Premium
Mulberroside A suppresses PXR‐mediated transactivation and gene expression of P‐gp in LS174T cells
Author(s) -
Li Yuhua,
Huang Ling,
Sun Jiahong,
Wei Xiaohua,
Wen Jinhua,
Zhong Guoping,
Huang Min,
Bi Huichang
Publication year - 2017
Publication title -
journal of biochemical and molecular toxicology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.526
H-Index - 58
eISSN - 1099-0461
pISSN - 1095-6670
DOI - 10.1002/jbt.21884
Subject(s) - transactivation , pregnane x receptor , chemistry , gene expression , gene , microbiology and biotechnology , biology , transcription factor , biochemistry , nuclear receptor
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.