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.
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http://dx.doi.org/10.1016/j.ijantimicag.2010.07.003 | DOI Listing |
Heliyon
December 2024
School of Chemistry and Physics, University of KwaZulu Natal, Westville Campus, Durban, 4000, South Africa.
[This corrects the article DOI: 10.1016/j.heliyon.
View Article and Find Full Text PDFSci Rep
January 2025
Departamento de Química, Centro de Ciências Exatas, Universidade Estadual de Londrina, Londrina, PR, Brasil.
This work investigates the anti-trypanosomal activities of ten thiohydantoin derivatives against the parasite Trypanosoma cruzi. Compounds with aliphatic chains (THD1, THD3, and THD5) exhibited the most promising IC against the epimastigote form of T. cruzi.
View Article and Find Full Text PDFChem Biodivers
December 2024
Universidad Nacional de Colombia, Antioquia, carrera 65 59a-110, 3840, Medellín, COLOMBIA.
Coumarin-chalcone hybrids are promising compounds that could be used as lead structures in the fight against parasitic diseases. In this work, sixteen hybrids of coumarin-chalcone (3-cinnamoyl-2H-chromen-2-ones) were synthesized, and their in vitro biological activity was evaluated against intracellular amastigotes of Leishmania braziliensis and Trypanosoma cruzi; as well as their cytotoxicity in the U-937 cell line. Compounds (E)-3-(3-(3-ethoxy-4-hydroxyphenyl)acryloyl)-7-methoxy-2H-chromen-2-one (H25) and (E)-7-(diethylamino)-3-(4-(methoxyphenyl)acryloyl)-2H-chromen-2-one (H12) showed the highest antileishmanial activity with EC50 values of 18.
View Article and Find Full Text PDFPhytochemistry
March 2025
Centre for Natural and Human Sciences, Federal University of ABC, Santo Andre, SP, 09280-560, Brazil. Electronic address:
As part of our continuous study on the Annonaceae species Porcelia macrocarpa, in the present work, eight chemically related 2-alkyl-3-hydroxy-4-methyl-γ-lactones (1-8) were isolated. Their structures were characterised by NMR, MS, and VCD. Their antitrypanosomal activity was evaluated in vitro against intracellular amastigotes with EC values ranged from 13.
View Article and Find Full Text PDFJ Parasitol Res
November 2024
Plant Development Department, Centre for Plant Medicine Research, Mampong-Akuapem, Ghana.
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