Isochromophilones III-VI, inhibitors of acyl-CoA:cholesterol acyltransferase produced by Penicillium multicolor FO-3216

N Arai; K Shiomi; H Tomoda; N Tabata; D J Yang; R Masuma; T Kawakubo; S Omura

doi:10.7164/antibiotics.48.696

Isochromophilones III-VI, inhibitors of acyl-CoA:cholesterol acyltransferase produced by Penicillium multicolor FO-3216

J Antibiot (Tokyo). 1995 Jul;48(7):696-702. doi: 10.7164/antibiotics.48.696.

Authors

N Arai¹, K Shiomi, H Tomoda, N Tabata, D J Yang, R Masuma, T Kawakubo, S Omura

Affiliation

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

PMID: 7649870
DOI: 10.7164/antibiotics.48.696

Abstract

New azaphilones named isochromophilones III-VI were isolated from the culture broth of Penicillium multicolor FO-3216 as inhibitors of acyl-CoA: cholesterol acyltransferase (ACAT). Their structures were elucidated by NMR and other spectroscopic analyses. The IC50 values of isochromophilones III, IV, V and VI for ACAT activity in an enzyme assay using rat liver microsomes were calculated to be 110, 50, 50 and 120 microM, respectively.

MeSH terms

Animals
Benzopyrans / chemistry
Benzopyrans / isolation & purification*
Benzopyrans / pharmacology*
Fermentation
Microbial Sensitivity Tests
Microsomes, Liver / drug effects
Microsomes, Liver / enzymology
Molecular Structure
Penicillium
Rats
Stereoisomerism
Sterol O-Acyltransferase / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Benzopyrans
isochromophilone III
isochromophilone IV
isochromophilone V
isochromophilone VI
Sterol O-Acyltransferase