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

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

1
,
2,3
,
2
 and
1,*
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.
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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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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