High antitrypanosomal activity of plant-derived sulphur-containing amides.
Chagas disease, caused by Trypanosoma cruzi, represents an important public health problem in endemic geographic regions in Middle and South America, affecting 15 million infected people. Treatment options are still limited due to the toxicity of available drugs, parasite resistance and poor drug activity during the chronic phase of the disease. In this study, we investigated the in vitro antitrypanosomal activity of 15 tropical plant-derived compounds with the aim of finding new drug candidates. Three novel sulphur-containing amides (methyldambullin, methylgerambullin and sakambullin) showed promising antitrypanosomal activities, with 50% effective concentrations (EC₅₀ values) after 72 h exposure of 1.7, 1.23 and 5.18 μM, respectively, compared with EC₅₀ values for amphotericin B and benznidazole of 0.71 μM and 30.89 μM, respectively.
Astelbauer
Florian
F
Institute of Specific Prophylaxis and Tropical Medicine, Center for Pathophysiology, Infectiology and Immunology, Medical University of Vienna, Kinderspitalgasse 15, A-1090 Vienna, Austria.
Obwaller
Andreas
A
Raninger
Adriane
A
Brem
Brigitte
B
Greger
Harald
H
Duchêne
Michael
M
Wernsdorfer
Walther
W
Walochnik
Julia
J
D000577:Amides / Q000302:isolation & purification / Q000494:pharmacology*; D000981:Antiprotozoal Agents / Q000302:isolation & purification / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D010936:Plant Extracts / Q000302:isolation & purification / Q000494:pharmacology*; D010944:Plants / Q000737:chemistry*; D013457:Sulfur Compounds / Q000302:isolation & purification / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects*
D000577:Amides; D000981:Antiprotozoal Agents; D010936:Plant Extracts; D013457:Sulfur Compounds