title: Mulberroside A suppresses PXR-mediated transactivation and gene expression of P-gp in LS174T cells.
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.
authors.affiliation: Department of Pharmacy, The First Affiliated Hospital of Nanchang University, Nanchang, 330006, People's Republic of China.|Laboratory of Drug Metabolism and Pharmacokinetics, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, 510006, People's Republic of China.
authors.forename: Yuhua
authors.initials: Y
authors.lastname: Li
authors.affiliation: School of Pharmaceutical Sciences, Hainan Medical University, Haikou, 571199, People's Republic of China.
authors.forename: Ling
authors.initials: L
authors.lastname: Huang
authors.affiliation: Laboratory of Drug Metabolism and Pharmacokinetics, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, 510006, People's Republic of China.
authors.forename: Jiahong
authors.initials: J
authors.lastname: Sun
authors.affiliation: Department of Pharmacy, The First Affiliated Hospital of Nanchang University, Nanchang, 330006, People's Republic of China.
authors.forename: Xiaohua
authors.initials: X
authors.lastname: Wei
authors.affiliation: Department of Pharmacy, The First Affiliated Hospital of Nanchang University, Nanchang, 330006, People's Republic of China.
authors.forename: Jinhua
authors.initials: J
authors.lastname: Wen
authors.affiliation: Laboratory of Drug Metabolism and Pharmacokinetics, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, 510006, People's Republic of China.
authors.forename: Guoping
authors.initials: G
authors.lastname: Zhong
authors.affiliation: Laboratory of Drug Metabolism and Pharmacokinetics, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, 510006, People's Republic of China.
authors.forename: Min
authors.initials: M
authors.lastname: Huang
authors.affiliation: Laboratory of Drug Metabolism and Pharmacokinetics, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, 510006, People's Republic of China.
authors.forename: Huichang
authors.initials: H
authors.lastname: Bi
mesh_terms: D018435:ATP Binding Cassette Transporter, Subfamily B / Q000096:biosynthesis; D045744:Cell Line, Tumor; D004187:Disaccharides / Q000494:pharmacology*; D005786:Gene Expression Regulation / Q000187:drug effects*; D006801:Humans; D000077297:Pregnane X Receptor; D011987:Receptors, Steroid / Q000378:metabolism*; D013267:Stilbenes / Q000494:pharmacology*
chemical_list: C513055:ABCB1 protein, human; D018435:ATP Binding Cassette Transporter, Subfamily B; D004187:Disaccharides; D000077297:Pregnane X Receptor; D011987:Receptors, Steroid; D013267:Stilbenes; C420606:mulberroside A
keywords: Mulberroside A; P-glycoprotein; pregnane X receptor; rifampicin; transactivation