Pyripyropenes, novel inhibitors of acyl-CoA:cholesterol acyltransferase produced by Aspergillus fumigatus. I. Production, isolation, and biological properties.
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.
Tomoda
H
H
Research Center for Biological Function, Kitasato Institute, Tokyo, Japan.
Kim
Y K
YK
Nishida
H
H
Masuma
R
R
Omura
S
S
D000818:Animals; D001232:Aspergillus fumigatus / Q000737:chemistry*; D002851:Chromatography, High Pressure Liquid; D005285:Fermentation; D008826:Microbial Sensitivity Tests; D008862:Microsomes, Liver / Q000187:drug effects / Q000201:enzymology; D011725:Pyridines / Q000302:isolation & purification* / Q000494:pharmacology*; D051381:Rats; D012717:Sesquiterpenes / Q000302:isolation & purification* / Q000494:pharmacology*; D002785:Sterol O-Acyltransferase / Q000037:antagonists & inhibitors* / Q000378:metabolism
D011725:Pyridines; D012717:Sesquiterpenes; C082792:pyripyropene A; C082793:pyripyropene B; C082794:pyripyropene C; C082795:pyripyropene D; D002785:Sterol O-Acyltransferase