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In vitro and in vivo evaluation of genotoxicity, cytotoxicity, and protective effects of synthetic chalcones (E)-3-(4-chlorophenyl)-1-phenyl-2-propen-1-one (4-CL) and (E)-3-(3,4-dimethoxyphenyl)-1- phenyl-2-propen-1-one (DMF)

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Submitted   Jan 25, 2022
Published   Mar 3, 2022
Issue    Vol 3 No 2 (2021)
DOI   10.25082/JPBR.2021.01.005

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Eliane Blanco Nunes
Molecular Genetics and Cytogenetics Laboratory, Biological Sciences Institute, Federal University of Goiás, Goiânia, Goiás, Brazil
Priscila Zei Melo
Radiobiology and Mutagenesis Laboratory, Biological Sciences Institute, Federal University of Goiás, Goiânia, Goiás, Brazil
Jefté Barbosa
Radiobiology and Mutagenesis Laboratory, Biological Sciences Institute, Federal University of Goiás, Goiânia, Goiás, Brazil
Jefferson Hollanda Veras
Radiobiology and Mutagenesis Laboratory, Biological Sciences Institute, Federal University of Goiás, Goiânia, Goiás, Brazil
Carolina Ribeiro e Silva
Department of Morphology, Biological Sciences Institute, Federal University of Goiás, Goiânia, Goiás, Brazil
Wanderlene Blanco Nunes
Department of Histology, Embriology and Cell Biology, Biological Sciences Institute, Federal University of Goiás, Goiânia, Goiás, Brazil
Lee Chen-Chen
Radiobiology and Mutagenesis Laboratory, Biological Sciences Institute, Federal University of Goiás, Goiânia, Goiás, Brazil
Caridad Noda Pérez
Chemistry Institute, Federal University of Goiás, Goiânia, Goiás, Brazil
Stanislau Parreira Cardozo
Veterinary and Zootechnics School, Federal University of Goiás, Goiânia, Goiás, Brazil
Aline Bernardes corresponding author
Federal Institute of Education, Science and Technology of Mato Grosso, Cuiabá, Mato Grosso, Brazil
Elisângela de Paula Silveira Lacerda
Molecular Genetics and Cytogenetics Laboratory, Biological Sciences Institute, Federal University of Goiás, Goiânia, Goiás, Brazil

Abstract

The chalcones (E)-3-(4-chlorophenyl)-1-phenyl-2-propen-1-one (4-CL) and (E)-3-(3,4-dimethoxyphenyl)-1-phenyl-2 -propen-1-one (DMF) are versatile and easily synthesized into low-cost compounds that have a wide spectrum of biological activities. In this study, the cytotoxic, genotoxic and modulatory activities of 4-CL and DMF were evaluated using the Ames test and the mouse micronucleus assay. The results of the Ames test revealed that both chalcones did not show mutagenic activity in Salmonella typhimurium strains TA98 and TA100, and demonstrated significant antimutagenicity (p< 0.05) when co-administered with sodium azide (SA) in strain TA100. In the micronucleus assay, both showed a significant increase in the frequency of micronucleated polychromatic erythrocytes (MNPCE) at 24 h and 48 h, revealing a genotoxic effect. In the co-treatment with mitomycin C (MMC) there was a significant decrease (p< 0.05) in the frequency of MNPCE both in chalcones at 24h and in the less concentrated dose of DMF at 48h, demonstrating its antigenotoxic activity. 4-CL showed a significant decrease in the polychromatic/ normochromatic erythrocyte (PCE/ NCE) ratio at 24 and 48 h (p< 0.05), indicating cytotoxicity. However, 4-CL and DMF when co-administered with MMC showed a significant increase in the PCE/NCE ratio within 24 hours, demonstrating anticytotoxicity. Furthermore, a biphasic dose-response behavior was observed in both chalcones, 4-CL in the co-administration with SA, in the Ames Test and DMF in the co-treatment with MMC, at 48 hours of exposure, in the micronucleus assay. In this study, 4-CL and DMF showed genotoxic, cytotoxic, antigenotoxic, anticytotoxic and no mutagenic properties.

Keywords
Salmonella typhimurium, mutagenicity, genotoxicity, chlorochalcone, dimethoxychalcone, micronucleus, OECD

Article Details

Supporting Agencies
Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq), Fundação de Apoio à Pesquisa de Goiás (FAPEG) and Coordenação de Aperfeiçoamento de Pessoal de Ensino Superior - Brazil (CAPES)
How to Cite
Nunes, E., Melo, P., Barbosa, J., Veras, J., e Silva, C., Nunes, W., Chen-Chen, L., Pérez, C., Cardozo, S., Bernardes, A., & Lacerda, E. de P. (2022). In vitro and in vivo evaluation of genotoxicity, cytotoxicity, and protective effects of synthetic chalcones (E)-3-(4-chlorophenyl)-1-phenyl-2-propen-1-one (4-CL) and (E)-3-(3,4-dimethoxyphenyl)-1- phenyl-2-propen-1-one (DMF). Journal of Pharmaceutical and Biopharmaceutical Research, 3(2), 206-217. https://doi.org/10.25082/JPBR.2021.01.005
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This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.

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