2. Academic Validation
  3. Epi-cochlioquinone A, a novel acyl-CoA : cholesterol acyltransferase inhibitor produced by Stachybotrys bisbyi

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

  • J Antibiot (Tokyo). 1996 May;49(5):409-13. doi: 10.7164/antibiotics.49.409.
T Fujioka 1,  K Yao,  K Hamano,  T Hosoya,  T Kagasaki,  Y Furukawa,  H Haruyama,  S Sato,  T Koga,  Y Tsujita
Affiliations

Affiliation

  • 1 Pharmacology Research Laboratory, Sankyo Co., Ltd., Tokyo, Japan.
PMID: 8682715 DOI: 10.7164/antibiotics.49.409
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 1.7 microM. 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.

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