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.

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.

Elderberry (Sambucus nigra)

What is Elderberry?

Elder is an invasive tree spread throughout most of the world.

It can be found in cold climates like Canada and Scandinavian countries, as well as tropical areas in Central and South America, Southeast Asia, and Australia.

Elder trees are even frequently found in remote areas like the Pacific Islands.

Elder has many uses, especially for upper respiratory infections for its antitussive and antiviral activity.

As an antiviral, it has a relatively narrow range of efficacy, which is specific to enveloped viruses like influenza, and will only have a potent effect in the early stages of viral infection. Elder is highly effective for early-stage viral infection and one of the best herbs to keep around in in the event of early signs of cold or flu.

Featured Elder Products

Elder Extract

Herb Pharm

Made from the berries of Sambucus nigra

Shop Now

Elder Berries

Starwest Botanicals

Dried berries of Sambucus nigra

Shop Now

Sambucol® Syrup

PharmaCare

Made from Sambucus nigra

Shop Now

What is Elder Used For?

Elder is primarily used in the acute stage of respiratory infections. it has the unique ability to structurally inhibit the reproductive cycle of the influenza virus. If used in the early stages of infection elder can be used to prevent widespread infection.

elder is also used for its ability to interact with the central nervous system. For this effect, elder is often used for nerve-related pain.

Traditional Uses of Elder

The use of elder dates back a very long time. Evidence of elder seeds, pollen, and dried fruits have been found at a Bronze Age archaeological site in Tuscany (Italy) [12], a Neolithic site in the French Alps [13], and Durankulak site the Black Sea coast and north-eastern Bulgaria [13].

Elder is used in Ayurvedic medicine, but not in depth. Its berries are used primarily as a diuretic, and aperient, while the bark as a hydragogue, cathartic and anti-epileptic.

In traditional Chinese medicine, elder is known as "mao gu xiao" (Sambucus formosana or Sambucus chinensis) is used (rarely) to treat liver disease. It's considered to be a warm bitter, useful for dispelling blood stasis.

In Indonesia, elder (Sambucus javanica) is used for pain relief, beri beri, and jaundice.

In Western herbal medicine, elder is most commonly used to treat sore throats, and as a purgative or emetic. It's also used to treat wounds (the leaves mainly), or as a diuretic (whole plant).

Elder was commonly combined with herbs like yarrow or boneset in the treatmeent of cold and flu.

Herb Details: Elder

Herbal Actions:

• Antiviral
• Emetic (high doses)
• Antitussive
• Nervine (leaves)

Weekly Dose

• (1:2 Liquid Extract)
  15-40 mL
• View Dosage Chart

Part Used

Flowers and berries

In some cases the leaves, bark, and roots can also be used with caution.

Family Name

Caprifoliaceae

Distribution

Invasive the world over. Common in North America, Western Asia, Europe, The Pacific Islands, and Austalia.

Sambucus australasica and Sambucus gaudichaudiana (Australian white elder) are found primarily in Australia and South America.

Constituents of Interest

• Cyanidin-3-O-glucoside
• Ribosome-inactivating proteins (RIPs)

Common Names

• Elder
• Black Elder
• Elderberry
• European Elder

Botanical Information:

There are about 30 different species of elder, 3 of which are most commonly used as medicine. The common names for these species include blue elder (Sambucus nigra), red elder (Sambucus racemosa), and white elder (Sambucus australasica).

Phytochemistry

+ Constituent Breakdown:

Elder contains several hundred compounds.

This includes phosphorous (high), vitamins A, B6, and C.

Also contained are polyphenols, anthocyanins (blue-berries)(cyanidin 3-glucoside, cyanidin-3-sambubioside, cyanidin-3, 5-diglucoside, and cyanidin-3-sambubioside-5-glucoside), anthoxanthins (white berries), ribosome-inactivating proteins (RIPs) (TYPE 2 RIPs; nigrin b, basic nigrin b, SNA, SNA1, and SNLRP, nigrin f, nigrin s, ebulin 1, ebulin r1, ebulin r2. TYPE 1 RIPs; ebulitins), flavonol glycosides (quercetin-3-O-rutinoside, kaempferol-3-O-rutinoside and isorhamnetin-3-O-rutinoside (about 90% of the total flavonoid content)), phenolic acids (5-O-cafeoylquinic acid and 1,5-di-O-caVeoylquinic acid (about 70% of the total phenolic acid content)), triterpenoids (ursolic acid),

Key Compounds Found in Elder:

Chemical class	Chemical Name	Pharmacology
Flavonoid pigments	Anthocyanins (S. nigra/canadensis) and anthoxanthins (S. australasica)	Water soluble flavonoids that are absorbed through the small intestine and reach peak concentration systemically after 30-60 minutes. They Remain mostly un metabolised before being excreted in the urine.
Flavonol glycosides	quercetin-3-O-rutinoside, kaempferol-3-O-rutinoside and isorhamnetin-3-O-rutinoside (about 90% of the total flavonoid content)	Some have been found to bind to viral membranes, possibly delivering main mechanism of actions through hemagglutinin, M2 ion channel, and neuraminidase inhibition.
Phenolic acids	5-O-caVeoylquinic acid and 1,5-di-O-caVeoylquinic acid (about 70% of the total phenolic acid content).	Caffeoylquinic acids are mainly found in the plasma and urine as hydroxycinnamate metabolites. Research has suggested that most of the absorption is done in the upper GIT. Peak concentration varies greatly, ranging from 30 min to 6 hours (Tmax).
Triterpenes	Ursolic acid	Downregulates MMP-9 and inhibits COX-2. Reach peak concentration in the blood after 1 hour. Half life is 4 hours.
Lignans	Nigrin b, basic nigrin b, SNA, SNA1, and SNLRP, nigrin f, nigrin s, ebulin 1, ebulin r1, ebulin r2 (type 2 RIPs). ebulitins (Type 1 RIP)	RIPs have been shown to bind to viral envelop proteins, and have shown activity on sialic acid in the GIT (not confirmed in the repiratory epithelial tissue). The pharmacokinetics are not well understood.

What's The Deal With Elders Toxicity Claims?

A group of compounds found in elder called lectins are closely related to the common rat poison — ricin.

Leptins are essentially proteins that can bind with sugars. If leptins like ricin get into the cells, they can interact with our ribosomes (the organelle that does most of the manufacturing of proteins and various other compounds).

The common name given to leptins like ricin that stop the ribosomes from working is referred to as "Ribosome-Inactivating Proteins" or RIPs for short.

RIPs are also thought to be protective against viruses and predators, as well as a way for the plant to store nitrogen.

Several RIPs have been isolated from black elder [18-20].

Similar lectin-compounds can be found in other medicinal plants with similar uses (antiviral), and limitations (emetic) — Phytolacca americana (Phytolacca antiviral protein or PAP).

There are three types of RIPs: Type 1, type 2, and type 3. [19, 20].

Both ebulin and ricin are type two RIPs.

How Elder Leptins Are Different Than Ricin

Despite structural similarities, elder isn't as toxic as ricin — and it's not as toxic as we once thought.

The Ld50 of ebulin 1 was 250 mg/kg, compared to ricins 0.023 µg/kg (intraperitoneal) and 0.0075 µg/kg (intravenous) [22] — that's a huge difference. You would essentially need more than 9000 times the dose of ebulin 1 compared to ricin to reach the same toxic dose.

There are some exceptions.

RIPs such as ebulin f and SELfd are toxic and resist breakdown in the stomach — leading to gastrointestinal irritation and upset.

The solution to this problem is to heat it before using it. The heat breaks reverse the ability for these RIPs to be broken down by pepsin in the stomach — thus preventing the toxic side-effects of ebulin f. [21, 25].

Clinical Applications Of Elder:

Elder is a great antiviral herb, especially for Influenza and some of the other enveloped viral species if used at the early stages of infection.

Cautions:

Elder is an emetic, especially in preparations that contain fresh plant material (unheated). If nausea occurs, dial back the dose. Contrary to popular belief elder is NOT poisonous. Emetics are frequently misinterpreted to be dangerously poisonous.

Elder is thought to decrease the effectiveness of morphine.

