Induction of UGT1A1 expression by praeruptorin A and praeruptorin C through hCAR pathway.
- Author:
Xu-Nian ZHOU
1
;
Hui-Chang BI
;
Jing JIN
;
Rong-Rong DENG
;
Meng-Jia YING
;
Yong-Tao WANG
;
Min HUANG
Author Information
1. Laboratory of Drug Metabolism and Pharmacokinetics, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
- Publication Type:Journal Article
- MeSH:
Apiaceae;
chemistry;
Coumarins;
isolation & purification;
pharmacology;
Drugs, Chinese Herbal;
pharmacology;
Glucuronosyltransferase;
genetics;
metabolism;
Hep G2 Cells;
Humans;
Plant Roots;
chemistry;
Plants, Medicinal;
chemistry;
RNA, Messenger;
metabolism;
RNA, Small Interfering;
genetics;
metabolism;
Receptors, Cytoplasmic and Nuclear;
genetics;
metabolism;
Signal Transduction;
Transfection
- From:
Acta Pharmaceutica Sinica
2013;48(5):794-798
- CountryChina
- Language:Chinese
-
Abstract:
This study is purposed to investigate the effects of praeruptorin A (PA) and praeruptorin C (PC) on UGT1A1 in HepG2 cells through hCAR pathway. PA and PC were incubated with HepG2 cells for 24 h and 48 h, mRNA and protein expressions of UGT1A1 were determined by real-time PCR and Western blotting assays. Additionally, effects of PA and PC on UGT1A1 mRNA and protein expressions were also measured after transient transfection of a specific CAR siRNA for 72 h in HepG2 cells. UGT1A1 mRNA and protein expression levels were significantly increased by PA and PC after incubation for 48 h. Moreover, the mRNA and protein up-regulations of UGT1A1 were attenuated by transient transfection of a specific CAR siRNA, suggesting the induction was mediated by CAR. The results suggest that PA and PC can significantly up-regulate UGT1A1 expression partially via the CAR-mediated pathway.
