New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities
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 analysi...
| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2011-09-01
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| Series: | Marine Drugs |
| Subjects: | |
| Online Access: | http://www.mdpi.com/1660-3397/9/10/1682/ |
| _version_ | 1818007908702486528 |
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| author | Ute Hentschel Chris M. Ireland Tanja Schirmeister Jason Reppart Gerhard Bringmann Tobias A.M. Gulder Tim S. Bugni Verena Buback Sheila M. Pimentel-Elardo |
| author_facet | Ute Hentschel Chris M. Ireland Tanja Schirmeister Jason Reppart Gerhard Bringmann Tobias A.M. Gulder Tim S. Bugni Verena Buback Sheila M. Pimentel-Elardo |
| author_sort | Ute Hentschel |
| collection | DOAJ |
| description | 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 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. |
| first_indexed | 2024-04-14T05:22:55Z |
| format | Article |
| id | doaj.art-dcc5ef8320c0400ea11a0d91bbe569d0 |
| institution | Directory Open Access Journal |
| issn | 1660-3397 |
| language | English |
| last_indexed | 2024-04-14T05:22:55Z |
| publishDate | 2011-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Marine Drugs |
| spelling | doaj.art-dcc5ef8320c0400ea11a0d91bbe569d02022-12-22T02:10:08ZengMDPI AGMarine Drugs1660-33972011-09-019101682169710.3390/md9101682New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory ActivitiesUte HentschelChris M. IrelandTanja SchirmeisterJason ReppartGerhard BringmannTobias A.M. GulderTim S. BugniVerena BubackSheila M. Pimentel-ElardoFour 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.http://www.mdpi.com/1660-3397/9/10/1682/tetromycinanti-trypanosomalprotease inhibitionStreptomyces axinellaemarine sponge |
| spellingShingle | Ute Hentschel Chris M. Ireland Tanja Schirmeister Jason Reppart Gerhard Bringmann Tobias A.M. Gulder Tim S. Bugni Verena Buback Sheila M. Pimentel-Elardo New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities Marine Drugs tetromycin anti-trypanosomal protease inhibition Streptomyces axinellae marine sponge |
| title | New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities |
| title_full | New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities |
| title_fullStr | New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities |
| title_full_unstemmed | New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities |
| title_short | New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities |
| title_sort | new tetromycin derivatives with anti trypanosomal and protease inhibitory activities |
| topic | tetromycin anti-trypanosomal protease inhibition Streptomyces axinellae marine sponge |
| url | http://www.mdpi.com/1660-3397/9/10/1682/ |
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