槲皮素对P-糖蛋白转录调控机制的研究

STUDY ON THE TRANSCRIPTION REGULATION MECHANISM OF QUERCETIN ON P-GP

目的:探讨槲皮素对P-糖蛋白的转录调节机制。方法:利用构建的双荧光素酶报告基因系统,将hVDR真核表达载体、P-糖蛋白报告基因载体和内对照载体共同瞬时转染COS-7细胞,以100nM的1,25(OH)2D3为阳性对照,用不同浓度(10、15、20μmol/L)的槲皮素处理细胞48h后,检测双荧光素酶活性。结果:荧光素酶活性检测显示,槲皮素孵育后可激活P-糖蛋白的表达,各浓度处理组的双荧光素酶活性值显著升高(P<0.01)。结论:槲皮素可诱导P-糖蛋白的表达,其可能机制是通过hVDR介导。

Objective：To investigate the transcription regulation mechanism of quercetin on P-glycoprotein（p-gp） .Methods：hVDR eukaryotic expression vector and reporter gene plasmid of MDR1 were constructed based upon the dual luciferase reporter gene platform,and co-transfected into COS-7 cells. The dual-luciferase activity was detected after the transfected cells were treated with quercetin of various concentration（10,15,20 μmol/L） for 48h,and 1,25（OH） 2D3（100nmol/L） was taken as positive control.Results：Quercetin could activiate expression of p-gp,the dual-luciferase activity of each quercetin concentration group increased obviously（P0.01） .Conclusions：Quercetin may induce expression of p-gp mediated by nuclear hVDR.