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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

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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Author(s):
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Correa, Rodrigo S. [1, 2] ; da Silva, Monize M. [2] ; Graminha, Angelica E. [2] ; Meira, Cassio S. [3] ; dos Santos, Jamyle A. F. [3] ; Moreira, Diogo R. M. [3] ; Soares, Milena B. P. [3, 4] ; Von Poelhsitz, Gustavo [5] ; Castellano, Eduardo E. [6] ; Bloch, Jr., Carlos [7] ; Cominetti, Marcia R. [8] ; Batista, Alzir A. [2]
Total Authors: 12
Affiliation:
[1] Univ Fed Ouro Preto, ICEB, Dept Quim, BR-35400000 Ouro Preto, MG - Brazil
[2] Univ Fed Sao Carlos, Dept Quim, CP 676, BR-13565905 Sao Carlos, SP - Brazil
[3] Fiocruz MS, Ctr Pesquisas Goncalo Moniz, BR-40296710 Salvador, BA - Brazil
[4] Hosp Sao Rafael, Ctr Biotecnol & Terapia Celular, Ave Sao Rafael 2152, BR-41253190 Salvador, BA - Brazil
[5] Univ Fed Uberlandia, Inst Quim, CP 593, BR-38400902 Uberlandia, MG - Brazil
[6] Univ Sao Paulo, Inst Fis, CP 369, BR-13560970 Sao Carlos, SP - Brazil
[7] EMBRAPA, Ctr Nacl Pesquisa Recursos Genet & Biotecnol, Estacao Parque Biol, BR-70910900 Brasilia, DF - Brazil
[8] Univ Fed Sao Carlos, Dept Gerontol, CP 676, BR-13565905 Sao Carlos, SP - Brazil
Total Affiliations: 8
Document type: Journal article
Source: Journal of Inorganic Biochemistry; v. 156, p. 153-163, MAR 2016.
Web of Science Citations: 26
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 (K-b) values in range of 1.0-4.9 x 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. (C) 2015 Elsevier Inc. All rights reserved. (AU)

FAPESP's process: 12/06013-4 - Study of apoptosis gene expression, celular cyclic, DNA repair and oxidative stress in cells of human lang carcinoma treated with complexes with general formula [Ru(AA)(dppb)(bipy)]PF6
Grantee:Alzir Azevedo Batista
Support Opportunities: Regular Research Grants
FAPESP's process: 09/08131-1 - Ruthenium complexes containing ligands with biologic interest: chemical and structural aspects and evaluation of their citotoxicity against tumoral cells
Grantee:Rodrigo de Souza Corrêa
Support Opportunities: Scholarships in Brazil - Doctorate
FAPESP's process: 13/26559-4 - Structural modifications in biologically active Ru(II) complexes toward the design of new metallodrug candidates
Grantee:Rodrigo de Souza Corrêa
Support Opportunities: Scholarships in Brazil - Post-Doctoral