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FR901277,一种来自抗真菌链霉菌的新型人白细胞弹性蛋白酶抑制剂。产生菌、发酵、分离、理化性质及生物学特性。

FR901277, a novel inhibitor of human leukocyte elastase from Streptomyces resistomycificus. Producing organism, fermentation, isolation, physico-chemical and biological properties.

作者信息

Fujie K, Shinguh Y, Hatanaka H, Shigematsu N, Murai H, Fujita T, Yamashita M, Okamoto M, Okuhara M

机构信息

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

出版信息

J Antibiot (Tokyo). 1993 Jun;46(6):908-13. doi: 10.7164/antibiotics.46.908.

Abstract

A novel human leukocyte elastase inhibitor, FR901277 was discovered in the fermentation broth of Streptomyces resistomycificus No. 7622. FR901277 has a molecular weight of 961 and a molecular formula of C47H63N9O13. The mode of inhibition is competitive, with a Ki of 1.2 x 10(-8) M. Oral administration of FR901277 at doses from 32 to 320 mg/kg significantly prevented human leukocyte elastase-induced foot edema in mice.

摘要

一种新型人白细胞弹性蛋白酶抑制剂FR901277是从抗霉菌链霉菌7622号菌株的发酵液中发现的。FR901277的分子量为961,分子式为C47H63N9O13。其抑制模式为竞争性,抑制常数Ki为1.2×10(-8)M。以32至320mg/kg的剂量口服FR901277可显著预防人白细胞弹性蛋白酶诱导的小鼠足部水肿。

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