Berberine is an isoquinoline alkaloid found in several plant species and appears to have multiple pharmacological effects. It has a molecular weight of 336 grams per mole and the chemical formula is C20H18NO4.
Berberine has a brilliant yellow color and is found in the bark and roots of several plant species including:
- Hydrastis canadensis (Goldenseal)
- Coptis chenensis (Coptis or Golden Thread)
- Berberis aquafolium (Oregon Grape)
- Berberis vulgaris (Barberry)
- Berberis aristata (Tree Tumeric)
The alkaloid is used in some medical staining processes -and in the yellow dyeing of wool in India.
Medical Uses
Berberine-containing herbs have been utilized in traditional healing systems for well over 3000 years. Conventional modern medicine has substantiated these uses and discovered fascinating properties for this unique alkaloid.
Pharmacological properties of berberine include:
- antimicrobial effects
- gastrointestinal support
- antiparasitic activities
- cardiovascular support
- inhibition of inflammation
- fever lowering
- hypoglycemic effects
- destruction of cancerous cells
Antimicrobial Effects
Berberine exhibits antimicrobial effects against several types of bacteria and fungi. It inhibits the ability of E. coli and cholera species to attach to endothelial tissues and erythrocytes. It also inhibits the secretion of toxins by these bacteria that cause diarrhea. Berberine is effective in addressing gastrointestinal challenges from protozoa like giardia and entamoeba histolytica. In addition, it also shows promise against trachimonas species.
Cardiovascular Effects
Extensive animal and human studies have substantiated the abilities of berberine to positively influence cardiovascular health. It increases cardiovascular efficiency in conditions like congestive heart failure and aids in the treatment of arrhythmias like premature ventricular contractions (PVCs). It has a positive inotropic effect while mildly increasing systemic vasodilation. Quite often, patients experience temporary normalization of chronic arrhythmias when they are prescribed berberine for unrelated conditions like traveller's diarrhea.
Mechanisms for cardiovascular pharmacology include:
- calcium channel agonist (enhancer)
- potassium channel blocking
- inhibition of cellular entry of extracellular calcium
- inhibition of catecholamine synthesis
Inflammation
Berberine decreases platelet aggregation, adhesion, and thromboxane A2 release. It also inhibits thrombosis formation. One of the mechanisms for this is the blocking of the creation of products needed for synthesis of inflammatory cytokines. For instance, it appears to inhibit the release of arachidonic acid from cell membrane phospholipids which is required for the creation of inflammatory prostaglandins. Berberine may also modulate levels of prostacyclin.
Additional Uses
Research indicates that berberine disrupts the mitochondrial membranes and induces cell death in some types of cancers. It also appears to reduce the excretion of protein in kidney conditions and is three times as effective at lowering fevers.
Toxic Potential and Side Effects
No severe effects have been documented but gastrointestinal discomfort is not uncommon with large doses. Studies have found no mutagenic activity and the lethal dose for 50% of mice is 25 mg/Kg. Lethal doses for larger animals are much higher.
Expected side effects from very large doses may include:
- hypotension (decreased blood pressure)
- dyspnea (shortness of breath)
- influenza-like fatigue and aches
- gastrointestinal discomfort
- cardiovascular damage
Additionally, herbs containing berberine are considered to be emmenogogue -uterine stimulants. Therefore they are contraindicated in pregnancy.
Dosage Recommendations
While berberine should not be prescribed without the management of a qualified healthcare professional, the recommended therapeutic dosage appears to be 200 mg twice or three times a day.
Supplementary References
Akhter MH, Sabir M, Bhide NK. Antiinflammatory effect of berberine in rats
injected locally with cholera toxin. Indian J Med Res1977;65:133-141.
Lee MK, Kim HS. Inhibitory effects of protoberberine alkaloids from the roots of Coptis japonica on catecholamine biosynthesis in PC12 cells. Planta Med 1996;62:31-34.
Rabbani GH, Butler T, Knight J, et al. Randomized controlled trial of berberine sulfate therapy for diarrhea due to enterotoxigenic Escherichia coli and Vibrio cholerae. J Inf Dis 1987;155:979-984.
Sack RB, Froehlich JL. Berberine inhibits intestinal secretory response of Vibrio cholerae and Escherichia coli enterotoxins. Infect Immun 1982;35:471-475.
Zhu B, Ahrens FA. Effect of berberine on intestinal secretion mediated by Escherichia coli heat-stable enterotoxin in jejunum of pigs. Am J Vet Res1982;43:1594-1598.
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