Investigation on the pharmacological profile of antimony(III) complexes with hydroxyquinoline derivatives: anti-trypanosomal activity and cytotoxicity against human leukemia cell lines |
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Authors: | Débora C Reis Mauro C X Pinto Elaine M Souza-Fagundes Lucas F Rocha Valéria R A Pereira Cristiane M L Melo Heloisa Beraldo |
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Institution: | 1.Departamento de Química,Universidade Federal de Minas Gerais,Belo Horizonte,Brazil;2.Departamento de Fisiologia,Universidade Federal de Minas Gerais,Belo Horizonte,Brazil;3.Laboratório de Imunogenética, Departamento de Imunologia,Instituto Aggeu Magalh?es – FIOCRUZ,Pernambuco,Brazil |
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Abstract: | Complexes Sb(QN)2Cl] (1), Sb(QC)2Cl] (2) and Sb(QI)2Cl] (3) were obtained with 8-hydroxyquinoline (HQN), 5-chloro-8-hydroxyquinoline (HQC) and 5-chloro-7-iodo-8-hydroxyquinoline (clioquinol,
HQI). The quinoline derivatives and their antimony(III) complexes were evaluated for their anti-trypanosomal activity as well
as for their cytotoxicity against HL-60 and Jurkat human leukemia cell lines. Upon coordination to antimony(III) the anti-trypanosomal
activity of HQC and HQI increases, the highest improvement being observed for complex (3), which was the most active among all studied compounds against both epimastigote and trypomastigote forms of Trypanosoma cruzi. All quinoline derivatives proved to be cytotoxic against both leukemia cell lineages. Upon coordination to antimony(III)
the cytotoxicity of HQN improved against Jurkat leukemia cells. While SbCl3 proved to be cytotoxic against HL-60 cells, it was not active against Jurkat cells. However, its coordination to the quinoline
derivatives resulted in complexes with significant cytotoxicity against Jurkat cells. |
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