Library of Selenocyanate and Diselenide Derivatives as In Vivo Antichagasic Compounds Targeting Trypanosoma Cruzi Mitochondrion
Metadatos
Mostrar el registro completo del ítemAutor
Martín-Escolano, Rubén; Molina Carreño, Daniel; Rosales Lombardo, María José; Sánchez Moreno, Manuel; Marín Sánchez, ClotildeEditorial
MDPI
Materia
American trypanosomiasis Chagas disease Chemotherapy Drug Discovery Neglected tropical diseases Screening cascade Selenium derivatives Target product profile Trypanosoma cruzi
Fecha
2021Referencia bibliográfica
Martín-Escolano, R.; Molina-Carreño, D.; Plano, D.; Espuelas, S.; Rosales, M.J.; Moreno, E.; Aydillo, C.; Sanmartín, C.; Sánchez-Moreno, M.; Marín, C. Library of Selenocyanate and Diselenide Derivatives as In Vivo Antichagasic Compounds Targeting Trypanosoma Cruzi Mitochondrion. Pharmaceuticals 2021, 14, 419. https:// doi.org/10.3390/ph14050419
Patrocinador
Ministerio de Economia, Industria y Competitividad, grant number CSD2010–00065 and CTQ2017–90852-REDC; Conserjería de Economía, Conocimiento, Empresas y Universidad de la Junta de Andalucia, grant number A-CTS-383-UGR18; Institute of Tropical Health of University of Navarre (ISTUN); Caixa Foundation; Roviralta and Ubesol; Alfonso Martín Escudero FoundationResumen
Chagas disease is usually caused by tropical infection with the insect-transmitted protozoan
Trypanosoma cruzi. Currently, Chagas disease is a major public health concern worldwide due
to globalization, and there are no treatments neither vaccines because of the long-term nature
of the disease and its complex pathology. Current treatments are limited to two obsolete drugs,
benznidazole and nifurtimox, which lead to serious drawbacks. Taking into account the urgent need
for strict research efforts to find new therapies, here, we describe the in vitro and in vivo trypanocidal
activity of a library of selected forty-eight selenocyanate and diselenide derivatives that exhibited
leishmanicidal properties. The inclusion of selenium, an essential trace element, was due to the wellknown extensive pharmacological activities for selenium compounds including parasitic diseases as
T. cruzi. Here we present compound 8 as a potential compound that exhibits a better profile than
benznidazole both in vitro and in vivo. It shows a fast-acting behaviour that could be attributed to
its mode of action: it acts in a mitochondrion-dependent manner, causing cell death by bioenergetic
collapse. This finding provides a step forward for the development of a new antichagasic agent.