RT Journal Article
T1 Selenium Derivatives as Promising Therapy for Chagas Disease: In Vitro and In Vivo Studies.
A1 Martin-Escolano, Ruben
A1 Etxebeste-Mitxeltorena, Mikel
A1 Martin-Escolano, Javier
A1 Plano, Daniel
A1 Rosales, Maria J
A1 Espuelas, Socorro
A1 Moreno, Esther
A1 Sanchez-Moreno, Manuel
A1 Sanmartin, Carmen
A1 Marin, Clotilde
K1 Chagas disease
K1 Trypanosoma cruzi
K1 chemotherapy
K1 drug discovery
K1 selenium derivatives
AB 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.
PB American Chemical Society
YR 2021
FD 2021-04-19
LK http://hdl.handle.net/10668/17600
UL http://hdl.handle.net/10668/17600
LA en
NO 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.
NO This work was financially supported by the Ministerio deEconomia, Industria y Competitividad (CONSOLIDERCSD2010−00065 and CTQ2017−90852−REDC). R.M.-E. isgrateful for the fellowship from the Alfonso Martín EscuderoFoundation.
DS RISalud
RD Apr 8, 2025