Effects of Coix-seed Reactive Derivatives (CRD) on Cytochrome P450 Isoforms CYP3A4, CYP2D6, CYP2C9 In Vitro / 日本補完代替医療学会誌

ABSTRACT

CRD, a Coix-seed Reactive Derivatives, has a novel mechanism in the treatment of various diseases. In the present study, a fluorometric-based high throughput method using cytochrome P450 (CYP)screening kit was adopted to evaluate in vitro inhibition potential of CRD (CRD 1 and CRD 2) on CYP isoenzymes by calculating remaining enzyme activities and inhibitory potential (IC50 values) using the determined values of fluorescence intensity. IC50　of CRD 1 and CRD 2 were as follows: CYP3A4; >500 µg/ml, 490 µg/ml, CYP2D6; >500 µg/ml，>500 µg/ml，CYP2C9; >500 µg/ml，339 µg/ml, respectively. The result showed that CRD exhibited little activity in the inhibition of CYP3A4, CYP2D6 and CYP2C9.