FR901277, a novel inhibitor of human leukocyte elastase from Streptomyces resistomycificus. Producing organism, fermentation, isolation, physico-chemical and biological properties.
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.
Fujie
K
K
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan.
Shinguh
Y
Y
Hatanaka
H
H
Shigematsu
N
N
Murai
H
H
Fujita
T
T
Yamashita
M
M
Okamoto
M
M
Okuhara
M
M
D000818:Animals; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D005285:Fermentation; D019272:Leukocyte Elastase; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors*; D013302:Streptomyces / Q000737:chemistry*
D004791:Enzyme Inhibitors; D010196:Pancreatic Elastase; D019272:Leukocyte Elastase