[N01WA-735E, a human leukocyte elastase inhibitor from metabolites of microorganisms].
Human leukocyte elastase is an important selection target of inflammation and cancer. In this paper, a high throughput screening model was established for screening human leukocyte elastase inhibitors from thousands of strains of actinomycetes. As a result, a strain, N01WA-735 with potent suppression activity was isolated. Firstly, the strain N01WA-735 was identified as Streptomyces according to morphology and biochemical analysis. The Streptomyces N01WA-735 was processed by solvent extraction, silica column chromatography, Sephadex LH-20 column chromatography and crystallization to get a pure active compound named N01WA-735E. Its chemical structure was elucidated as the same as that of the compound named BE-52440A by physicochemical properties and spectral data of UV, MS, 1H-NMR and 13C-NMR respectively. The compound showed a strong inhibitory activity against human leukocyte elastase with IC50 of 3.02 micromol/L. The compound is reported as a human leukocyte elastase inhibitor for the first time.
Wei
Ya-Shan
YS
College of Life Science, Hebei Normal University Shijiazhuang 050016, China.
Zhang
Hua
H
Lu
Xin-Hua
XH
Dong
Yue-Sheng
YS
Zhao
Bao-Hua
BH
D006801:Humans; D019272:Leukocyte Elastase / Q000037:antagonists & inhibitors*; D011480:Protease Inhibitors / Q000302:isolation & purification* / Q000378:metabolism*; D013302:Streptomyces / Q000302:isolation & purification / Q000378:metabolism*
D011480:Protease Inhibitors; D019272:Leukocyte Elastase