Avaliação da atividade biológica de triazenos inéditos complexados com Au(I)
Autor(a) principal: | |
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Data de Publicação: | 2013 |
Tipo de documento: | Dissertação |
Idioma: | por |
Título da fonte: | Biblioteca Digital de Teses e Dissertações do UFSM |
Texto Completo: | http://repositorio.ufsm.br/handle/1/6012 |
Resumo: | The Triazenes are compounds with proven antibacterial and cytotoxic activity. Variations in the chemical structure such as complexation with metals like gold (I) can confer different biological activities. The antineoplastic temozolomide and dacarbazine are examples of commercially available triazenes used in the treatment of solid tumors and acute leukemias. In this study, the following compounds were synthesized triazenes complexed with novel gold (I): 1) [1,3-Bis (2-fluorophenyl) triazenido] (triphenylphosphine) gold (I); 2) [1,3-Bis (2- chlorophenyl) triazenido] (triphenylphosphine) gold (I) 3) [1,3-Bis (2-bromophenyl) triazenido] (triphenylphosphine) gold (I), 4) [1,3-Bis (2-iodophenyl) triazenido] (triphenylphosphine ) gold (I). Cytotoxicity of these compounds was evaluated by the MTT colorimetric assay of cell culture effecting bone marrow of patients with different types of leukemia, in addition to controlling patient without the disease. For the analysis of the antimicrobial activity was utilized quantitative methodology of microdilution with the determination of minimum inhibitory concentration (MIC). To determine the activity of nuclease cleavage assays were performed in double-stranded plasmid DNA using the method of electrophoresis in agarose gel. The results showed a considerable activity against different types of leukemia (acute myeloid leukemia, chronic myeloid leukemia, acute lymphoblastic leukemia, chronic lymphocytic leukemia) with a small IC50 value of 0.0057 μmol mL-1 for compound 4 in cells of acute myeloid leukemia, all the active compounds in different types of leukemia but not so selective. The antibacterial activity was higher against gram-positive bacteria mainly in different strains of Staphylococcus aureus (MIC value of equal to 16 ug/ml). Any of the four compounds analyzed in this study was able to cleave the plasmid DNA. Thus, all tested triazenes have biological potential, or may be the subject of further studies as alternatives to anticancer and antimicrobial drugs existent. |
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2015-10-272015-10-272013-03-22KEMPFER, Cláudia Barbisan. EVALUATION OF BIOLOGICAL ACTIVITY OF UNPUBLISHED TRIAZENES COMPLEXED WITH Au (I). 2013. 86 f. Dissertação (Mestrado em Farmacologia) - Universidade Federal de Santa Maria, Santa Maria, 2013.http://repositorio.ufsm.br/handle/1/6012The Triazenes are compounds with proven antibacterial and cytotoxic activity. Variations in the chemical structure such as complexation with metals like gold (I) can confer different biological activities. The antineoplastic temozolomide and dacarbazine are examples of commercially available triazenes used in the treatment of solid tumors and acute leukemias. In this study, the following compounds were synthesized triazenes complexed with novel gold (I): 1) [1,3-Bis (2-fluorophenyl) triazenido] (triphenylphosphine) gold (I); 2) [1,3-Bis (2- chlorophenyl) triazenido] (triphenylphosphine) gold (I) 3) [1,3-Bis (2-bromophenyl) triazenido] (triphenylphosphine) gold (I), 4) [1,3-Bis (2-iodophenyl) triazenido] (triphenylphosphine ) gold (I). Cytotoxicity of these compounds was evaluated by the MTT colorimetric assay of cell culture effecting bone marrow of patients with different