Identification of Plakortide E from the Caribbean Sponge Plakortis halichondroides as a Trypanocidal Protease Inhibitor using Bioactivity-Guided Fractionation
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 μM and without cytotoxic effects against J774.1 macrophages at 100...
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| Format: | Article |
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MDPI AG
2014-05-01
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| Series: | Marine Drugs |
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| Online Access: | http://www.mdpi.com/1660-3397/12/5/2614 |
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| author | Swarna Oli Usama Ramadan Abdelmohsen Ute Hentschel Tanja Schirmeister |
| author_facet | Swarna Oli Usama Ramadan Abdelmohsen Ute Hentschel Tanja Schirmeister |
| author_sort | Swarna Oli |
| collection | DOAJ |
| description | 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 μM and without cytotoxic effects against J774.1 macrophages at 100 μM 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. |
| first_indexed | 2024-04-11T22:36:24Z |
| format | Article |
| id | doaj.art-1ec95aff0be54aed9fa6d7ba56f5addb |
| institution | Directory Open Access Journal |
| issn | 1660-3397 |
| language | English |
| last_indexed | 2024-04-11T22:36:24Z |
| publishDate | 2014-05-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Marine Drugs |
| spelling | doaj.art-1ec95aff0be54aed9fa6d7ba56f5addb2022-12-22T03:59:11ZengMDPI AGMarine Drugs1660-33972014-05-011252614262210.3390/md12052614md12052614Identification of Plakortide E from the Caribbean Sponge Plakortis halichondroides as a Trypanocidal Protease Inhibitor using Bioactivity-Guided FractionationSwarna Oli0Usama Ramadan Abdelmohsen1Ute Hentschel2Tanja Schirmeister3Institute of Pharmacy and Biochemistry, Johannes Gutenberg-University of Mainz, Staudinger Weg 5, Mainz 55128, GermanyDepartment of Botany II, Julius-von-Sachs-Institute for Biological Sciences, University of Würzburg, Julius-von-Sachs Platz 3, Würzburg 97082, GermanyDepartment of Botany II, Julius-von-Sachs-Institute for Biological Sciences, University of Würzburg, Julius-von-Sachs Platz 3, Würzburg 97082, GermanyInstitute of Pharmacy and Biochemistry, Johannes Gutenberg-University of Mainz, Staudinger Weg 5, Mainz 55128, GermanyIn 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 μM and without cytotoxic effects against J774.1 macrophages at 100 μM 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.http://www.mdpi.com/1660-3397/12/5/2614Plakortis halichondroidesplakortide Eprotease inhibitorslowly-binding reversible inhibitorcathepsinrhodesain |
| spellingShingle | Swarna Oli Usama Ramadan Abdelmohsen Ute Hentschel Tanja Schirmeister Identification of Plakortide E from the Caribbean Sponge Plakortis halichondroides as a Trypanocidal Protease Inhibitor using Bioactivity-Guided Fractionation Marine Drugs Plakortis halichondroides plakortide E protease inhibitor slowly-binding reversible inhibitor cathepsin rhodesain |
| title | Identification of Plakortide E from the Caribbean Sponge Plakortis halichondroides as a Trypanocidal Protease Inhibitor using Bioactivity-Guided Fractionation |
| title_full | Identification of Plakortide E from the Caribbean Sponge Plakortis halichondroides as a Trypanocidal Protease Inhibitor using Bioactivity-Guided Fractionation |
| title_fullStr | Identification of Plakortide E from the Caribbean Sponge Plakortis halichondroides as a Trypanocidal Protease Inhibitor using Bioactivity-Guided Fractionation |
| title_full_unstemmed | Identification of Plakortide E from the Caribbean Sponge Plakortis halichondroides as a Trypanocidal Protease Inhibitor using Bioactivity-Guided Fractionation |
| title_short | Identification of Plakortide E from the Caribbean Sponge Plakortis halichondroides as a Trypanocidal Protease Inhibitor using Bioactivity-Guided Fractionation |
| title_sort | identification of plakortide e from the caribbean sponge plakortis halichondroides as a trypanocidal protease inhibitor using bioactivity guided fractionation |
| topic | Plakortis halichondroides plakortide E protease inhibitor slowly-binding reversible inhibitor cathepsin rhodesain |
| url | http://www.mdpi.com/1660-3397/12/5/2614 |
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