HERBS: New Uses of Berberine, A Valuable Alkaloid from Herbs (REMEDIES)

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NEW USES OF BERBERINE

A Valuable Alkaloid from Herbs for " Damp-Heat " Syndromes

by Subhuti Dharmananda, Ph.D., Director, Institute for Traditional

Medicine, Portland, Oregon

 

BACKGROUND

 

Berberine is an isoquinoline alkaloid with a bright yellow color that is

easily seen in most of the herb materials that contain any significant

amount of this compound. Among Chinese herbs, the primary sources are

phellodendron and coptis (similar isoquinoline alkaloids, in these

herbs, such as jateorrhizine, coptisine, palmatine, and columbamine,

also have a yellowish color). Berberine has long been used as a dye; it

is currently known as " natural yellow 18, " being one of about 35 yellow

dyes from natural sources.

 

Coptis chinensis rhizomes (huanglian; literally " yellow thread " ) and

related species used as its substitutes have about 4-8% berberine, while

Phellodendron amurense bark (huangbo, literally " yellow bo, " where bo is

this particular type of tree) has about half as much, at 2-4% berberine.

This compound is also found in the less commonly used Chinese herb

sankezhen (B. sargentiana) and in the Japanese barberry (woody portion

of Berberis thunbergii). All of these herbs are known as therapies for

damp-heat syndromes, particularly for intestinal and lung infections,

and they are used topically for various skin diseases. Several Western

herbs also contain berberine, such as barberry root bark (Berberis

vulgaris), Oregon grape root (Berberis aquifolium), and goldenseal root

(Hydrastis canadensis). Berberine was isolated and used as an herbal

drug in China 50 years ago (the drug forms are usually the hydrochloride

or sulfate; the chloride, as used in the dye, may have the strongest

antiseptic action). It has since become an ingredient in several Western

herbal products, particularly for treatment of intestinal infections.

 

Coptis and phellodendron have been used in China for treating

gastrointestinal diseases with reported success; applications have

included acute gastroenteritis, cholera, and bacillary dysentery. So,

the first applications of isolated berberine were for treatment of these

conditions. Recent clinical trials have yielded conflicting results as

to which of the disease organisms causing intestinal symptoms are

responsive to berberine (1, 2). Tests of the antiseptic action of

berberine against bacteria, yeasts, viruses, and amoebas have shown a

range of activity levels from apparent potent action to mild

suppression. Inhibition of giardia and of candida have been areas of

considerable interest and initial positive research results have led to

development of several herb products for those applications.

 

Soon after berberine was prepared as an isolated agent for clinical use,

it was noted that berberine had other potential benefits; for example,

it appeared to reduce high blood pressure at doses of about 1 gram per

day (3). The hypotensive action of berberine has been confirmed in

several pharmacology experiments, but follow-up clinical trials have

been lacking. Still, this effect of berberine fortunately led to further

testing of the compound for patients with cardiovascular disease risk

factors, and evidence developed to demonstrate a lowering of cholesterol

(and triglycerides) and of blood sugar. These new findings are the main

focus of this brief report.

 

CHOLESTEROL

 

There has been increased interest in lowering blood cholesterol, and

especially LDL-cholesterol, as a means of curtailing the high rates of

heart attack and stroke. In addition to recommended dietary changes,

many people are prescribed statin drugs for this goal. The statin drugs

are powerful, frequently effective, and may have other benefits, though

they also pose certain risks. During the 1990s, the Chinese herb

material " red rice yeast " (Monascus purpureus) was sold in the U.S. as a

natural supplement that contains, as one of its active ingredients,

small amounts of lovastatin, one of the widely used statin drugs (it

also contains several related compounds that contributed to the

cholesterol lowering action). After prolonged legal disputes between the

supplement providers, the drug companies, and the FDA about its content

of the drug substance, the sale of red rice yeast and its extracts as

natural cholesterol lowering agents was banned.

 

It was reported recently that berberine lowers cholesterol through a

mechanism different than that of the statin drugs, suggesting potential

use both as an alternative to the statins and as a complementary therapy

that might be used with statins in an attempt to gain better control

over cholesterol. In a controlled Chinese study (4), it was shown that

berberine, administered 500 mg twice per day for 3 months, reduced serum

cholesterol by 29%, triglycerides by 35% and LDL-cholesterol by 25%. The

apparent mechanism is increasing the production of a receptor protein in

the liver that binds the LDL-cholesterol, preparing it for elimination.

 

BLOOD SUGAR

 

Research on use of berberine for diabetes began with Ni Yanxi and his

colleagues in Changchun (a large city in Jilin Province) with diabetes

treatments. As an introduction to a 1995 English language publication on

this subject (presenting their earlier clinical data from 1983-1987),

they wrote (5): " It was found by accident that berberine had the

therapeutic effect on the decrease of blood glucose when the authors

used berberine to treat diarrhea in patients who suffered from diabetes. "

 

Dietary therapy was first introduced to the patients for one month. For

those who still had high fasting blood sugar, berberine was administered

orally at a dose of 300, 400, or 500 mg each time, three times daily,

adjusting the dosage according to the blood glucose levels; this

treatment was followed for 1-3 months. A control group without diabetes

was similarly treated, with no effect on blood sugar. For the diabetic

patients, it was reported that patients had less thirst, consumed less

water and urinated less, had improved strength, and had lower blood

pressure; the symptoms declined in correspondence with declining blood

glucose levels. Laboratory studies suggest that berberine may have at

least two functions in relation to reducing blood sugar: inhibiting

absorption of sugars from the intestine and enhancing production of

insulin. As relayed by Ni in his review of the literature, clinical

experience with berberine has shown that doses of 2 grams per day

produced no side effects.

 

 

REFERENCES

 

1. Rabbani GH, et al., Randomized controlled trial of berberine sulfate

therapy for diarrhea due to enterotoxigenic E. coli and Vibrio cholerae,

Journal of Infectious Diseases 1987; 155(5): 979-984.

 

2. Kaneda Y, et al., In vitro effects of berberine sulphate on the

growth and structure of Entamoeba histolytica, Giardia lamblia, and

Trichomonas vaginalis, Annals of Tropical Medicine and Parasitology

1991; 85(4); 417-425.

 

3. Chang HM and But PPH (editors), Pharmacology and Applications of

Chinese Materia Medica, (volume 2), 1986 World Scientific, Singapore.

 

4. Kong Weijia, et al., Berberine is a novel cholesterol-lowering drug

working through a unique mechanism distinct from statins, Nature

Medicine 2004; 10(12): 1344-1351.

 

5. Ni Yanxia, et al., Therapeutic effect of berberine on 60 patients

with non-insulin dependent diabetes mellitus and experimental research,

Chinese Journal of Integrated Traditional and Western Medicine 1995;

1(2); 91-95.

 

April 2005

 

http://www.itmonline.org/arts/berberine.htm

 

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