Selective cytotoxic and genotoxic activities of 5-(2-bromo-5-methoxybenzylidene)-thiazolidine-2,4-dione against NCI-H292 human lung carcinoma cells

Detalhes bibliográficos
Autor(a) principal: Rodrigues, Maria do D.
Data de Publicação: 2018
Outros Autores: Santiago, Priscila B. G. S., Marques, Karla M. R., Pereira, Valéria R. A., Castro, Maria C. A. B. de, Cantalice, Jeanne C. L. L., Silva, Teresinha G. da, Adam, Mônica L., Nascimento, Silene C. do, Albuquerque, Julianna F. C. de, Militao, Gardenia C. G.
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da FIOCRUZ (ARCA)
Texto Completo: https://www.arca.fiocruz.br/handle/icict/32942
Resumo: CNPq e FACEPE.
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spelling Rodrigues, Maria do D.Santiago, Priscila B. G. S.Marques, Karla M. R.Pereira, Valéria R. A.Castro, Maria C. A. B. deCantalice, Jeanne C. L. L.Silva, Teresinha G. daAdam, Mônica L.Nascimento, Silene C. doAlbuquerque, Julianna F. C. deMilitao, Gardenia C. G.2019-05-06T13:17:23Z2019-05-06T13:17:23Z2018RODRIGUES, M. do D. et al. Selective cytotoxic and genotoxic activities of 5-(2-bromo-5-methoxybenzylidene)-thiazolidine-2,4-dione against NCI-H292 human lung carcinoma cells. Pharmacological Reports, v. 70, n. 3, p. 446–454, 1 jun. 2018.1734-1140https://www.arca.fiocruz.br/handle/icict/3294210.1016/j.pharep.2017.11.008CNPq e FACEPE.Federal University of Pernambuco. Department of Antibiotics. Recife, PE, Brazil.Federal University of Pernambuco. Department of Antibiotics. Recife, PE, Brazil.Federal University of Pernambuco. Department of Antibiotics. Recife, PE, Brazil.Fundação Oswaldo Cruz. Instituto Aggeu Magalhães. Departamento de Imunologia. Recife, PE, Brasil.Fundação Oswaldo Cruz. Instituto Aggeu Magalhães. Departamento de Imunologia. Recife, PE, Brasil / Federal University of Pernambuco. Academic Center of Vitoria. Parasitology Laboratory. Recife, PE, Brazil.Federal University of Pernambuco. Department of Antibiotics. Recife, PE, Brazil.Federal University of Pernambuco. Department of Antibiotics. Recife, PE, Brazil.Federal University of Pernambuco. Academic Center of Victoria. Department of Biological Sciences. Recife, PE, Brazil.Federal University of Pernambuco. Department of Antibiotics. Recife, PE, Brazil.Federal University of Pernambuco. Department of Antibiotics. Recife, PE, Brazil.Federal University of Pernambuco. Department of Physiology and Pharmacology. Recife, PE, Brazil.BACKGROUND: Thiazolidine-2,4-dione ring system is used as a pharmacophore to build various heterocyclic compounds aimed to interact with biological targets. In the present study, benzylidene-2,4-thiazolidinedione derivatives (compounds 2-5) were synthesized and screened against cancer cell lines and the genotoxicity and cytotoxicity of the most active compound (5) was investigated on normal and lung cancer cell line. METHODS: For in vitro cytotoxic screening, the MTT assay was used for HL60 and K562 (leukemia), MCF-7 (breast adenocarcinoma), HT29 (colon adenocarcinoma), HEp-2 (cervix carcinoma) and NCI-H292 (lung carcinoma) tumor cell lines and Alamar-blue assay was used for non-tumor cells (PBMC, human peripheral blood mononuclear cells) were used. Cell morphology was visualized after Giemsa-May-Grunwald staining. DNA content, phosphatidylserine externalization and mitochondrial depolarization were measured by flow cytometry. Genotoxicity was assessed by Comet assay. RESULTS: 