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

A novel human leukocyte elastase inhibitor, FR901277 was discovered in the fermentation broth of Streptomyces resistomycificus No. 7622. FR9 01277 has a molecular weight of 961 and a molecular formula of C47H63N 9O13. 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 sign ificantly prevented human leukocyte elastase-induced foot edema in mic e.