+ Contraindications

• Small children
• Caution advised with larger doses

Author:

Justin Cooke, BHSc

The Sunlight Experiment

(Updated May 2019)

Recent Blog Posts:

References:

1. Zakay-Rones, Z., Varsano, N., Zlotnik, M., Manor, O., Regev, L., Schlesinger, M., & Mumcuoglu, M. (1995). Inhibition of several strains of influenza virus in vitro and reduction of symptoms by an elderberry extract (Sambucus nigra L.) during an outbreak of influenza B Panama. The Journal of Alternative and Complementary Medicine, 1(4), 361-369. [in vitro]

2. Chen, C., Zuckerman, D. M., Brantley, S., Sharpe, M., Childress, K., Hoiczyk, E., & Pendleton, A. R. (2014). Sambucus nigra extracts inhibit infectious bronchitis virus at an early point during replication. BMC veterinary research, 10(1), 24. [in vitro]

3. Mascolo, N., Capasso, F., Menghini, A., & Fasulo, M. P. (1987). Biological screening of Italian medicinal plants for anti‐inflammatory activity. Phytotherapy research, 1(1), 28-31.[in vitro]

4. Yeşilada, E., Üstün, O., Sezik, E., Takaishi, Y., Ono, Y., & Honda, G. (1997). Inhibitory effects of Turkish folk remedies on inflammatory cytokines: interleukin-1α, interleukin-1β and tumor necrosis factor α. Journal of Ethnopharmacology, 58(1), 59-73. [in vtro]

5. Harokopakis, E., Albzreh, M. H., Haase, E. M., Scannapieco, F. A., & Hajishengallis, G. (2006). Inhibition of proinflammatory activities of major periodontal pathogens by aqueous extracts from elder flower (Sambucus nigra). Journal of periodontology, 77(2), 271-279. [in vitro]

6. Abuja, P. M., Murkovic, M., & Pfannhauser, W. (1998). Antioxidant and prooxidant activities of elderberry (Sambucus nigra) extract in low-density lipoprotein oxidation. Journal of Agricultural and Food Chemistry, 46(10), 4091-4096. Link. [in vitro]

7. Murkovic, M., Adam, U., & Pfannhauser, W. (2000). Analysis of anthocyane glycosides in human serum. Fresenius' journal of analytical chemistry, 366(4), 379-381. [in vitro].

8. Serkedjieva, J., Manolova, N., Zgórniak‐Nowosielska, I., Zawilińska, B., & Grzybek, J. (1990). Antiviral activity of the infusion (SHS‐174) from flowers of Sambucus nigra L., aerial parts of Hypericum perforatum L., and roots of Saponaria officinalis L. against influenza and herpes simplex viruses. Phytotherapy Research, 4(3), 97-100. [in vitro]

9. Konlee, M. (1998). A new triple combination therapy. Positive health news, (17), 12. [case report]

10. Ulbricht, C., Basch, E., Cheung, L., Goldberg, H., Hammerness, P., Isaac, R., ... & Weissner, W. (2014). An evidence-based systematic review of elderberry and elderflower (Sambucus nigra) by the Natural Standard Research Collaboration. Journal of dietary supplements, 11(1), 80-120. Link. [review article]

11. Christensen, L. P., Kaack, K., & Fretté, X. C. (2008). Selection of elderberry (Sambucus nigra L.) genotypes best suited for the preparation of elderflower extracts rich in flavonoids and phenolic acids. European Food Research and Technology, 227(1), 293-305. Link. Other.

12. Mariotti-Lippi, L.; Bellini, C.; Mori, S. Palaeovegetational reconstruction based on pollen and seeds/fruits from a bronze age archaeological site in Tuscany (Italy). Plant. Biosyst. 2010, 144, 902–908. [OTHER]

13. Martin, L.; Jacomet, S.; Thiebault, S. Plant economy during the Neolithic in a mountain context: The case of “Le Chenet des Pierres” in the french Alps (Bozel-Savoie, France). Veg. Hist. Archaeobot. 2008, 17, s113–s122. [OTHER]

14. Marinova, E.; Atanassova, J. Anthropogenic impact on vegetation and environment during the
    Bronze Age in the area of Lake Durankulak, NE Bulgaria: Pollen, microscopic charcoal,
    non-pollen palynomorphs and plant macrofossils. Rev. Palaeobot. Palynol. 2006, 141, 165–178. [OTHER]

15. Mikulic-Petkovsek, M.; Schmitzer, V.; Slatnar, A.; Todorovic, B.; Veberic, R.; Stampar, F.; Ivancic, A. Investigation of anthocyanin profile of four elderberry species and interspecific hybrids. J. Agric. Food Chem. 2014, 62, 5573–5580. [Chemical profiling].

16. Ding, M.; Feng, R.; Wang, S.Y.; Bowman, L.; Lu, Y.; Qian, Y.; Castranova, V.; Jiang, B.H.; Shi, X. Cyanidin-3-glucoside, a natural product derived from blackberry, exhibits chemopreventive and chemotherapeutic activity. J. Biol. Chem. 2006, 281, 17359–17368.

17. Parikh, B.A.; Tumer, N.E. (2004). Antiviral activity of ribosome inactivating proteins in medicine. Mini Rev. Med. Chem. 2004, 4, 523–543.

18. Girbes, T.; Ferreras, J.M.; Arias, F.J.; Stirpe, F. Description, distribution, activity and phylogenetic relationship of ribosome-inactivating proteins in plants, fungi and bacteria. Mini Rev. Med. Chem. 2004, 4, 461–476.

19. Stirpe, F. Ribosome-inactivating proteins. Toxicon 2004, 44, 371–383.

20. Lapadula, W.J.; Sánchez Puerta, M.V.; Juri Ayub, M. Revising the taxonomic distribution, origin
    and evolution of ribosome inactivating protein genes. PLoS One 2013, 8, e72825.

21. Jiménez, P., Tejero, J., Cordoba-Diaz, D., Quinto, E. J., Garrosa, M., Gayoso, M. J., & Girbés, T. (2015). Ebulin from dwarf elder (Sambucus ebulus L.): a mini-review. Toxins, 7(3), 648-658. Link. [review article].

22. He, X.; McMahon, S.; Henderson, T.D.; Griffey, S.M.; Cheng, L.W. Ricin toxicokinetics and its sensitive detection in mouse sera or feces using immuno-PCR. PLoS One 2010, 5, e12858. [Animal study]

23. Iglesias, R.; Citores, L.; Ferreras, J.M.; Pérez, Y.; Jiménez, P.; Gayoso, M.J.; Olsnes, S.; Tamburino, R.; di Maro, A.; Parente, A.; et al. Sialic acid-binding dwarf elder four-chain lectin displays nucleic acid N-glycosidase activity. Biochimie 2010, 92, 71–80.

24. Vimr, E.; Lichtensteiger, C. To sialylate, or not to sialylate: that is the question. Trends Microbiol. 2002, 10, 254–257.

25. Jimenez, P.; Cabrero, P.; Basterrechea, J.E.; Tejero, J.; Cordoba-Diaz, D.; Girbes, T. Isolation and molecular characterization of two lectins from dwarf elder (Sambucus ebulus L.) blossoms related to the Sam n1 allergen. Toxins 2013, 5, 1767–1779

Reishi (Ganoderma lucidum)

What is Reishi?

Reishi is a medicinal forest-grown fungus. It's revered in traditional medical systems across Asia for its powerful immune-enhancing and longevity-promoting benefits.

Medicinal mushrooms are notorious for their complex effects on the immune system — often working in both directions (stimulation and inhibition), depending on what’s needed.

Reishi is no different — it's one of the most important medicinal herbs for longevity and immune health in the world.

This saprophytic (tree-eating) fungus is often used for the prevention and treatment of immune-related illness — including cancer, autoimmunity, infection, inflammation, and allergic reaction.

Reishi is also used for anxiety, depression, insomnia, and as a general adaptogen for overall health and wellbeing.

What is Reishi Used For?

Reishi has the unique ability to act bidirectionally on the immune system — which means it can increase immune activity, and decrease immune activity. It appears it will push the immune system in whatever direction it needs to go. In patients with low immunity or cancer, reishi up-regulates the immune response.

however, in patients with hyperactive immune activity — such as autoimmune disease or allergic reaction — reishi has an opposite effect, toning down the immune response.

This is an effect not well understood to this day, but gives the mushroom an incredibly versatile set of benefits.

Traditionally, reishi is considered a shen tonic — which is used to calm the nerves, ease anxiety, and promote healthy sleep (without being directly sedative).

Most people use reishi as a general health and immune tonic. It’s used by people with known immune-related illness — such as frequent infection, autoimmunity, chronic inflammation, cancer, and more.

Others use the herb as a prophylactic against common infections like colds and flus, or to keep chronic viral infection at bay (such as herpes or shingles).

Traditional Uses of Reishi

+ Traditional Chinese Medicine

In Traditional Chinese Medicine this fungus has been used for (altitude sickness and is often combined with chrysanthemum, rhodiola, and safflower seed.

Taste:

Sweet [5]

Energy:

Neutral [5]

Channels:

Heart, liver, lung [5]

Actions:

Tonifies, the heart, calms and anchors the Shen, stops cough, stops wheezing, dislodges phlegm, tonifies the spleen, tonifies the Qi, tonifies blood [5]

Indications:

Suitable during pregnancy [5].

