Inhibition of lipid droplet accumulation in mouse macrophages by stemphone derivatives

J Antibiot (Tokyo). 2008 Aug;61(8):509-14. doi: 10.1038/ja.2008.68.

Abstract

From a study on the biological activity of fungal stemphones and their derivatives, five derivatives having an O-alkyl moiety at C-11 of stemphone C were found to inhibit lipid droplet accumulation in macrophages without any cytotoxic effect. Among the derivatives, those having O-isopropyl and O-isobutyl were the most potent inhibitors by blocking the synthesis of both cholesteryl ester (CE) and triacylglycerol (TG), the main constituents of lipid droplets in macrophages.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Atherosclerosis / metabolism
  • Atherosclerosis / prevention & control
  • Benzoquinones / pharmacology*
  • Cholesterol / metabolism
  • Cholesterol Esters / biosynthesis
  • Diacylglycerol O-Acyltransferase / antagonists & inhibitors
  • Diacylglycerol O-Acyltransferase / metabolism
  • Foam Cells / drug effects
  • Foam Cells / metabolism*
  • Lipid Metabolism / drug effects*
  • Macrophages, Peritoneal / drug effects
  • Macrophages, Peritoneal / metabolism
  • Mice
  • Sterol O-Acyltransferase / antagonists & inhibitors
  • Sterol O-Acyltransferase / metabolism
  • Triglycerides / biosynthesis

Substances

  • Benzoquinones
  • Cholesterol Esters
  • Triglycerides
  • stemphone
  • Cholesterol
  • DGAT2 protein, mouse
  • Diacylglycerol O-Acyltransferase
  • Sterol O-Acyltransferase
  • sterol O-acyltransferase 1