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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。
OBJECTIVE: In recent years, the clinical application of traditional Chinese medicine has become increasingly widespread. However, its composition is complicated and easily leads to the occurrence of drug interactions and adverse reactions. Cytochrome P-450 Monooxygenase 3A4 (CYP3A4) is an important isozyme in the cytochrome P450 (CYP450) family of members that is responsible for the oxidative metabolism of many compounds both in vitro and in vivo, with pregnane X receptor (PXR) as CYP3A4 Key transcription regulators regulate the activity and expression of CYP3A4. The change of CYP3A4 is believed to be the key to the interaction and toxicity of drugs. The molecular mechanisms by which common Chinese herbal components mediate the transcriptional regulation of CYP3A4 through PXR are described in this article.