Dose:

3-15g decocted20 mins [5]

Considered to be warming, astringent, nourishing, detoxifying, and tonifying. Protects qi of the heart, used to repair a knotted, tight chest. Traditionally in this system, it was recommended to take this herb over long periods to reap the benefits of longevity.

The spores are suggested to contain high amounts of jing and considered an elixir of life [1].

Other uses include Hashimoto's disease, in foot baths for gout, altitude sickness prevention, and immune regulation. [1].

+ Ayurveda

A related species — Ganoderma applanatum — has been used extensively in Ayurvedic systems in the pine region of India. Its uses include stopping excessive salivation in the mouth, as a styptic.

+ Other Historical Uses

Reishi has been used medicinally in Asian countries for at least 4000 years and is the most widely depicted mushroom in Japan, Korea, and China, which can be found on temples, tapestries, statues, and paintings.

Reishis rarity and subsequent value made it most accessible to the privileged like emperors and royalty. It has long been associated with longevity and was included in many ancient medical texts for this purpose.

Used to treat liver ailments, lung conditions, kidney disease, nerve pain, hypertension, gastric ulcers, and insomnia. The antler growth pattern is considered very rare and is the most desired for promoting sexual function in both men and women.

Other uses include its use as a means to ward off evil by hanging dried specimens over the door. Similarly, it has been placed on the graves of shamans to protect from evil souls or spirits.

Reishi has been used in nearly every format imaginable including tinctures, teas/decoctions, powdered preparations, brewed into beers and wines, and eaten raw.

Herb Details: Reishi

Herbal Actions:

• Adaptogen
• Immunomodulator
• Analgesic
• Muscle relaxant
• Nervine Relaxant
• Hepatoprotective
• Pulmonary trophorestorative
• Cardiotonic
• Chemoprotective
• Anti-Cancer
• Antiviral
• Antibacterial

Weekly Dose

• (1:2 Liquid Extract)
  30-60 mL
• View Dosage Chart

Part Used

• Fruiting body, Spores, Mycelium

Family Name

• Ganodermataceae

Distribution

• Asia, Europe, and North America

Constituents of Interest

• Beta-glucans
• Ergosterol
• Triterpenoids
• Polysaccharides

Common Names

• Reishi
• Ling Zhi
• Saiwai-Take
• Kishiban

CYP450

• Unknown

Quality

• Neutral

Pregnancy

• No adverse reactions expected.

Taste

• Bitter

Duration of Use

• Suitable for long term use.

Mycological Information

There are about 80 different species of Ganoderma, many of which are used as medicine. The Ganodermataceae contains 8 genera and roughly 300 different species.

Reishi is a saprophyte, meaning it only eats dying or decaying organic matter such as wood. It's mainly found growing on dying trees, stumps, and fallen logs.

Ganoderma spp. is long-lived — releasing approximately 30 billion spores everyday for up to 6 months or a year [1].

Habitat Ecology, & Distribution:

Wild Ganoderma lucidum is rare but is indigenous to forested regions of Asia including Japan, China, and Russia. Other species are found in North America and Europe.

It grows on Elm (Ulmus spp.), alder (Alnus spp.), oak (Quercus spp.), maple (Acer spp.) and some strains on conifers. Other species of Ganoderma such as G. tsugae or G. oregonense grow better and almost exclusively on conifers. G. lucidum, however, prefers hardwoods.

G. lucidum can be found very rarely in the Pacific Northwest, and a similar species (G. curtisii), is seen more commonly in eastern Canada around the great lakes region [1]. This species is actually a yellow form of the red G. lucidum.

Most reishi products on the market are cultivated in a sterile environment on logs or sawdust in large laboratories.

Harvesting Collection, & Preparation:

Both the mycelium, fruiting body, and spores are used medicinally. The red and purple varieties are considered the most valuable. These phenotypes are also thought to be the most potent in their effects [1].

The spores can be either taken raw or can be cracked. This basically involves the germination, then drying of the spores and is suggested to provide stronger medicinal effects after this germination process has taken place.

Another, much more expensive way of ingesting the spores it to run it through a supercritical CO2 extractor. This method creates a product that is roughly equivalent to 20-40 of the raw spore capsules [1].

A mushroom oil can also be extracted from the fruiting body waxes, can be used as is topically, or added to lotions, and salves.

Cosmetically it is useful as a sunscreen due to its radio-protective effects, as well as in anti-aging creams, and to remove warts [1].

As with most hard, polypores, chop the fungus into strips (better when wet or a saw may have to be used), and crumble into small pieces.

Decoct in water, then strain and freeze the leftover mush, doing this will cause the cell walls to burst and allow more constituents to be extracted during the next process. Next, after it has been frozen for 24 hours or so, de-thaw, and mix with 95% alcohol for at least 2 weeks.

In the end, strain, and combine with the decoction made earlier to a standardized amount.

Pharmacology & Medical Research

+ Antibacterial

Ganoderma applanatum is an effective inhibitor of:

• Bacillus cereus
• Cornybacterium diphtheria
• Escherichia coli
• Pseudomonas aeruginosa
• Staphylococcus aureus
• Streptococcus pyogenes

Gram-positive bacteria were more affected than gram-negative [1].

It has been suggested that the polysaccharides in Ganoderma spp. are more antibacterial — while the triterpenoids are more antiviral.

More research is needed to elucidate on this further.

+ Anti-diabetic

Ganoderma has been reported to produce potent lens aldose reductase inhibition, and significant inhibition of serum glucose and sorbitol accumulation in the lens of the eye, red blood cells, and sciatic nerves in diabetic rats (based on earlier studies) [1]. This shows potential as a treatment for diabetic induced retinopathy and other diabetes-related damage in the body.

Has been shown to lower blood sugar levels in hyperglycemic models (fruiting body), and involved the ganoderan B and C [1].

In a study on type 2 diabetics not on insulin, were given reishi extracts, and compared to the placebo control group, were found to have significantly decreased glycosylated hemoglobin (8.4%-7.6%), in as little as 12 weeks. Fasting insulin levels, 2-hour -post-prandial insulin, fasting C-peptide, and post-prandial C-peptide all showed significant improvement in the reishi group [1].

Spores have also shown evidence for anti-diabetic effects [1].

+ Antioxidant

Methanol extracts of G. tsugae were found to be more potent in antioxidant effects that alpha-tocopherol, and exhibited significant inhibition of lipid peroxidation as such.

The antioxidant effects are not considered as reliable as G. lucidum but are very close. It is the phenol content that has been deemed responsible for these effects. [1].

G. tsugae fruiting body extract was shown to increase intracellular glutathione levels, which in turn protect against oxidative damage [1].

+ Antiulcer effects:

Polysaccharides from Ganoderma spp. protects the gastric mucosa by improving PGE2. This backs up some of its uses in the form of tea for treating ulcers.

+ Antiviral

G. lucidum fruiting body extracts have been shown to inhibit HIV, and HPV [1].

Rogers, (2011) reports that Ganaderiol-F, ganodermadiol, ganoderic acid beta, and lucidumol have all been identified as antiviral agents.

G. resinaceum (and most likely G. tsugae, and G. lucidum as well), have been shown to inhibit punta toro, pichinde, and H1N1 [1].

+ Blood Tonic

Reishi been shown to enhance the production of interleukin-1 in vitro, and increase white blood cell and haemoglobin levels in mice [1].

+ Cardiotonic

Reishi has been shown to improve symptoms of coronary heart disease [1].

G. lucidum has been shown to provide anti-cholesterol, anti-diabetic, reduced platelet aggregation, anti atherosclerotic, and antihypotensive effects, which all play a role in the development of cardiovascular disease.

Suggested to produce angiotensin-converting enzyme inhibition through its ganoderic acid B, C2, D, and F [1].

+ Chemoprotective

Has been shown to increase natural killer cell activity of splenocytes by up to 52% [1]

+ Hepatoprotective

The triterpenoids contained in the mycelium of G. tsugae have shown hepatoprotective activity [1].

Ganodereic acid B has shown hepatoprotective effects [1].

+ Immunomodulatory

The polysaccharides from the mycelium were found to be both anti-inflammatories, and immune-stimulating, Rogers, (2011), suggests contradiction from these two effects suggest bi-directional (immunomodulatory) effects on immune response, rather than just stimulating. This appears to be dose-dependent and may be through modulation of cytokine production.

Reishi has been shown to both reduce inflammation and increase immune response — which is contradictory in that an increased immune response should correlate with inflammation. It's has been suggested that G. lucidum produces this apparent modulatory effect through the enteric mucosal pathway. Its effects on the immune system do not appear to be through IgE antibody synthesis, rather through a modulating effect on immunoglobulin levels [1].

+ Sedative

The spores are suggested to produce sedative and hypnotic effects in mice [1].

