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 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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Main Authors: Velásquez,Angela M. A., Souza,Rodrigo A. de, Passalacqua,Thaís G., Ribeiro,Aline R., Scontri,Mateus, Chin,Chung M., Almeida,Leticia de, Cistia,Mayara L. Del, Rosa,João A. da, Mauro,Antonio E., Graminha,Marcia A. S.
Format: Digital revista
Language:English
Published: Sociedade Brasileira de Química 2016
Online Access:http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532016000601032
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spelling oai:scielo:S0103-505320160006010322016-06-21Antiprotozoal Activity of the Cyclopalladated Complexes Against Leishmania amazonensis and Trypanosoma cruziVelásquez,Angela M. A.Souza,Rodrigo A. dePassalacqua,Thaís G.Ribeiro,Aline R.Scontri,MateusChin,Chung M.Almeida,Leticia deCistia,Mayara L. DelRosa,João A. daMauro,Antonio E.Graminha,Marcia A. S. cyclopalladated leishmaniasis Chagas disease Leishmania amazonensis Trypanosoma cruzi trypanosomiasis 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.info:eu-repo/semantics/openAccessSociedade Brasileira de QuímicaJournal of the Brazilian Chemical Society v.27 n.6 20162016-06-01info:eu-repo/semantics/articletext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532016000601032en10.5935/0103-5053.20150360
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language English
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author Velásquez,Angela M. A.
Souza,Rodrigo A. de
Passalacqua,Thaís G.
Ribeiro,Aline R.
Scontri,Mateus
Chin,Chung M.
Almeida,Leticia de
Cistia,Mayara L. Del
Rosa,João A. da
Mauro,Antonio E.
Graminha,Marcia A. S.
spellingShingle Velásquez,Angela M. A.
Souza,Rodrigo A. de
Passalacqua,Thaís G.
Ribeiro,Aline R.
Scontri,Mateus
Chin,Chung M.
Almeida,Leticia de
Cistia,Mayara L. Del
Rosa,João A. da
Mauro,Antonio E.
Graminha,Marcia A. S.
Antiprotozoal Activity of the Cyclopalladated Complexes Against Leishmania amazonensis and Trypanosoma cruzi
author_facet Velásquez,Angela M. A.
Souza,Rodrigo A. de
Passalacqua,Thaís G.
Ribeiro,Aline R.
Scontri,Mateus
Chin,Chung M.
Almeida,Leticia de
Cistia,Mayara L. Del
Rosa,João A. da
Mauro,Antonio E.
Graminha,Marcia A. S.
author_sort Velásquez,Angela M. A.
title Antiprotozoal Activity of the Cyclopalladated Complexes Against Leishmania amazonensis and Trypanosoma cruzi
title_short Antiprotozoal Activity of the Cyclopalladated Complexes Against Leishmania amazonensis and Trypanosoma cruzi
title_full Antiprotozoal Activity of the Cyclopalladated Complexes Against Leishmania amazonensis and Trypanosoma cruzi
title_fullStr Antiprotozoal Activity of the Cyclopalladated Complexes Against Leishmania amazonensis and Trypanosoma cruzi
title_full_unstemmed Antiprotozoal Activity of the Cyclopalladated Complexes Against Leishmania amazonensis and Trypanosoma cruzi
title_sort antiprotozoal activity of the cyclopalladated complexes against leishmania amazonensis and trypanosoma cruzi
description 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.
publisher Sociedade Brasileira de Química
publishDate 2016
url http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532016000601032
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