期刊
MARINE DRUGS
卷 9, 期 10, 页码 1682-1697出版社
MDPI
DOI: 10.3390/md9101682
关键词
tetromycin; anti-trypanosomal; protease inhibition; Streptomyces axinellae; marine sponge
资金
- Deutsche Forschungsgemeinschaft [SFB 630 TP A5, TP A4, TP A2]
- NIH [CA36622]
Four new tetromycin derivatives, tetromycins 1-4 and a previously known one, tetromycin B (5) were isolated from Streptomyces axinellae Pol001(T) cultivated from the Mediterranean sponge Axinella polypoides. Structures were assigned using extensive 1D and 2D NMR spectroscopy as well as HRESIMS analysis. The compounds were tested for antiparasitic activities against Leishmania major and Trypanosoma brucei, and for protease inhibition against several cysteine proteases such as falcipain, rhodesain, cathepsin L, cathepsin B, and viral proteases SARS-CoV M-pro, and PLpro. The compounds showed antiparasitic activities against T. brucei and time-dependent inhibition of cathepsin L-like proteases with K-i values in the low micromolar range.
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