+ Other

There's some evidence to support the effects of reishi towards bronchitis and other lung disorders . The chemicals suggested to be responsible for these effects are gonoderic acids A, B, C1, and C2 [1].

Phytochemistry

+ Compounds by Anatomy

Fruiting Body

Carbohydrates, amino acids (including adenosine), steroids (ergosterols), protease, lysosomes, lipids, triterpenes, alkaloids, vitamins B2 and C, minerals (zinc, manganese, iron, copper, germanium), beta-glucans (up to 40.6%), [1].

Mycelium

Sterols, alkaloids, lactones, erogone, polysaccharides, triterpinoids,

Spores

choline, triterpenes, betaine, palmitic acid, stearic acid, ergosta7,22-dien-3b-ol, tetracosanoic acid, behenic acid, nonadecanoic acid, ergosterol, beta sitosterol, pyrophosphatidic acid, hentriacontane, tetracosane, ganodermasides (A and B) [1].

+ Species Specific Breakdown

Ganoderma tsugae

3 α-acetoxy-5α-lanosta-8,24-dien-21-oic acid, 2β,3α,9α-trihydroxy-5α-ergosta-7,22-dien, 3alpha-acetoxy-16alpha-tsugarioside B and C, ganoderic acid C2, ganoderic acid B, lucidone A, and glycans (various) [1].

Ganoderma applanatum

Ergosterol (and its peroxide), ergosta-7,22-dien-3b-ol, ergasta-7,22-dien-3-one, β-D-glucan, fungisterol, alnusenone, friedelin, triterpenoids (including ganoderenic, furanoganoderic, ganoderic acids), applanoxidic acids (A, B, C, and D), lanostandoid triterpenes E-H, lucidone A, ganoderma aldehyde, 3 linoleic acid steryl esters. To compare with G. lucidum, ganoderenic acid, and ganoderic acid is found in both [1].

Ganoderma lucidum

Still compiling research.

Clinical Applications Of Reishi:

Reishi is used as a supportive agent for cancer, autoimmune conditions, cardiovascular dysfunctions, respiratory dysfunctions, viral and bacterial infection, and hypertension. It's rarely used on its own, but makes for a great addition to herbal formulations.

Cautions:

Caution advised in combination with ACE inhibitor medications due to potential drug interactions.

Synergy

For altitude sickness: Combines well with rhodiola for this purpose.

It has been suggested that vitamin C helps absorb this mushroom, however, more research is needed to confirm this. Pineapple and ginger may also increase the absorption of reishi constituents.

Author:

Justin Cooke

The Sunlight Experiment

(Updated May 2019)

Recent Blog Posts:

References:

1. Rogers, R. D. (2011). The fungal pharmacy: The complete guide to medicinal mushrooms and lichens of North America [Adobe Digital Editions version].

2. Berovic, M., J. Habijanic, I. Zore, B. Wraber, D. Hodzar, B. Boh and F. Pohleven. Submerged cultivation of Ganoderma lucidum biomass and immunostimulatory effects of fungal polysaccharides. J. Biotechnol. 103: 77–86, 2003

3. Jiang, Y., H. Wang, L. Lu and G.Y. Tian. Chemistry of polysaccharide Lzps-1 from Ganoderma lucidum spore and anti-tumor activity of its total polysaccharides. Yao. Xue. Xue. Bao. 40: 347–350, 2005.

4. Cheng, K.C., H.C. Huang, J.H. Chen, J.W. Hsu, H.C. Cheng, C.H. Ou, W.B. Yang, S.T. Chen, C.H. Wong and H.F. Juan. Ganoderma lucidum polysaccharides in human monocytic leukemia cells: from gene expression to network construction. BMC Genomics 8: 411, 2007.

5. Hempen, C. H., & Fischer, T. (2009). A Materia Medica for Chinese Medicine: Plants, Minerals, and Animal Products. (Pg. 436-437).

6. Thyagarajan, A., J. Jiang, A. Hopf, J. Adamec and D. Sliva. Inhibition of oxidative stress-induced invasiveness of cancer cells by Ganoderma lucidum is mediated through the suppression of interleukin-8 secretion. Int. J. Mol. Med. 18: 657–664, 2006.

7. Xie, J.T., C.Z. Wang, S. Wicks, J.J. Yin, J. Kong, J. Li, Y. C. Li and C.S. Yuan. Ganoderma lucidum extract inhibits proliferation of SW 480 human colorectal cancer cells. Exp. Oncol. 28: 25–29, 2006.

8. Paterson, R.R. Ganoderma — a therapeutic fungal biofactory. Phytochemistry. 67: 1985–2001, 2006.

9. Lin, Y.L., Y.C. Liang, S.S. Lee and B.L. Chiang. (2005). Polysaccharide purified from Ganoderma lucidum induced activation and maturation of human monocyte-derived dendritic cells by the NFkappaB and p38 mitogen-activated protein kinase pathways. J. Leukoc. Biol. 78: 533–543.

Cannabis (Cannabis sativa/indica)

Cannabis Overview

Cannabis is well known for its psychoactive effects, causing temporary changes in visual and auditory perception.

The cannabis plant is also a rich source of medicinal compounds. Cannabinoids related to THC exert medicinal action through the endocannabinoid system — a critical component of homeostasis.

Many of these cannabinoids aren't psychoactive, and wont produce the 'high' associated with the plant in their isolated forms.

Compounds like CBD, have become especially popular as a supplement recently for its broad medicinal benefits.

There are plenty of uses for cannabis — however, product selection, strain choice, and cannabinoid profiles make a big difference in the effects produced by the plant. It's important to use the right type of cannabis for the job.

Jump to Section

What is Cannabis Used For?
Technical Details
Botanical Information
Phytochemistry
— CBC
— CBD
— CBG
— THC
— THCV
— Other Cannabinoids
— Terpenes
Clinical Applications of Cannabis
Cautions
References

Buy CBD Oil

What is Cannabis Used For?

Using cannabis as medicine poses challenges due to the large variety of effects each cannabinoid possesses. Different cannabinoid and terpene ratios can produce different effect profiles.

The plant has many claimed benefits, and though a lot of them can be validated, it's not a miracle plant.

Cannabis is especially reliable for a few key symptoms:

• Lowering various forms of inflammation
• Improving microbiome diversity (through CB2 receptor activity)
• Reducing nervous excitability
• Reducing convulsions
• Improving sleep onset and maintenance
• Lowering pain

Using cannabis as medicine should be attempted with caution due to the degree of variability the plant produces in terms of effect profile. What this means is that some cannabis extracts will make symptoms like anxiety worse, while others can dramatically improve it.

Choosing the right strain or extract is of the utmost importance when using cannabis as medicine.

The effects of cannabis can be contradictory:

• It's both a stimulant and a sedative
• It increases appetite, and suppresses it
• It increases immune activity, and suppresses inflamamtion

These effects all contradict themselves in most cases. The reason this happens is because the cannabinoids work through a regulatory pathway (endocannabinoid system) rather than on a particular organ function.

It's similar to how adaptogens like ginseng, ashwagandha, or reishi produce often contradictory or bidirectional results.

+ Indications

• Anorexia
• Cancer
• Crohn's disease
• Dystonia
• Epilepsy
• General anxiety disorder
• Glaucoma
• Gout
• Insomnia
• Menstrual cramping
• Multiple Sclerosis
• Neuropathic pain
• Osteoarthritis
• Rheumatoid Arthritis
• Schizophrenia (Caution)
• Social anxiety disorder
• Substance abuse/addiction
• Ulcerative colitis
  

+ Contraindications

• Only use cannabis medicinally following the direction of a qualified medical practitioner.
• Caution with anxious or depression.
• May worsen symptoms of psychosis
• Avoid use alongside medications unless first discussing with your doctor.
  

+ Potential Side-Effects

• Apathy (long-term use)
• Bronchitis (smoking)
• Cough (smoking)
• Depression
• Dizziness
• Dry eyes
• Dry mouth
• Eye reddening
• Fatigue
• Hallucinations
• Headache
• Heart palpitations
• Hypertension/Hypotension
• Increased appetite
• Lightheadedness
• Menstrual changes
• Nausea/vomiting
• Numbness
• Paranoia
• Tachycardia

Herb Details: Cannabis

Weekly Dose

• (CBD content in mg)
  70–700 mg
• View Dosage Chart

Part Used

• Leaves, flowers, seeds

Family Name

• Cannabacea

Distribution

• Worldwide

Herbal Actions:

• Sedative/Stimulant
• Anti-emetic
• Anti-spasmodic
• Anti-convulsant
• Analgesic
• Antinflammatory
• Appetite Suppressant/Stimulant
• Adaptogen
• Anti-cancer
• Antioxidant

Common Names

• Cannabis
• Marijuana
• Hemp
• Mary Jane
• Herb

Pregnancy

• Avoid use while pregnant and nursing.

