Título:
Looking for combination of benznidazole and trypanosoma cruzitriosephosphate isomerase inhibitors for chagas disease treatment
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Autor:
Aguilera, Elena
Varela Ubillos, Javier Alejandro
Serna, Elva
Torres, Susana
Yaluff, Gloria
De Bilbao, Ninfa Vera
Cerecetto, Hugo
Álvarez, Guzmán
González, Mercedes
Varela Ubillos, Javier Alejandro
Serna, Elva
Torres, Susana
Yaluff, Gloria
De Bilbao, Ninfa Vera
Cerecetto, Hugo
Álvarez, Guzmán
González, Mercedes
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Tipo de documento:
Artículo
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Palabras clave:
Chagas disease
Synergism
Isobologram
In vivo studies
Synergism
Isobologram
In vivo studies
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Año de publicación:
2018
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Resumen:
BACKGROUND The current chemotherapy for Chagas disease is based on monopharmacology with low efficacy and drug tolerance. Polypharmacology is one of the strategies to overcome these limitations. OBJECTIVES Study the anti-Trypanosoma cruzi activity of associations of benznidazole (Bnz) with three new synthetic T. cruzi-triosephosphate isomerase inhibitors, 2, 3, and 4, in order to potentiate their actions. METHODS The in vitro effect of the drug combinations were determined constructing the corresponding isobolograms. In vivo activities were assessed using an acute murine model of Chagas disease evaluating parasitaemias, mortalities and IgG anti-T. cruzi antibodies. FINDINGS The effect of Bnz combined with each of these compounds, on the growth of epimastigotes, indicated an additive action or a synergic action, when combining it with 2 or 3, respectively, and an antagonic action when combining it with 4. In vivo studies, for the two chosen combinations, 2 or 3 plus one fifth equivalent of Bnz, showed that Bnz can also potentiate the in vivo therapeutic effects. For both combinations a decrease in the number of trypomastigote and lower levels of anti-T. cruzi IgG-antibodies were detected, as well clear protection against death. MAIN CONCLUSIONS These results suggest the studied combinations could be used in the treatment of Chagas disease.
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Fundacao Oswaldo Cruz
EN:
Memorias do Instituto Oswaldo Cruz, 2018, 113(3): 153-160.
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Citación:
Aguilera, E., Varela, J., Serna, E., y otros. "Looking for combination of benznidazole and trypanosoma cruzitriosephosphate isomerase inhibitors for chagas disease treatment". Memorias do Instituto Oswaldo Cruz. [en línea] 2018, 113(3): 153-160. 8 h.
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0074-0276
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Licencia Creative Commons Atribución (CC - By 4.0)
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| Ficheros | Descripción | Tamaño | Formato | ||
|---|---|---|---|---|---|
| 101590007402760170267.pdf | — | 1.39 MB | Adobe PDF |