title: Selective inhibition of acyl-CoA:cholesterol acyltransferase 2 isozyme by flavasperone and sterigmatocystin from Aspergillus species.
abstract: Five known fungal metabolites, aurasperone A, aurasperone D, averufanin, flavasperone and sterigmatocystin, were isolated from the culture broths of Aspergillus species as inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT) in the cell-based assay using ACAT1- and ACAT2-expressing CHO cells. These compounds share a similar polycyclic skeleton. Among them, flavasperone and sterigmatocystin, having an angular skeleton, showed selective inhibition toward ACAT2 isozyme, while the others having a linear one had no selectivity in inhibition.
authors.affiliation: School of Pharmacy, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan.
authors.forename: Kent
authors.initials: K
authors.lastname: Sakai
authors.forename: Satoshi
authors.initials: S
authors.lastname: Ohte
authors.forename: Taichi
authors.initials: T
authors.lastname: Ohshiro
authors.forename: Daisuke
authors.initials: D
authors.lastname: Matsuda
authors.forename: Rokuro
authors.initials: R
authors.lastname: Masuma
authors.forename: Lawrence L
authors.initials: LL
authors.lastname: Rudel
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Tomoda
mesh_terms: D000818:Animals; D001230:Aspergillus / Q000378:metabolism*; D016466:CHO Cells; D002867:Chromones / Q000737:chemistry / Q000494:pharmacology*; D006224:Cricetinae; D003412:Cricetulus; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D013241:Sterigmatocystin / Q000737:chemistry / Q000494:pharmacology*; D002785:Sterol O-Acyltransferase / Q000037:antagonists & inhibitors*; D000097587:Sterol O-Acyltransferase 2
chemical_list: D002867:Chromones; D004791:Enzyme Inhibitors; D013241:Sterigmatocystin; D002785:Sterol O-Acyltransferase; D000097587:Sterol O-Acyltransferase 2; C535085:flavasperone; C493492:sterol O-acyltransferase 1