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烟曲霉产生的新型ACAT抑制剂——吡啶并吡咯烯类化合物。IV. 吡啶并吡咯烯类化合物M至R的结构解析

Pyripyropenes, novel ACAT inhibitors produced by Aspergillus fumigatus. IV. Structure elucidation of pyripyropenes M to R.

作者信息

Tomoda H, Tabata N, Yang D J, Namatame I, Tanaka H, Omura S, Kaneko T

机构信息

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

出版信息

J Antibiot (Tokyo). 1996 Mar;49(3):292-8. doi: 10.7164/antibiotics.49.292.

DOI:10.7164/antibiotics.49.292
PMID:8626247
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-alpha-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 3.80 microM in rat liver microsomes, but pyripyropenes N to R showed moderate inhibitory activity (IC50 11.0 approximately 78.0 microM).

摘要

从烟曲霉FO - 1289 - 2501的广口瓶发酵液的乙酸乙酯提取物中分离出6种新的吡喃并吡咯烯类化合物,即M至R。结构解析表明,所有吡喃并吡咯烯类化合物都具有与吡喃并吡咯烯A至L相同的吡啶基-α-吡喃酮倍半萜核心。其中,吡喃并吡咯烯M对大鼠肝微粒体中的酰基辅酶A:胆固醇酰基转移酶活性表现出最强的抑制作用,IC50值为3.80微摩尔,而吡喃并吡咯烯N至R表现出中等抑制活性(IC50为11.0至78.0微摩尔)。

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