Alkaloids and saponins as cytochrome P450 inhibitors from blue cohosh (Caulophyllum thalictroides) in an in vitro assay

Planta medica
Vamsi L M MadgulaShabana I Khan

Abstract

Blue cohosh, Caulophyllum thalictroides (L.) Michx. is a popular herb, roots and rhizomes of which have been extensively used for women's health. Alkaloids and saponins are considered to be responsible for its pharmacological effects. In this investigation the methanolic extract of the roots of blue cohosh, the alkaloidal fraction and isolated constituents were evaluated for their inhibition of major drug metabolizing cytochrome P450 (CYP450) enzymes. The methanolic extract did not show any effect but the alkaloidal fraction showed a strong inhibition of CYP 2C19, 3A4, 2D6, and 1A2 (>80% inhibition at 100 microg/mL) with IC50 values in the range of 2-20 microg/mL. Among the isolated alkaloids, a piperidine-type alkaloid (caulophyllumine B) and three lysine-derived alkaloids (O-acetlybaptifolin, anagyrine, and lupanine) inhibited these enzymes to various extents (IC50:2.5-50 microM). N-Methylcytisine weakly inhibited CYP3A4 only (32% inhibition at 100 microM). An equimolar mixture of alkaloids exhibited a more pronounced inhibitory effect on all four enzymes as compared to the isolated alkaloids. Among the saponins, caulosides C and D inhibited CYP3A4 at the highest test concentration of 100 microM (43% and 35% inhibition, respe...Continue Reading

Citations

Jun 30, 2011·European Journal of Drug Metabolism and Pharmacokinetics·Tingting LiQidong You
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