Pyripyropenes, novel inhibitors of acyl-CoA:cholesterol acyltransferase produced by Aspergillus fumigatus. I. Production, isolation, and biological properties

H Tomoda; Y K Kim; H Nishida; R Masuma; S Omura

doi:10.7164/antibiotics.47.148

Pyripyropenes, novel inhibitors of acyl-CoA:cholesterol acyltransferase produced by Aspergillus fumigatus. I. Production, isolation, and biological properties

J Antibiot (Tokyo). 1994 Feb;47(2):148-53. doi: 10.7164/antibiotics.47.148.

Authors

H Tomoda¹, Y K Kim, H Nishida, R Masuma, S Omura

Affiliation

¹ Research Center for Biological Function, Kitasato Institute, Tokyo, Japan.

PMID: 8150709
DOI: 10.7164/antibiotics.47.148

Abstract

Aspergillus fumigatus FO-1289, a soil isolate, was found to produce a series of novel inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT). Four active compounds, named pyripyropenes A, B, C and D, were isolated from the fermentation broth of the producing strain by solvent extraction, silica gel column chromatography, ODS column chromatography and preparative HPLC. Pyripyropenes A, B, C and D show very potent ACAT inhibitory activity in an enzyme assay system using rat liver microsomes with IC50 values of 58, 117, 53 and 268 nM, respectively.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Aspergillus fumigatus / chemistry*
Chromatography, High Pressure Liquid
Fermentation
Microbial Sensitivity Tests
Microsomes, Liver / drug effects
Microsomes, Liver / enzymology
Pyridines / isolation & purification*
Pyridines / pharmacology*
Rats
Sesquiterpenes / isolation & purification*
Sesquiterpenes / pharmacology*
Sterol O-Acyltransferase / antagonists & inhibitors*
Sterol O-Acyltransferase / metabolism

Substances

Pyridines
Sesquiterpenes
pyripyropene A
pyripyropene B
pyripyropene C
pyripyropene D
Sterol O-Acyltransferase