Ruthenium(II) complexes of 1,3-thiazolidine-2-thione : cytotoxicity against tumor cells and anti-Trypanosoma cruzi activity enhanced upon combination with benznidazole

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dc.contributor.authorCorrea, Rodrigo de Souza
dc.contributor.authorSilva, Monize Martins da
dc.contributor.authorGraminha, Angelica Ellen
dc.contributor.authorMeira, Cássio Santana
dc.contributor.authorSantos, Jamyle Andrade Ferreira dos
dc.contributor.authorMoreira, Diogo Rodrigo de Magalhães
dc.contributor.authorSoares, Milena Botelho Pereira
dc.contributor.authorPoelhsitz, Gustavo Von
dc.contributor.authorCastellano, Eduardo Ernesto
dc.contributor.authorBloch Junior, Carlos
dc.contributor.authorCominetti, Márcia Regina
dc.contributor.authorBatista, Alzir Azevedo
dc.date.accessioned2016-11-07T13:17:56Z
dc.date.available2016-11-07T13:17:56Z
dc.date.issued2016
dc.description.abstractThree 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
dc.identifier.citationCORREA, R. de 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. Disponível em: <http://www.sciencedirect.com/science/article/pii/S0162013415301501>. Acesso em: 26 set. 2016.pt_BR
dc.identifier.doihttps://doi.org/10.1016/j.jinorgbio.2015.12.024
dc.identifier.issn0162-0134
dc.identifier.urihttp://www.repositorio.ufop.br/handle/123456789/7067
dc.language.isopt_BRpt_BR
dc.rightsabertopt_BR
dc.rights.licenseO periódico Journal of Inorganic Biochemistry concede permissão para depósito deste artigo no Repositório Institucional da UFOP. Número da licença: 3958741353996.pt_BR
dc.subjectCytotoxicitypt_BR
dc.subjectTrypanosoma cruzipt_BR
dc.titleRuthenium(II) complexes of 1,3-thiazolidine-2-thione : cytotoxicity against tumor cells and anti-Trypanosoma cruzi activity enhanced upon combination with benznidazolept_BR
dc.typeArtigo publicado em periodicopt_BR
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