吴茱萸次碱在人肝微粒体中对细胞色素P450酶的抑制作用

目的研究吴茱萸次碱(WZY)在人肝微粒体中对细胞色素P450酶的抑制作用。方法对照组和抑制组酶活性均用探针药测定,探针药物及其代谢产物用HPLC进行检测。用代谢产物与母药比值来表达酶的活性。结果加入50μmol·L-1吴茱萸次碱组CYP1A2,CYP2C19,CYP2E1和CYP2D6的活性显著降低,CYP3A4和CYP2C9活性无显著变化。结论吴茱萸次碱对CYP1A2,CYP2C19,CYP2E1和CYP2D6的活性有显著抑制作用,而对CYP2C9和CYP3A4的活性无显著影响。

Inhibitory effect of rutaecarpine on cytochrome P450s in human liver microsome

OBJECTIVE To determine the inhibitory effect of rutaecarpine(WZY)on cytochrome P450s in human liver microsome.METHODS Probe drugs were incubated with and without adding WZY to study the changes of the enzyme activities.Enzyme activities were represented by the concentration ratio of metabolites to probe drugs.Concentration of the probe drug and their metabolites in the incubated mixture were detected by HPLC.RESULTS The activities of CYP1A2,CYP2C19,CYP2D6 and CYP2E1 were significantly reduced in WZY group. CYP3A4 and CYP2C9 activities were not significantly changed.CONCLUSIONS WZY has a significant inhibitory effect on CYP1A2,CYP2C19,CYP2E1,and CYP2D6,but not on CYP2C9 and CYP3A4.