5-(2-Bromo-5-methoxybenzylidene)-thiazolidine-2,4-dione (5) presented the most potent cytotoxicity, especially against NCI-H292 lung cancer cell line, with IC50 value of 1.26μg/mL after 72h incubation. None of the compounds were cytotoxic to PBMC. After 48h incubation, externalization of phosphatidylserine, mitochondrial depolarization, internucleosomal DNA fragmentation and morphological alterations consistent with apoptosis were observed in NCI-H292 cells treated with compound (5). In addition, compound (5) also induced genotoxicity in NCI-H292 cells (2.8-fold increase in damage index compared to the negative control), but not in PBMC. CONCLUSION: Compound 5 presented selective cytotoxic and genotoxic activity against pulmonary carcinoma (NCI-H292 cells).engSelective cytotoxic and genotoxic activities of 5-(2-bromo-5-methoxybenzylidene)-thiazolidine-2,4-dione against NCI-H292 human lung carcinoma cellsinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleCytotoxicityGenotoxicity5-Benzylidene-2,4-thiazolidinedioneLungcancerAntineoplásicos / farmacologiaApoptose / efeitos de drogasLinha Celular, TumorEnsaio Cometa / métodosCitotoxinas / farmacologiaFragmentação de DNA / efeitos de drogasCélulas HL-60HumanosCélulas K562Leucócitos Mononucleares / efeitos de drogasNeoplasias Pulmonares / quimioterapiaCélulas MCF-7Mutagénicos / farmacologiaTiazolidinedionas / farmacologiainfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txtlicense.txttext/plain; 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dc.title.pt_BR.fl_str_mv Selective cytotoxic and genotoxic activities of 5-(2-bromo-5-methoxybenzylidene)-thiazolidine-2,4-dione against NCI-H292 human lung carcinoma cells
title Selective cytotoxic and genotoxic activities of 5-(2-bromo-5-methoxybenzylidene)-thiazolidine-2,4-dione against NCI-H292 human lung carcinoma cells
spellingShingle Selective cytotoxic and genotoxic activities of 5-(2-bromo-5-methoxybenzylidene)-thiazolidine-2,4-dione against NCI-H292 human lung carcinoma cells
Rodrigues, Maria do D.
Cytotoxicity
Genotoxicity
5-Benzylidene-2,4-thiazolidinedione
Lungcancer
Antineoplásicos / farmacologia
Apoptose / efeitos de drogas
Linha Celular, Tumor
Ensaio Cometa / métodos
Citotoxinas / farmacologia
Fragmentação de DNA / efeitos de drogas
Células HL-60
Humanos
Células K562
Leucócitos Mononucleares / efeitos de drogas
Neoplasias Pulmonares / quimioterapia
Células MCF-7
Mutagénicos / farmacologia
Tiazolidinedionas / farmacologia
title_short Selective cytotoxic and genotoxic activities of 5-(2-bromo-5-methoxybenzylidene)-thiazolidine-2,4-dione against NCI-H292 human lung carcinoma cells
title_full Selective cytotoxic and genotoxic activities of 5-(2-bromo-5-methoxybenzylidene)-thiazolidine-2,4-dione against NCI-H292 human lung carcinoma cells
title_fullStr Selective cytotoxic and genotoxic activities of 5-(2-bromo-5-methoxybenzylidene)-thiazolidine-2,4-dione against NCI-H292 human lung carcinoma cells
title_full_unstemmed Selective cytotoxic and genotoxic activities of 5-(2-bromo-5-methoxybenzylidene)-thiazolidine-2,4-dione against NCI-H292 human lung carcinoma cells
title_sort Selective cytotoxic and genotoxic activities of 5-(2-bromo-5-methoxybenzylidene)-thiazolidine-2,4-dione against NCI-H292 human lung carcinoma cells
author Rodrigues, Maria do D.
author_facet Rodrigues, Maria do D.
Santiago, Priscila B. G. S.
Marques, Karla M. R.
Pereira, Valéria R. A.
Castro, Maria C. A. B. de
Cantalice, Jeanne C. L. L.
