Identification of plakortide E from the Caribbean sponge Plakortis halichondroides as a trypanocidal protease inhibitor using bioactivity-guided fractionation
- Publication type:
- Journal article
- Metadata:
-
- Autoren
- Swarna Oli
- Usama Ramadan Abdelmohsen
- Ute Hentschel
- Tanja Schirmeister
- Sammlungen
- metadata
- ISSN
- 1660-3397
- Ausgabe der Veröffentlichung
- 5
- Zeitschrift
- Marine drugs
- Schlüsselwörter
- 570 Biowissenschaften
- 570 Life sciences
- Sprache
- eng
- Paginierung
- Seiten: 2614 - 2622
- Datum der Veröffentlichung
- 2014
- Herausgeber
- Molecular Diversity Preservation International
- Herausgeber URL
- http://dx.doi.org/10.3390/md12052614
- Datum der Datenerfassung
- 2020
- Datum, an dem der Datensatz öffentlich gemacht wurde
- 2020
- Zugang
- Public
- Titel
- Identification of plakortide E from the Caribbean sponge Plakortis halichondroides as a trypanocidal protease inhibitor using bioactivity-guided fractionation
- Ausgabe der Zeitschrift
- 12
Data source: METADATA.UB
- Other metadata sources:
-
- Autoren
- Swarna Oli
- Usama Ramadan Abdelmohsen
- Ute Hentschel
- Tanja Schirmeister
- Autoren-URL
- https://www.webofscience.com/api/gateway?GWVersion=2&SrcApp=fis-test-1&SrcAuth=WosAPI&KeyUT=WOS:000337160500015&DestLinkType=FullRecord&DestApp=WOS_CPL
- DOI
- 10.3390/md12052614
- eISSN
- 1660-3397
- Externe Identifier
- Clarivate Analytics Document Solution ID: AI8JU
- PubMed Identifier: 24798927
- Ausgabe der Veröffentlichung
- 5
- Zeitschrift
- MARINE DRUGS
- Schlüsselwörter
- Plakortis halichondroides
- plakortide E
- protease inhibitor
- slowly-binding reversible inhibitor
- cathepsin
- rhodesain
- Paginierung
- 2614 - 2622
- Datum der Veröffentlichung
- 2014
- Status
- Published
- Titel
- Identification of Plakortide E from the Caribbean Sponge <i>Plakortis halichondroides</i> as a Trypanocidal Protease Inhibitor using Bioactivity-Guided Fractionation
- Sub types
- Article
- Ausgabe der Zeitschrift
- 12
Data source: Web of Science (Lite)
- Autoren
- Swarna Oli
- Usama Abdelmohsen
- Ute Hentschel
- Tanja Schirmeister
- DOI
- 10.3390/md12052614
- eISSN
- 1660-3397
- Ausgabe der Veröffentlichung
- 5
- Zeitschrift
- Marine Drugs
- Sprache
- en
- Online publication date
- 2014
- Paginierung
- 2614 - 2622
- Status
- Published online
- Herausgeber
- MDPI AG
- Herausgeber URL
- http://dx.doi.org/10.3390/md12052614
- Datum der Datenerfassung
- 2019
- Titel
- Identification of Plakortide E from the Caribbean Sponge Plakortis halichondroides as a Trypanocidal Protease Inhibitor using Bioactivity-Guided Fractionation
- Ausgabe der Zeitschrift
- 12
Data source: Crossref
- Abstract
- 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.
- Addresses
- Institute of Pharmacy and Biochemistry, Johannes Gutenberg-University of Mainz, Staudinger Weg 5, Mainz 55128, Germany. swarnoli@uni-mainz.de.
