Avaliação das atividades citotóxica e antibacteriana de compostos triazenos

Detalhes bibliográficos
Ano de defesa: 2013
Autor(a) principal: Sousa, Liliana Urdangarin de
Orientador(a): Não Informado pela instituição
Banca de defesa: Não Informado pela instituição
Tipo de documento: Dissertação
Tipo de acesso: Acesso aberto
dARK ID: ark:/26339/00130000097t2
Idioma: por
Instituição de defesa: Universidade Federal de Santa Maria
BR
Farmacologia
UFSM
Programa de Pós-Graduação em Ciências Farmacêuticas
Programa de Pós-Graduação: Não Informado pela instituição
Departamento: Não Informado pela instituição
País: Não Informado pela instituição
Palavras-chave em Português:
Link de acesso: http://repositorio.ufsm.br/handle/1/6009
Resumo: Neoplasms are a major cause of death worldwide and have been worrying about the medical and scientific community, as most anticancer vector does not act on cancer cells, triggering numerous side-effects and, in some cases, resistance to treatment. No less worrying is the resistance acquired by bacteria, which culminate in strains with the phenomenon of multi-drug resistance commercially available. In this context, many research groups that adopted the medicinal chemistry, turn their studies to the discovery of new molecules that may be more selective therapeutic approaches with fewer side effects than currently exist. Triazenes compounds represent a class of compounds having wide versatility with proven pharmacological antimicrobial and antitumor activities. Similarly, considering the results from several studies relevant complexes of palladium (II) have been considered as promising therapeutic agents. As a result, two novel compounds were synthesized, and a binder, and a triazene triazenido complex with palladium (II), which according to the IUPAC nomenclature rules were so named, respectively: 1,3-Bis(4-sulfonamidephenyl)triazene (1) and {trans-Bis-[1,3-bis-(4sulfonamidephenyl)triazenide]bis(piridine)palladium(II)}{piridine)4palladium(II)} {potassim(I)}.water (2). We assess the cytotoxic potential of such compounds by colorimetric assay bromide 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT). Mononuclear cells from different types of leukemia and control samples were incubated for 24 hours with the compounds at concentrations 12.5, 50 and 100 μmol mL-1. To examine the antimicrobial activity of the compounds we used the measurement method of broth microdilution by determining the minimum inhibitory concentration (MIC) against the gram positive and gram negative bacteria. The results showed that the compounds showed significant cytotoxicity in the tested samples, but the compound 2 had lower IC50 than 1. Significant differences were observed between the compounds in the samples of CML and at concentrations 12,5 e 50 μmol mL-1. The antibacterial activity was found narrow spectrum, focused on gram-positive strains.
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spelling Avaliação das atividades citotóxica e antibacteriana de compostos triazenosActivities evaluation cytotoxic and antibacterial of compound triazenesTriazenosPaládioCitotoxicidadeAtividade antibacterianaLeucemiaTriazenesPalladiumAntibacterial activityLeukemiaCytotoxicityCNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIANeoplasms are a major cause of death worldwide and have been worrying about the medical and scientific community, as most anticancer vector does not act on cancer cells, triggering numerous side-effects and, in some cases, resistance to treatment. No less worrying is the resistance acquired by bacteria, which culminate in strains with the phenomenon of multi-drug resistance commercially available. In this context, many research groups that adopted the medicinal chemistry, turn their studies to the discovery of new molecules that may be more selective therapeutic approaches with fewer side effects than currently exist. Triazenes compounds represent a class of compounds having wide versatility with proven pharmacological antimicrobial and antitumor activities. Similarly, considering the results from several studies relevant complexes of palladium (II) have been considered as promising therapeutic agents. As a result, two novel compounds were synthesized, and a binder, and a triazene triazenido complex with palladium (II), which according to the IUPAC nomenclature rules were so named, respectively: 1,3-Bis(4-sulfonamidephenyl)triazene (1) and {trans-Bis-[1,3-bis-(4sulfonamidephenyl)triazenide]bis(piridine)palladium(II)}{piridine)4palladium(II)} {potassim(I)}.water (2). We assess the cytotoxic potential of such compounds by colorimetric assay bromide 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT). Mononuclear cells from different types of leukemia and control samples were incubated for 24 hours with the compounds at concentrations 12.5, 50 and 100 μmol mL-1. To examine the antimicrobial activity