title: [N01WA-735E, a human leukocyte elastase inhibitor from metabolites of microorganisms].
abstract: 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.
authors.affiliation: College of Life Science, Hebei Normal University Shijiazhuang 050016, China.
authors.forename: Ya-Shan
authors.initials: YS
authors.lastname: Wei
authors.forename: Hua
authors.initials: H
authors.lastname: Zhang
authors.forename: Xin-Hua
authors.initials: XH
authors.lastname: Lu
authors.forename: Yue-Sheng
authors.initials: YS
authors.lastname: Dong
authors.forename: Bao-Hua
authors.initials: BH
authors.lastname: Zhao
mesh_terms: D006801:Humans; D019272:Leukocyte Elastase / Q000037:antagonists & inhibitors*; D011480:Protease Inhibitors / Q000302:isolation & purification* / Q000378:metabolism*; D013302:Streptomyces / Q000302:isolation & purification / Q000378:metabolism*
chemical_list: D011480:Protease Inhibitors; D019272:Leukocyte Elastase