常见中药组分对孕烷X受体介导的CYP3A4转录调节机制的研究进展  

Pregnane X receptor mediated transcriptional regulation mechanism of CYP3A4 by the common components of traditional Chinese medicine

作　　者：曹昌娥[1] 赖泳[2] 杜一民[1] 

机构地区：[1]大理大学药学与化学学院药理学教研室,云南大理671000 [2]大理大学药学与化学学院药理学教研室云南省昆虫生物医药研发重点实验室,云南大理671000

出　　处：《中国医院药学杂志》2016年第7期594-598,共5页Chinese Journal of Hospital Pharmacy

基　　金：国家自然科学基金项目(编号:81241139;81360511)

摘　　要：目的:近年来中药在临床上的应用日益广泛,但其成分复杂,易导致药物相互作用和不良反应的发生。细胞色素P-450单氧酶3A4(CYP3A4)是细胞色素P450(CYP450)家族成员中一种重要的同工酶,负责体内外很多化合物的氧化代谢,孕烷X受体(PXR)作为CYP3A4的关键转录调节因子,可以调节CYP3A4的活性和表达,CYP3A4的改变被认为是药物发生相互作用和毒性反应的关键,本文将阐述常见中药组分通过PXR介导CYP3A4转录调节的分子机制。Traditional Chinese medicines have been widely used in clinical practice,but they can so easily cause drug-drug interactions and adverse reactions because of their complex components.Cytochrome P450 monooxygenase 3A4（CYP3A4）is a crucial isoenzyme of CYP450 family,and is responsible for oxidation and metabolism of many compounds in vivo and in vitro.As a key transcription regulation factor of CYP3A4,pregnane X receptor（PXR）can modulate its activity and expression,and change of CYP3A4 is regarded as the key for drug-drug interaction and toxicity.In this review,we will summarize PXR-mediated molecular mechanism on transcriptional regulation of CYP3A4 by common Chinese medicinal components.

关 键 词：中药组分 PXR CYP3A4 

分 类 号：R966[医药卫生—药理学]