Duration of Use

• Long-term use acceptable. Recommended to take breaks periodically.

CYP450

• CYP2C9
• CYP3A4

Botanical Information

Cannabis plants are members of the Cannabacea family. This small family comprises only 11 different genuses, and about 170 species.

Some common members of the family are hops (Humulus spp.) and celtis (Celtis spp.). The celtis genus contains the largest collection of species by far, with over 100 different species. Cannabis and Humulus are the closest related genus' in the group by far.

There are three species of cannabis:

1. Cannabis sativa

Cannabis sativa is a tall, fibrous plant. It's high in cannabinoids, terpenes, and other phytochemicals — giving it many uses medicinally.

Cannabis sativa is the most commonly cultivated species. There are hundreds, if not thousands of different phenotypes of this species — the most important being hemp — which is a non-psychoactive, high fiber plant valued as both a health supplement and textile. It's also used for food (seeds), and to make biodeisel.

There are also Cannabis sativa strains high in the psychoactive component — THC — which make it popular as both medicine and recreational intoxicant.

2. Cannabis indica

Cannabis indica grows as s shorter, bushier plant. It's hgiher in THC, and there are few low-THC phenotypes available for this plant.

This species of cannabis is most often used recreationally.

3. Cannabis ruderalis

Cannabis ruderalis is a small, herbaceus plant more closely related to Cannabis sativa than Cannabis indica. It's low in cannabinoids, and terpenes, as well as fiber — limiting its value to humans.

This species has the unique ability to initiate flower production irrelevant to day length. Plant breeders have started mixing the plant with other species to gain these benefits. This makes cultivation easier in areas where day length is too short or too long for optimal cannabis cultivation.

Phytochemistry

There are 421 compounds in the cannabis plant [1], at least 66 of these are cannabinoids — some sources report as many as 112.

The top 6 cannabinoids in the plant (CBD, CBG, CNN, THC, THCV, and CBC), account for the vast majority of the cannabinoid profile.

The phenotype of the cannabis used is the primary determining factor for the cannabinoid profile of each plant.

Hemp plants for example, contain much higher levels of CBD, and lower levels of THC. Marijuana strains are the opposite, contianing high THC, and lower CBD.

Depending on the strain, this can vary dramatically — and you can find almost any combination of cannabinoid possible.

The Cannabinoids:

Cannabinoids are a class of phytochemical compounds resembling the structure of our naturally occurring ecosanoid endocannabinoids; anandamide, and 2-AG. There are roughly 66 of these compounds in the cannabis plant, and a few found in other species of plants as well — such as helichrysum and echinacea.

Although the cannabinoids are very similar, their binding activity varies a lot [14]. Some bind to CB1 receptors (located primarily in the central nervous system), others bind to CB2 receptors (found primarily in immune tissue). Some cannabinoids will even bind to both, or work by increasing the concentrations of naturally occurring endocannabinoids instead.

Due to the wide range of variability between each cannabinoid, it’s useful to go over them in greater detail individually.

1. CBC

Cannabichromene

CBC is the third most abundant cannabinoid in the cannabis plant.

It’s non-psychoactive.

CBC is far less studied than the two preceding cannabinoids CBD, and THC, though early research is starting to suggest it’s even better for treating conditions like anxiety than the famed CBD.

CBC content can be increased in the cannabis plant by inducing light-stress on the plant [5].

CBC Medicinal Actions

• Antidepressant

• Mild sedative

Receptors Affected

• Vanilloid receptor agonist (TRPV3 and TRPV4) [4]

2. CBD

Cannabidiol

In many cases, CBD is the most abundant cannabinoid. Only selectively bred cannabis strains will have higher THC concentrations than CBD.

CBD is famed for many reasons. It offers a wide range of medicinal benefits, and has been well-studied and validated over the past two decades.

CBD oils, e-liquids, and edibles have become highly popular in recent years as more of this research is being released and translated for the general public.

CBD Medicinal Actions

• Antinflammatory

• Mild appetite suppressant

• Lowers stress

• Adaptogenic

• Mild sedative

• Anti-emetic

Receptors Affected

• Adenosine (A2a) reuptake inhibitor [6]

• Vanilloid pain receptors (TRPV1, TRPV2, TRPV3) [7]

• 5HT1A receptor agonist (serotonin receptor) [6]

• FAAH (–) [6, 7]

• PPARγ nuclear receptor (+) [48]

• Mg2+‐ATPase (−) [11]

• Arylalkylamine N‐acetyltransferase (−) [44]

• Indoleamine‐2,3‐dioxygenase (−) [45]

• 15‐lipoxygenase (−) [46]

• Phospholipase A2 (+) [11]

• Glutathione peroxidase (+) [47]

• Glutathione reductase (+) [47]

• 5‐lipoxygenase (−) [46]

Metabolism

• CYP1A1 (−) [40]

• CYP1A2 & CYP1B1 (−) [40]

• CYP2B6 (−) [41]

• CYP2D6 (−) [42]

• CYP3A5 (−) [43]

Shop Now

Shop Now

Enter KATS15 for a 15% Discount

Shop Now

3. CBG

Cannabigerol

CBG is an early precursor for many of the other cannabinoids including THC.

Plants harvested early will be high in this compound.

Many users report that strains high in CBG are less likely to cause anxiety, and are good for people experiencing acute stress.

This is likely due to its role in blocking the serotonergic effects of THC through the 5-HT1A serotonin receptors [9].

CBG Medicinal Actions

• Anti-anxiety

• Adaptogenic

• Mild sedative

Receptors Affected

• A2-adrenoceptor antagonist [9]

• CB1 and CB2 receptors agonist [9]

• 5-HT1A receptors antagonist (serotonin receptor) [9]

• Vanilloid receptor agonist (TRPA1) [8]

• TRPM8 receptor antagonist [8]

4. CBN

Cannabinol

CBN is made from THC. As THC content breaks down with time, or heat, CBN levels increase overall.

Older harvested plants that have gone past their window of ripeness will be much higher in CBN.

It’s mostly non-psychoactive but may have some mild psychoactivity in some people.

Products or strains high in CBN will produce more of a heavy feeling and are best used for treating conditions like insomnia or anxiety.

This cannabinoid is potentially the most sedative of the group.

CBN Medicinal Actions

• Sedative

• Anti-anxiety

• Appetite stimulant

Receptors Affected

• CB1 receptor agonist [10].

Metabolism

• CYP2C9

5. THC

Tetrahydrocannabinol

THC is the main psychoactive compound in the cannabis plant.

There are two main types:

• Delta-8-THC — contained in very small amounts

• Delta-9-THC — the most abundant form of THC in the cannabis plant

THC activates both CB1 and CB2 endocannabinoid receptors, causing changes in neurotransmitters like dopamine, norepinephrine, and most importantly, serotonin. It’s this change in neurotransmitter levels that produce the bulk of the high experienced by this compound.

Aside from its psychoactive effects, THC has medicinal benefits of its own.

It’s mentally stimulating and has some potent antidepressant effects through its euphoric effects.

THC Medicinal Actions

• Appetite stimulant

• Sedative (low doses)

• Stimulant (high doses)

Receptors Affected

• CB1 and CB2 agonist [11]

• PPAR gamma receptor agonist [11, 15].

Metabolism

• CYP2C9

6. THCV

Tetrahydrocannabivarin

THCV is the fraternal twin of THC.

It’s virtually identical except for one slight chemical difference — THCV is missing two carbon atoms.

This makes the effects of THCV very similar to THC — but is much weaker in its effects.

One study reported THCV as being 20-25% as strong as THC in its psychoactive effects [12].

There are others affected by this, including CBCV, and CBDV, though they are in far less concentrations.

THCV Medicinal Actions

• Appetite suppressant

• Euphoric

• Antispasmodic

• Paranoic

Receptors Affected

• Vanilloid receptor agonist (TRPV3 and TRPV4) [13].

7. Other Cannabinoids

There are also a lot of cannabinoids that can be found in much lower concentrations.

These make up the bottom 5% of the cannabinoid profile.

Few of these cannabinoids have many studies on them aside from chemical mapping to identify their structure.

We may see more research on these cannabinoids in the near future.

Some Novel Cannabinoids Include:

• CBCV (cannabichromevarin)

• CBDV (cannabidivarin)

• CBE (cannabielsoin)

• CBGM (cannabigerol monomethyl ether)

• CBGV (cannabigerovarin)

• CBL (cannabicyclol)

• CBT (cannabicitran)

• CBV (cannabivarin)

A Note On Synthetic Cannabinoids

There are also synthetic cannabinoids. These are compounds that are similar in shape and function to cannabinoids produced in our bodies, or in the cannabis plant.

It’s recommended that you stay far away from the synthetic cannabinoids — not only do they lack many of the medicinal actions of cannabis, they have the potential to cause serious harm.

