Please use this identifier to cite or link to this item: https://www.arca.fiocruz.br/handle/icict/30796
Title: Investigation on the pharmacological profile of antimony(III) complexes with hydroxyquinoline derivatives: anti-trypanosomal activity and cytotoxicity against human leukemia cell lines
Authors: Reis, Débora C.
Pinto, Mauro C. X.
Souza-Fagundes, Elaine M.
Rocha, Lucas F.
Pereira, Valéria R. A.
Melo, Cristiane M. L.
Beraldo, Heloisa
Affilliation: Universidade Federal de Minas Gerais. Departamento de Química. Belo Horizonte, MG, Brasil.
Universidade Federal de Minas Gerais. Departamento de Fisiologia. Belo Horizonte, MG, Brasil.
Universidade Federal de Minas Gerais. Departamento de Fisiologia. Belo Horizonte, MG, Brasil.
Fundação Oswaldo Cruz. Instituto Aggeu Magalhães. Departamento de Imunologia. Laboratório de Imunogenética. Recife, PE, Brasil.
Fundação Oswaldo Cruz. Instituto Aggeu Magalhães. Departamento de Imunologia. Laboratório de Imunogenética. Recife, PE, Brasil.
Fundação Oswaldo Cruz. Instituto Aggeu Magalhães. Departamento de Imunologia. Laboratório de Imunogenética. Recife, PE, Brasil.
Universidade Federal de Minas Gerais. Departamento de Química. Belo Horizonte, MG, Brasil.
Abstract: Complexes [Sb(QN)(2)Cl] (1), [Sb(QC)(2)Cl] (2) and [Sb(QI)(2)Cl] (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 SbCl(3) 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.
Keywords: 8-Hydroxyquinoline
5-Chloro-8- hydroxyquinoline
5-Chloro-7-iodo-8- hydroxyquinoline (clioquinol)
Antimony(III) complexes
Cytotoxicity
Anti-trypanosomal
DeCS: Animais
Antimônio / Química
Antineoplásicos / síntese química
Antineoplásicos / química
Antineoplásicos / farmacologia
Agentes Antiprotozoários / síntese química
Agentes Antiprotozoários / química
Agentes Antiprotozoários / Farmacologia
Linha Celular , Tumor
Proliferação Celular / efeitos de drogas
Ensaios de Rastreio de Fármacos Antitumorais
Células HL-60
Humanos
Hidroxiquinolinas / química
Masculino
Ratos
Ratos, endogâmicos BALB C
Compostos Organometálicos / síntese química
Compostos Organometálicos / química
Compostos Organometálicos / Farmacologia
Testes de Sensibilidade Parasitária
Baço / citologia
Baço / efeitos de drogas
Relação Estrutura- Atividade
Trypanosoma cruzi / efeitos de drogas
Trypanosoma cruzi / crescimento & desenvolvimento
Issue Date: 2011
Citation: REIS, Débora C. et al. Investigation on the Pharmacological Profile of Antimony(III) Complexes with Hydroxyquinoline Derivatives: Anti-Trypanosomal Activity and Cytotoxicity against Human Leukemia Cell Lines. BioMetals, v. 24, n. 4, p. 595–601, 1 ago. 2011.
DOI: 10.1007/s10534-011-9407-8
ISSN: 1572-8773
Copyright: restricted access
Appears in Collections:PE - IAM - Artigos de Periódicos

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