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Introduction: The aim of the present study was to compare cytotoxicity and genotoxicity of synthetic flavonoid 3-aminoflavone (3-AF) and its platinum(II) coordination complex [Pt(Cl)2(3-AF)2]. Material and methods: The study was performed on cultured human bladder carcinoma EJ cells using the MTT [3-(4, 5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide] and alkaline single cell gel electrophoresis (comet) assays. Results: The results of the MTT assay indicated that EJ cells were sensitive to [Pt(Cl)2(3-AF)2] and to cisplatin which was used as a reference compound. The IC50 values were ~18 μM and 1,5 μM for [Pt(Cl)2(3-AF)2] and cisplatin, respectively. 3-AF was not toxic to EJ cells up to the highest tested concentration 100 μM. Despite fact that 3-AF did not inhibit EJ cells proliferation, this compound exhibited low genotoxic activity as significant increase (P<0.05) of DNA content in comet tail was observed at drug concentrations exceeding 10 μM. No DNA damage was detected by the comet assay in EJ cells treated for 1 h with [Pt(Cl)2(3- AF)2] Conclusions: This result suggest that kinetics of DNA lesions formation by [Pt(Cl)2(3-AF)2] is slow and resembles of that cisplatin which is known to produce DNA damage peaking several hours after drug treatment. (Clin Exp Med Lett 2007; 48(3):165-168)

Keywords: 3-aminoflavone, 3-aminoflavone complex of platinum(II), EJ cells, comet assay, MTT assay