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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: Correa, Rodrigo de Souza
Silva, Monize Martins da
Graminha, Angelica Ellen
Meira, Cássio Santana
Santos, Jamyle Andrade Ferreira dos
Moreira, Diogo Rodrigo de Magalhães
Soares, Milena Botelho Pereira
Poelhsitz, Gustavo Von
Castellano, Eduardo Ernesto
Bloch Junior, Carlos
Cominetti, Márcia Regina
Batista, Alzir Azevedo
Keywords: Cytotoxicity
Trypanosoma cruzi
Issue Date: 2016
Citation: CORREA, 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: <>. Acesso em: 26 set. 2016.
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.
ISSN: 0162-0134
metadata.dc.rights.license: O periódico Journal of Inorganic Biochemistry concede permissão para depósito deste artigo no Repositório Institucional da UFOP. Número da licença: 3958741353996.
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