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Öğe CYTOTOXIC AND GENOTOXIC EVALUATION OF SOME NEWLY SYNTHESIZED SULFONAMIDE DERIVATIVES(Parlar Scientific Publications (P S P), 2017) Sen, Selen; Berber, Ahmet Ali; Demirci, Tuna; Arslan, Mustafa; Aksoy, HuseyinIn the present study, it was aimed to assess the genotoxic potentials of [4,4-Dimethyl-2,6dioxocyclohexylidene) methylamino) benzene sulfonamide] (2b) and [4-((1,3-Dimethy1-2,4,6trioxo-tetrahydropyrimidin-5(6H)-ylidene) methyla mino) benzenesulfonamide] (2e) compounds which were synthesized considering that they may be used as drug raw materials and detected to inhibit human carbonic anhydrase I, II isoenzymes. For this purpose, chromosomal aberration, micronucleus and comet tests were implemented in human peripheral blood lymphocytes. 2b was used at the concentrations of 2.12, 1.06, 0.53 mu g/mL. 2e was used at the concentrations of 2.52, 1.26, 0.63 mu g/mL for these in vitro assays. We observed that 2b and 2e had no significant difference in all our application doses for chromosomal abnormalities and micronucleus assay. 2b and 2e showed different responses for tail length, tail intensity and tail moment in Comet assay. 2b reduced the mitotic index in all concentrations in 48 h application compared to both control groups, whereas 2e only reduced mitotic index at 2.52 mu g/mL compared to negative control and in all concentrations compared to the solvent control. According to the obtained results, the test substances are cytotoxic at high concentrations and long-term exposure but they are not genotoxic in human peripheral lymphocytes.Öğe Genotoxic effects of chlorophenoxy herbicide diclofop-methyl in mice in vivo and in human lymphocytes in vitro(Taylor & Francis Ltd, 2011) Unal, Fatma; Yuzbasioglu, Deniz; Yilmaz, Serkan; Akinci, Nihan; Aksoy, HuseyinDiclofop-methyl (DM) is a chlorophenoxy derivative used in large quantities for the control of annual grasses in grain and vegetable crops. In this study, the genotoxic effects of DM were investigated by measuring chromosomal aberrations (CAs) in mouse bone-marrow cells and CA and the comet assay in human peripheral lymphocytes. Mice were treated with 15.63, 31.25, 62.5, and 125 mg/kg body weight of DM intraperitoneally for 24 hours, and 15.63-, 31.25-, 62.5-, 125-, and 250-mu g/mL concentrations were applied to human lymphocytes for both 24 and 48 hours. In in vivo treatments, DM significantly, but not dose dependently, increased the total chromosome aberrations, compared to both negative and solvent controls. Cell proliferation was significantly, but not dose dependently, affected by all doses. In in vitro treatments, DM (except 15.63 mu g/mL) significantly and dose dependently increased the frequency of chromosome aberrations. Also, 250 mu g/mL of 48-hour treatment was found to be toxic. Cell proliferation was significantly and dose dependently affected by DM applications, when compared to negative control. In in vitro treatments, DM significantly decreased the mitotic index only at the highest concentration for 24 hours, and 62.5- and 125-mu g/mL concentrations for 48 hours. In the comet assay, a significant and dose-dependent increase in comet-tail intensity was observed at 62.5-, 125-, and 250-mu g/mL concentrations. The mean comet-tail length was significantly increased in all concentrations. Our results demonstrate that DM is genotoxic in mammalian cells in vivo and in vitro.Öğe Genotoxicity evaluation of a new phthalazine substituted ?-lactam derivative in human lymphocytes(Acad Brasileira De Ciencias, 2022) Aygun, Betul; Berber, Ahmet A.; Doganci, Merve A.; Berber, Nurcan; Sen, Selen; Yildiz, Esra; Aksoy, HuseyinThe aim of present study, to evaluate the genotoxic potential of 1-(4-(3,3-dimethyl-1,6-dioxo-2,3,4,6,11,13-hexahydro-1H-indazolo[1,2b] phthalazine-13yl) phenyl)-2-phenylazetidine-3-yl-acetate which was synthesised assuming that it may be a pharmaceutical raw material and found to inhibit human carbonic anhydrase I, II isozymes. To determine the genotoxic potential of this phthalazine substituted beta-lactam compound, chromosomal aberration (CA) and micronucleus (MN) tests were implemented in human peripheral blood lymphocytes. In these tests, lymphocyte cultures were treated with four concentrations (30, 15, 7.5, 3.75 mu g/mL) of test compound and simultaneously with negative control (sterile distilled water), solvent control (DMSO) positive control (MMC). According to our results, CA frequencies were significantly increased in two high applied concentrations (30, 15 mu g/mL) compared with negative and solvent control. MN frequencies were significantly increased in three applied concentrations (30, 15, 7.5 mu g/mL) except lowest concentration (3.75 mu g/mL) compared with solvent control. Mitotic indices were also affected by treatment with test compound. The obtained results provide evidence to demonstrate that new phthalazine substituted beta-lactam derivative can exert genotoxic and cytotoxic effects in peripheral human lymphocytes especially at high concentrations.