Silva, Teresinha G. da
Adam, Mônica L.
Nascimento, Silene C. do
Albuquerque, Julianna F. C. de
Militao, Gardenia C. G.
author_role author
author2 Santiago, Priscila B. G. S.
Marques, Karla M. R.
Pereira, Valéria R. A.
Castro, Maria C. A. B. de
Cantalice, Jeanne C. L. L.
Silva, Teresinha G. da
Adam, Mônica L.
Nascimento, Silene C. do
Albuquerque, Julianna F. C. de
Militao, Gardenia C. G.
author2_role author
author
author
author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv Rodrigues, Maria do D.
Santiago, Priscila B. G. S.
Marques, Karla M. R.
Pereira, Valéria R. A.
Castro, Maria C. A. B. de
Cantalice, Jeanne C. L. L.
Silva, Teresinha G. da
Adam, Mônica L.
Nascimento, Silene C. do
Albuquerque, Julianna F. C. de
Militao, Gardenia C. G.
dc.subject.en.pt_BR.fl_str_mv Cytotoxicity
Genotoxicity
5-Benzylidene-2,4-thiazolidinedione
Lungcancer
topic Cytotoxicity
Genotoxicity
5-Benzylidene-2,4-thiazolidinedione
Lungcancer
Antineoplásicos / farmacologia
Apoptose / efeitos de drogas
Linha Celular, Tumor
Ensaio Cometa / métodos
Citotoxinas / farmacologia
Fragmentação de DNA / efeitos de drogas
Células HL-60
Humanos
Células K562
Leucócitos Mononucleares / efeitos de drogas
Neoplasias Pulmonares / quimioterapia
Células MCF-7
Mutagénicos / farmacologia
Tiazolidinedionas / farmacologia
dc.subject.decs.pt_BR.fl_str_mv Antineoplásicos / farmacologia
Apoptose / efeitos de drogas
Linha Celular, Tumor
Ensaio Cometa / métodos
Citotoxinas / farmacologia
Fragmentação de DNA / efeitos de drogas
Células HL-60
Humanos
Células K562
Leucócitos Mononucleares / efeitos de drogas
Neoplasias Pulmonares / quimioterapia
Células MCF-7
Mutagénicos / farmacologia
Tiazolidinedionas / farmacologia
description CNPq e FACEPE.
publishDate 2018
dc.date.issued.fl_str_mv 2018
dc.date.accessioned.fl_str_mv 2019-05-06T13:17:23Z
dc.date.available.fl_str_mv 2019-05-06T13:17:23Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
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status_str publishedVersion
dc.identifier.citation.fl_str_mv RODRIGUES, M. do D. et al. Selective cytotoxic and genotoxic activities of 5-(2-bromo-5-methoxybenzylidene)-thiazolidine-2,4-dione against NCI-H292 human lung carcinoma cells. Pharmacological Reports, v. 70, n. 3, p. 446–454, 1 jun. 2018.
dc.identifier.uri.fl_str_mv https://www.arca.fiocruz.br/handle/icict/32942
dc.identifier.issn.pt_BR.fl_str_mv 1734-1140
dc.identifier.doi.none.fl_str_mv 10.1016/j.pharep.2017.11.008
identifier_str_mv RODRIGUES, M. do D. et al. Selective cytotoxic and genotoxic activities of 5-(2-bromo-5-methoxybenzylidene)-thiazolidine-2,4-dione against NCI-H292 human lung carcinoma cells. Pharmacological Reports, v. 70, n. 3, p. 446–454, 1 jun. 2018.
1734-1140
10.1016/j.pharep.2017.11.008
url https://www.arca.fiocruz.br/handle/icict/32942
dc.language.iso.fl_str_mv eng
language eng
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.source.none.fl_str_mv reponame:Repositório Institucional da FIOCRUZ (ARCA)
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instacron:FIOCRUZ
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instacron_str FIOCRUZ
institution FIOCRUZ
reponame_str Repositório Institucional da FIOCRUZ (ARCA)
collection Repositório Institucional da FIOCRUZ (ARCA)
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