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.

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.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Acetophenones / pharmacology*
  • Cell Line, Tumor
  • Cholesterol 7-alpha-Hydroxylase / genetics*
  • Dose-Response Relationship, Drug
  • Gene Expression Regulation, Enzymologic / drug effects
  • Humans
  • Microsomes / drug effects
  • Microsomes / enzymology
  • RNA, Messenger / genetics
  • RNA, Messenger / metabolism
  • Reverse Transcriptase Polymerase Chain Reaction

Substances

  • Acetophenones
  • RNA, Messenger
  • 2,4,6-trihydroxyacetophenone
  • Cholesterol 7-alpha-Hydroxylase