The street drug known as “spice” is a combination of various synthetic cannabinoids. They were designed as an attempt to circumvent the legal hurdles preventing the sale of cannabis products for recreational use — and have since become a major cause of addiction and abuse.

+ Side-Effects of Synthetic Cannabinoid Use

• Agitation and anxiety
• Blurred vision
• Chest pain
• Death
• Hallucinations
• Heart attack
• High blood pressure
• Kidney failure
• Nausea and vomiting
• Paranoia
• Psychosis
• Racing heart
• Seizures
• Shortness of breath

+ List of Synthetic Cannabinoids

• JWH-018
• JWH-073
• JWH-200
• AM-2201
• UR-144
• XLR-11
• AKB4
• Cannabicyclohexanol
• AB-CHMINACA
• AB-PINACA
• AB-FUBINACA

Cannabis Terpenes

Terpenes are a class of compounds characterized by their volatile nature, and hydrocarbon-based structure. These are contained in high amounts in the essential oil of plants.

Terpenes have a very low molecular weight, and will evaporate under low temperatures. This, combined with their characteristic aromas is what gives many plants their scent. Conifer trees, fruits, and many flowers (including cannabis) all owe their aroma to their terpene profile.

Each plant can contains hundreds of different terpenes — many of which will even overlap into unrelated plant species. Cannabis shares terpenes with pine trees, many different flowers, citrus fruits, and nutmeg, among others.

Terpenes add flavor as well as additional medicinal benefits. Terpenes often have antibacterial, antiviral, antinflammatory, and anxiolytic effects.

+ List of Cannabis Terpenes

• A-humulene
• a-Terpenine
• Alpha Bisabolol
• alpha-Terpineol
• Alpha/Beta Pinene
• Beta-Caryophyllene
• Bisabolol
• Borneol
• Camphene
• Caryophyllene oxide
• D-Linalool
• Eucalyptol (1, 8 cineole)
• Geraniol
• Guaiol
• Isopulegol
• Limonene
• Myrecene
• Nerolidol
• p-Cymene
• Phytol
• Pulegone
• Terpineol-4-ol
• Terpinolene
• Trans Ocimene
• Valencene
• ∆-3-carene

Pharmacokinetics/Pharmacodynamics

Cannabinoids work by mimicking the endocannabinoids anandamide and 2-AG.

Learn more about cannabinoid metabolism.

Clinical Applications of Cannabis

As an herb, cannabis is very useful. It works through a set of receptors most other plants don’t interact with — the endocannabinoid system.

The endocannabinoid system plays a major role in maintaining homeostasis. This gives cannabis an effect profile similar to adaptogens — but through different mechanisms.

Cannabis is similar to adaptogens in that it offers a bidirectional effect profile — which means it can both increase, and decrease tissue function according to its homeostatic baseline.

But cannabis isn’t quite an adaptogen because it can’t increase the bodies resistance to stress, and doesn’t appear to exert any action on the hypothalamus or adrenal glands directly.

Although cannabis has broad actions and therefore can provide benefit to a wide range of body systems — choosing the right product, strain, and phenotype for the job is critical.

An experienced herbalist or naturopath using cannabis will take into account the cannabinoid profile, terpene content, and anecdotal effects of each strain or CBD product being used.

Unlike other herbs, you have to be very particular about the type of cannabis being used for each condition.

What Constitutes “Medicinal” Cannabis?

There’s a big difference between using cannabis because “it’s healthy”, and using it as a therapeutic agent aimed at treating a specific disease process.

Although it can be used as both, daily supplementing cannabis or extracts like CBD don’t constitute medical cannabis.

However, you can use cannabis to address the symptoms, or underlying causes for some conditions.

Cautions:

Caution advised whenever using cannabis due to the potential for intoxicating side-effects. Without careful consideration of cannabinoid profile, some strains, or cannabis products may make symptoms for certain conditions worse — especially anxiety, psychosis, bipolar disorder, and insomnia.

Author

Justin Cooke, BHSc

The Sunlight Experiment

(Updated Jan 2019)

Recent Blog Posts:

References:

1. Sharma P, Murthy P, Bharath M.M.S. (2012). Chemistry, Metabolism, and Toxicology of Cannabis: Clinical Implications. Iran J Psychiatry 2012; 7:4: 149-156

2. Aizpurua-Olaizola, O., Soydaner, U., Öztürk, E., Schibano, D., Simsir, Y., Navarro, P., ... & Usobiaga, A. (2016). Evolution of the cannabinoid and terpene content during the growth of Cannabis sativa plants from different chemotypes. Journal of natural products, 79(2), 324-331.

3. Shevyrin, V. A., & Morzherin, Y. Y. (2015). Cannabinoids: structures, effects, and classification. Russian Chemical Bulletin, 64(6), 1249-1266.

4. De Petrocellis, L., Orlando, P., Moriello, A. S., Aviello, G., Stott, C., Izzo, A. A., & Di Marzo, V. (2012). Cannabinoid actions at TRPV channels: effects on TRPV3 and TRPV4 and their potential relevance to gastrointestinal inflammation. Acta physiologica, 204(2), 255-266.

5. De Meijer, E. P. M., Hammond, K. M., & Micheler, M. (2009). The inheritance of chemical phenotype in Cannabis sativa L.(III): variation in cannabichromene proportion. Euphytica, 165(2), 293-311.

6. Nelson, K., Walsh, D., Deeter, P., & Sheehan, F. (1994). A phase II study of delta-9-tetrahydrocannabinol for appetite stimulation in cancer-associated anorexia. Journal of palliative care.

7. Bisogno, T., Hanuš, L., De Petrocellis, L., Tchilibon, S., Ponde, D. E., Brandi, I., ... & Di Marzo, V. (2001). Molecular targets for cannabidiol and its synthetic analogues: effect on vanilloid VR1 receptors and on the cellular uptake and enzymatic hydrolysis of anandamide. British journal of pharmacology, 134(4), 845-852.

8. De Petrocellis, L., Vellani, V., Schiano-Moriello, A., Marini, P., Magherini, P. C., Orlando, P., & Di Marzo, V. (2008). Plant-derived cannabinoids modulate the activity of transient receptor potential channels of ankyrin type-1 and melastatin type-8. Journal of Pharmacology and Experimental Therapeutics, 325(3), 1007-1015.

9. Cascio, M. G., Gauson, L. A., Stevenson, L. A., Ross, R. A., & Pertwee, R. G. (2010). Evidence that the plant cannabinoid cannabigerol is a highly potent α2‐adrenoceptor agonist and moderately potent 5HT1A receptor antagonist. British journal of pharmacology, 159(1), 129-141.

10. Farrimond, J. A., Whalley, B. J., & Williams, C. M. (2012). Cannabinol and cannabidiol exert opposing effects on rat feeding patterns. Psychopharmacology, 223(1), 117-129.

11. Pertwee, R. G. (2008). The diverse CB1 and CB2 receptor pharmacology of three plant cannabinoids: Δ9‐tetrahydrocannabinol, cannabidiol and Δ9‐tetrahydrocannabivarin. British journal of pharmacology, 153(2), 199-215.

12. Hollister, L. E. (1974). Structure-activity relationships in man of cannabis constituents, and homologs and metabolites of Δ9-tetrahydrocannabinol. Pharmacology, 11(1), 3-11.

13. Pertwee, R. G. (2006). The pharmacology of cannabinoid receptors and their ligands: an overview. International journal of obesity, 30(S1), S13.

14. Compton, D. R., Rice, K. C., De Costa, B. R., Razdan, R. K., Melvin, L. S., Johnson, M. R., & Martin, B. R. (1993). Cannabinoid structure-activity relationships: correlation of receptor binding and in vivo activities. Journal of Pharmacology and Experimental Therapeutics, 265(1), 218-226.

15. Burstein, S. (2005). PPAR-γ: a nuclear receptor with affinity for cannabinoids. Life sciences, 77(14), 1674-1684.García-Arencibia, M., González, S., de Lago, E., Ramos, J. A., Mechoulam, R., & Fernández-Ruiz, J. (2007). Evaluation of the neuroprotective effect of cannabinoids in a rat model of Parkinson's disease: importance of antioxidant and cannabinoid receptor-independent properties. Brain research, 1134, 162-170.

16. Martín-Moreno, A. M., Reigada, D., Ramírez, B. G., Mechoulam, R., Innamorato, N., Cuadrado, A., & de Ceballos, M. L. (2011). Cannabidiol and other cannabinoids reduce microglial activation in vitro and in vivo: relevance to Alzheimers′ disease. Molecular pharmacology, mol-111.

