| 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, Rodrigo 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, Mar. 2016. | pt_BR |
| ISSN | 0162-0134 | |
| URI | https://www.arca.fiocruz.br/handle/icict/14266 | |
| Language | eng | pt_BR |
| Publisher | Elsevier | pt_BR |
| Rights | restricted 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 | 10.1016/j.jinorgbio.2015.12.024 | |
| Abstract | Three new mixed 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 1.0-4.9×10(3)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 | Thiazolidines | pt_BR |
| Embargo date | 2030-12-31 | |
