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Selenium Derivatives as Promising Therapy for Chagas Disease: In Vitro and In Vivo Studies
dc.contributor.author | Martín Escolano, Rubén | |
dc.contributor.author | Rosales Lombardo, María José | |
dc.contributor.author | Sánchez Moreno, Manuel | |
dc.contributor.author | Marín Sánchez, Clotilde | |
dc.date.accessioned | 2022-02-11T07:32:24Z | |
dc.date.available | 2022-02-11T07:32:24Z | |
dc.date.issued | 2021-04-19 | |
dc.identifier.citation | ACS Infect. Dis. 2021, 7, 6, 1727–1738. [https://doi.org/10.1021/acsinfecdis.1c00048] | es_ES |
dc.identifier.uri | http://hdl.handle.net/10481/72790 | |
dc.description | This work was financially supported by the Ministerio de Economia, Industria y Competitividad (CONSOLIDER CSD2010-00065 and CTQ2017-90852-REDC). R.M.-E. is grateful for the fellowship from the Alfonso Martin Escudero Foundation. | es_ES |
dc.description.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. | es_ES |
dc.description.sponsorship | Spanish Government CONSOLIDER CSD2010-00065 CTQ2017-90852-REDC | es_ES |
dc.description.sponsorship | Alfonso Martin Escudero Foundation | es_ES |
dc.language.iso | eng | es_ES |
dc.publisher | American Chemical Society | es_ES |
dc.rights | Atribución 3.0 España | * |
dc.rights.uri | http://creativecommons.org/licenses/by/3.0/es/ | * |
dc.subject | Chagas disease | es_ES |
dc.subject | Chemotherapy | es_ES |
dc.subject | Drug discovery | es_ES |
dc.subject | Selenium derivatives | es_ES |
dc.subject | Trypanosoma cruzi | es_ES |
dc.title | Selenium Derivatives as Promising Therapy for Chagas Disease: In Vitro and In Vivo Studies | es_ES |
dc.type | info:eu-repo/semantics/article | es_ES |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | es_ES |
dc.identifier.doi | 10.1021/acsinfecdis.1c00048 | |
dc.type.hasVersion | info:eu-repo/semantics/publishedVersion | es_ES |