Drug intelligence / Profile preview

berberine

Development stage
Phase 4
Modality
Small Molecules
Administration
Oral, Topical
01

Overview

Berberine is a quaternary ammonium salt from the protoberberine group of benzylisoquinoline alkaloids. It occurs naturally in several plants including Coptis chinensis (goldthread), Hydrastis canadensis (goldenseal), and Berberis species. Structurally it features a tetracyclic skeleton with a dihydroisoquinoline and isoquinoline ring system. In clinical use—primarily in China—it is an over-the-counter drug for diarrhea due to bacterial infections such as *E. coli* and *Shigella*. Pharmacologically it exhibits antimicrobial activity (notably antibacterial and antifungal), positive inotropic effects on the heart muscle, negative chronotropic effects (slowing heart rate), antiarrhythmic properties, vasodilation activity as well as hypoglycemic and lipid-lowering effects observed in preclinical studies. Its mechanism includes inhibition of CYP3A4 enzyme activity affecting drug metabolism[1][2][3][6]. In Western countries it is widely marketed as a dietary supplement but not approved by regulatory agencies for any specific medical indication.

Brand names
MAGNA Berberine
Other names
UmbellatineBerberinBerbericineBerbinium7,8,13,13a-tetradehydro-9,10-dimethoxy-2,3-[methylenebis(oxy)]berbinium9,10-Dimethoxy-[1,3]dioxolo[4,5-g]isoquinolino[3,2-a]isoquinolin-7-ylium chloride (various salt forms)
02

Targets

CYP3A4 (Cytochrome P450 3A4)

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