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Identification of Plakortide E from the Caribbean Sponge Plakortis halichondroides as a Trypanocidal Protease Inhibitor using Bioactivity-Guided Fractionation
Zitieren Sie bitte immer diese URN: urn:nbn:de:bvb:20-opus-116536
- In this paper, we report new protease inhibitory activity of plakortide E towards cathepsins and cathepsin-like parasitic proteases. We further report on its anti-parasitic activity against Trypanosoma brucei with an IC50 value of 5 mu M and without cytotoxic effects against J774.1 macrophages at 100 mu M concentration. Plakortide E was isolated from the sponge Plakortis halichondroides using enzyme assay-guided fractionation and identified by NMR spectroscopy and mass spectrometry. Furthermore, enzyme kinetic studies confirmed plakortide E asIn this paper, we report new protease inhibitory activity of plakortide E towards cathepsins and cathepsin-like parasitic proteases. We further report on its anti-parasitic activity against Trypanosoma brucei with an IC50 value of 5 mu M and without cytotoxic effects against J774.1 macrophages at 100 mu M concentration. Plakortide E was isolated from the sponge Plakortis halichondroides using enzyme assay-guided fractionation and identified by NMR spectroscopy and mass spectrometry. Furthermore, enzyme kinetic studies confirmed plakortide E as a non-competitive, slowly-binding, reversible inhibitor of rhodesain.…
| Autor(en): | Swarna Oli, Usama Ramadan Abdelmohsen, Ute Hentschel, Tanja Schirmeister |
|---|---|
| URN: | urn:nbn:de:bvb:20-opus-116536 |
| Dokumentart: | Artikel / Aufsatz in einer Zeitschrift |
| Institute der Universität: | Fakultät für Biologie / Julius-von-Sachs-Institut für Biowissenschaften |
| Sprache der Veröffentlichung: | Englisch |
| Titel des übergeordneten Werkes / der Zeitschrift (Englisch): | MARINE DRUGS |
| ISSN: | 1660-3397 |
| Erscheinungsjahr: | 2014 |
| Band / Jahrgang: | 12 |
| Heft / Ausgabe: | 5 |
| Seitenangabe: | 2614-2622 |
| Originalveröffentlichung / Quelle: | Marine Drugs 2014, 12, 2614-2622; doi:10.3390/md12052614 marine |
| DOI: | https://doi.org/10.3390/md12052614 |
| PubMed-ID: | https://pubmed.ncbi.nlm.nih.gov/24798927 |
| Allgemeine fachliche Zuordnung (DDC-Klassifikation): | 5 Naturwissenschaften und Mathematik / 59 Tiere (Zoologie) / 593 Wirbellose des Meeres und der Meeresküste |
| Freie Schlagwort(e): | cathepsin; cathepsin-L; cysteine protease; in-vitro; malaria parasites; plakortide E.; plakortis halichondroides; protease inhibitor; rhodesain; slowly-binding reversible inhibitor; trypanosoma brucei |
| Datum der Freischaltung: | 30.07.2015 |
| Lizenz (Deutsch): |  CC BY: Creative-Commons-Lizenz: Namensnennung |