温肾咳喘片主要成分对HepG2细胞中CYP相关基因表达的影响

观察温肾咳喘片组方中5种主要单体成分甘草酸、厚朴酚、和厚朴酚、蛇床子素和 欧前胡素对细胞色素P450(cytochrome P450, CYP) 1A2，2D6，2E1和3A4基因表达的影 响. 采用实时荧光定量PCR技术检测HepG2细胞中药物处理后各CYP mRNA的表达.厚朴酚 、和厚朴酚、蛇床子素和欧前胡素在不同浓度均能明显的诱导CYP2E1和CYP3A4，同时欧 前胡素也能诱导CYP1A2的表达，而甘草酸、厚朴酚、和厚朴酚、蛇床子素和欧前胡素在 不同浓度对CYP2D6的表达均具有较弱的抑制作用.甘草酸、厚朴酚、和厚朴酚、蛇床子 素和欧前胡素能明显影响CYP1A2、2D6、2E1或3A4的表达.此研究为中西药物代谢性相互 作用及毒理学的研究提供实验依据.

Effect of Five Components of Wenshen Kechuan Tablet on CYP Related Gene Expression in HepG2 Cells

The application of botanical supplements or herbal medicinal products with synthetic drugs that are cytochrome P450 enzyme substrates may induce significant herb-drug interaction and may alter pharmacotherapy.In this study,we have investigated potential influence of the five bioactive compounts of Wenshenkechuan tablet on cytochrome P450 enzyme(CYP)1A2,2D6,2E1 and 3A4 mRNA expression.The mRNA expression levels of four CYP enzymes were determined by real-time quantitative PCR using specific target primers for P450 genes.The results demonstrated that magnolol,honokiol,osthole and imperatorin induced CYP2E1 and CYP3A4 at different concentrations.And imperatorin also induced CYP1A2 at different concentrations.However,the level of CYP2D6 expression could be decreased by glycyrrhizic acid,magnolol,honokiol,osthole and imperatorin at the different concentrations.The level of CYP expression could be significantly induced or inhibited by glycyrrhizic acid,magnolol,honokiol,osthole and imperatorin.The results could supply the evidence for the interaction of herb-drug based on cytochrome P450 and toxicity,so cares should be taken when glycyrrhizic acid,magnolol,honokiol,osthole and imperatorin are co-administered with other drugs.