A new nitrosyl ruthenium complex: Synthesis, chemical characterization, in vitro and in vivo antitumor activities and probable mechanism of action

This study describes the synthesis of a new ruthenium nitrosyl complex with the formula [RuCl 2NO(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 biolo...

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Veröffentlicht in:European journal of medicinal chemistry 2011-09, Vol.46 (9), p.3616-3622
Hauptverfasser: 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.
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Sprache:eng
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Zusammenfassung:This study describes the synthesis of a new ruthenium nitrosyl complex with the formula [RuCl 2NO(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 [RuCl 2NO(BPA)]is effective in reducing tumor mass. Also, our results suggest that the mechanism of action of [RuCl 2NO(BPA)] includes binding to DNA, causing fragmentation of this biological molecule, which leads to apoptosis. A new nitrosyl ruthenium complex was synthesized, chemically characterized and evaluated for its cytotoxicity and antitumor properties. A possible mechanism of action is discussed. [Display omitted] ► A new nitrosyl ruthenium complex is synthesized. ► Chemical characterization is performed. ► in vitro and in vivo characterization reveals potent cytotoxic and antitumor activities, respectively. ► A probable mechanism of action is suggested.
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2011.04.064