Avaliação das atividades citotóxica e antibacteriana de compostos triazenos
| Ano de defesa: | 2013 |
|---|---|
| Autor(a) principal: | |
| Orientador(a): | |
| Banca de defesa: | |
| 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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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 |
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info:eu-repo/semantics/publishedVersion |
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info:eu-repo/semantics/masterThesis |
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masterThesis |
| status_str |
publishedVersion |
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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 |
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http://repositorio.ufsm.br/handle/1/6009 |
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Universidade Federal de Santa Maria BR Farmacologia UFSM Programa de Pós-Graduação em Ciências Farmacêuticas |
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Universidade Federal de Santa Maria BR Farmacologia UFSM Programa de Pós-Graduação em Ciências Farmacêuticas |
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reponame:Manancial - Repositório Digital da UFSM instname:Universidade Federal de Santa Maria (UFSM) instacron:UFSM |
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