types of leukemia, in addition to controlling patient without the disease. For the analysis of the antimicrobial activity was utilized quantitative methodology of microdilution with the determination of minimum inhibitory concentration (MIC). To determine the activity of nuclease cleavage assays were performed in double-stranded plasmid DNA using the method of electrophoresis in agarose gel. The results showed a considerable activity against different types of leukemia (acute myeloid leukemia, chronic myeloid leukemia, acute lymphoblastic leukemia, chronic lymphocytic leukemia) with a small IC50 value of 0.0057 μmol mL-1 for compound 4 in cells of acute myeloid leukemia, all the active compounds in different types of leukemia but not so selective. The antibacterial activity was higher against gram-positive bacteria mainly in different strains of Staphylococcus aureus (MIC value of equal to 16 ug/ml). Any of the four compounds analyzed in this study was able to cleave the plasmid DNA. Thus, all tested triazenes have biological potential, or may be the subject of further studies as alternatives to anticancer and antimicrobial drugs existent.Os triazenos são compostos com comprovada atividade citotóxica e antibacteriana. Variações na sua estrutura química, como por exemplo a complexação com metais como o ouro (I), podem lhe conferir diferenciadas atividades biológicas. Os antineoplásicos dacarbazina e temozolomida constituem exemplos de triazenos disponíveis comercialmente utilizados no tratamento de tumores sólidos e leucemias agudas. Neste estudo foram sintetizados os seguintes compostos triazenos inéditos complexados com ouro (I): 1) [1,3- Bis(2-fluorofenil)triazenido](trifenilfosfina)ouro(I); 2) [1,3-Bis(2 clorofenil)triazenido] (trifenilfosfina)ouro(I); 3) [1,3-Bis(2-bromofenil)triazenido](trifenilfosfina)ouro(I); 4) [1,3- Bis(2 iodofenil)triazenido](trifenilfosfina)ouro(I). A citotoxicidade desses compostos foi avaliada através do ensaio colorimétrico do MTT efetuando cultura de células de medula óssea de pacientes com diferentes tipos de leucemias, além de paciente controle, sem a doença. Para a análise da atividade antimicrobiana foi utilizada a metodologia quantitativa da microdiluição em caldo com a determinação da concentração inibitória mínima (CIM). Para a determinação da atividade de nuclease foram efetuados ensaios de clivagem do DNA plasmidial fita dupla utilizando a metodologia de eletroforese em gel de agarose. Os resultados mostraram uma considerável atividade frente a diferentes tipos de leucemias (leucemia mielóide aguda, leucemia mielóide crônica, leucemia linfóide aguda, leucemia linfóide crônica) com um pequeno valor de IC50 de 0,0057 μmol mL-1 para o composto 4 em células de leucemia mielóide aguda, sendo todos os compostos ativos em diferentes tipos de leucemias, porém de forma não seletiva. A maior atividade antibacteriana foi frente a bactérias gram-positivas principalmente em diferentes cepas de Staphylococcus aureus (com valor de CIM igual a 16 ug/mL). Nenhum dos 4 compostos analisados nesse estudo conseguiu clivar o DNA plasmidial. Desta forma, todos os triazenos testados possuem potencial biológico, ou seja, podem ser objeto de mais estudos como alternativas aos fármacos antimicrobianos e antineoplásicos existentes.Conselho Nacional de Desenvolvimento Científico e Tecnológicoapplication/pdfporUniversidade Federal de Santa MariaPrograma de Pós-Graduação em Ciências FarmacêuticasUFSMBRAnálises Clínicas e ToxicológicasTriazenosOuroCitotoxicidadeS. aureusLeucemiaTriazenesGoldCytotoxicityS. aureusLeukemiaCNPQ::CIENCIAS DA SAUDE::FARMACIAAvaliação da atividade