Avaliação da atividade citotóxica e antibacteriana de um composto triazenido complexado com íon ouro (I)

Detalhes bibliográficos
Autor(a) principal: Nunes, Melise Silveira
Data de Publicação: 2015
Tipo de documento: Dissertação
Idioma: por
Título da fonte: Manancial - Repositório Digital da UFSM
dARK ID: ark:/26339/001300000pjfk
Texto Completo: http://repositorio.ufsm.br/handle/1/6029
Resumo: Cancer represents one of the leading causes of death worldwide and efforts to discover more effective anticancer therapies have led to the synthesis of a wide diversity of molecular species. Another major challenge is the anti-infective treatment, because despite the large arsenal of active substances available, many show inefficiency due to the rapid emergence of resistant bacterial strains. As a result, arises the necessity of finding new active substances, more effective and targeted properties in both treatments of neoplasms as microbial resistance. Notably, the Triazenes compounds (TZCs) have been asserting itself as a promising class of metallodrugs with relevant antimicrobial and antiproliferative activity. Moreover, the association of pharmacophoric radical TZC with metal ions, such as gold, leads to a significant increase in biological activity. Because of this wide pharmacological versatility, this study aimed the evaluating in vitro of the biological activity of a compound TZC complexed with ion gold (I). The antibacterial activity was carried out by the conventional method of broth microdilution, through the technique of the minimum inhibitory concentration (MIC), against bacterial strains reference standard American Type Culture Collection (ATCC), clinical isolates with multidrug resistance (MDR) and clinical isolates biofilm producers. Cytotoxicity was evaluated by colorimetric assay based on the reduction of bromide of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) (MTT) against the standard cell line K562 (Chronic Myeloid Leukemia). The results obtained demonstrate that the compound in study present a narrow spectrum of action, being active only against microorganisms classified as Gram positive, moreover, proved to be active against all isolates producing biofilm when compared to non-producing strains of biofilm. Also showed remarkable cytotoxic activity, with IC50 4.96 μM. Thus, these results demonstrate an alternative to the design of a new class of antibacterial and antitumor metallodrugs with activity.
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spelling Avaliação da atividade citotóxica e antibacteriana de um composto triazenido complexado com íon ouro (I)Evaluation of cytotoxic and antibacterial activity of a compound triazenide complexed with gold ion (I)TriazenosÍon ouroResistência bacterianaCitotoxicidadeTriazenesIon goldBacterial resistanceCytotoxicityCNPQ::CIENCIAS DA SAUDE::FARMACIACancer represents one of the leading causes of death worldwide and efforts to discover more effective anticancer therapies have led to the synthesis of a wide diversity of molecular species. Another major challenge is the anti-infective treatment, because despite the large arsenal of active substances available, many show inefficiency due to the rapid emergence of resistant bacterial strains. As a result, arises the necessity of finding new active substances, more effective and targeted properties in both treatments of neoplasms as microbial resistance. Notably, the Triazenes compounds (TZCs) have been asserting itself as a promising class of metallodrugs with relevant antimicrobial and antiproliferative activity. Moreover, the association of pharmacophoric radical TZC with metal ions, such as gold, leads to a significant increase in biological activity. Because of this wide pharmacological versatility, this study aimed the evaluating in vitro of the biological activity of a compound TZC complexed with ion gold (I). The antibacterial activity was carried out by the conventional method of broth microdilution, through the technique of the minimum inhibitory concentration (MIC), against bacterial strains reference standard American Type Culture Collection (ATCC), clinical isolates with multidrug resistance (MDR) and clinical isolates