Identification of Plakortide E from the Caribbean Sponge Plakortis halichondroides as a Trypanocidal Protease Inhibitor using Bioactivity-Guided Fractionation
Please always quote using this 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.…
Author: | Swarna Oli, Usama Ramadan Abdelmohsen, Ute Hentschel, Tanja Schirmeister |
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URN: | urn:nbn:de:bvb:20-opus-116536 |
Document Type: | Journal article |
Faculties: | Fakultät für Biologie / Julius-von-Sachs-Institut für Biowissenschaften |
Language: | English |
Parent Title (English): | MARINE DRUGS |
ISSN: | 1660-3397 |
Year of Completion: | 2014 |
Volume: | 12 |
Issue: | 5 |
Pagenumber: | 2614-2622 |
Source: | 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 |
Dewey Decimal Classification: | 5 Naturwissenschaften und Mathematik / 59 Tiere (Zoologie) / 593 Wirbellose des Meeres und der Meeresküste |
Tag: | cathepsin; cathepsin-L; cysteine protease; in-vitro; malaria parasites; plakortide E.; plakortis halichondroides; protease inhibitor; rhodesain; slowly-binding reversible inhibitor; trypanosoma brucei |
Release Date: | 2015/07/30 |
Licence (German): | CC BY: Creative-Commons-Lizenz: Namensnennung |