Publication:
Selenium Derivatives as Promising Therapy for Chagas Disease: In Vitro and In Vivo Studies.

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Date

2021-04-19

Authors

Martin-Escolano, Ruben
Etxebeste-Mitxeltorena, Mikel
Martin-Escolano, Javier
Plano, Daniel
Rosales, Maria J
Espuelas, Socorro
Moreno, Esther
Sanchez-Moreno, Manuel
Sanmartin, Carmen
Marin, Clotilde

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American Chemical Society
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Abstract

Chagas disease is a tropical infection caused by the protozoan parasite Trypanosoma cruzi and a global public health concern. It is a paradigmatic example of a chronic disease without an effective treatment. Current treatments targeting T. cruzi are limited to two obsolete nitroheterocyclic drugs, benznidazole and nifurtimox, which lead to serious drawbacks. Hence, new, more effective, safer, and affordable drugs are urgently needed. Selenium and their derivatives have emerged as an interesting strategy for the treatment of different prozotoan diseases, such as African trypanosomiasis, leishmaniasis, and malaria. In the case of Chagas disease, diverse selenium scaffolds have been reported with antichagasic activity in vitro and in vivo. On the basis of these premises, we describe the in vitro and in vivo trypanocidal activity of 41 selenocompounds against the three morphological forms of different T. cruzi strains. For the most active selenocompounds, their effect on the metabolic and mitochondrial levels and superoxide dismutase enzyme inhibition capacity were measured in order to determine the possible mechanism of action. Derivative 26, with a selenocyanate motif, fulfills the most stringent in vitro requirements for potential antichagasic agents and exhibits a better profile than benznidazole in vivo. This finding provides a step forward for the development of a new antichagasic agent.

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MeSH Terms

Chagas Disease
Humans
Pharmaceutical Preparations
Selenium
Trypanocidal Agents
Trypanosoma cruzi

DeCS Terms

Enfermedad de chagas
Humanos
Preparaciones farmacéuticas
Selenio
Tripanocidas
Trypanosoma cruzi

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Keywords

Chagas disease, Trypanosoma cruzi, chemotherapy, drug discovery, selenium derivatives

Citation

Martín-Escolano R, Etxebeste-Mitxeltorena M, Martín-Escolano J, Plano D, Rosales MJ, Espuelas S, et al. Selenium Derivatives as Promising Therapy for Chagas Disease: In Vitro and In Vivo Studies. ACS Infect Dis. 2021 Jun 11;7(6):1727-1738.