New tetromycin derivatives with anti-trypanosomal and protease inhibitory activities |
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| Authors: | Pimentel-Elardo Sheila M Buback Verena Gulder Tobias A M Bugni Tim S Reppart Jason Bringmann Gerhard Ireland Chris M Schirmeister Tanja Hentschel Ute |
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| Institution: | Julius-von-Sachs Institute for Biological Sciences, University of Würzburg, Julius-von-Sachs-Platz 3, Würzburg 97082, Germany. elardos@mcmaster.ca |
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| Abstract: | 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 PL(pro). 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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| Keywords: | tetromycin anti-trypanosomal protease inhibition Streptomyces axinellae marine sponge |
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