N01WA-735E, a human leukocyte elastase inhibitor from metabolites of microorganisms.
- Author:
Ya-Shan WEI
1
;
Hua ZHANG
;
Xin-Hua LU
;
Yue-Sheng DONG
;
Bao-Hua ZHAO
Author Information
1. College of Life Science, Hebei Normal University Shijiazhuang 050016, China.
- Publication Type:Journal Article
- MeSH:
Humans;
Leukocyte Elastase;
antagonists & inhibitors;
Protease Inhibitors;
isolation & purification;
metabolism;
Streptomyces;
isolation & purification;
metabolism
- From:
Chinese Journal of Biotechnology
2007;23(6):1112-1115
- CountryChina
- Language:Chinese
-
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.
