Antiprotozoal activity of the cyclopalladated complexes against leishmania amazonensis and trypanosoma cruzi

The present study describes the antiprotozoal activities of four cyclopalladated compounds, [Pd(dmba)(μ-Cl)]2 , [Pd(dmba)(NCO)(isn)], [Pd(dmba)(N3)(isn)] and [Pd(dmba)(μ-NCO)]2 , (dmba: N,N'-dimethylbenzylamine and isn: isonicotinamide), against the diseases leishmaniasis (Leishmania amazonensi...

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Detalles Bibliográficos
Autores: Velásquez, Angela M. A. [UNESP], De Souza, Rodrigo A. [UNESP], Passalacqua, Thaís G. [UNESP], Ribeiro, Aline R., Scontri, Mateus [UNESP], Chin, Chung M. [UNESP], De Almeida, Leticia [UNESP], Cistia, Mayara L. Del [UNESP], Rosa, João A. Da [UNESP], Mauro, Antonio E. [UNESP], Graminha, Marcia A. S. [UNESP]
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2016
País:Brasil
Institución:Universidade Estadual Paulista (UNESP)
Repositorio:Repositório Institucional da UNESP
Idioma:inglés
OAI Identifier:oai:repositorio.unesp.br:11449/178060
Acceso en línea:http://dx.doi.org/10.5935/0103-5053.20150360
http://hdl.handle.net/11449/178060
Access Level:acceso abierto
Palabra clave:Chagas disease
Cyclopalladated
Leishmania amazonensis
Leishmaniasis
Trypanosoma cruzi
Trypanosomiasis
Descripción
Sumario:The present study describes the antiprotozoal activities of four cyclopalladated compounds, [Pd(dmba)(μ-Cl)]2 , [Pd(dmba)(NCO)(isn)], [Pd(dmba)(N3)(isn)] and [Pd(dmba)(μ-NCO)]2 , (dmba: N,N'-dimethylbenzylamine and isn: isonicotinamide), against the diseases leishmaniasis (Leishmania amazonensis and Leishmania infantum), Chagas disease (Trypanosoma cruzi) and human African trypanosomiasis (Trypanosoma brucei). [Pd(dmba)(μ-NCO)]2 exhibited good leishmanicidal and trypanocidal activities against L. amazonensis and T. cruzi intracellular amastigote forms, with a 50% inhibitory concentration (IC50 ) value of less than 9 μM and selectivity indexes of 14.47 and 28.42, respectively. Stability essays were conducted in phosphate buffer saline (PBS) pH 7.0 and showed that [Pd(dmba)(μ-NCO)]2 is the most stable molecule. These findings indicate that this compound presented higher selectivity for these parasites than the other tested compounds. The data presented here suggest that this compound should be considered in the development of new and more potent drugs for the treatment of leishmaniasis and Chagas disease.

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