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Título : In Vitro Anti-Trypanosoma cruzi Activity of Dronedarone, a Novel Amiodarone Derivative with an Improved Safety Profile
Autor : Benaím, Gustavo
Hernandez-Rodriguez, Vanessa
Mujica-Gonzalez, Sheira
Parra-Gimenez, Nereida
Plaza-Rojas, Lourdes
Silva, May Li
Garcia-Marchan, Yael
paniz-mondolfi, Alberto
Uzcanga, Graciela
Palabras clave : Trypanosoma cruzi
Amiodarone Dronedarona
anti-Trypanosoma cruzi agent
parental drug
Drug Administration
(FDA)
Fecha de publicación : 2012
Editorial : Antimicrobial agents and chemotherapy
Citación : Vol. 56, Nº 7, p. 3720–3725
Resumen : Amiodarone, a commonly used antiarrhythmic, is also a potent and selective anti-Trypanosoma cruzi agent. Dronedarone is an amiodarone derivative in which the 2,5-diiodophenyl moiety of the parental drug has been replaced with an unsubstituted phe- nyl group aiming to eliminate the thyroid toxicity frequently observed with amiodarone treatment. Dronedarone has been ap- proved by the Food and Drug Administration (FDA), and its use as a safe antiarrhythmic has been extensively documented. We show here that dronedarone also has potent anti-T. cruzi activity, against both extracellular epimastigotes and intracellular amastigotes, the clinically relevant form of the parasite. The 50% inhibitory concentrations against both proliferative stages are lower than those previously reported for amiodarone. The mechanism of action of dronedarone resembles that of amiodarone, as it induces a large increase in the intracellular Ca21 concentration of the parasite, which results from the release of this ion from intracellular storage sites, including a direct effect of the drug on the mitochondrial electrochemical potential, and through alkalinization of the acidocalcisomes. Our results suggest a possible future repurposed use of dronedarone for the treatment of Chagas’ disease.
URI : http://saber.ucv.ve/jspui/handle/123456789/4389
ISSN : 0066-4804
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