Allicin and derivates are cysteine protease inhibitors with antiparasitic activity |
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| Authors: | Thilo Waag Christoph Gelhaus Jennifer Rath August Stich Matthias Leippe Tanja Schirmeister |
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| Institution: | 1. Institute of Pharmacy and Food Chemistry, University of Würzburg, Am Hubland, 97074 Würzburg, Germany;2. Department of Zoophysiology, Zoological Institute, University of Kiel, Olshausenstr. 40, 24098 Kiel, Germany;3. Department of Tropical Medicine, Medical Mission Institute, Salvatorstr. 7, 97074 Würzburg, Germany |
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| Abstract: | Allicin and derivatives thereof inhibit the CAC1 cysteine proteases falcipain 2, rhodesain, cathepsin B and L in the low micromolar range. The structure–activity relationship revealed that only derivatives with primary carbon atom in vicinity to the thiosulfinate sulfur atom attacked by the active-site Cys residue are active against the target enzymes. Some compounds also show potent antiparasitic activity against Plasmodium falciparum and Trypanosoma brucei brucei. |
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