Pyripyropenes, Novel AC AT Inhibitors Produced by Aspergillm fumigatus IV. Structure Elucidation of Pyripyropenes M to R

HIROSHI TOMODA; NORIKO TABATA; DA-JUN YANG; ICHIJI NAMATAME; HARUO TANAKA; SATOSHI OMURA; TAKUSHI KANEKO

doi:10.7164/antibiotics.49.292

Pyripyropenes, Novel AC AT Inhibitors Produced by Aspergillm fumigatus

IV. Structure Elucidation of Pyripyropenes M to R

HIROSHI TOMODA, NORIKO TABATA, DA-JUN YANG, ICHIJI NAMATAME, HARUO TANAKA, SATOSHI OMURA, TAKUSHI KANEKO

Author information

HIROSHI TOMODA
Research Center for Biological Function, The Kitasato Institute, and School of Pharmaceutical Sciences, Kitasato University
NORIKO TABATA
Research Center for Biological Function, The Kitasato Institute, and School of Pharmaceutical Sciences, Kitasato University
DA-JUN YANG
Research Center for Biological Function, The Kitasato Institute, and School of Pharmaceutical Sciences, Kitasato University
ICHIJI NAMATAME
Research Center for Biological Function, The Kitasato Institute, and School of Pharmaceutical Sciences, Kitasato University
HARUO TANAKA
Research Center for Biological Function, The Kitasato Institute, and School of Pharmaceutical Sciences, Kitasato University
SATOSHI OMURA
Research Center for Biological Function, The Kitasato Institute, and School of Pharmaceutical Sciences, Kitasato University
TAKUSHI KANEKO
Central Research Division, Pfizer Inc.

JOURNAL FREE ACCESS

1996 Volume 49 Issue 3 Pages 292-298

DOI https://doi.org/10.7164/antibiotics.49.292

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Abstract

Six new pyripyropenes, M to R, were isolated from the ethyl acetate extracts of the jar fermentation broth of Aspergillus fumigatus FO-1289-2501. Structural elucidation indicated that all the pyripyropenes have the same pyridino-α-pyrone sesquiterpene core as pyripyropenes A to L. Among them pyripyropene M showed the most potent inhibition against acyl-CoA: cholesterol acyltransferase activity with an IC₅₀ value of 3.80μM in rat liver microsomes, but pyripyropenes N to R showed moderate inhibitory activity (IC₅₀ 11.0-78.0μM).

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