of the compounds we used the measurement method of broth microdilution by determining the minimum inhibitory concentration (MIC) against the gram positive and gram negative bacteria. The results showed that the compounds showed significant cytotoxicity in the tested samples, but the compound 2 had lower IC50 than 1. Significant differences were observed between the compounds in the samples of CML and at concentrations 12,5 e 50 μmol mL-1. The antibacterial activity was found narrow spectrum, focused on gram-positive strains.As neoplasias constituem uma das principais causas de morte no mundo e vêm preocupando a comunidade médica e científica, visto que a maioria dos antineoplásicos não age de forma vetorizada nas células cancerosas, desencadeando inúmeros efeitos colateriais e, em determinados casos, refratariedade ao tratamento. Não menos preocupante, são as resistências adquiridas pelas bactérias, as quais culminam em cepas com fenômeno de multirresistência aos fármacos disponíveis comercialmente. Neste contexto, muitos grupos de pesquisas os quais adotam a química medicinal, voltam seus estudos para a descoberta de novas moléculas que possam constituir abordagens terapêuticas mais seletivas e com menos efeitos colaterais que as existentes atualmente. Os compostos triazenos representam uma classe de compostos com ampla versatilidade farmacológica com comprovadas atividades antitumorais e antimicrobianas. De maneira semelhante, considerando os resultados de vários estudos relevantes, complexos de Paládio(II) vêm sendo considerados como promissores agentes terapêuticos. Em vista disso, foram sintetizados dois compostos inéditos, sendo um ligante triazeno e um complexo triazenido com paládio(II), os quais de acordo com as normas de nomenclatura da IUPAC, foram assim denominados, respectivamente: 1,3-Bis(4-sulfonamidafenil)triazeno (1) e {trans-bis-[1,3-bis-(4-sulfonamidafenil)triazenido-κN1]bis(piridina κN -)paládio(II)}{tetra(piridina- κN)paládio(II)}bis(potássio)}·monohidratado (2). Avaliamos o potencial citotóxico desses compostos através do ensaio colorimétrico com brometo de 3-(4,5-dimetiltiazol-2-il)-2,5-difeniltetrazólio (MTT). As células mononucleares de diferentes tipos de leucemia e a amostra controle, foram incubadas durante 24 horas com os compostos nas concentrações 12,5, 50 e 100 μmol mL-1. Para analisar a atividade antimicrobiana dos compostos, utilizou-se a metodologia quantitativa microdiluição em caldo, com a determinação da concentração inibitória mínima (CIM), frente à bactérias gram positivas e gram negativas. Os resultados demonstraram que os compostos apresentaram citotoxicidade importante nas amostras testadas, porém o composto 2 obteve menores IC50 que o 1. Diferenças significativas entre os compostos foram observadas nas amostras de LMC e nas concentrações 12,5 e 50 μmol mL-1. A atividade antibacteriana encontrada foi de estreito espectro, voltada às cepas gram positivas.Universidade Federal de Santa MariaBRFarmacologiaUFSMPrograma de Pós-Graduação em Ciências FarmacêuticasHorner, Rosmarihttp://lattes.cnpq.br/5907084134183708Rodrigues Junior, Luiz Carloshttp://lattes.cnpq.br/6354567436180190Cóser, Virgínia Mariahttp://lattes.cnpq.br/4601008307298787Sousa, Liliana Urdangarin de2015-10-262015-10-262013-12-13info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisapplication/pdfapplication/pdfSOUSA, Liliana Urdangarin de. ACTIVITIES EVALUATION CYTOTOXIC AND ANTIBACTERIAL OF COMPOUND TRIAZENES. 2013. 80 f. Dissertação (Mestrado em Farmacologia) - Universidade Federal de Santa Maria, Santa Maria, 2013.http://repositorio.ufsm.br/handle/1/6009ark:/26339/00130000097t2porinfo:eu-repo/semantics/openAccessreponame:Manancial - Repositório Digital da UFSMinstname:Universidade Federal de Santa Maria (UFSM)instacron:UFSM2022-08-17T12:44:04Zoai:repositorio.ufsm.br:1/6009Biblioteca Digital de Teses e Dissertaçõeshttps://repositorio.ufsm.br/PUBhttps://repositorio.ufsm.br/oai/requestatendimento.sib@ufsm.br||tedebc@gmail.com||manancial@ufsm.bropendoar:2022-08-17T12:44:04Manancial - Repositório Digital da UFSM - Universidade Federal de Santa Maria (UFSM)false
dc.title.none.fl_str_mv Avaliação das atividades citotóxica e antibacteriana de compostos triazenos
Activities evaluation cytotoxic and antibacterial of compound triazenes
title Avaliação das atividades citotóxica e antibacteriana de compostos triazenos
spellingShingle Avaliação das atividades citotóxica e antibacteriana de compostos triazenos
Sousa, Liliana Urdangarin de
Triazenos
Paládio
Citotoxicidade
Atividade antibacteriana
Leucemia
Triazenes
Palladium
Antibacterial activity
Leukemia
Cytotoxicity
CNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIA
title_short Avaliação das atividades citotóxica e antibacteriana de compostos triazenos
title_full Avaliação das atividades citotóxica e antibacteriana de compostos triazenos
