Inhibition of DNA topoisomerase I activity and induction of apoptosis by thiazacridine derivatives
| Autor(a) principal: | |
|---|---|
| Data de Publicação: | 2013 |
| Outros Autores: | , , , , , , , , , , , , , |
| Tipo de documento: | Artigo |
| Idioma: | eng |
| Título da fonte: | Repositório Institucional da FIOCRUZ (ARCA) |
| Texto Completo: | https://www.arca.fiocruz.br/handle/icict/20786 |
Resumo: | Bezerra, Daniel Pereira “Documento produzido em parceria ou por autor vinculado à Fiocruz, mas não consta à informação no documento”. |
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Barros, Francisco Washington AraujoBezerra, Daniel PereiraFerreira, Paulo Michel PereiraCavalcanti, Bruno CoelhoSilva, Teresinha Gonçalves daPitta, Marina Galdino da RochaLima, Maria do Carmo Alves deGaldino, Suely LPitta, Ivan da RochaLotufo, Letícia Veras CostaMoraes Filho, Manoel Odorico deBurbano, Rommel Mario RodríguezGuecheva, Temenouga NikolovaHenriques, João Antonio PegasPessoa, Cláudia do Ó2017-08-28T18:45:32Z2017-08-28T18:45:32Z2013BARROS, F. W. A. et al. Inhibition of DNA topoisomerase I activity and induction of apoptosis by thiazacridine derivatives. Toxicology and Applied Pharmacology, v. 268, p. 37–46, 2013.0041-008Xhttps://www.arca.fiocruz.br/handle/icict/2078610.1016/j.taap.2013.01.010Bezerra, Daniel Pereira “Documento produzido em parceria ou por autor vinculado à Fiocruz, mas não consta à informação no documento”.Brazilian National Research Council, National Institute of Science and Technology for Pharmaceutical Innovation (CNPq/RENORBIO/INCT-IF) and INCT-BioanalíticaFederal University of Ceará. School of Medicine. Department of Physiology and Pharmacology. Fortaleza, CE, BrazilFederal University of Sergipe. Department of Physiology. São Cristóvão, SE, BrazilFederal University of Piauí. Department of Biological Sciences. Picos, PI, BrazilFederal University of Ceará. School of Medicine. Department of Physiology and Pharmacology. Fortaleza, CE, BrazilFederal University of Pernambuco. Department of Antibiotics. Recife, PE, BrazilFederal University of Pernambuco. Department of Antibiotics. Recife, PE, BrazilFederal University of Pernambuco. Department of Antibiotics. Recife, PE, BrazilFederal University of Pernambuco. Department of Antibiotics. Recife, PE, BrazilFederal University of Pernambuco. Department of Antibiotics. Recife, PE, BrazilFederal University of Ceará. School of Medicine. Department of Physiology and Pharmacology. Fortaleza, CE, BrazilFederal University of Ceará. School of Medicine. Department of Physiology and Pharmacology. Fortaleza, CE, BrazilFederal University of Pará. Institute of Biological Sciences. Belém, PA, BrazilFederal University of Rio Grande do Sul. Biotechnology Center. Porto Alegre, RGS, BrazilFederal University of Rio Grande do Sul. Biotechnology Center. Porto Alegre, RGS, BrazilFederal University of Ceará. School of Medicine. Department of Physiology and Pharmacology. Fortaleza, CE, BrazilThiazacridine derivatives (ATZD) are a novel class of cytotoxic agents that combine an acridine and thiazolidine nucleus. In this study, the cytotoxic action of four ATZD were tested in human colon carcinoma HCT-8 cells: (5Z)-5-acridin-9-ylmethylene-3-(4-methylbenzyl)-thiazolidine-2,4-dione - AC-4; (5ZE)-5-acridin-9-ylmethylene-3-(4-bromo-benzyl)-thiazolidine-2,4-dione - AC-7; (5Z)-5-(acridin-9-ylmethylene)-3-(4-chloro-benzyl)-1,3-thiazolidine-2,4-dione - AC-10; and (5ZE)-5-(acridin-9-ylmethylene)-3-(4-fluoro-benzyl)-1,3-thiazolidine-2,4-dione - AC-23. All of the ATZD tested reduced the proliferation of HCT-8 cells in a concentration- and time-dependent manner. There were significant increases in internucleosomal DNA fragmentation without affecting membrane integrity. For morphological analyses, hematoxylin-eosin and acridine orange/ethidium bromide were used to stain HCT-8 cells treated with ATZD, which presented the typical hallmarks of apoptosis. ATZD also induced mitochondrial depolarisation and phosphatidylserine exposure and increased the activation of caspases 3/7 in HCT-8 cells, suggesting that this apoptotic cell death was caspase-dependent. In an assay using Saccharomyces cerevisiae mutants with defects in DNA topoisomerases 1 and 3, the ATZD showed enhanced activity, suggesting an interaction between ATZD and DNA topoisomerase enzyme activity. In addition, ATZD inhibited DNA topoisomerase I action in a cell-free system. Interestingly, these ATZD did not cause genotoxicity or inhibit the telomerase activity in human lymphocyte cultures at the experimental levels tested. In conclusion, the ATZD inhibited the DNA topoisomerase I activity and induced tumour cell death through apoptotic pathways.engElsevierAcridinasTiazolidinasTiazacridinaDNA Topoisomerase IApoptoseAcridineThiazolidineThiazacridineDNA topoisomerase IApoptosisInhibition of DNA topoisomerase I activity and induction of apoptosis by thiazacridine derivativesinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleinfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txtlicense.txttext/plain; charset=utf-82991https://www.arca.fiocruz.br/bitstream/icict/20786/1/license.txt5a560609d32a3863062d77ff32785d58MD51ORIGINALBarros FWA Inhibition of DNA.....pdfBarros FWA Inhibition of DNA.....pdfapplication/pdf1103679https://www.arca.fiocruz.br/bitstream/icict/20786/2/Barros%20FWA%20Inhibition%20of%20DNA.....pdf0ad61a7527339f4fdc7938cca9438ffeMD52TEXTBarros FWA Inhibition of DNA.....pdf.txtBarros FWA Inhibition of DNA.....pdf.txtExtracted texttext/plain56143https://www.arca.fiocruz.br/bitstream/icict/20786/3/Barros%20FWA%20Inhibition%20of%20DNA.....pdf.txta182e9c7f01bbae2f7393e7b04a9c41eMD53icict/207862023-03-15 14:34:10.313oai:www.arca.fiocruz.br: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ório 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| dc.title.pt_BR.fl_str_mv |
