Clonoamide, a new inhibitor of sterol O-acyltransferase, produced by Clonostachys sp. BF-0131

J Antibiot (Tokyo). 2015 Oct;68(10):615-9. doi: 10.1038/ja.2015.37. Epub 2015 Apr 22.

Abstract

A new compound designated as clonoamide was isolated from a culture broth of the fungus Clonostachys sp. BF-0131 by solvent extraction, Diaion HP20 column chromatography, octadecylsilyl column chromatography and preparative HPLC as an inhibitor of sterol O-acyltransferase (SOAT). The structure of clonoamide was elucidated as 2-oxo-9E,11E-tridecandienyl acetamide by various spectral analyses including NMR. The compound inhibited SOAT1 and SOAT2 isozymes with IC50 values of 39 and 110 μm, respectively, in a cell-based assay using SOAT1- and SOAT2-expressing Chinese hamster ovary cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetamides / chemistry*
  • Acetamides / metabolism
  • Animals
  • Anti-Infective Agents / pharmacology
  • CHO Cells
  • Chlorocebus aethiops
  • Cricetinae
  • Cricetulus
  • Enzyme Inhibitors / pharmacology*
  • Fermentation
  • Fungi / chemistry*
  • Isoenzymes / antagonists & inhibitors
  • Macrophages, Peritoneal / drug effects
  • Macrophages, Peritoneal / enzymology
  • Magnetic Resonance Spectroscopy
  • Mice
  • Microbial Sensitivity Tests
  • Microsomes / drug effects
  • Microsomes / enzymology
  • Sterol O-Acyltransferase / antagonists & inhibitors*

Substances

  • Acetamides
  • Anti-Infective Agents
  • Enzyme Inhibitors
  • Isoenzymes
  • clonoamide
  • Sterol O-Acyltransferase