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焦曲霉产生的新型乙酰辅酶A酰基转移酶（ACAT）抑制剂——焦曲霉烯类。III. 焦曲霉烯类E至L的结构解析

Pyripyropenes, Novel ACAT inhibitors produced by Aspergillus fumigatus. III. Structure elucidation of pyripyropenes E to L.

作者信息

Tomoda H, Tabata N, Yang D J, Takayanagi H, Nishida H, Omura S, Kaneko T

机构信息

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

出版信息

J Antibiot (Tokyo). 1995 Jun;48(6):495-503. doi: 10.7164/antibiotics.48.495.

DOI:10.7164/antibiotics.48.495
PMID:7622436
Abstract

Eight new pyripyropenes, E to L, were isolated from the culture broth of Aspergillus fumigatus FO-1289-2501 selected as a higher producer by NTG mutation. Structural elucidation indicated that all the pyripyropenes have the same pyridino-alpha-pyrone sesquiterpene core as pyripyropenes A to D. Among them, pyripyropene L showed the most potent inhibition against acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 value of 0.27 microM in rat liver microsomes.

摘要

从经NTG诱变筛选出的高产烟曲霉FO - 1289 - 2501的培养液中分离出8种新的吡喃并吡咯类化合物E至L。结构解析表明，所有吡喃并吡咯类化合物都具有与吡喃并吡咯类化合物A至D相同的吡啶基-α-吡喃酮倍半萜核心结构。其中，吡喃并吡咯类化合物L对大鼠肝微粒体中的酰基辅酶A：胆固醇酰基转移酶（ACAT）活性表现出最强的抑制作用，IC50值为0.27微摩尔。

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