Induction of human cholesterol 7alpha-hydroxylase in HepG2 cells by 2,4,6-trihydroxyacetophenone. Eur J Pharmacol 2005 May 16;515(1-3):43-6
Date
05/18/2005Pubmed ID
15896733DOI
10.1016/j.ejphar.2005.03.039Scopus ID
2-s2.0-20344362658 (requires institutional sign-in at Scopus site) 7 CitationsAbstract
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.
Author List
Charoenteeraboon J, Nithipatikom K, Campbell WB, Piyachaturawat P, Wilairat P, Rongnoparut PAuthor
William B. Campbell PhD Professor in the Pharmacology and Toxicology department at Medical College of WisconsinMESH terms used to index this publication - Major topics in bold
AcetophenonesCell Line, Tumor
Cholesterol 7-alpha-Hydroxylase
Dose-Response Relationship, Drug
Gene Expression Regulation, Enzymologic
Humans
Microsomes
RNA, Messenger
Reverse Transcriptase Polymerase Chain Reaction