Abstract
Gelsemium elegans (GE), widely distributed in East Asia, South East Asia and Northern America, is a kind of well-known toxic plant throughout the world. Yet it has been used as a Chinese folk medicine for treatment of malignant tumors, pain, rheumatic arthritis, psoriasis and immune function. The present study was to investigate the potential inhibitory effects of G. elegans (GE) roots on four major cytochrome P450 (CYP450) isoforms (CYP1A2, CYP2A6, CYP2E1 and CYP3A4) in vitro. Four extracts (petroleum ether, dichloromethane, EtOAc and aqueous) of GE and two commercially available alkaloids (koumine and humantenmine) were screened for their CYP isoforms inhibitory activity. Four enzyme inhibition assays were examined according to the method of the literature. Phenacetin, coumarin, chlorzoxazone and testosterone were used as probe substrates in order to determine CYP1A2, CYP2A6, CYP2E1 and CYP3A4 catalytic activity, respectively. Each probe substrate was incubated with or without each extract and active constituent for corresponding isoform, followed by determination of the kinetics parameters, IC50 and Ki, to characterize inhibitory effects. GE dichloromethane extract selectively inhibited activities of CYP2E1 (IC50=29.04µg/ml)...Continue Reading
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