Inhibition of diacylglycerol acyltransferase by phenylpyropenes produced by Penicillium griseofulvum F1959

J Microbiol Biotechnol. 2008 Nov;18(11):1785-8. doi: 10.4014/jmb.0800.079.

Abstract

Phenylpyropenes A, B, and C, isolated from Penicillium griseofulvum F1959, inhibited DGAT in rat liver microsomes with IC50 values of 78.7+/-1.6, 21.7+/-0.2, and 11.04+/-0.2 mM, respectively. In addition, a kinetic analysis using a Lineweaver-Burk plot revealed that phenylpyropene C was a noncompetitive inhibitor of DGAT. The apparent Michaelis constant (Km) value and inhibition constant (Ki) value were calculated to be 8 mM and 10.4 mM, respectively. Moreover, phenylpyropene C inhibited triglyceride formation in HepG2 cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Diacylglycerol O-Acyltransferase / antagonists & inhibitors*
  • Diacylglycerol O-Acyltransferase / metabolism
  • Heterocyclic Compounds, 4 or More Rings / chemistry
  • Heterocyclic Compounds, 4 or More Rings / metabolism*
  • Heterocyclic Compounds, 4 or More Rings / pharmacology*
  • Humans
  • Kinetics
  • Liver / ultrastructure
  • Male
  • Microsomes / enzymology
  • Penicillium / growth & development
  • Penicillium / metabolism*
  • Rats
  • Rats, Sprague-Dawley
  • Triglycerides / metabolism

Substances

  • Heterocyclic Compounds, 4 or More Rings
  • Triglycerides
  • phenylpyropene A
  • phenylpyropene B
  • phenylpyropene C
  • Diacylglycerol O-Acyltransferase