Identification of Plakortide E from the Caribbean Sponge Plakortis halichondroides as a Trypanocidal Protease Inhibitor using Bioactivity-Guided Fractionation.

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Oli, Swarna, Abdelmohsen, Usama, Hentschel, Ute and Schirmeister, Tanja (2014) Identification of Plakortide E from the Caribbean Sponge Plakortis halichondroides as a Trypanocidal Protease Inhibitor using Bioactivity-Guided Fractionation. Open Access Marine Drugs, 12 (5). pp. 2614-2622. DOI 10.3390/md12052614.

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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

Document Type: Article
Keywords: Plakortis halichondroides; plakortide E; protease inhibitor; slowly-binding reversible inhibitor; cathepsin; rhodesain
Refereed: Yes
Open Access Journal?: Yes
Publisher: MDPI
Date Deposited: 02 Jul 2015 08:59
Last Modified: 14 Jul 2020 11:45
URI: https://oceanrep.geomar.de/id/eprint/29114

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