Author | Corrêa, Rodrigo S | |
Author | Silva, Monize Martins da | |
Author | Graminha, Angelica Ellen | |
Author | Meira, Cássio Santana | |
Author | Santos, Jamyle Andrade Ferreira dos | |
Author | Moreira, Diogo Rodrigo Magalhães | |
Author | Soares, Milena Botelho Pereira | |
Author | Poelhsitz, Gustavo Von | |
Author | Castellano, Eduardo Ernesto | |
Author | Bloch Junior, Carlos | |
Author | Cominetti, Marcia Regina | |
Author | Batista, Alzir Azevedo | |
Access date | 2016-05-13T13:34:13Z | |
Available date | 2016-05-13T13:34:13Z | |
Document date | 2016 | |
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. | pt_BR |
ISSN | 0162-0134 | |
URI | https://www.arca.fiocruz.br/handle/icict/14266 | |
Language | eng | pt_BR |
Publisher | Elsevier | pt_BR |
Rights | open access | pt_BR |
Title | Ruthenium(II) complexes of 1,3-thiazolidine-2-thione: Cytotoxicity against tumor cells and anti-Trypanosoma cruzi activity enhanced upon combination with benznidazole. | pt_BR |
Type | Article | pt_BR |
DOI | /dx.doi.org/10.1016/j.jinorgbio.2015.12.024 | |
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 | pt_BR |
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 | pt_BR |
Affilliation | Universidade Federal de São Carlos. Departamento de Química. São Carlos, SP, Brasil | pt_BR |
Affilliation | Universidade Federal de São Carlos. Departamento de Química. São Carlos, SP, Brasil | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil / Hospital São Rafael. Centro de Biotecnologia e Terapia Celular. Salvador, BA, Brasil | pt_BR |
Affilliation | Universidade Federal de Uberlândia. Instituto de Química. Uberlândia, MG, Brasil | pt_BR |
Affilliation | Universidade de São Paulo. Instituto de Física. São Carlos, SP, Brasil | pt_BR |
Affilliation | EMBRAPA. Centro Nacional de Pesquisa de Recursos Genéticos e Biotecnologia. Brasília, DF, Brasil | pt_BR |
Affilliation | Universidade Federal de São Carlos. Departamento de Gerontologia. São Carlos, SP, Brasil | pt_BR |
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 | pt_BR |
Subject | Ru(II) complexes | pt_BR |
Subject | Cytotoxicity | pt_BR |
Subject | Trypanosoma cruzi | pt_BR |
Subject | ctDNA-binding | pt_BR |
Subject | 1,3-Thiazolidine-2-thione | pt_BR |