, G., Amroyan, E., Gabrielyan, E., Malmström, C., & Panossian, A. (2007). Clinical trial of Rhodiola rosea L. extract SHR-5 in the treatment of mild to moderate depression. Nordic journal of psychiatry, 61(5), 343-348.

18. Perfumi, M., & Mattioli, L. (2007). Adaptogenic and central nervous system effects of single doses of 3% rosavin and 1% salidroside Rhodiola rosea L. extract in mice. Phytotherapy Research, 21(1), 37-43.

19. Panossian, A., Nikoyan, N., Ohanyan, N., Hovhannisyan, A., Abrahamyan, H., Gabrielyan, E., & Wikman, G. (2008). Comparative study of Rhodiola preparations on behavioral despair of rats. Phytomedicine, 15(1-2), 84-91.

20. Priest, R. G., Gimbrett, R., Roberts, M., & Steinert, J. (1995). Reversible and selective inhibitors of monoamine oxidase A in mental and other disorders. Acta Psychiatrica Scandinavica, 91(s386), 40-43.

21. Olsson, E. M., von Schéele, B., & Panossian, A. G. (2009). A randomised, double-blind, placebo-controlled, parallel-group study of the standardised extract shr-5 of the roots of Rhodiola rosea in the treatment of subjects with stress-related fatigue. Planta medica, 75(02), 105-112.

22. Panossian, A., Hambardzumyan, M., Hovhanissyan, A., & Wikman, G. (2007). The adaptogens Rhodiola and Schizandra modify the response to immobilization stress in rabbits by suppressing the increase of phosphorylated stress-activated protein kinase, nitric oxide and cortisol. Drug target insights, 2, 117739280700200011.

23. Xia, N., Li, J., Wang, H., Wang, J., & Wang, Y. (2016). Schisandra chinensis and Rhodiola rosea exert an anti-stress effect on the HPA axis and reduce hypothalamic c-Fos expression in rats subjected to repeated stress. Experimental and therapeutic medicine, 11(1), 353-359.

24. Luckman, S. M., Dyball, R. E., & Leng, G. (1994). Induction of c-fos expression in hypothalamic magnocellular neurons requires synaptic activation and not simply increased spike activity. Journal of Neuroscience, 14(8), 4825-4830.

Chinese Clubmoss (Huperzia serrata)

What is Chinese Club Moss?

Chinese clubmoss, (otherwise known as Chinese firmoss) is a type of moss found in subtropical parts of Southern China, India, and the United States.

The whole herb can be used as a cognitive enhancer, and to treat organophosphate poisoning and neurodegenerative disorders like Alzheimer's disease and Parkinson's disease.

The main form this herb can be found in, however, is its concentrated extract of the alkaloid huperzine-A.

Huperzine-A is a popular addition to nootropic formulas for its ability to inhibit acetylcholinesterase. Thus improving reaction times, memory retrieval and storage, and preventing or slowing the onset of Alzheimer's disease. The potency of this chemical is astounding, as less than a mg of the extract is necessary to reach a therapeutic dose.

Huperzine-A can be found alone but is best taken in a formulation or stacked with other nootropic formulas. It's especially beneficial when in combination with racetams like piracetam or aniracetam, or choline donors like alpha-GPC.

You can find huperzine-A in formulas like Onnit Alpha-Brain, or by itself.

+ Mechanisms

• Acetylcholinesterase inhibitor
• NDMA modulator
• Antiglutamate

What is Chinese Clubmoss Used For?

Clubmoss isn't commonly used in Western herbal medicine but has a long history of use in traditional Chinese medicine. With that said, the most common uses for this herb are for treating neurological disorders — primarily involving memory loss.

The nootropic supplement huperzine-A is popular for enhancing focus and concentration. There is virtually no clinical research on the safety or effectiveness of this compound, however.

Traditional Uses of Chinese Clubmoss (Firmoss)

Usage of this herb can be traced all the way back to the Tang dynasty in China. It was mainly used during this time to treat rheumatism, colds and flus, and to relax the muscles and tendons.

More modern Chinese medicinal uses include bruises, sprains, poor circulation, swelling, organophosphate poisoning, myasthenia gravis, schizophrenia, and Alzheimers.

Herb Details: Chinese Clubmoss

Herbal Actions:

• Nootropic
• Neuroprotective
• Antioxidant

Daily Dose

• (Concentrated Huperzine-A Extract)
  50–200 mcg/day
• View Dosage Chart

Otheer Relevant Species

• Lycopodium serratum
• Huperzia elmeri
• Huperzia carinat
• Huperzia aqualupian

Part Used

• Whole herb

Family Name

• Lycopodiaceae

Distribution

• Clubmoss is found worldwide — thee species most commonly used for its huperzinee-A content (Huperzia serrata) is found predominantly in Asia.

Constituents of Interest

• Huperzine-A

Common Names

• Chinese Firmoss
• Qian Ceng Ta (China)
• "Thousand layer pagoda"
• Ground pine
• Creeping cedar
• Shi Song (China)

CYP450

Unknown

Duration of Use

• Avoid long-term use in therapeutic doses.

Botanical Information

All club mosses differ from true mosses by their vascular structure. Like other moss, Chinese clubmoss reproduces via spores instead of seeds.

These plants can live a very long time, and only grow up to 10 cm in height.

