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Sheng Wu Gong Cheng Xue Bao ; 23(6): 1112-5, 2007 Nov.
Artigo em Zh | MEDLINE | ID: mdl-18257246

RESUMO

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.


Assuntos
Elastase de Leucócito/antagonistas & inibidores , Inibidores de Proteases/isolamento & purificação , Inibidores de Proteases/metabolismo , Streptomyces/metabolismo , Humanos , Streptomyces/isolamento & purificação
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