Mulberroside A suppresses PXR-mediated transactivation and gene expression of P-gp in LS174T cells
Mulberroside A suppresses PXR-mediated transactivation and gene expression of P-gp in LS174T cells
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Mulberroside A 抑制 LS174T 细胞中 PXR 介导的反式激活和 P-gp 基因表达
DOI：
10.1002/jbt.21884
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发表时间：
2017-05-01
影响因子：
3.6
通讯作者：
Bi, Huichang
中科院分区：
文献类型：
--
作者：
Li, Yuhua;Huang, Ling;Bi, Huichang
桑白皮苷A(Mulberroside A，MUL A)是桑白皮的主要活性成分，已正式列入《中国药典》。孕烷X受体(PXR)被认为是人P-糖蛋白(P-gp)基因反式激活的关键介质。本研究探讨了MUL A对PXR介导的P-gp反式激活和基因表达的影响。结果发现，MUL A显著抑制PXR介导的利福平(Rif)诱导的P-gp荧光素酶活性。此外，Rif诱导P-gp表达和转运活性增加，这一作用可被MuL-A明显抑制，但在没有Rif的情况下，MuL A不抑制P-gp荧光素酶的活性、P-gp的表达和功能。这些结果表明，Mul A抑制PXR介导的反式激活和Rif诱导的P-gp表达。当MUL A或桑白皮与Rif或其他PXR激动剂药物联合给药时，应考虑这一点来预测任何潜在的草药相互作用。
Mulberroside A (Mul A) is the main bioactive constituents of Sangbaipi, which is officially listed in the Chinese Pharmacopoeia. The pregnane X receptor (PXR) has been recognized as the critical mediator of human P-glycoprotein (P-gp) gene transactivation. In this study, the effect of Mul A on PXR-mediated transactivation and gene expression of P-gp was investigated. It was found that Mul A significantly suppressed PXR-mediated P-gp luciferase activity induced by rifampicin (Rif). Furthermore, Rif induced an elevation of P-gp expression and transport activity, which was apparently suppressed by Mul A. However, Mul A did not suppress the P-gp luciferase activity, P-gp expression, and function in the absence of Rif. These findings suggest that Mul A suppresses PXR-mediated transactivation and P-gp expression induced by Rif. This should be taken into consideration to predict any potential herb-drug interactions when Mul A or Sangbaipi are co-administered with Rif or other PXR agonist drugs.