Artigo Produção Nacional Revisado por pares

Metal complexes with 2-acetylpyridine-N(4)-orthochlorophenylthiosemicarbazone: Cytotoxicity and effect on the enzymatic activity of thioredoxin reductase and glutathione reductase

2014; Elsevier BV; Volume: 84; Linguagem: Inglês

10.1016/j.ejmech.2014.07.055

ISSN

1768-3254

Autores

Gabrieli L. Parrilha, K.S.O. Ferraz, Josane A. Lessa, Kely Navakoski de Oliveira, Bernardo L. Rodrigues, Jonas Pereira Ramos, Elaine M. Souza–Fagundes, Ingo Ott, Heloísa Beraldo,

Tópico(s)

Redox biology and oxidative stress

Resumo

Metal complexes with 2-acetylpyridine-N(4)-orthochlorophenylthiosemicarbazone (H2Ac4oClPh) were assayed for their cytotoxicity against MCF-7 breast adenocarcinoma and HT-29 colon carcinoma cells. The thiosemicarbazone and most of the complexes were highly cytotoxic. H2Ac4oClPh and its gallium(III) and tin(IV) complexes did not show any inhibitory activity against thioredoxin reductase (TrxR) and glutathione reductase (GR). The palladium(II), platinum(II) and bismuth(III) complexes inhibited TrxR at micromolar concentrations but not GR. The antimony(III) and gold(III) complexes strongly inhibited TrxR at submicromolar doses with GR inhibition at higher concentrations. The selectivity of these complexes for TrxR suggests metal binding to a selenol residue in the active site of the enzyme. TrxR inhibition is likely a contributing factor to the mode of action of the gold and antimony derivatives.

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