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A new nitrosyl ruthenium complex: synthesis, chemical characterization, in vitro and in vivo antitumor activities and probable mechanism of action |
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| Authors: | Heinrich Tassiele A Von Poelhsitz Gustavo Reis Rosana I Castellano Eduardo E Neves Ademir Lanznaster Maurício Machado Sérgio P Batista Alzir A Costa-Neto Claudio M |
| Affiliation: | a Departamento de Bioquímica e Imunologia, Faculdade de Medicine de Ribeirão Preto, Universidade de São Paulo, Av. Bandeirantes, 3900-FMRP-USP, 14.049-900 Ribeirão Preto-SP, Brazil b Instituto de Química, Universidade Federal de Uberlândia, 38.400-902 Uberlândia-MG, Brazil c Instituto de Física de São Carlos, Universidade de São Paulo, 13.560-970 São Carlos-SP, Brazil d Departamento de Química, Universidade Federal de Santa Catarina, 88.040-900 Florianópolis-SC, Brazil e Instituto de Química, Universidade Federal Fluminense, 24.020-141 Niterói-RJ, Brazil f Instituto de Química, Universidade Federal do Rio de Janeiro, 21.941-909 Rio de Janeiro-RJ, Brazil g Departamento de Química, Universidade Federal de São Carlos, 13.561-901 São Carlos-SP, Brazil |
| Abstract: | This study describes the synthesis of a new ruthenium nitrosyl complex with the formula [RuCl2NO(BPA)] [BPA = (2-hydroxybenzyl)(2-methylpyridyl)amine ion], which was synthesized and characterized by spectroscopy, cyclic voltammetry, X-ray crystallography, and theoretical calculation data. The biological studies of this complex included in vitro cytotoxic assays, which revealed its activity against two different tumor cell lines (HeLa and Tm5), with efficacy comparable to that of cisplatin, a metal-based drug that is administered in clinical treatment. The in vivo studies showed that [RuCl2NO(BPA)]is effective in reducing tumor mass. Also, our results suggest that the mechanism of action of [RuCl2NO(BPA)] includes binding to DNA, causing fragmentation of this biological molecule, which leads to apoptosis. |
| Keywords: | Ruthenium complex 2-hydroxybenzyl(2-methylpyridyl)amine Cytotoxicity Melanoma DNA interaction Apoptosis |
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