@article{OliAbdelmohsenHentscheletal.2014, author = {Oli, Swarna and Abdelmohsen, Usama Ramadan and Hentschel, Ute and Schirmeister, Tanja}, title = {Identification of Plakortide E from the Caribbean Sponge Plakortis halichondroides as a Trypanocidal Protease Inhibitor using Bioactivity-Guided Fractionation}, series = {MARINE DRUGS}, volume = {12}, journal = {MARINE DRUGS}, number = {5}, issn = {1660-3397}, doi = {10.3390/md12052614}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-116536}, pages = {2614-2622}, year = {2014}, 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 mu M and without cytotoxic effects against J774.1 macrophages at 100 mu M 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.}, language = {en} }