Synthetic thiophenes induce chromosomal damage and trigger apoptosis in human cancer cell lines
Thiophenes are heterocyclic compounds containing a five-membered ring with sulphur as the heteroatom. This class of substances has been shown to have several biological activities, including specific anti-proliferative effects against some cancer cell lines. The aim of the present study was to evalu...
| Main Authors: | , , , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Elsevier
2022-04-01
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| Series: | European Journal of Medicinal Chemistry Reports |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S277241742200005X |
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| author | Filipe N. Franco Júlia T. Oliveira Kimberly B. Tecchio Flaviana A. Santos Moacyr J.B.M. Rêgo Francisco J.B. Mendonça-Júnior Maira G.R. Pitta Michelly C. Pereira Rosy I.M.A. Ribeiro Vanessa J.S.V. Santos Fabio V. Santos |
| author_facet | Filipe N. Franco Júlia T. Oliveira Kimberly B. Tecchio Flaviana A. Santos Moacyr J.B.M. Rêgo Francisco J.B. Mendonça-Júnior Maira G.R. Pitta Michelly C. Pereira Rosy I.M.A. Ribeiro Vanessa J.S.V. Santos Fabio V. Santos |
| author_sort | Filipe N. Franco |
| collection | DOAJ |
| description | Thiophenes are heterocyclic compounds containing a five-membered ring with sulphur as the heteroatom. This class of substances has been shown to have several biological activities, including specific anti-proliferative effects against some cancer cell lines. The aim of the present study was to evaluate in vitro possible cytotoxic, genotoxic, and mutagenic properties of synthetic thiophenes using cell lines derived from human solid tumours. Different methodologies were employed to assess the cytotoxic effects of the compounds here named SB44, SB83, and SB200 (a 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide [MTT] assay, clonogenic assay, and annexin V staining) and to elucidate the chromosomal damage possibly involved in the triggered cell death (micronucleus, comet, and γ-H2AX assays). All tested thiophenes reduced cell survival regardless of the dose and duration of treatment. By contrast, compound SB200 manifested an attractive selectivity index towards the tumour cell lines under study. All the evaluated compounds caused chromosomal damage in vitro in the same way. The results imply that these compounds induce cell death by apoptosis as a consequence of chromosomal damage. Taken together, the data suggest that the thiophenes tested herein are useful prototypes for the development of anti-cancer drugs. |
| first_indexed | 2024-12-22T06:41:05Z |
| format | Article |
| id | doaj.art-29e6509260e641fdb8b6977e00fd66d8 |
| institution | Directory Open Access Journal |
| issn | 2772-4174 |
| language | English |
| last_indexed | 2024-12-22T06:41:05Z |
| publishDate | 2022-04-01 |
| publisher | Elsevier |
| record_format | Article |
| series | European Journal of Medicinal Chemistry Reports |
| spelling | doaj.art-29e6509260e641fdb8b6977e00fd66d82022-12-21T18:35:26ZengElsevierEuropean Journal of Medicinal Chemistry Reports2772-41742022-04-014100033Synthetic thiophenes induce chromosomal damage and trigger apoptosis in human cancer cell linesFilipe N. Franco0Júlia T. Oliveira1Kimberly B. Tecchio2Flaviana A. Santos3Moacyr J.B.M. Rêgo4Francisco J.B. Mendonça-Júnior5Maira G.R. Pitta6Michelly C. Pereira7Rosy I.M.A. Ribeiro8Vanessa J.S.V. Santos9Fabio V. Santos10Laboratory of Cell Biology and Mutagenesis (LaBCeM), Federal University of São João Del Rei (UFSJ), Divinópolis, BrazilLaboratory of Cell Biology and Mutagenesis (LaBCeM), Federal University of São João Del Rei (UFSJ), Divinópolis, BrazilLaboratory of Cell Biology and Mutagenesis (LaBCeM), Federal University of São João Del Rei (UFSJ), Divinópolis, BrazilLaboratory for