title_fullStr Avaliação das atividades citotóxica e antibacteriana de compostos triazenos
title_full_unstemmed Avaliação das atividades citotóxica e antibacteriana de compostos triazenos
title_sort Avaliação das atividades citotóxica e antibacteriana de compostos triazenos
author Sousa, Liliana Urdangarin de
author_facet Sousa, Liliana Urdangarin de
author_role author
dc.contributor.none.fl_str_mv Horner, Rosmari
http://lattes.cnpq.br/5907084134183708
Rodrigues Junior, Luiz Carlos
http://lattes.cnpq.br/6354567436180190
Cóser, Virgínia Maria
http://lattes.cnpq.br/4601008307298787
dc.contributor.author.fl_str_mv Sousa, Liliana Urdangarin de
dc.subject.por.fl_str_mv Triazenos
Paládio
Citotoxicidade
Atividade antibacteriana
Leucemia
Triazenes
Palladium
Antibacterial activity
Leukemia
Cytotoxicity
CNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIA
topic Triazenos
Paládio
Citotoxicidade
Atividade antibacteriana
Leucemia
Triazenes
Palladium
Antibacterial activity
Leukemia
Cytotoxicity
CNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIA
description Neoplasms are a major cause of death worldwide and have been worrying about the medical and scientific community, as most anticancer vector does not act on cancer cells, triggering numerous side-effects and, in some cases, resistance to treatment. No less worrying is the resistance acquired by bacteria, which culminate in strains with the phenomenon of multi-drug resistance commercially available. In this context, many research groups that adopted the medicinal chemistry, turn their studies to the discovery of new molecules that may be more selective therapeutic approaches with fewer side effects than currently exist. Triazenes compounds represent a class of compounds having wide versatility with proven pharmacological antimicrobial and antitumor activities. Similarly, considering the results from several studies relevant complexes of palladium (II) have been considered as promising therapeutic agents. As a result, two novel compounds were synthesized, and a binder, and a triazene triazenido complex with palladium (II), which according to the IUPAC nomenclature rules were so named, respectively: 1,3-Bis(4-sulfonamidephenyl)triazene (1) and {trans-Bis-[1,3-bis-(4sulfonamidephenyl)triazenide]bis(piridine)palladium(II)}{piridine)4palladium(II)} {potassim(I)}.water (2). We assess the cytotoxic potential of such compounds by colorimetric assay bromide 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT). Mononuclear cells from different types of leukemia and control samples were incubated for 24 hours with the compounds at concentrations 12.5, 50 and 100 μmol mL-1. To examine the antimicrobial activity of the compounds we used the measurement method of broth microdilution by determining the minimum inhibitory concentration (MIC) against the gram positive and gram negative bacteria. The results showed that the compounds showed significant cytotoxicity in the tested samples, but the compound 2 had lower IC50 than 1. Significant differences were observed between the compounds in the samples of CML and at concentrations 12,5 e 50 μmol mL-1. The antibacterial activity was found narrow spectrum, focused on gram-positive strains.
publishDate 2013
dc.date.none.fl_str_mv 2013-12-13
2015-10-26
2015-10-26
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.uri.fl_str_mv SOUSA, Liliana Urdangarin de. ACTIVITIES EVALUATION CYTOTOXIC AND ANTIBACTERIAL OF COMPOUND TRIAZENES. 2013. 80 f. Dissertação (Mestrado em Farmacologia) - Universidade Federal de Santa Maria, Santa Maria, 2013.
http://repositorio.ufsm.br/handle/1/6009
dc.identifier.dark.fl_str_mv ark:/26339/00130000097t2
identifier_str_mv SOUSA, Liliana Urdangarin de. ACTIVITIES EVALUATION CYTOTOXIC AND ANTIBACTERIAL OF COMPOUND TRIAZENES. 2013. 80 f. Dissertação (Mestrado em Farmacologia) - Universidade Federal de Santa Maria, Santa Maria, 2013.
ark:/26339/00130000097t2
url http://repositorio.ufsm.br/handle/1/6009
dc.language.iso.fl_str_mv por
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application/pdf
dc.publisher.none.fl_str_mv Universidade Federal de Santa Maria
BR
Farmacologia
UFSM
Programa de Pós-Graduação em Ciências Farmacêuticas
publisher.none.fl_str_mv Universidade Federal de Santa Maria
BR
Farmacologia
UFSM
Programa de Pós-Graduação em Ciências Farmacêuticas
dc.source.none.fl_str_mv reponame:Manancial - Repositório Digital da UFSM
instname:Universidade Federal de Santa Maria (UFSM)
instacron:UFSM
instname_str Universidade Federal de Santa Maria (UFSM)
instacron_str UFSM
institution UFSM
reponame_str Manancial - Repositório Digital da UFSM
collection Manancial - Repositório Digital da UFSM
repository.name.fl_str_mv Manancial - Repositório Digital da UFSM - Universidade Federal de Santa Maria (UFSM)
repository.mail.fl_str_mv atendimento.sib@ufsm.br||tedebc@gmail.com||manancial@ufsm.br
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