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Regulatory agencies require demonstration of non-genotoxicity of new chemical entities prior to their use as pharmaceuticals or additives. Consequently, the in vitro cytotoxicity, genotoxicity and apoptoxicity of five novel monoazo colourants (8-hydroxy-3,6-disulphonaphthyl azohydroxynaphthalenes, 3...
| Format: | Article |
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| Published: |
2023
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| LEADER | 00000njm a2000000a 4500 | ||
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| 001 | oai:repository.ui.edu.ng:123456789/12107 | ||
| 042 | |a dc | ||
| 720 | |a Thomas, O. E. |e author | ||
| 720 | |a Adegoke, O. A. |e author | ||
| 720 | |a Mukherjee, A. |e author | ||
| 720 | |a Banerjee, R. |e author | ||
| 260 | |c 2023 | ||
| 520 | |a Regulatory agencies require demonstration of non-genotoxicity of new chemical entities prior to their use as pharmaceuticals or additives. Consequently, the in vitro cytotoxicity, genotoxicity and apoptoxicity of five novel monoazo colourants (8-hydroxy-3,6-disulphonaphthyl azohydroxynaphthalenes, 3a-e) on human lymphocytes were evaluated using a cell viability assay, alkaline comet assay, DNA diffusion assay, DFT calculations and molecular docking. The test concentrations of the compounds varied from 0 to 3.4 mM. Relative to negative control, the compounds at concentrations up to 0.5mM induced small dose-dependent reduction (< 20%) in viability of lymphocytes. Statistically significant changes (p<0.05) in DNA damage parameters (percent tail DNA, tail extent moment, olive tail moment) were observed at all concentrations of 3a, 3b while 3c-e showed genotoxicity at 2.8, 0.17 and 3.4 mM respectively. Compounds 3a, 3b, 3d induced apoptosis at concentrations below cytotoxic doses while 3c and 3e were non-apoptoxic at all test concentrations. DFT calculations showed the genotoxicity of 3a-e increased with electrophilicity and ionization potentials of the compounds. Molecular docking of 3a-e with apoptosis-associated proteins revealed binding affinity patterns that were consistent with observed experimental apoptoxicity. The structure-genotoxicity relationships of five novel monoazo compounds, which can be employed in the design of safer congeners, have been elucidated. | ||
| 024 | 8 | |a 2230-7532 | |
| 024 | 8 | |a ui_art_thomas_invitro_2023 | |
| 024 | 8 | |a Analytical Chemistry Letters Vol 13(1), pp. 1-16 | |
| 024 | 8 | |a https://repository.ui.edu.ng/handle/123456789/12107 | |
| 653 | |a Azo compounds | ||
| 653 | |a Alkaline comet assay | ||
| 653 | |a DNA diffusion assay | ||
| 653 | |a DFT calculation | ||
| 653 | |a Molecular docking. | ||
| 245 | 0 | 0 | |a In vitro cytotoxicity, genotoxicity and apoptoxicity of 8-hydroxy-3,6-disulphonaphthyl azohydroxynaphthalenes using Human Lymphocytes: Experimental and theoretical profiling |