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AutorPinto, Mauro Cunha Xavier
AutorDias, Danielle Ferreira
AutorDel Puerto, Helen Lima
AutorMartins, Almir de Sousa
AutorCarvalho, Andréa Teixeira
AutorMartins Filho, Olindo Assis
AutorBadet, Bernard
AutorDurand, Philippe
AutorAlves, Ricardo José
AutorFagundes, Elaine Maria de Souza
Fecha de acceso2014-11-28T13:36:12Z
Fecha de disponibilización2014-11-28T13:36:12Z
Fecha de publicación2011
ReferenciaPINTO, Mauro Cunha Xavier et al. Discovery of cytotoxic and pro-apoptotic compounds against leukemia cells: Tert-butyl-4-[(3-nitrophenoxy) methyl]-2,2-dimethyloxazolidine-3-carboxylate. LIFE SCI, v. 89, n. 21-22, p. 786-794, 2011.pt_BR
ISSN0024-3205
ISSN10.1016/j.lfs.2011.09.012
URIhttps://www.arca.fiocruz.br/handle/icict/9000
Idiomaengpt_BR
EditorElsevierpt_BR
Derechos de autoropen accesspt_BR
TítuloDiscovery of cytotoxic and pro-apoptotic compounds against leukemia cells: Tert-butyl-4-[(3-nitrophenoxy) methyl]-2,2-dimethyloxazolidine-3-carboxylatept_BR
Tipo del documentoArticlept_BR
Resumen en InglésAims: We evaluated biological activity in leukemia cells lines of R and S enantiomers of tert-butyl 4-[(3-nitrophenoxy)-methyl]-2,2-dimethyloxazolidine-3-carboxylate (BNDC). Main methods: Cytotoxic activity was assessed by MTT assay. Flow cytometry assays were used to determined DNA fragmentation (Propidium Iodide-PI staining) and phosphatidylserine exposure (Annexin-V and PI staining). DNA condensation was evaluated by fluorescence microscopy using double-staining in leukemia cells (Hoechst and PI). Caspase activities were measured using Z-VAD-FMK, a non-selective caspase inhibitor, by flow cytometry and Z-DEVD-AMC, a selective caspase-3 substrate, by fluorescence spectrometry. Key findings: Both enantiomers displayed cytotoxic activity against leukemia cell lines (HL60, HL60.Bcl-2, HL60.Bcl-XL and Jurkat) with low toxicity against human peripheral blood mononuclear cell — PBMC based on IC50values. In HL60 cell lines, compounds induce exposure of phosphatidylserine and DNA fragmentation, which could be blocked by pretreatment of cells with Z-VAD-FMK. Confirming this observation, both enantiomers induced caspase-3 activation. Additional analysis revealed an increased percentage of apoptotic cells (defined as those with fragmented nuclei and condensed chromatin) after treatment with compounds. Significance: Taken together, the results indicate that BNDC compounds exhibited cytotoxic and pro-apoptotic activities and have a potential for developing a new class of anticancer drugs.pt_BR
AfiliaciónUniversidade Federal de Minas Gerais. Instituto de Ciências Biológicas. Belo Horizonte, MG, Brasilpt_BR
AfiliaciónUniversidade Federal de Minas Gerais. Faculdade de Farmácia. Belo Horizonte, MG, Brasilpt_BR
AfiliaciónUniversidade Federal de Minas Gerais. Instituto de Ciências Biológicas. Belo Horizonte, MG, Brasilpt_BR
AfiliaciónUniversidade Federal de Minas Gerais. Instituto de Ciências Biológicas. Belo Horizonte, MG, Brasilpt_BR
AfiliaciónFundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Belo Horizonte, MG, Brasilpt_BR
AfiliaciónFundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Belo Horizonte, MG, Brasilpt_BR
AfiliaciónInstitut de Chimie des Substances Naturelles-CNRS. Gif-sur-Yvette, Francept_BR
AfiliaciónInstitut de Chimie des Substances Naturelles-CNRS. Gif-sur-Yvette, Francept_BR
AfiliaciónUniversidade Federal de Minas Gerais. Faculdade de Farmácia. Belo Horizonte, MG, Brasilpt_BR
AfiliaciónUniversidade Federal de Minas Gerais. Instituto de Ciências Biológicas. Belo Horizonte, MG, Brasilpt_BR
Palavras clave en InglêsApoptosispt_BR
Palavras clave en InglêsDrug discoverypt_BR
Palavras clave en InglêsHit compoundpt_BR
Palavras clave en InglêsScaffoldpt_BR
Palavras clave en InglêsAnti-cancerpt_BR


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