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.…
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 |
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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): | CC BY: Creative-Commons-Lizenz: Namensnennung |