摘要
目的:观察7种中药的粗提取物能否通过活化人孕烷X受体(PXR)诱导CYP3A4的转录表达.方法:采用浸提法和回流法制备中药的粗提取物.用PXR依赖的瞬时转染报告基因试验检测7种中药粗提取物的诱导作用.结果:菊花、枸杞子、丹参水提取物,菊花、山楂、金银花、山药、丹参醇提取物等均能通过活化PXR诱导HepG2细胞CYP3A4基因的转录表达.结论:菊花水提取物、枸杞子水提取物、丹参水提取物、菊花醇提取物、山楂醇提取物、枸杞子醇提取物、金银花醇提取物、山药醇提取物和丹参醇提取物等7种中药的提取物均能诱导CYP3A4基因的转录表达,其作用机制是通过活化PXR.菊花、山楂、枸杞子、金银花、山药和丹参的摄入可能影响其他CYP3A4底物在体内的代谢.
Abstract
Objective: To test whether 7 herbs stimulate human pregnane X receptor (PXR)-mediated CYP3A4 transcription.Method: Transient cotransfection reporter gene assays were performed with human PXR expression plasmids and a reporter plasmid containing the XRES in the CYP3A4 gene promoter in HepG2 cells. Result: The aqueous extracts of Chrysanthemi Flos, Lycii Fructus,and Salviae Miltiorrhizae Radix et Rhizoma, and the methanol extracts of Chrysanthemi Flos, Crataegi Fructus, Lycii Fructus, Lonicerae Japonicae Flos, Dioscoreae Rhizoma,and Salviae Miltiorrhizae Radix et Rhizoma, activated human PXR-mediated transcription. Conclusion: The aqueous extracts of Chrysanthemi Flos, Lycii Fructus, and Salviae Miltiorrhizae Radix et Rhizoma, and the methanol extracts of Chrysanthemi Flos, Crataegi Fructus, Lycii Fructus, Lonicerae Japonicae Flos, Dioscoreae Rhizoma, and Salviae Miltiorrhizae Radix et Rhizoma are inducers of CYP3A4 by activating PXR, and thus may influence the metabolism of other substrates on CYP3A4.
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