Genotoxicity testing of the furylethylene derivative 1-(5-bromofur-2-yl)-2- bromo-2-nitroethene in cultured human lymphocytes

The genotoxic potential of the compound 1-(5-bromofur-2-yl)-2-bromo-2- nitroethene (G-1) was evaluated in peripheral blood lymphocytes cultured in vitro, at concentrations ranging from 1 to 20 μg/ml. Micronuclei (MN) and sister-chromatid exchanges (SCE) were scored as biomarkers of genotoxic effects. To detect the role of metabolic enzymes on the genotoxicity of this furylethylenic derivative, cultures for MN and SCE demonstrations were treated for 3 h with and without the S9 microsomal fraction as well as for 48 h without S9. Under the conditions of the study, the test agent did not induce significant increases in the frequency of micronucleated cells, irrespective of the presence/absence of the metabolic fraction. Nevertheless, a slight/moderate increase in the SCE frequency was observed in those cultures treated without the S9 mix. In addition, cytotoxic/cytostatic effects of the G-1 compound were observed mainly in cultures without S9 fraction, as indicated by the reduction of cell proliferation measured by the cytokinesis block proliferation index (CBPI) and the proliferative rate index (PRI). © 2003 Elsevier Ltd. All rights reserved.