Epi-cochlioquinone A, a novel acyl-CoA:cholesterol acyltransferase inhibitor produced by Stachybotrys bisbyi

被引：29

作者：

Fujioka, T

Yao, K

Hamano, K

Hosoya, T

Kagasaki, T

Furukawa, Y

Haruyama, H

Sato, S

Koga, T

Tsujita, Y

机构：

[1] SANKYO CO LTD,RES INST,BIOMED RES LABS,SHINAGAWA KU,TOKYO 140,JAPAN

[2] SANKYO CO LTD,RES INST,ANALYT & METAB RES LABS,SHINAGAWA KU,TOKYO 140,JAPAN

[3] SANKYO CO LTD,TSUKUBA RES LABS,TSUKUBA,IBARAKI 305,JAPAN

[4] SCI INFORMAT CO LTD,SHINAGAWA KU,TOKYO 140,JAPAN

来源：

JOURNAL OF ANTIBIOTICS | 1996年 / 49卷 / 05期

关键词：

D O I：

10.7164/antibiotics.49.409

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

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 1.7 mu M. 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 75 mg/kg.

引用

页码：409 / 413

页数：5

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