中药材2017，Vol.40Issue(3)：684-688,5.DOI:10.13863/j.issn1001-4454.2017.03.040
苦参碱对人孕烷X受体介导的CYP3A4调节及药物相互作用分析
Study on the Effect of Matrine on CYP3A4 Through Human Pregnane X Receptor in vitro
摘要
Abstract
Objective:To investigate the effect of Matrine on CYP3A4 in transcriptional activation and the induction,and to evaluate the interaction of herb-drug in combination.Methods:The cells proliferation effect of Matrine on LS174T and HepG2 cells was determined by CCK-8 assay.Matrine affected on CYP3A4 through human pregnane X receptor transfected into cells and luciferase activities were measured by ransient co-transfection reporter gene assay.Real-time PCR was applied to determine the mRNA expression of pregnane X receptor and CYP3A4 in LS174T and HepG2 cells.Results:In a certain concentration range of Matrine,there was an obvious anti-proliferative effects on HepG2 and LS174T cells.For HepG2 cells,Matrine could induce CYP3A4 transcription by activating human pregnane X receptor,and induce mRNA expression of pregnane X receptor to up-regulate the mRNA expression of CYP3 A4.For LS174T cells,Matrine could induce CYP3A4 transcription by activating human pregnane X receptor,and induce mRNA expression of pregnane X receptor to up-regulate the mRNA expression of CYP3A4,the action was in concentration dependent.Conclusion:The effect of Matrine on CYP3A4 maybe relate to the activation of pregnane X receptor,which indicate that Matrine might has an influence on the metabolism with other drugs in combination.关键词
苦参碱/孕烷X受体/CYP3A4/药物相互作用Key words
Matrine/Pregnane X receptor/CYP3A4/Interaction of drugs分类
医药卫生引用本文复制引用
古月瑜,廖晓忠,刘嘉辉,陈玉玲,林美桂,张丽娜,莫穗林..苦参碱对人孕烷X受体介导的CYP3A4调节及药物相互作用分析[J].中药材,2017,40(3):684-688,5.基金项目
国家自然科学基金面上项目(81274135) （81274135）
