TY - JOUR A1 - Pimentel-Elardo, Sheila M. A1 - Buback, Verena A1 - Gulder, Tobias A. M. A1 - Bugni, Tim S. A1 - Reppart, Jason A1 - Bringmann, Gerhard A1 - Ireland, Chris M. A1 - Schirmeister, Tanja A1 - Hentschel, Ute T1 - New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities JF - Marine drugs N2 - 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. KW - cysteine protease KW - drugs KW - streptomyces KW - discovery KW - anti-trypanosomal KW - protease inhibition KW - Streptomyces axinellae KW - marine sponge KW - tetromycin Y1 - 2011 U6 - http://nbn-resolving.de/urn/resolver.pl?urn:nbn:de:bvb:20-opus-141171 VL - 9 IS - 10 ER - TY - JOUR A1 - Kunz, Anna Lena A1 - Labes, Antje A1 - Wiese, Jutta A1 - Bruhn, Torsten A1 - Bringmann, Gerhard A1 - Imhoff, Johannes F. T1 - Nature's Lab for Derivatization: New and Revised Structures of a Variety of Streptophenazines Produced by a Sponge-Derived Streptomyces Strain JF - Marine Drugs N2 - Eight streptophenazines (A-H) have been identified so far as products of Streptomyces strain HB202, which was isolated from the sponge Halichondria panicea from the Baltic Sea. The variation of bioactivities based on small structural changes initiated further studies on new derivatives. Three new streptophenazines (I-K) were identified after fermentation in the present study. In addition, revised molecular structures of streptophenazines C, D, F and H are proposed. Streptophenazines G and K exhibited moderate antibacterial activity against the facultative pathogenic bacterium Staphylococcus epidermidis and against Bacillus subtilis. All tested compounds (streptophenazines G, I-K) also showed moderate activities against PDE 4B. KW - marine natural product KW - phenazine KW - Baltic Sea KW - streptomyces KW - halichondria panicea KW - obstructive pulmonary disease KW - phosphodiesterase-4 inhibitor KW - absolute configuration KW - biosynthesis KW - rofumilast Y1 - 2014 U6 - http://nbn-resolving.de/urn/resolver.pl?urn:nbn:de:bvb:20-opus-116816 SN - 1660-3397 VL - 12 IS - 4 ER -