中草药对孕烷X受体和组成型雄烷受体等核受体通路影响的研究进展

摘要

孕烷X受体( pregnane X receptor, PXR)是核受体亚家族的成员之一,参与大量的外源性和内源性化学物质的生物转化,能被多种中草药激活,调节下游靶基因的表达,在药物代谢酶和转运体的调节中起重要作用。组成型雄烷受体(constitutive androstane receptor,CAR)和PXR一样能与外源性配体结合调节CYP2B6、CYP3A4、CYP2C19、UGT1A1的表达,共同参与CYP药物代谢酶的调节,成为药物作用的靶标。%Pregnane X receptor ( PXR) , a member of the nuclear receptor subfamily, plays an important role in the regulation of drug metabolic enzymes and transporters. PXR can regulate the expression of downstream target genes through transforming a large number of exogenous and endogenous chemical substances, and can be activated by a variety of Chinese herbal medicines. The same as PXR, constitutive androstane receptor ( CAR) can participate in the regulation of drug metabolic enzyme CYP450 and become the targets of drug action through combining with exogenous ligands to regulate the expression of CYP2B6, CYP3A4, CYP2C19 and UGT1A1.