title: Pyripyropenes, novel ACAT inhibitors produced by Aspergillus fumigatus. IV. Structure elucidation of pyripyropenes M to R.
abstract: Six new pyripyropenes, M to R, were isolated from the ethyl acetate extracts of the jar fermentation broth of Aspergillus fumigatus FO-1289-2501. Structural elucidation indicated that all the pyripyropenes have the same pyridino-alpha-pyrone sesquiterpene core as pyripyropenes A to L. Among them pyripyropene M showed the most potent inhibition against acyl-CoA : cholesterol acyltransferase activity with an IC50 value of 3.80 microM in rat liver microsomes, but pyripyropenes N to R showed moderate inhibitory activity (IC50 11.0 approximately 78.0 microM).
authors.affiliation: Research Center for Biological Function, Kitasato University, Kitasato Institute, Tokyo, Japan.
authors.forename: H
authors.initials: H
authors.lastname: Tomoda
authors.forename: N
authors.initials: N
authors.lastname: Tabata
authors.forename: D J
authors.initials: DJ
authors.lastname: Yang
authors.forename: I
authors.initials: I
authors.lastname: Namatame
authors.forename: H
authors.initials: H
authors.lastname: Tanaka
authors.forename: S
authors.initials: S
authors.lastname: Omura
authors.forename: T
authors.initials: T
authors.lastname: Kaneko
mesh_terms: D000818:Animals; D001232:Aspergillus fumigatus / Q000378:metabolism; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002851:Chromatography, High Pressure Liquid; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D008862:Microsomes, Liver / Q000187:drug effects / Q000201:enzymology; D015394:Molecular Structure; D011725:Pyridines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D012717:Sesquiterpenes / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D002785:Sterol O-Acyltransferase / Q000037:antagonists & inhibitors*
chemical_list: D004791:Enzyme Inhibitors; D011725:Pyridines; D012717:Sesquiterpenes; C099308:pyripyropene M; C099309:pyripyropene N; C099310:pyripyropene O; C099311:pyripyropene P; C099312:pyripyropene Q; D002785:Sterol O-Acyltransferase