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Open AccessCommunication
Mar. Drugs 2014, 12(5), 2614-2622; doi:10.3390/md12052614

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

1
Institute of Pharmacy and Biochemistry, Johannes Gutenberg-University of Mainz, Staudinger Weg 5, Mainz 55128, Germany
2
Department of Botany II, Julius-von-Sachs-Institute for Biological Sciences, University of Würzburg, Julius-von-Sachs Platz 3, Würzburg 97082, Germany
3
Department of Pharmacognosy, Faculty of Pharmacy, Minia University, Minia 61519, Egypt
*
Author to whom correspondence should be addressed.
Received: 20 February 2014 / Revised: 7 March 2014 / Accepted: 19 March 2014 / Published: 2 May 2014
(This article belongs to the Special Issue Advances and New Perspectives in Marine Biotechnology)
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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. View Full-Text
Keywords: Plakortis halichondroides; plakortide E; protease inhibitor; slowly-binding reversible inhibitor; cathepsin; rhodesain Plakortis halichondroides; plakortide E; protease inhibitor; slowly-binding reversible inhibitor; cathepsin; rhodesain
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Oli, S.; Abdelmohsen, U.R.; Hentschel, U.; Schirmeister, T. Identification of Plakortide E from the Caribbean Sponge Plakortis halichondroides as a Trypanocidal Protease Inhibitor using Bioactivity-Guided Fractionation. Mar. Drugs 2014, 12, 2614-2622.

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