Please use this identifier to cite or link to this item: http://www.arca.fiocruz.br/handle/icict/14266
Title: Ruthenium(II) complexes of 1,3-thiazolidine-2-thione: Cytotoxicity against tumor cells and anti-Trypanosoma cruzi activity enhanced upon combination with benznidazole.
Authors: Corrêa, Rodrigo S
Silva, Monize Martins da
Graminha, Angelica Ellen
Meira, Cássio Santana
Santos, Jamyle Andrade Ferreira dos
Moreira, Diogo Rodrigo Magalhães
Soares, Milena Botelho Pereira
Poelhsitz, Gustavo Von
Castellano, Eduardo Ernesto
Bloch Junior, Carlos
Cominetti, Marcia Regina
Batista, Alzir Azevedo
Affilliation: Universidade Federal de São Carlos. Departamento de Química. São Carlos, SP, Brasil / Universidade Federal de Ouro Preto. Departamento de Química. ICEB. Ouro Preto, MG, Brasil
Universidade Federal de São Carlos. Departamento de Química. São Carlos, SP, Brasil
Universidade Federal de São Carlos. Departamento de Química. São Carlos, SP, Brasil
Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil
Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil
Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil
Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil / Hospital São Rafael. Centro de Biotecnologia e Terapia Celular. Salvador, BA, Brasil
Universidade Federal de Uberlândia. Instituto de Química. Uberlândia, MG, Brasil
Universidade de São Paulo. Instituto de Física. São Carlos, SP, Brasil
EMBRAPA. Centro Nacional de Pesquisa de Recursos Genéticos e Biotecnologia. Brasília, DF, Brasil
Universidade Federal de São Carlos. Departamento de Gerontologia. São Carlos, SP, Brasil
Universidade Federal de São Carlos. Departamento de Química. São Carlos, SP, Brasil / Universidade Federal de Ouro Preto. Departamento de Química. ICEB. Ouro Preto, MG, Brasil
Abstract: Three newmixed and mononuclear Ru(II) complexes containing 1,3-thiazolidine-2-thione (tzdtH) were synthesized and characterized by spectroscopic analysis, molar conductivity, cyclic voltammetry, high-resolution electrospray ionization mass spectra and X-ray diffraction. The complexes presented unique stereochemistry and the proposed formulae are: [Ru(tzdt)(bipy)(dppb)]PF6 (1), cis-[Ru(tzdt)2(PPh3)2] (2) and trans- [Ru(tzdt)(PPh3)2(bipy)]PF6 (3), where dppb = 1,4-bis(diphenylphosphino)butane and bipy= 2,2′-bipyridine. These complexes demonstrated strong cytotoxicity against cancer cell lines when compared to cisplatin. Specifically, complex 2 was the most potent cytotoxic agent against MCF-7 breast cells, while complexes 1 and 3 were more active in DU-145 prostate cells. Binding of complexes to ctDNA was determined by UV–vis titration and viscosity measurements and revealed binding constant (Kb) values in range of 1.0–4.9 × 103 M−1, which are characteristic of compounds possessing weak affinity to ctDNA. In addition, these complexes presented antiparasitic activity against Trypanosoma cruzi. Specifically, complex 3 demonstrated strong potency, moderate selectivity index and acted in synergism with the approved antiparasitic drug, benznidazole. Additionally, complex 3 caused parasite cell death through a necrotic process. In conclusion, we demonstrated that Ru(II) complexes have powerful pharmacological activity, while the metal-free tzdtH does not provoke the same outcome
Keywords: Ru(II) complexes
Cytotoxicity
Trypanosoma cruzi
ctDNA-binding
1,3-Thiazolidine-2-thione
Issue Date: 2016
Publisher: Elsevier
Citation: CORRÊA, R. S. et al. Ruthenium(II) complexes of 1,3-thiazolidine-2-thione: Cytotoxicity against tumor cells and anti-Trypanosoma cruzi activity enhanced upon combination with benznidazole. Journal of Inorganic Biochemistry, v. 156, p. 153-163, 2016.
DOI: /dx.doi.org/10.1016/j.jinorgbio.2015.12.024
ISSN: 0162-0134
Copyright: open access
Appears in Collections:IGM - Artigos de Periódicos

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