biológica de triazenos inéditos complexados com Au(I)Evaluation of biological activity of unpublished triazenes complexed with Au (I)info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisHorner, Rosmarihttp://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4707613Z5Krause, Luciana Maria Fontanarihttp://lattes.cnpq.br/9844890896121847Cóser, Virgínia Mariahttp://lattes.cnpq.br/4601008307298787http://lattes.cnpq.br/0787981293432612Kempfer, Cláudia Barbisan2010000000004003003003003005fdaffc5-abc5-4607-8952-fc5c4760b00432556794-40ea-47e1-88dc-2c2d0fd2531ca310dec0-114a-4a8c-836d-d08756d18299ce77d84d-25c9-4b42-90be-7a829ae7f940info:eu-repo/semantics/openAccessreponame:Biblioteca Digital de Teses e Dissertações do UFSMinstname:Universidade Federal de Santa Maria (UFSM)instacron:UFSMORIGINALKEMPFER, CLAUDIA BARBISAN.pdfapplication/pdf2695915http://repositorio.ufsm.br/bitstream/1/6012/1/KEMPFER%2c%20CLAUDIA%20BARBISAN.pdff2ae0495e4ce24854c5ffe672c3fb64bMD51TEXTKEMPFER, CLAUDIA BARBISAN.pdf.txtKEMPFER, CLAUDIA BARBISAN.pdf.txtExtracted texttext/plain164555http://repositorio.ufsm.br/bitstream/1/6012/2/KEMPFER%2c%20CLAUDIA%20BARBISAN.pdf.txt7c9490f99f94209df2ddddfe71086b73MD52THUMBNAILKEMPFER, CLAUDIA BARBISAN.pdf.jpgKEMPFER, CLAUDIA BARBISAN.pdf.jpgIM Thumbnailimage/jpeg4975http://repositorio.ufsm.br/bitstream/1/6012/3/KEMPFER%2c%20CLAUDIA%20BARBISAN.pdf.jpg6041bfc696f8102fb97978fe4d019c7eMD531/60122022-10-14 16:12:14.172oai:repositorio.ufsm.br:1/6012Biblioteca Digital de Teses e Dissertaçõeshttps://repositorio.ufsm.br/ONGhttps://repositorio.ufsm.br/oai/requestatendimento.sib@ufsm.br||tedebc@gmail.comopendoar:2022-10-14T19:12:14Biblioteca Digital de Teses e Dissertações do UFSM - Universidade Federal de Santa Maria (UFSM)false |
dc.title.por.fl_str_mv |
Avaliação da atividade biológica de triazenos inéditos complexados com Au(I) |
dc.title.alternative.eng.fl_str_mv |
Evaluation of biological activity of unpublished triazenes complexed with Au (I) |
title |
Avaliação da atividade biológica de triazenos inéditos complexados com Au(I) |
spellingShingle |
Avaliação da atividade biológica de triazenos inéditos complexados com Au(I) Kempfer, Cláudia Barbisan Triazenos Ouro Citotoxicidade S. aureus Leucemia Triazenes Gold Cytotoxicity S. aureus Leukemia CNPQ::CIENCIAS DA SAUDE::FARMACIA |
title_short |
Avaliação da atividade biológica de triazenos inéditos complexados com Au(I) |
title_full |
Avaliação da atividade biológica de triazenos inéditos complexados com Au(I) |
title_fullStr |
Avaliação da atividade biológica de triazenos inéditos complexados com Au(I) |
title_full_unstemmed |
Avaliação da atividade biológica de triazenos inéditos complexados com Au(I) |
title_sort |
Avaliação da atividade biológica de triazenos inéditos complexados com Au(I) |
author |
Kempfer, Cláudia Barbisan |
author_facet |
Kempfer, Cláudia Barbisan |
author_role |
author |
dc.contributor.advisor1.fl_str_mv |
Horner, Rosmari |
dc.contributor.advisor1Lattes.fl_str_mv |
http://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4707613Z5 |
dc.contributor.referee1.fl_str_mv |
Krause, Luciana Maria Fontanari |
dc.contributor.referee1Lattes.fl_str_mv |
http://lattes.cnpq.br/9844890896121847 |
dc.contributor.referee2.fl_str_mv |
Cóser, Virgínia Maria |
dc.contributor.referee2Lattes.fl_str_mv |
http://lattes.cnpq.br/4601008307298787 |
dc.contributor.authorLattes.fl_str_mv |
http://lattes.cnpq.br/0787981293432612 |
dc.contributor.author.fl_str_mv |
Kempfer, Cláudia Barbisan |
contributor_str_mv |
Horner, Rosmari Krause, Luciana Maria Fontanari Cóser, Virgínia Maria |
dc.subject.por.fl_str_mv |