- Autoren
- Swarna Oli
- Usama Ramadan Abdelmohsen
- Ute Hentschel
- Tanja Schirmeister
- DOI
- 10.3390/md12052614
- eISSN
- 1660-3397
- Externe Identifier
- PubMed Identifier: 24798927
- PubMed Central ID: PMC4052307
- Open access
- true
- ISSN
- 1660-3397
- Ausgabe der Veröffentlichung
- 5
- Zeitschrift
- Marine drugs
- Schlüsselwörter
- Animals
- Humans
- Porifera
- Trypanosoma brucei brucei
- Dioxanes
- Cathepsins
- Cysteine Endopeptidases
- Protease Inhibitors
- Antiparasitic Agents
- Trypanocidal Agents
- Drug Screening Assays, Antitumor
- Sprache
- eng
- Medium
- Electronic
- Online publication date
- 2014
- Open access status
- Open Access
- Paginierung
- 2614 - 2622
- Datum der Veröffentlichung
- 2014
- Status
- Published
- Publisher licence
- CC BY
- Datum der Datenerfassung
- 2014
- Titel
- Identification of plakortide E from the Caribbean sponge Plakortis halichondroides as a trypanocidal protease inhibitor using bioactivity-guided fractionation.
- Sub types
- Research Support, Non-U.S. Gov't
- research-article
- Journal Article
- Ausgabe der Zeitschrift
- 12
Files
https://www.mdpi.com/1660-3397/12/5/2614/pdf?version=1424782904 https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/24798927/pdf/?tool=EBI https://europepmc.org/articles/PMC4052307?pdf=render
Data source: Europe PubMed Central
- Abstract
- 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.
- Date of acceptance
- 2014
- Autoren
- Swarna Oli
- Usama Ramadan Abdelmohsen
- Ute Hentschel
- Tanja Schirmeister
- Autoren-URL
- https://www.ncbi.nlm.nih.gov/pubmed/24798927
- DOI
- 10.3390/md12052614
- eISSN
- 1660-3397
- Externe Identifier
- PubMed Central ID: PMC4052307
- Ausgabe der Veröffentlichung
- 5
- Zeitschrift
- Mar Drugs
- Schlüsselwörter
- Animals
- Antiparasitic Agents
- Cathepsins
- Cysteine Endopeptidases
- Dioxanes
- Drug Screening Assays, Antitumor
- Humans
- Porifera
- Protease Inhibitors
- Trypanocidal Agents
- Trypanosoma brucei brucei
- Sprache
- eng
- Country
- Switzerland
- Paginierung
- 2614 - 2622
- PII
- md12052614
- Datum der Veröffentlichung
- 2014
- Status
- Published online
- Datum, an dem der Datensatz öffentlich gemacht wurde
- 2014
- Titel
- Identification of plakortide E from the Caribbean sponge Plakortis halichondroides as a trypanocidal protease inhibitor using bioactivity-guided fractionation.
- Sub types
- Journal Article
- Research Support, Non-U.S. Gov't
- Ausgabe der Zeitschrift
- 12
Data source: PubMed
- Author's licence
- CC-BY
- Autoren
- Swarna Oli
- Usama Ramadan Abdelmohsen
- Ute Hentschel
- Tanja Schirmeister
- Hosting institution
- Universitätsbibliothek Mainz
- Sammlungen
- DFG-OA-Publizieren (2012 - 2017)
- Resource version
- Published version
- DOI
- 10.3390/md12052614
- Funding acknowledgements
- DFG, Open Access-Publizieren Universität Mainz / Universitätsmedizin
- File(s) embargoed
- false
- Open access
- true
- ISSN
- 1660-3397
- Ausgabe der Veröffentlichung
- 5
- Zeitschrift
- Marine drugs
- Schlüsselwörter
- 570 Biowissenschaften
- 570 Life sciences
- Sprache
- eng
- Open access status
- Open Access
- Paginierung
- 2614 - 2622
- Datum der Veröffentlichung
- 2014
- Public URL
- https://openscience.ub.uni-mainz.de/handle/20.500.12030/6969
- Herausgeber
- Molecular Diversity Preservation International
- Herausgeber URL
- http://dx.doi.org/10.3390/md12052614
- Datum der Datenerfassung
- 2022
- Datum, an dem der Datensatz öffentlich gemacht wurde
- 2022
- Zugang
- Public
- Titel
- Identification of plakortide E from the Caribbean sponge Plakortis halichondroides as a trypanocidal protease inhibitor using bioactivity-guided fractionation
- Ausgabe der Zeitschrift
- 12
Files
identification_of_plakortide_-20220510090302657.pdf
Data source: OPENSCIENCE.UB
- Beziehungen:
- Property of