FR901277, A NOVEL INHIBITOR OF HUMAN-LEUKOCYTE ELASTASE FROM STREPTOMYCES-RESISTOMYCIFICUS - PRODUCING ORGANISM, FERMENTATION, ISOLATION, PHYSICOCHEMICAL AND BIOLOGICAL PROPERTIES

被引:13
作者
FUJIE, K [1 ]
SHINGUH, Y [1 ]
HATANAKA, H [1 ]
SHIGEMATSU, N [1 ]
MURAI, H [1 ]
FUJITA, T [1 ]
YAMASHITA, M [1 ]
OKAMOTO, M [1 ]
OKUHARA, M [1 ]
机构
[1] FUJISAWA PHARMACEUT CO LTD,EXPLORAT RES LABS,5-2-3 TOKODAI,TSUKUBA,IBARAKI 30026,JAPAN
关键词
D O I
10.7164/antibiotics.46.908
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
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.
引用
收藏
页码:908 / 913
页数:6
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