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

Marine Drugs

Swarna Oli²  Usama Ramadan Abdelmohsen¹  Ute Hentschel¹ 

[1] Department of Botany II, Julius-von-Sachs-Institute for Biological Sciences, University of Würzburg, Julius-von-Sachs Platz 3, Würzburg 97082, Germany; E-Mails:;Institute of Pharmacy and Biochemistry, Johannes Gutenberg-University of Mainz, Staudinger Weg 5, Mainz 55128, Germany; E-Mail:

关键词: Plakortis halichondroides;    plakortide E;    protease inhibitor;    slowly-binding reversible inhibitor;    cathepsin;    rhodesain;   

DOI  :  10.3390/md12052614

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.