17. Dirikoc, S., Priola, S. A., Marella, M., Zsürger, N., & Chabry, J. (2007). Nonpsychoactive cannabidiol prevents prion accumulation and protects neurons against prion toxicity. Journal of Neuroscience, 27(36), 9537-9544.

18. Malfait, A. M., Gallily, R., Sumariwalla, P. F., Malik, A. S., Andreakos, E., Mechoulam, R., & Feldmann, M. (2000). The nonpsychoactive cannabis constituent cannabidiol is an oral anti-arthritic therapeutic in murine collagen-induced arthritis. Proceedings of the National Academy of Sciences, 97(17), 9561-9566.

19. Specter, S., Lancz, G., & Hazelden, J. (1990). Marijuana and immunity: tetrahydrocannabinol mediated inhibition of lymphocyte blastogenesis. International journal of immunopharmacology, 12(3), 261-267.

20. Klein, T. W., Kawakami, Y., Newton, C., & Friedman, H. (1991). Marijuana components suppress induction and cytolytic function of murine cytotoxic T cells in vitro and in vivo. Journal of Toxicology and Environmental Health, Part A Current Issues, 32(4), 465-477.

21. McCoy, K. L., Gainey, D., & Cabral, G. A. (1995). delta 9-Tetrahydrocannabinol modulates antigen processing by macrophages. Journal of Pharmacology and Experimental Therapeutics, 273(3), 1216-1223.

22. Coffey, R. G., Yamamoto, Y., Snella, E., & Pross, S. (1996). Tetrahydrocannabinol inhibition of macrophage nitric oxide production. Biochemical pharmacology, 52(5), 743-751.

23. Formukong, E. A., Evans, A. T., & Evans, F. J. (1988). Analgesic and antiinflammatory activity of constituents ofCannabis sativa L. Inflammation, 12(4), 361-371.

24. Watzl, B., Scuderi, P., & Watson, R. R. (1991). Marijuana components stimulate human peripheral blood mononuclear cell secretion of interferon-gamma and suppress interleukin-1 alpha in vitro. International journal of immunopharmacology, 13(8), 1091-1097.

25. Srivastava, M. D., Srivastava, B. I. S., & Brouhard, B. (1998). Δ9 tetrahydrocannabinol and cannabidiol alter cytokine production by human immune cells. Immunopharmacology, 40(3), 179-185.

26. Pan, H., Mukhopadhyay, P., Rajesh, M., Patel, V., Mukhopadhyay, B., Gao, B., ... & Pacher, P. (2009). Cannabidiol attenuates cisplatin-induced nephrotoxicity by decreasing oxidative/nitrosative stress, inflammation, and cell death. Journal of Pharmacology and Experimental Therapeutics, 328(3), 708-714.

27. Mecha, M., Feliú, A., Iñigo, P. M., Mestre, L., Carrillo-Salinas, F. J., & Guaza, C. (2013). Cannabidiol provides long-lasting protection against the deleterious effects of inflammation in a viral model of multiple sclerosis: a role for A2A receptors. Neurobiology of disease, 59, 141-150.

28. Notcutt, W., Langford, R., Davies, P., Ratcliffe, S., & Potts, R. (2012). A placebo-controlled, parallel-group, randomized withdrawal study of subjects with symptoms of spasticity due to multiple sclerosis who are receiving long-term Sativex®(nabiximols). Multiple Sclerosis Journal, 18(2), 219-228.

29. Woerly, S., Marchand, R., & Lavallée, G. (1991). Interactions of copolymeric poly (glyceryl methacrylate)-collagen hydrogels with neural tissue: effects of structure and polar groups. Biomaterials, 12(2), 197-203.

30. Wade, D. T., Collin, C., Stott, C., & Duncombe, P. (2010). Meta-analysis of the efficacy and safety of Sativex (nabiximols), on spasticity in people with multiple sclerosis. Multiple Sclerosis Journal, 16(6), 707-714.

31. Brady, C. M., DasGupta, R., Dalton, C., Wiseman, O. J., Berkley, K. J., & Fowler, C. J. (2004). An open-label pilot study of cannabis-based extracts for bladder dysfunction in advanced multiple sclerosis. Multiple Sclerosis Journal, 10(4), 425-433.

32. Barnes, M. P. (2006). Sativex®: clinical efficacy and tolerability in the treatment of symptoms of multiple sclerosis and neuropathic pain. Expert opinion on pharmacotherapy, 7(5), 607-615.

33. Leung, L. (2011). Cannabis and its derivatives: review of medical use. The Journal of the American Board of Family Medicine, 24(4), 452-462.

34. Grotenhermen, F., & Müller-Vahl, K. (2012). The therapeutic potential of cannabis and cannabinoids. Deutsches Ärzteblatt International, 109(29-30), 495.

35. Kwiatkoski, M., Guimaraes, F. S., & Del-Bel, E. (2012). Cannabidiol-treated rats exhibited higher motor score after cryogenic spinal cord injury. Neurotoxicity research, 21(3), 271-280.

36. Chagas, M. H. N., Zuardi, A. W., Tumas, V., Pena-Pereira, M. A., Sobreira, E. T., Bergamaschi, M. M., ... & Crippa, J. A. S. (2014). Effects of cannabidiol in the treatment of patients with Parkinson’s disease: an exploratory double-blind trial. Journal of Psychopharmacology, 28(11), 1088-1098.

37. Iuvone, T., Esposito, G., De Filippis, D., Scuderi, C., & Steardo, L. (2009). Cannabidiol: a promising drug for neurodegenerative disorders?. CNS neuroscience & therapeutics, 15(1), 65-75.

38. Fernández‐Ruiz, J., Sagredo, O., Pazos, M. R., García, C., Pertwee, R., Mechoulam, R., & Martínez‐Orgado, J. (2013). Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?. British journal of clinical pharmacology, 75(2), 323-333.

39. Yamaori, S., Kushihara, M., Yamamoto, I., & Watanabe, K. (2010). Characterization of major phytocannabinoids, cannabidiol and cannabinol, as isoform-selective and potent inhibitors of human CYP1 enzymes. Biochemical pharmacology, 79(11), 1691-1698.

40. Yamaori, S., Maeda, C., Yamamoto, I., & Watanabe, K. (2011). Differential inhibition of human cytochrome P450 2A6 and 2B6 by major phytocannabinoids. Forensic Toxicology, 29(2), 117-124.

41. Yamaori, S., Okamoto, Y., Yamamoto, I., & Watanabe, K. (2011). Cannabidiol, a major phytocannabinoid, as a potent atypical inhibitor for cytochrome P450 2D6. Drug Metabolism and Disposition, dmd-111.

42. Yamaori, S., Ebisawa, J., Okushima, Y., Yamamoto, I., & Watanabe, K. (2011). Potent inhibition of human cytochrome P450 3A isoforms by cannabidiol: role of phenolic hydroxyl groups in the resorcinol moiety. Life sciences, 88(15-16), 730-736.

43. Yamaori, S., Ebisawa, J., Okushima, Y., Yamamoto, I., & Watanabe, K. (2011). Potent inhibition of human cytochrome P450 3A isoforms by cannabidiol: role of phenolic hydroxyl groups in the resorcinol moiety. Life sciences, 88(15-16), 730-736.

44. Koch, M., Dehghani, F., Habazettl, I., Schomerus, C., & Korf, H. W. (2006). Cannabinoids attenuate norepinephrine‐induced melatonin biosynthesis in the rat pineal gland by reducing arylalkylamine N‐acetyltransferase activity without involvement of cannabinoid receptors. Journal of neurochemistry, 98(1), 267-278.

45. Jenny, M., Santer, E., Pirich, E., Schennach, H., & Fuchs, D. (2009). Δ9-Tetrahydrocannabinol and cannabidiol modulate mitogen-induced tryptophan degradation and neopterin formation in peripheral blood mononuclear cells in vitro. Journal of neuroimmunology, 207(1-2), 75-82.

46. Takeda, S., Usami, N., Yamamoto, I., & Watanabe, K. (2009). Cannabidiol-2', 6'-dimethyl ether, a cannabidiol derivative, is a highly potent and selective 15-lipoxygenase inhibitor. Drug Metabolism and Disposition.

47. Usami, N., Yamamoto, I., & Watanabe, K. (2008). Generation of reactive oxygen species during mouse hepatic microsomal metabolism of cannabidiol and cannabidiol hydroxy-quinone. Life sciences, 83(21-22), 717-724.

48. Pertwee, R. G., Howlett, A. C., Abood, M. E., Alexander, S. P. H., Di Marzo, V., Elphick, M. R., ... & Mechoulam, R. (2010). International Union of Basic and Clinical Pharmacology. LXXIX. Cannabinoid receptors and their ligands: beyond CB1 and CB2. Pharmacological reviews, 62(4), 588-631.

Graviola (Annona muricata)

What is Graviola?

