人体内细胞色素P450 3A探针的研究进展

Advances in research on human cytochrome P450 3A probes

人体内细胞色素P450 3A(CYP3A)是细胞色素P450酶系中最主要的一类。评价CYP3A的活性可用于研究药动学、药物或毒物的代谢、药物相互作用、药物代谢酶的遗传多态性及疾病与代谢酶的相互影响,从而预测最佳给药剂量,达到提高药物治疗效果和减少不良反应的目的。评价CYP3A的活性一般采用探针法,其评价结果的优劣取决于探针的特异性、安全性和方法的科学性。本文就目前被广泛应用的几种CYP3A探针的研究进展作一综述和评价。

The main one in cytochrome P450 subfamily is cytochrome P450 3A（CYP3A）. Evaluation of CYP3A activity can be used to study pharmacokinetics, drug or toxicant metabolism, drug interaction,polymorphism and interaction of disease and metabolic enzymes, thus predicting an optimal dose range to elevate efficacy and reduce adverse reactions of drugs. Probe technique is usually used in evaluation of CYP3A activity. The result is determined by specificity or safety of probe and scientific methods. This review highlights recent advances of the most common and newest in vivo probe substrates.