Triazenos Ouro Citotoxicidade S. aureus Leucemia |
topic |
Triazenos Ouro Citotoxicidade S. aureus Leucemia Triazenes Gold Cytotoxicity S. aureus Leukemia CNPQ::CIENCIAS DA SAUDE::FARMACIA |
dc.subject.eng.fl_str_mv |
Triazenes Gold Cytotoxicity S. aureus Leukemia |
dc.subject.cnpq.fl_str_mv |
CNPQ::CIENCIAS DA SAUDE::FARMACIA |
description |
The Triazenes are compounds with proven antibacterial and cytotoxic activity. Variations in the chemical structure such as complexation with metals like gold (I) can confer different biological activities. The antineoplastic temozolomide and dacarbazine are examples of commercially available triazenes used in the treatment of solid tumors and acute leukemias. In this study, the following compounds were synthesized triazenes complexed with novel gold (I): 1) [1,3-Bis (2-fluorophenyl) triazenido] (triphenylphosphine) gold (I); 2) [1,3-Bis (2- chlorophenyl) triazenido] (triphenylphosphine) gold (I) 3) [1,3-Bis (2-bromophenyl) triazenido] (triphenylphosphine) gold (I), 4) [1,3-Bis (2-iodophenyl) triazenido] (triphenylphosphine ) gold (I). Cytotoxicity of these compounds was evaluated by the MTT colorimetric assay of cell culture effecting bone marrow of patients with different types of leukemia, in addition to controlling patient without the disease. For the analysis of the antimicrobial activity was utilized quantitative methodology of microdilution with the determination of minimum inhibitory concentration (MIC). To determine the activity of nuclease cleavage assays were performed in double-stranded plasmid DNA using the method of electrophoresis in agarose gel. The results showed a considerable activity against different types of leukemia (acute myeloid leukemia, chronic myeloid leukemia, acute lymphoblastic leukemia, chronic lymphocytic leukemia) with a small IC50 value of 0.0057 μmol mL-1 for compound 4 in cells of acute myeloid leukemia, all the active compounds in different types of leukemia but not so selective. The antibacterial activity was higher against gram-positive bacteria mainly in different strains of Staphylococcus aureus (MIC value of equal to 16 ug/ml). Any of the four compounds analyzed in this study was able to cleave the plasmid DNA. Thus, all tested triazenes have biological potential, or may be the subject of further studies as alternatives to anticancer and antimicrobial drugs existent. |
publishDate |
2013 |
dc.date.issued.fl_str_mv |
2013-03-22 |
dc.date.accessioned.fl_str_mv |
2015-10-27 |
dc.date.available.fl_str_mv |
2015-10-27 |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/masterThesis |
format |
masterThesis |
status_str |
publishedVersion |
dc.identifier.citation.fl_str_mv |
KEMPFER, Cláudia Barbisan. EVALUATION OF BIOLOGICAL ACTIVITY OF UNPUBLISHED TRIAZENES COMPLEXED WITH Au (I). 2013. 86 f. Dissertação (Mestrado em Farmacologia) - Universidade Federal de Santa Maria, Santa Maria, 2013. |
dc.identifier.uri.fl_str_mv |
http://repositorio.ufsm.br/handle/1/6012 |
identifier_str_mv |
KEMPFER, Cláudia Barbisan. EVALUATION OF BIOLOGICAL ACTIVITY OF UNPUBLISHED TRIAZENES COMPLEXED WITH Au (I). 2013. 86 f. Dissertação (Mestrado em Farmacologia) - Universidade Federal de Santa Maria, Santa Maria, 2013. |
url |
http://repositorio.ufsm.br/handle/1/6012 |
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Universidade Federal de Santa Maria |
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UFSM |
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Análises Clínicas e Toxicológicas |
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Universidade Federal de Santa Maria |
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