CYP450酶与中药代谢相互作用及酶活性测定研究进展.docVIP

CYP450酶与中药代谢相互作用及酶活性测定研究进展 　　[摘要] 药物对于人体属于外源性化合物，进入人体后将被许多酶所代谢。CYP450酶作为主要的代谢酶，且是重要的药物I相代谢酶，人体约75%的药物代谢是通过CYP450酶进行，而且CYP450酶是引起中药-中药（药对）、中药-西药等联合用药时药物相互作用产生的关键因素。为明确代谢酶与中药代谢的相互作用关系，普遍以酶活性作为评价指标，即以CYP450酶活性的增强和降低来推断中药有效成分及提取物等对酶的诱导或抑制作用。目前，代谢酶活性测定的常用方法是Cocktail探针药物法，其中探针底物的选择是关键。这对研究药物在机体内的吸收、分布、代谢及排泄（ADME）过程有着重大意义。该文就中药、中药有效成分、中药提取物及Cocktail探针底物等与CYP450酶的相互作用进行了综述，以期对将来的相关研究有借鉴和指导意义。 　　[关键词] 中药;有效成分;CYP450酶;代谢;探针底物 　　Interaction between CYP450 enzymes and metabolism of traditional 　　Chinese medicine as well as enzyme activity assay 　　LU Tu-lin1，2， SU Lian-lin1， JI De1，2， GU Wei1， MAO Chun-qin1* 　　（1.College of Pharmacy， Nanjing University of Chinese Medicine， Nanjing 210023， China; 　　2. Jiangsu Provincial Key Laboratory of Chinese Medicine Processing， Nanjing University of Chinese Medicine， Nanjing 210023， China） 　　[Abstract] Drugs are exogenous compounds for human bodies， and will be metabolized by many enzymes after administration. CYP450 enzyme， as a major metabolic enzyme， is an important phase I drug metabolizing enzyme. In human bodies， about 75% of drug metabolism is conducted by CYP450 enzymes， and CYP450 enzymes is the key factor for drug interactions between traditional Chinese medicine（TCM）-TCM， TCM-medicine and other drug combination. In order to make clear the interaction between metabolic enzymes and TCM metabolism， we generally chose the enzymatic activity as an evaluation index. That is to say， the enhancement or reduction of CYP450 enzyme activity was used to infer the inducing or inhibitory effect of active ingredients and extracts of traditional Chinese medicine on enzymes. At present， the common method for measuring metabolic enzyme activity is Cocktail probe drugs， and it is the key to select the suitable probe substrates. This is of great significance for study drug′s absorption， distribution， metabolism and excretion （ADME） process in organisms. The study focuses on the interaction between TCMs， active ingredients， herbal extracts，