Mulberroside A suppresses PXR‐mediated transactivation and gene expression of P‐gp in LS174T cells. Issue 5 (5th December 2016)

• Record Type: Journal Article
• Authors: Li, Yuhua; Huang, Ling; Sun, Jiahong; Wei, Xiaohua; Wen, Jinhua; Zhong, Guoping; Huang, Min; Bi, Huichang
• Is Part Of: Journal of biochemical and molecular toxicology. Volume 31:Issue 5(2017)
• Page Start: N/A
• Page End: N/A
• Publication Date: 2016-12-05
• Subjects: Mulberroside A -- pregnane X receptor -- P‐glycoprotein -- rifampicin -- transactivation; Biochemistry -- Periodicals; Molecular biology -- Periodicals; Toxicology -- Periodicals; 574
• DOI: 10.1002/jbt.21884
• Languages: English
• ISSNs: 1095-6670

Abstract

Abstract: 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.