中国药理学通报2013，Vol.29Issue(4)：501-506,6.DOI:10.3969/j.issn.1001-1978.2013.04.014
白藜芦醇通过拮抗hPXR对P-gp的影响
Effect of resveratrol on expression and activity of P-gp through human pregnane X receptor pathway
摘要
Abstract
Aim To investigate the effect of resveratrol on rifampicin-induced P-gp expression through PXR pathway.Methods Dual-Luciferase reporter assays were performed to detect the activity of MDR1 reporter gene in LS174T cells.Real-Time PCR and Western blot were used to detect mRNA and protein expression of P-gp.In addition, rhodamine 123 ( Rh123 ) accumulation assay was used to investigate the P-gp activity.Results Resveratrol ( RES ) could significantly down regulate the rifampicin-induced MDR1 reporter activation both in concentration of 25 and 50 μmol· L-1( P <0.01 ).Besides, RES could also significantly down regulate rifampicin-induced P-gp mRNA expression only in hPXR-transfected cells, but P-gp protein expression was decreased both in hPXR-transfected and non-transfected cells.Furthermore, 25 and 50 μmol· L-1 RES significantly increased rifampicin-inhibited Rh123 accumulation from 77.7% to 91.7% and 95.1%( P <0.05 ), Which indicated that RES could reduce the induction of P-gp activity by rifampicin.Conclusion Resveratrol could affect P-gp expression and activity as an antagonist of human PXR.关键词
孕烷受体/P-糖蛋白/白藜芦醇/拮抗剂/RT-PCR/利福平/酮康唑Key words
pregnane X receptor/ P-gp/ resveratrol/antagonist/ RT-PCR/ rifampicin/ ketoconazole分类
医药卫生引用本文复制引用
邓蓉蓉,毕惠嫦,金晶,周许年,应梦佳,黄民..白藜芦醇通过拮抗hPXR对P-gp的影响[J].中国药理学通报,2013,29(4):501-506,6.基金项目
国家"十二五"科技重大专项(No 2012ZX09506001-004) （No 2012ZX09506001-004）
国家科技支撑计划参与项目(No 2012BAI29B09) （No 2012BAI29B09）
广州市科技计划项目(No 2011J4300098) （No 2011J4300098）
