Induction of human cholesterol 7alpha-hydroxylase in HepG2 cells by 2,4,6-trihydroxyacetophenone.
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.
Charoenteeraboon
Juree
J
Department of Biochemistry, Faculty of Science, Mahidol University, Rama VI Rd, Phyatai, Bangkok 10400, Thailand.
Nithipatikom
Kasem
K
Campbell
William B
WB
Piyachaturawat
Pawinee
P
Wilairat
Prapon
P
Rongnoparut
Pornpimol
P
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
D000098:Acetophenones; D012333:RNA, Messenger; C107067:2,4,6-trihydroxyacetophenone; D002790:Cholesterol 7-alpha-Hydroxylase