烟曲霉产生的新型酰基辅酶A：胆固醇酰基转移酶抑制剂——吡啶并吡喃类化合物。I. 产生、分离及生物学特性

Pyripyropenes, novel inhibitors of acyl-CoA:cholesterol acyltransferase produced by Aspergillus fumigatus. I. Production, isolation, and biological properties.

作者信息

Tomoda H, Kim Y K, Nishida H, Masuma R, Omura S

机构信息

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

出版信息

J Antibiot (Tokyo). 1994 Feb;47(2):148-53. doi: 10.7164/antibiotics.47.148.

DOI:10.7164/antibiotics.47.148

PMID:8150709

Abstract

Aspergillus fumigatus FO-1289, a soil isolate, was found to produce a series of novel inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT). Four active compounds, named pyripyropenes A, B, C and D, were isolated from the fermentation broth of the producing strain by solvent extraction, silica gel column chromatography, ODS column chromatography and preparative HPLC. Pyripyropenes A, B, C and D show very potent ACAT inhibitory activity in an enzyme assay system using rat liver microsomes with IC50 values of 58, 117, 53 and 268 nM, respectively.

摘要

烟曲霉FO - 1289是一种从土壤中分离得到的菌株，被发现能产生一系列新型的酰基辅酶A：胆固醇酰基转移酶（ACAT）抑制剂。通过溶剂萃取、硅胶柱色谱、ODS柱色谱和制备型高效液相色谱从该产生菌的发酵液中分离出四种活性化合物，分别命名为吡啶并吡喃类化合物A、B、C和D。在使用大鼠肝微粒体的酶分析系统中，吡啶并吡喃类化合物A、B、C和D表现出非常强的ACAT抑制活性，其IC50值分别为58、117、53和268 nM。