Cocktail探针药物法在中药细胞色素P450酶代谢研究中的应用.doc

Cocktail探针药物法在中药细胞色素P450酶代谢研究中的应用 刘高峰 甄立棉 (哈尔滨医科大学附属第二医院药学部，黑龙江省高校重点实验室，黑龙江 哈尔滨150086) 摘 要：细胞色素P450是人体内最重要的药物代谢酶，中药可抑制或诱导某个或某些细胞色素P450亚酶，从而影响合用药物的代谢，导致药物相互作用发生。对于中药的代谢研究，是中药现代化研究的重要方面，并可提高中药使用的有效性和安全性，促进临床合理用药。Cocktail探针药物法能全面、真实地反映药物代谢的过程，其优点在于多个代谢途径的信息可在单个实验过程获得，并将个体间影响降至最低，此法省时、经济。Cocktail探针药物法用于中药的代谢研究还是一个比较新的研究领域，近几年开始有文献报道。本文介绍了Cocktail法在中药细胞色素P450酶代谢研究中的国内外应用进展，以期系统了解并指导该领域的研究。 关键词：细胞色素P450；中药；Cocktail探针药物法；代谢；研究进展 Review on the effects of Traditional Chinese Medicines on cytochrome P450 system by Cocktail probe drugs LIU Gao-feng ZHEN Li-mian (Department of Pharmacy, the Second Affiliated Hospital of Harbin Medical University, Key Laboratory of University in Heilongjiang Province, Harbin 150086, China) [ABSTRACT] Cytochrome P450 are the most important enzymes for drug metabolism. Some Traditional Chinese Medicines (TCM) can reduce or induce one or some cytochrome P450, and therefore affect combined drug metabolism and result in drug interactions. Studies on metabolism of TCM could enhance effectiveness and safety of the drug use, and promote reasonable clinical use for drugs, meanwhile accelerate the modern study process of TCM. Cocktail probe drugs can reflect the process of drug metabolism wholly and actually. It can gain more information of several metabolic pathways in only one experiment. It can also reduce the interindividual variation to the lowest. It can save time and money. Studies development of the effects of TCM on cytochrome P450 System by Cocktail are introduced and summed up in this paper, in order to systematically understand and guide studies in this field. [KEY WORDS] cytochrome P450（CYP450）Traditional Chinese Medicine；Cocktail probe drugs；metabolism；study development 1 Cocktail探针药物法的应用特点 细胞色素P450酶系(CYP450) 是人体内最重要的药物代谢酶，与药物代谢密切相关的同工酶有 CYP1A2,CYP2A6,CYP2C9,CYP2C19,CYP2D6,CYP2E1和CYP3A4[1]。药物可显著影响药酶细胞色素P450的活性，使其诱导或抑制，并加速或减缓底物和其他药物代谢，这些构成了药物体内过程和药物相互作用的主要机制[2]。 探针药物法指经CYP450代谢的药物,以其代谢物和原型药的比例或速率衡量酶代谢能力变化的方法。两种及两种以上经不同酶代谢的药物同时给予的方法称为“Cockt