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Purpactins, new inhibitors of acyl-CoA:cholesterol acyltransferase produced by Penicillium purpurogenum. III. Chemical modification of purpactin A.

作者信息

Nishida H, Tomoda H, Cao J, Araki S, Okuda S, Omura S

机构信息

Research Center for Biological Function, Kitasato Institute, Tokyo, Japan.

出版信息

J Antibiot (Tokyo). 1991 Feb;44(2):152-9. doi: 10.7164/antibiotics.44.152.

DOI:10.7164/antibiotics.44.152
PMID:2010355
Abstract

Acylated derivatives of the C-1' and/or C-11 hydroxy group(s) of penicillide were synthesized and their inhibitory activity against acyl-CoA:cholesterol acyltransferase (ACAT) was studied. Introduction of long acyl group into either or both hydroxy residue(s) decreased the inhibitory activity. A small acyl moiety such as acetyl or n-butyryl at the C-1' hydroxy group is responsible for potent inhibitory activity against ACAT. The 1'-O-acetyl-11-O-tetrahydropyranyl derivative (11-O-2''-tetrahydropyranylpurpactin A) showed high selectivity (cytotoxic dose vs. effective dose) in a cell assay using J774 macrophages.

摘要

相似文献

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