title: Pyripyropenes, novel inhibitors of acyl-CoA:cholesterol acyltransferase produced by Aspergillus fumigatus. I. Production, isolation, and biological properties.
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.
authors.affiliation: Research Center for Biological Function, Kitasato Institute, Tokyo, Japan.
authors.forename: H
authors.initials: H
authors.lastname: Tomoda
authors.forename: Y K
authors.initials: YK
authors.lastname: Kim
authors.forename: H
authors.initials: H
authors.lastname: Nishida
authors.forename: R
authors.initials: R
authors.lastname: Masuma
authors.forename: S
authors.initials: S
authors.lastname: Omura
mesh_terms: 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
chemical_list: D011725:Pyridines; D012717:Sesquiterpenes; C082792:pyripyropene A; C082793:pyripyropene B; C082794:pyripyropene C; C082795:pyripyropene D; D002785:Sterol O-Acyltransferase