The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Epi-cochlioquinone A, a Novel Acyl-CoA: Cholesterol Acyltransferase Inhibitor Produced by Stachybotrys bisbyi
TOMOYUKI FUJIOKAKEIKO YAOKIYOSHI HAMANOTSUYOSHI HOSOYATAKESHI KAGASAKIYOJI FURUKAWAHIDEYUKI HARUYAMASADAO SATOTEIICHIRO KOGAYOSHIO TSUJITA
Author information
JOURNALS FREE ACCESS

1996 Volume 49 Issue 5 Pages 409-413

Details
Abstract

A novel acyl-CoA: cholesterol acyltransferase (ACAT) inhibitor, designated epi-cochlioquinone A has been isolated from the fermentation broth of Stachybotrys bisbyi SANK 17777. The molecular formula, physicochemical properties, NMR spectroscopic analysis and X-ray crystallographic analysis revealed that this compound was a stereoisomer of cochlioquinone A, which has been previously reported as a nematocidal agent. It inhibited ACAT activity in an enzyme assay using rat liver microsomes with an IC50 value of 1.7μM. However, it showed about 10-fold less potent inhibitory effect on plasma lecithin cholesterol acyltransferase (LCAT) than on ACAT. In addition, it inhibited in vivo cholesterol absorption in rats by 50% at 75mg/kg.

Information related to the author
© Japan Antibiotics Research Association
Next article
feedback
Top