一种新型芳香化酶抑制剂，FR901537。I. 分类、发酵、分离、理化特性及生物活性。

A new aromatase inhibitor, FR901537. I. Taxonomy, fermentation, isolation, physiochemical characteristics and biological activities.

作者信息

Oohata N, Hori Y, Yamagishi Y, Fujita T, Takase S, Yamashita M, Terano H, Okuhara M

机构信息

Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan.

出版信息

J Antibiot (Tokyo). 1995 Aug;48(8):757-62. doi: 10.7164/antibiotics.48.757.

DOI:10.7164/antibiotics.48.757

PMID:7592017

Abstract

FR901537 is a new aromatase inhibitor produced by a bacterium Bacillus sp. No. 3072. Structural studies of FR901537 suggested that it was a novel naphthol derivative having pantetheine in its structure. FR901537 showed a potent inhibitory activity against aromatase from human placenta or rat ovary, but did not inhibit the activity of 11 beta-hydroxylase from bovine adrenal cortex. Lineweaver-Burk plot analysis revealed that FR901537 is a competitive inhibitor.

摘要

FR901537是由芽孢杆菌属3072号菌株产生的一种新型芳香化酶抑制剂。对FR901537的结构研究表明，它是一种结构中含有泛酰巯基乙胺的新型萘酚衍生物。FR901537对人胎盘或大鼠卵巢的芳香化酶显示出强效抑制活性，但不抑制牛肾上腺皮质11β-羟化酶的活性。Lineweaver-Burk作图分析表明FR901537是一种竞争性抑制剂。