Immunomodulation and New Therapeutic Approaches, Federal University of Pernambuco (UFPE), Recife, BrazilLaboratory for Immunomodulation and New Therapeutic Approaches, Federal University of Pernambuco (UFPE), Recife, BrazilLaboratory Synthesis and Vectoring Molecules, Department of Biological Sciences, State University of Paraíba (UEPB), João Pessoa, BrazilLaboratory for Immunomodulation and New Therapeutic Approaches, Federal University of Pernambuco (UFPE), Recife, BrazilLaboratory for Immunomodulation and New Therapeutic Approaches, Federal University of Pernambuco (UFPE), Recife, BrazilLaboratory of Experimental Pathology, Federal University of São João Del Rei (UFSJ), Divinópolis, BrazilLaboratory of Cell Biology and Mutagenesis (LaBCeM), Federal University of São João Del Rei (UFSJ), Divinópolis, BrazilLaboratory of Cell Biology and Mutagenesis (LaBCeM), Federal University of São João Del Rei (UFSJ), Divinópolis, Brazil; Corresponding author. Avenida Sebastião Gonçalves Coelho, 400, 35501-296, Divinópolis, MG, Brazil.Thiophenes are heterocyclic compounds containing a five-membered ring with sulphur as the heteroatom. This class of substances has been shown to have several biological activities, including specific anti-proliferative effects against some cancer cell lines. The aim of the present study was to evaluate in vitro possible cytotoxic, genotoxic, and mutagenic properties of synthetic thiophenes using cell lines derived from human solid tumours. Different methodologies were employed to assess the cytotoxic effects of the compounds here named SB44, SB83, and SB200 (a 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide [MTT] assay, clonogenic assay, and annexin V staining) and to elucidate the chromosomal damage possibly involved in the triggered cell death (micronucleus, comet, and γ-H2AX assays). All tested thiophenes reduced cell survival regardless of the dose and duration of treatment. By contrast, compound SB200 manifested an attractive selectivity index towards the tumour cell lines under study. All the evaluated compounds caused chromosomal damage in vitro in the same way. The results imply that these compounds induce cell death by apoptosis as a consequence of chromosomal damage. Taken together, the data suggest that the thiophenes tested herein are useful prototypes for the development of anti-cancer drugs.http://www.sciencedirect.com/science/article/pii/S277241742200005XThiopheneGenotoxicityMutagenicityIn vitroAnticancer candidate |
| spellingShingle | Filipe N. Franco Júlia T. Oliveira Kimberly B. Tecchio Flaviana A. Santos Moacyr J.B.M. Rêgo Francisco J.B. Mendonça-Júnior Maira G.R. Pitta Michelly C. Pereira Rosy I.M.A. Ribeiro Vanessa J.S.V. Santos Fabio V. Santos Synthetic thiophenes induce chromosomal damage and trigger apoptosis in human cancer cell lines European Journal of Medicinal Chemistry Reports Thiophene Genotoxicity Mutagenicity In vitro Anticancer candidate |
| title | Synthetic thiophenes induce chromosomal damage and trigger apoptosis in human cancer cell lines |
| title_full | Synthetic thiophenes induce chromosomal damage and trigger apoptosis in human cancer cell lines |
| title_fullStr | Synthetic thiophenes induce chromosomal damage and trigger apoptosis in human cancer cell lines |
| title_full_unstemmed | Synthetic thiophenes induce chromosomal damage and trigger apoptosis in human cancer cell lines |
| title_short | Synthetic thiophenes induce chromosomal damage and trigger apoptosis in human cancer cell lines |
| title_sort | synthetic thiophenes induce chromosomal damage and trigger apoptosis in human cancer cell lines |
| topic | Thiophene Genotoxicity Mutagenicity In vitro Anticancer candidate |
| url | http://www.sciencedirect.com/science/article/pii/S277241742200005X |
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