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

dc.creatorCorrêa, Rodrigo S
dc.creatorSilva, Monize Martins da
dc.creatorGraminha, Angelica Ellen
dc.creatorMeira, Cássio Santana
dc.creatorSantos, Jamyle Andrade Ferreira dos
dc.creatorMoreira, Diogo Rodrigo Magalhães
dc.creatorSoares, Milena Botelho Pereira
dc.creatorPoelhsitz, Gustavo Von
dc.creatorCastellano, Eduardo Ernesto
dc.creatorBloch Junior, Carlos
dc.creatorCominetti, Marcia Regina
dc.creatorBatista, Alzir Azevedo
dc.date2016-05-13T13:34:13Z
dc.date2016-05-13T13:34:13Z
dc.date2016
dc.date.accessioned2023-09-27T00:13:26Z
dc.date.available2023-09-27T00:13:26Z
dc.identifierCORRÊA, 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.
dc.identifier0162-0134
dc.identifierhttps://www.arca.fiocruz.br/handle/icict/14266
dc.identifier/dx.doi.org/10.1016/j.jinorgbio.2015.12.024
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/8898681
dc.descriptionThree 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
dc.formatapplication/pdf
dc.languageeng
dc.publisherElsevier
dc.rightsopen access
dc.subjectRu(II) complexes
dc.subjectCytotoxicity
dc.subjectTrypanosoma cruzi
dc.subjectctDNA-binding
dc.subject1,3-Thiazolidine-2-thione
dc.titleRuthenium(II) complexes of 1,3-thiazolidine-2-thione: Cytotoxicity against tumor cells and anti-Trypanosoma cruzi activity enhanced upon combination with benznidazole.
dc.typeArticle


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