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    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, Huseyin
    In 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.
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    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, Huseyin
    The 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.