Selective inhibition of acyl-CoA:cholesterol acyltransferase 2 isozyme by flavasperone and sterigmatocystin from Aspergillus species.
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.
Sakai
Kent
K
School of Pharmacy, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan.
Ohte
Satoshi
S
Ohshiro
Taichi
T
Matsuda
Daisuke
D
Masuma
Rokuro
R
Rudel
Lawrence L
LL
Tomoda
Hiroshi
H
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
D002867:Chromones; D004791:Enzyme Inhibitors; D013241:Sterigmatocystin; D002785:Sterol O-Acyltransferase; D000097587:Sterol O-Acyltransferase 2; C535085:flavasperone; C493492:sterol O-acyltransferase 1