Aromatic glycosyl disulfide derivatives: Evaluation of their inhibitory activities against Trypanosoma cruzi |
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| Authors: | Bessy Gutiérrez Christian Muñoz Luis Osorio Krisztina Fehér Tünde-Zita Illyés Zsuzsa Papp Ambati Ashok Kumar Katalin E Kövér Hernán Sagua Jorge E Araya Patricio Morales László Szilágyi Jorge González |
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| Institution: | 1. Department of Medical Technology, Faculty of Health Sciences, University of Antofagasta, P.O. Box 170, Antofagasta, Chile;2. Department of Organic Chemistry, University of Ghent, 9000 Ghent, Belgium;3. Department of Chemistry, University of Debrecen, P.O. Box 20, H-4010 Debrecen, Hungary;4. Biomedical Department, Faculty of Health Sciences, University of Antofagasta, P.O. Box 170, Antofagasta, Chile |
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| Abstract: | Aromatic oligovalent glycosyl disulfides and some diglycosyl disulfides were tested against three different Trypanosoma cruzi strains. Di-(β-d-galactopyranosyl-dithiomethylene) benzenes 2b and 4b proved to be the most active derivatives against all three strains of cell culture-derived trypomastigotes with IC50 values ranging from 4 to 11 μM at 37 °C. The inhibitory activities were maintained, although somewhat lowered, at a temperature of 4 °C as well. Three further derivatives displayed similar activities against at least one of the three strains. Low cytotoxicities of the active compounds, tested on confluent HeLa, Vero and peritoneal macrophage cell cultures, resulted in significantly higher selectivity indices (SI) than that of the reference drug benznidazole. Remarkably, several molecules of the tested panel strongly inhibited the parasite release from T. cruzi infected HeLa cell cultures suggesting an effect against the intracellular development of T. cruzi amastigotes as well. |
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| Keywords: | Chagas disease Disulfide Carbohydrate |
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