New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities
Zitieren Sie bitte immer diese URN: urn:nbn:de:bvb:20-opus-141171
- 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 proteasesFour 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.…
Autor(en): | Sheila M. Pimentel-Elardo, Verena Buback, Tobias A. M. Gulder, Tim S. Bugni, Jason Reppart, Gerhard Bringmann, Chris M. Ireland, Tanja Schirmeister, Ute Hentschel |
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URN: | urn:nbn:de:bvb:20-opus-141171 |
Dokumentart: | Artikel / Aufsatz in einer Zeitschrift |
Institute der Universität: | Fakultät für Biologie / Julius-von-Sachs-Institut für Biowissenschaften |
Fakultät für Chemie und Pharmazie / Institut für Organische Chemie | |
Fakultät für Chemie und Pharmazie / Institut für Pharmazie und Lebensmittelchemie | |
Sprache der Veröffentlichung: | Englisch |
Titel des übergeordneten Werkes / der Zeitschrift (Englisch): | Marine drugs |
Erscheinungsjahr: | 2011 |
Band / Jahrgang: | 9 |
Heft / Ausgabe: | 10 |
Seitenangabe: | 1682-1697 |
Originalveröffentlichung / Quelle: | Mar. Drugs 2011, 9, 1682-1697; doi:10.3390/md9101682 |
DOI: | https://doi.org/10.3390/md9101682 |
Allgemeine fachliche Zuordnung (DDC-Klassifikation): | 5 Naturwissenschaften und Mathematik / 54 Chemie / 547 Organische Chemie |
Freie Schlagwort(e): | Streptomyces axinellae; anti-trypanosomal; cysteine protease; discovery; drugs; marine sponge; protease inhibition; streptomyces; tetromycin |
Datum der Freischaltung: | 07.01.2019 |
Lizenz (Deutsch): | CC BY: Creative-Commons-Lizenz: Namensnennung |