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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.show moreshow less

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Metadaten
Author: Swarna Oli, Usama Ramadan Abdelmohsen, Ute Hentschel, Tanja Schirmeister
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:http://www.ncbi.nlm.nih.gov/pubmed?term=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):License LogoCC BY: Creative-Commons-Lizenz: Namensnennung