Journal
MARINE DRUGS
Volume 9, Issue 10, Pages 1682-1697Publisher
MDPI
DOI: 10.3390/md9101682
Keywords
tetromycin; anti-trypanosomal; protease inhibition; Streptomyces axinellae; marine sponge
Categories
Funding
- Deutsche Forschungsgemeinschaft [SFB 630 TP A5, TP A4, TP A2]
- NIH [CA36622]
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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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