体外代谢体系中中药及其成分对肝脏CYP450代谢酶抑制作用的研究进展

Review of the in vitro inhibitory effects of traditional Chinese medicine and its components on CYP450 enzymes in liver microsomes

细胞色素P450(CYP450)是肝微粒体中参与体内I相代谢反应的酶,临床上90%以上的药物都经CYP450氧化代谢,其被诱导或抑制是引起药物相互作用的主要机制。通过离体器官、细胞或酶系统进行的体外代谢研究以其精准、简化等特点近年来发展迅速。中药的体外代谢研究可推断药物可能的代谢途径和参与代谢的CYP450酶,研究药物的相互作用,更好地解释中药及其成分的作用机制,促进临床合理用药。本文就中药、中药成分、中药提取物在不同种属肝微粒体中对CYP450代谢酶活性的抑制作用进行综述,以期为中药-中药、中药-化学药物之间相互作用研究提供借鉴与参考。

Cytochrome P450s(CYP450)is a superfamily of phase I metabolic enzymes,which participates in more than 90%of drug oxidation.The induction or inhibition of CYP450 s is the main mechanism of drug-drug interaction.In recent years,in vitro metabolism studies conducted through isolated organs,cells,or enzyme systems have developed rapidly,due to their precision and simplicity.Therefore,profiles of the in vitro metabolism studies of traditional Chinese medicines can infer the possible metabolic pathways of drugs,predict the potential drug interactions,and may enhance the rational use of drugs in clinic.This article reviews the in vitro inhibitory effects of traditional Chinese medicine,ingredients,and extracts on the activities of CYP450 enzymes in the liver microsomes,which can provide a reference for further researches on the interaction between Chinese medicine and chemical medicine.