Habitat Ecology, & Distribution:

Huperzia serrata originates from India, and Southeast China, but are distributed worldwide. They tend to be easily found in subtropical zones in the United States and Southern China.

Due to the value of this herb as a cognitive enhancer, it has been over-harvested in many places where it can be found.

Pharmacology & Medical Research

+ Cognitive Enhancement:

Huperzia serrata contains an alkaloid known as huperzine-A. This alkaloid has been shown to produce anti-acetylcholinesterase activities in the brain [6-]. With fewer enzymes breaking down the acetylcholine, this neurotransmitter becomes more abundant and is more readily available for presynaptic neurons.

Huperzine-A is more effective at inhibiting acetylcholinesterase due to its ability to pass the blood-brain barrier more readily than other medications [9].

Additionally, huperzine-A has been reported to act as an NDMA receptor agonist. This results in a greater release of nerve growth factor (NGF) in the brain.

+ Alzheimer's Disease

There have been several reviews, including a Cochrane review on this herb for the treatment of Alzheimer's disease. All of these studies have noted a possible improvement in Alzheimer's therapy following Huperzine-A containing species. However, all noted a lack of large, long-term, clinical trials on the subject. [6-8].

The primary mechanism of action is suggested to be through a reduction in acetylcholinesterase, and subsequent amyloid beta plaquing on the neurons. [6].

+ Anti-Seizure

C#urrently, huperzine-A has been shown to posess anticonvulsant activity in mice [10]. Further studies are now underway.

+ Parkinson's Disease

Currently, only mice trials have been conducted. Protective effects have been noted in these mice trials, however. [11].

Phytochemistry

An alkaloid known as huperzine-A is currently regarded as the main active ingredient for the cognitive enhancing effects of Huperzia serrata.

This alkaloid is suggested to account for roughly 0.1% of the dry weight of the herb [1]. Analogs of both Huperzine-A and Huperzine-B have both been made. [3-5].

A similar alkaloid is also contained known as fordine.

In total, this herb contains flavonoids, alkaloids (lycopodine, lycodines including huperzine-A, fawcettimines, and more), triterpenes, flavones, and phenolic acids. [2].

Cautions

This is a very safe herb to use, even in its concentrated extraction form of Huperzine-A. Side effects of the concentrated extract can include gastrointestinal discomfort and upset, restlessness, headaches, high blood pressure, sweating, appetite suppression. 

Never use huperzine-A supplements while pregnant or breastfeeding.  

Chinese clubmoss is not recommended for people with heart disease, seizure disorders, emphysema, or urinary tract blockages.

Consult your doctor if taking other medications and wish to take Huperzia spp. supplements or concentrated extracts.

Synergy

A common addition to nootropic formulas for its cholinergic actions. It's suggested to be especially beneficial with racetams like piracetam due to similar effects on acetylcholine.

Author:

Justin Cooke, BHSc

The Sunlight Experiment

(Updated May 2019)

Recent Blog Posts:

References:

1. Yu CM, Tang XC, Liu JS, Han YY, inventors. Huperzines and analogs. US Patent 5,177,082. January 5, 1993.

2. Ma X, Tan C, Zhu D, Gang DR, Xiao P. Huperzine A from Huperzia species—an ethnopharmacolgical review. J Ethnopharmacol . 2007;113(1):15-34.

3. Darrouzain F, André C, Ismaili L, Matoga M, Guillaume YC. Huperzine A—human serum albumin association: chromatographic and thermodynamic approach. J Chromatogr B Analyt Technol Biomed Life Sci . 2005;820(2):283-288.

4. Jiang H, Luo X, Bai D. Progress in clinical, pharmacological, chemical and structural biological studies of huperzine A: a drug of traditional Chinese medicine origin for the treatment of Alzheimer's disease. Curr Med Chem . 2003;10(21):2231-2252.

5. Dvir H, Jiang HL, Wong DM, et al. X-ray structures of Torpedo californica acetylcholinesterase complexed with (+)-huperzine A and (-)-huperzine B: structural evidence for an active site rearrangement. Biochemistry . 2002;41(35):10810-10818.

6. Li J, Wu HM, Zhou RL, Liu GJ, Dong BR. Huperzine A for Alzheimer's disease. Cochrane Database Syst Rev . 2008;(2):CD005592

7. Desilets AR, Gickas JJ, Dunican KC. Role of huperzine A in the treatment of Alzheimer's disease. Ann Pharmacother . 2009;43(3):514-518.

8. Kelley BJ, Knopman DS. Alternative medicine and Alzheimer disease. Neurologist . 2008;14(5):299-306.

9. Wang R, Yan H, Tang XC. Progress in studies of huperzine A, a natural cholinesterase inhibitor from Chinese herbal medicine. Acta Pharmacol Sin . 2006;27(1):1-26.

10. Bialer M, Johannessen SI, Kupferberg HJ, Levy RH, Perucca E, Tomson T. Progress report on new antiepileptic drugs: a summary of the Eigth Eilat Conference (EILAT VIII). Epilepsy Res . 2007;73(1):1-52.

11. Chen LW, Wang YQ, Wei LC, Shi M, Chan YS. Chinese herbs and herbal extracts for neuroprotection of dopaminergic neurons and potential therapeutic treatment of Parkinson's disease. CNS Neurol Disord Drug Targets . 2007;6(4):273-281