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New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities

Please always quote using this URN: urn:nbn:de:bvb:20-opus-75465
  • Four new tetromycin derivatives, tetromycins 1–4 and a previously known one, tetromycin B (5) were isolated from Streptomyces axinellae Pol001T 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 proteasesFour new tetromycin derivatives, tetromycins 1–4 and a previously known one, tetromycin B (5) were isolated from Streptomyces axinellae Pol001T 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 Mpro, and PLpro. The compounds showed antiparasitic activities against T. brucei and time-dependent inhibition of cathepsin L-like proteases with Ki values in the low micromolar range.show moreshow less

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Metadaten
Author: Sheila M. Pimentel-Elardo, Verena Buback, Tobias A. M. Gulder, Tim S. Bugni, Jason Reppart, Gerhard Bringmann, Chris M. Ireland, Tanja Schirmeister, Ute Hentschel
URN:urn:nbn:de:bvb:20-opus-75465
Document Type:Journal article
Faculties:Fakultät für Biologie / Julius-von-Sachs-Institut für Biowissenschaften
Language:English
Year of Completion:2011
Source:In: Marine Drugs (2011) 9, 1682-1697; doi:10.3390/md9101682
Dewey Decimal Classification:6 Technik, Medizin, angewandte Wissenschaften / 61 Medizin und Gesundheit / 610 Medizin und Gesundheit
GND Keyword:Biologie
Tag:Streptomyces axinellae; anti-trypanosomal; marine sponge; protease inhibition; tetromycin
Release Date:2013/01/29
Licence (German):License LogoCC BY: Creative-Commons-Lizenz: Namensnennung