title: [Induction of UGT1A1 expression by praeruptorin A and praeruptorin C through hCAR pathway].
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.
authors.affiliation: Laboratory of Drug Metabolism and Pharmacokinetics, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
authors.forename: Xu-Nian
authors.initials: XN
authors.lastname: Zhou
authors.forename: Hui-Chang
authors.initials: HC
authors.lastname: Bi
authors.forename: Jing
authors.initials: J
authors.lastname: Jin
authors.forename: Rong-Rong
authors.initials: RR
authors.lastname: Deng
authors.forename: Meng-Jia
authors.initials: MJ
authors.lastname: Ying
authors.forename: Yong-Tao
authors.initials: YT
authors.lastname: Wang
authors.forename: Min
authors.initials: M
authors.lastname: Huang
mesh_terms: D019661:Apiaceae / Q000737:chemistry; D000090702:Constitutive Androstane Receptor; D003374:Coumarins / Q000302:isolation & purification / Q000494:pharmacology*; D004365:Drugs, Chinese Herbal / Q000494:pharmacology; D014453:Glucuronosyltransferase / Q000235:genetics / Q000378:metabolism*; D056945:Hep G2 Cells; D006801:Humans; D018517:Plant Roots / Q000737:chemistry; D010946:Plants, Medicinal / Q000737:chemistry; D012333:RNA, Messenger / Q000378:metabolism; D034741:RNA, Small Interfering / Q000235:genetics / Q000378:metabolism; D018160:Receptors, Cytoplasmic and Nuclear / Q000235:genetics / Q000378:metabolism*; D015398:Signal Transduction; D014162:Transfection; D000099148:UGT1A1 Enzyme
chemical_list: D000090702:Constitutive Androstane Receptor; D003374:Coumarins; D004365:Drugs, Chinese Herbal; D014453:Glucuronosyltransferase; D012333:RNA, Messenger; D034741:RNA, Small Interfering; D018160:Receptors, Cytoplasmic and Nuclear; D000099148:UGT1A1 Enzyme; C441070:praeruptorin A; C058808:praeruptorin C