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- cathepsin (1)
- cathepsin-L (1)
- cysteine protease (1)
- in-vitro (1)
- malaria parasites (1)
- plakortide E. (1)
- plakortis halichondroides (1)
- protease inhibitor (1)
- rhodesain (1)
- slowly-binding reversible inhibitor (1)
Institut
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.