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RESEARCH PRODUCT
New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities
Ute HentschelJason ReppartSheila Marie Pimentel-elardoVerena BubackTim S. BugniGerhard BringmannChris M. IrelandTobias A. M. GulderTanja Schirmeistersubject
Magnetic Resonance Spectroscopyanti-trypanosomalmedicine.medical_treatmentCathepsin LStreptomyces axinellaePharmaceutical ScienceCathepsin BCathepsin BCathepsin LCathepsin ODrug DiscoveryPharmacology Toxicology and Pharmaceutics (miscellaneous)lcsh:QH301-705.5Coronavirus 3C ProteasesLeishmania major0303 health sciencesbiology030302 biochemistry & molecular biologytetromycin; anti-trypanosomal; protease inhibition; <em>Streptomyces axinellae</em>; marine spongeTrypanocidal AgentsStreptomycesCysteine EndopeptidasesBiochemistrySevere acute respiratory syndrome-related coronavirusStreptomyces axinellaetetromycinBiologiemarine spongeddc:547ProteasesTrypanosoma brucei bruceiAntiprotozoal AgentsTrypanosoma bruceiHeterocyclic Compounds 4 or More RingsArticle03 medical and health sciencesViral ProteinsAxinellaparasitic diseasesmedicineAnimalsProtease Inhibitorsddc:610protease inhibition ; anti-trypanosomal ; Streptomyces axinellae ; tetromycin ; marine sponge030304 developmental biologyCathepsinProteasebiology.organism_classificationprotease inhibitionlcsh:Biology (General)biology.proteindescription
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.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2011-09-26 |