title: Induction of human cholesterol 7alpha-hydroxylase in HepG2 cells by 2,4,6-trihydroxyacetophenone.
abstract: In animal the plasma cholesterol-lowering activity of 2,4,6-trihydroxyacetophenone (THA) is due to enhanced cholesterol 7alpha-hydroxylase (CYP7A1) activity. We have examined the effect of THA on CYP7A1 activity and mRNA level in HepG2 cells. THA stimulated CYP7A1 activity in a concentration- and time-dependent manner. After exposure for 24 h, 1 muM THA induced CYP7A1 activity 160+/-8% and mRNA level 166+/-21% (mean+/-S.E.M.) of control. Moreover THA antagonized the inhibitory regulation of chenodeoxycholic acid on CYP7A1 mRNA expression. These results indicated that THA increases CYP7A1 activity in human HepG2 cells by stimulating mRNA transcription.
authors.affiliation: Department of Biochemistry, Faculty of Science, Mahidol University, Rama VI Rd, Phyatai, Bangkok 10400, Thailand.
authors.forename: Juree
authors.initials: J
authors.lastname: Charoenteeraboon
authors.forename: Kasem
authors.initials: K
authors.lastname: Nithipatikom
authors.forename: William B
authors.initials: WB
authors.lastname: Campbell
authors.forename: Pawinee
authors.initials: P
authors.lastname: Piyachaturawat
authors.forename: Prapon
authors.initials: P
authors.lastname: Wilairat
authors.forename: Pornpimol
authors.initials: P
authors.lastname: Rongnoparut
mesh_terms: D000098:Acetophenones / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002790:Cholesterol 7-alpha-Hydroxylase / Q000235:genetics*; D004305:Dose-Response Relationship, Drug; D015971:Gene Expression Regulation, Enzymologic / Q000187:drug effects; D006801:Humans; D008861:Microsomes / Q000187:drug effects / Q000201:enzymology; D012333:RNA, Messenger / Q000235:genetics / Q000378:metabolism; D020133:Reverse Transcriptase Polymerase Chain Reaction
chemical_list: D000098:Acetophenones; D012333:RNA, Messenger; C107067:2,4,6-trihydroxyacetophenone; D002790:Cholesterol 7-alpha-Hydroxylase