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

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.