Graviola is a large tropical tree with a rich history of traditional use for conditions like cancer, parasitic infection, insomnia, and dysentery. Modern use remains very similar, mainly focusing on tension headaches and muscle aches, insomnia, diabetes, cancer, hypertension, and parasitic infection.

Although the entire plant has been used as medicine by various traditional medical systems, the most common form the plant is available in today is as a leaf extract, and raw leaves intended for tea.

Graviola is gaining in popularity outside worldwide as a general health supplement, blood sugar regulator, and anticancer agent. As a result, it's getting easier to find the herb as time goes on. It is likely this tea will become a staple in Western herbal medicine in the coming years.

Featured Graviola

Shop Now

Shop Now

Shop Now

How Is Graviola Used?

Graviola is mainly used as an adjunctive treatment for cancer, especially leukemia and other haematological cancers, as well as prostate, colon, and breast cancers.

Graviola is also popular as an anti-diabetic herb, and can be used to reduce hypertension, especially in combination with diabetes or metabolic syndrome.

Graviola is a potent anti-parasitic, useful for a wide range of different parasitic species, including worms, protozoa, and bacterial parasites.

Traditional Uses of Graviola

+ South America

Graviola originated from South America and/or the Carribean. All parts of the plant were used as medicine for a wide range of conditions.

The most common use of the plant appears to involve cancer treatment and parasitic infection.

The darkest leaves on the plants were used primarily as a sedative or antispasmodic. They were used to treat insomnia, arthritic pains, colic, dysentery, muscle aches, headaches, and diabetes. The leaves were often placed inside a pillow or bedsheets to improve sleep.

In Brazil, the leaves were made into a tea for treating various liver conditions. The oil of the leaves and unripe fruits were used topically for treating neuralgia, and arthritis.

In Peru, the leaves were used to treat excess catarrh, and the bark and root were used for treating diabetes, insomnia, and muscle aches.

In Guyana, the leaves were used as a heart tonic.

+ Southeast Asia

In Southeast Asia, graviola was an important treatment for malaria. It was made into candies, ice cream, and syrups for treating malaria and other parasites.

Herb Details: Graviola

Herbal Actions:

• Anticancer
• Antinflammatory
• Antioxidant
• Antispasmodic
• Anticonvulsant
• Antidepressant
• Antidiabetic
• Antibacterial
• Antiarthritic
• Antilithic
• Antimalarial
• Bradycardic
• Digestive stimulant
• Febrifuge
• Hepatoprotective
• Hypotensive
• Sedative
• Vasodilator

Weekly Dose

• (1:2 Liquid Extract)
  40-80 mL
• View Dosage Chart

Part Used

• Leaves

Family Name

• Annonaceae

Distribution

• North & South America, The Caribbean, Indonesia, Western Africa, Pacific Islands

Constituents of Interest

• Acetogenins
• Alkaloids (reticulin, coreximine, coclarine and anomurine)
• Essential oils (β-caryophyllene, δ-cadinene, epi-α-cadinol and α-cadinol)
• Quercetin

Common Names

• Graviola
• Custard Apple Tree
• Soursop
• Annona
• Guanabana (South America)

Quality

• Cool*

Pregnancy

• Unknown

Taste

• Sour

Duration of Use

• Avoid long term use.

Botanical Information

Graviola is a large tree, growing to a height of 10m. It requires high humidity, warm weather, and high annual rainfall in order to thrive. It produces large, edible fruits with an acidic taste (hence the common name soursop).

There are over 130 different genera in the Annonaceae family, and around 2300 different species. The Annona genus itself has about 70 different species. Annona muricata is the most commonly grown worldwide.

Phytochemistry

There are over 100 annonaceous acetogenins in the plant, which are considered to be the primary active constituents of the plant. Structurally these chemicals are derivatives of long chain (C35 or C37) fatty acids. These compounds are cytotoxic against tumour cell lines, and molluscicidal.

Graviola is also rich in alkaloids, saponins, terpenoids, flavonoids, coumarins, lactones, anthraquinones, tannins, cardiac glycosides, phenols, and phytosterols.

+ Complete Phytochemical Makeup

Annonaceous Acetogenins

The leaves contain annomuricins A and B, gigantetrocin A, annonacin-10-one, muricatetrocins A and B, annonacin, goniothalamicin, muricatocins A and B, annonacin A, (2,4-trans)-isoannonacin, (2,4-cis)-isoannonacin, annomuricin C, muricatocin C, gigantetronenin, annomutacin, (2,4-trans)-10R-annonacin-A-one, (2,4-cis)-10R-annonacin-A-one, annopentocins A, B and C, cis- and trans-annomuricinD-ones, annomuricine, muricapentocin, muricoreacin and murihexocin C and annocatacin A and B.

Alkaloids

Graviola contains reticulin, coreximine, coclarine and anomurine.

Essential Oils

Graviola contains β-caryophyllene, δ-cadinene, epi-α-cadinol and α-cadinol.

Clinical Applications Of Graviola:

Graviola is useful for parasitic infection, including protozoan, and helminth parasites. It's used as a mild sedative and antispasmodic, and can be very useful for gastrointestinal inflammation and dysbiotic conditions.

Graviola is also a popular treatment for diabetes by slowing lipid per-oxidation, and restoring islet beta-cells in the pancreas.

It's commonly used as an adjunctive treatment of cancer, especially haematological cancers and colon cancer.

Cautions:

Graviola has been reported to increase symptoms of Parkinson's Disease.

Caution advised in combination with other hypoglycaemic drugs due to potential additive effect.

+ Contraindications

• May exacerbate Parkinson's Disease symptoms (Acetogenin content)
• Caution advised in combination with other hypoglycemic drugs due to potential additive effect.
  

Author:

Justin Cooke, BHSc

The Sunlight Experiment

(Updated November 2018)

Recent Blog Posts:

References:

1. Moghadamtousi, S. Z., Fadaeinasab, M., Nikzad, S., Mohan, G., Ali, H. M., & Kadir, H. A. (2015). Annona muricata (Annonaceae): a review of its traditional uses, isolated acetogenins and biological activities. International journal of molecular sciences, 16(7), 15625-15658.

2. De Sousa, O. V., Vieira, G. D. V., De Pinho, J. D. J. R., Yamamoto, C. H., & Alves, M. S. (2010). Antinociceptive and anti-inflammatory activities of the ethanol extract of Annona muricata L. leaves in animal models. International journal of molecular sciences, 11(5), 2067-2078.

3. Torres, M. P., Rachagani, S., Purohit, V., Pandey, P., Joshi, S., Moore, E. D., ... & Batra, S. K. (2012). Graviola: a novel promising natural-derived drug that inhibits tumorigenicity and metastasis of pancreatic cancer cells in vitro and in vivo through altering cell metabolism. Cancer letters, 323(1), 29-40.

4. Coria-Tellez, A. V., Montalvo-Gónzalez, E., Yahia, E. M., & Obledo-Vázquez, E. N. (2016). Annona muricata: A comprehensive review on its traditional medicinal uses, phytochemicals, pharmacological activities, mechanisms of action and toxicity. Arabian Journal of Chemistry.

5. Gavamukulya, Y., Abou-Elella, F., Wamunyokoli, F., & AEl-Shemy, H. (2014). Phytochemical screening, anti-oxidant activity and in vitro anticancer potential of ethanolic and water leaves extracts of Annona muricata (Graviola). Asian Pacific journal of tropical medicine, 7, S355-S363.

6. Arroyo, J., Martínez, J., Ronceros, G., Palomino, R., Villarreal, A., Bonilla, P., ... & Quino, M. (2009, September). Efecto hipoglicemiante coadyuvante del extracto etanólico de hojas de Annona muricata L (guanábana), en pacientes con diabetes tipo 2 bajo tratamiento de glibenclamida. In Anales de la Facultad de Medicina (Vol. 70, No. 3, pp. 163-167). UNMSM. Facultad de Medicina.

7. Adewole, S., & Ojewole, J. (2009). Protective effects of Annona muricata Linn.(Annonaceae) leaf aqueous extract on serum lipid profiles and oxidative stress in hepatocytes of streptozotocin-treated diabetic rats. African journal of traditional, complementary and alternative medicines, 6(1).

8. Adeyemi, D. O., Komolafe, O. A., Adewole, O. S., Obuotor, E. M., Abiodun, A. A., & Adenowo, T. K. (2010). Histomorphological and morphometric studies of the pancreatic islet cells of diabetic rats treated with extracts of Annona muricata. Folia morphologica, 69(2), 92-100.

9. Adewole, S. O., & Caxton-Martins, E. A. (2006). Morphological changes and hypoglycemic effects of Annona muricata linn.(annonaceae) leaf aqueous extract on pancreatic β-cells of streptozotocin-treated diabetic rats. African Journal of Biomedical Research, 9(3).