Inhibition of DNA topoisomerase I activity and induction of apoptosis by thiazacridine derivatives |
| title |
Inhibition of DNA topoisomerase I activity and induction of apoptosis by thiazacridine derivatives |
| spellingShingle |
Inhibition of DNA topoisomerase I activity and induction of apoptosis by thiazacridine derivatives Barros, Francisco Washington Araujo Acridinas Tiazolidinas Tiazacridina DNA Topoisomerase I Apoptose Acridine Thiazolidine Thiazacridine DNA topoisomerase I Apoptosis |
| title_short |
Inhibition of DNA topoisomerase I activity and induction of apoptosis by thiazacridine derivatives |
| title_full |
Inhibition of DNA topoisomerase I activity and induction of apoptosis by thiazacridine derivatives |
| title_fullStr |
Inhibition of DNA topoisomerase I activity and induction of apoptosis by thiazacridine derivatives |
| title_full_unstemmed |
Inhibition of DNA topoisomerase I activity and induction of apoptosis by thiazacridine derivatives |
| title_sort |
Inhibition of DNA topoisomerase I activity and induction of apoptosis by thiazacridine derivatives |
| author |
Barros, Francisco Washington Araujo |
| author_facet |
Barros, Francisco Washington Araujo Bezerra, Daniel Pereira Ferreira, Paulo Michel Pereira Cavalcanti, Bruno Coelho Silva, Teresinha Gonçalves da Pitta, Marina Galdino da Rocha Lima, Maria do Carmo Alves de Galdino, Suely L Pitta, Ivan da Rocha Lotufo, Letícia Veras Costa Moraes Filho, Manoel Odorico de Burbano, Rommel Mario Rodríguez Guecheva, Temenouga Nikolova Henriques, João Antonio Pegas Pessoa, Cláudia do Ó |
| author_role |
author |
| author2 |
Bezerra, Daniel Pereira Ferreira, Paulo Michel Pereira Cavalcanti, Bruno Coelho Silva, Teresinha Gonçalves da Pitta, Marina Galdino da Rocha Lima, Maria do Carmo Alves de Galdino, Suely L Pitta, Ivan da Rocha Lotufo, Letícia Veras Costa Moraes Filho, Manoel Odorico de Burbano, Rommel Mario Rodríguez Guecheva, Temenouga Nikolova Henriques, João Antonio Pegas Pessoa, Cláudia do Ó |
| author2_role |
author author author author author author author author author author author author author author |
| dc.contributor.author.fl_str_mv |
Barros, Francisco Washington Araujo Bezerra, Daniel Pereira Ferreira, Paulo Michel Pereira Cavalcanti, Bruno Coelho Silva, Teresinha Gonçalves da Pitta, Marina Galdino da Rocha Lima, Maria do Carmo Alves de Galdino, Suely L Pitta, Ivan da Rocha Lotufo, Letícia Veras Costa Moraes Filho, Manoel Odorico de Burbano, Rommel Mario Rodríguez Guecheva, Temenouga Nikolova Henriques, João Antonio Pegas Pessoa, Cláudia do Ó |
| dc.subject.other.pt_BR.fl_str_mv |
Acridinas Tiazolidinas Tiazacridina DNA Topoisomerase I Apoptose |
| topic |
Acridinas Tiazolidinas Tiazacridina DNA Topoisomerase I Apoptose Acridine Thiazolidine Thiazacridine DNA topoisomerase I Apoptosis |
| dc.subject.en.pt_BR.fl_str_mv |
Acridine Thiazolidine Thiazacridine DNA topoisomerase I Apoptosis |
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Bezerra, Daniel Pereira “Documento produzido em parceria ou por autor vinculado à Fiocruz, mas não consta à informação no documento”. |
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2013 |
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2013 |
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2017-08-28T18:45:32Z |
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2017-08-28T18:45:32Z |
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info:eu-repo/semantics/publishedVersion |
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info:eu-repo/semantics/article |
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BARROS, F. W. A. et al. Inhibition of DNA topoisomerase I activity and induction of apoptosis by thiazacridine derivatives. Toxicology and Applied Pharmacology, v. 268, p. 37–46, 2013. |
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https://www.arca.fiocruz.br/handle/icict/20786 |
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0041-008X |
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10.1016/j.taap.2013.01.010 |
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BARROS, F. W. A. et al. Inhibition of DNA topoisomerase I activity and induction of apoptosis by thiazacridine derivatives. Toxicology and Applied Pharmacology, v. 268, p. 37–46, 2013. 0041-008X 10.1016/j.taap.2013.01.010 |
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