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. doi: 10.1016/j.ejphar.2005.03.039.
Juree Charoenteeraboon  1 ,  Kasem Nithipatikom ,  William B Campbell ,  Pawinee Piyachaturawat ,  Prapon Wilairat ,  Pornpimol Rongnoparut
Affiliations
  • 1. Department of Biochemistry, Faculty of Science, Mahidol University, Rama VI Rd, Phyatai, Bangkok 10400, Thailand.
PMID: 15896733 DOI: 10.1016/j.ejphar.2005.03.039
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.

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