biofilm producers. Cytotoxicity was evaluated by colorimetric assay based on the reduction of bromide of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) (MTT) against the standard cell line K562 (Chronic Myeloid Leukemia). The results obtained demonstrate that the compound in study present a narrow spectrum of action, being active only against microorganisms classified as Gram positive, moreover, proved to be active against all isolates producing biofilm when compared to non-producing strains of biofilm. Also showed remarkable cytotoxic activity, with IC50 4.96 μM. Thus, these results demonstrate an alternative to the design of a new class of antibacterial and antitumor metallodrugs with activity.O câncer representa uma das principais causas de óbito no mundo e esforços para descobrir terapias antineoplásicas mais eficazes têm conduzido à síntese de inúmeras moléculas. Outro grande desafio é o tratamento anti-infeccioso, pois apesar do grande arsenal de substâncias ativas disponíveis, muitas mostram-se ineficazes devido ao rápido aparecimento de estirpes bacterianas resistentes. Em razão disso, surge a necessidade da descoberta de novas substâncias ativas, com propriedades mais eficazes e direcionadas, tanto nos tratamentos de neoplasias como de resistência microbiana. Notoriamente, os compostos Triazenos (TZCs) vêm afirmando-se como uma classe promissora de metalofármacos com relevante atividade antimicrobiana e antiproliferativa. Além disso, a associação do radical farmacofórico TZC com íons metálicos, como o ouro, leva a um aumento significativo na atividade biológica. Em virtude dessa ampla versatilidade farmacológica, este estudo teve como objetivo a avaliação in vitro da atividade biológica de um composto TZC complexados com íon ouro (I). A atividade antibacteriana foi realizada pelo método convencional da microdiluição em caldo, através da técnica da concentração inibitória mínima (CIM), frente às cepas bacterianas padrão de referência American Type Culture Collection (ATCC), isolados clínicos com resistência a múltiplas drogas (RMD) e isolados clínicos produtores de biofilme. A citotoxicidade foi analisada através do ensaio colorimétrico baseado na redução do brometo de 3-(4,5-dimetiltiazol-2-il)-2,5 difeniltetrazólio) (MTT), frente às células da linhagem padrão K562 (Leucemia Mieloide Crônica). Os resultados obtidos demonstram que o composto em estudo apresentou estreito espectro de ação, sendo ativo somente frente aos microrganismos classificados como Gram positivos, além disso, mostrou-se ativo frente a todos os isolados produtores de biofilme, quando comparado às cepas não produtoras de biofilme. Também demonstrou notável atividade citotóxica, tendo a IC50 4.96 μM. Sendo assim, esses resultados demonstram uma alternativa para a concepção de uma nova classe de metalofármacos com atividade antibacteriana e antitumoral.Universidade Federal de Santa MariaBRAnálises Clínicas e ToxicológicasUFSMPrograma de Pós-Graduação em Ciências FarmacêuticasHorner, Rosmarihttp://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4707613Z5Krause, Luciana Maria Fontanarihttp://lattes.cnpq.br/9844890896121847Cóser, Virgínia Mariahttp://lattes.cnpq.br/4601008307298787Nunes, Melise Silveira2015-12-012015-12-012015-05-15info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisapplication/pdfapplication/pdfNUNES, Melise Silveira. EVALUATION OF CYTOTOXIC AND ANTIBACTERIAL ACTIVITY OF A COMPOUND TRIAZENIDE COMPLEXED WITH GOLD ION (I). 2015. 69 f. Dissertação (Mestrado em Farmacologia) - Universidade Federal de Santa Maria, Santa Maria, 2015.http://repositorio.ufsm.br/handle/1/6029ark:/26339/001300000pjfkporinfo:eu-repo/semantics/openAccessreponame:Manancial - Repositório Digital da UFSMinstname:Universidade Federal de Santa Maria (UFSM)instacron:UFSM2022-10-17T14:37:01Zoai:repositorio.ufsm.br:1/6029Biblioteca Digital de Teses e Dissertaçõeshttps://repositorio.ufsm.br/ONGhttps://repositorio.ufsm.br/oai/requestatendimento.sib@ufsm.br||tedebc@gmail.comopendoar:2022-10-17T14:37:01Manancial - Repositório Digital da UFSM - Universidade Federal de Santa Maria (UFSM)false
dc.title.none.fl_str_mv Avaliação da atividade citotóxica e antibacteriana de um composto triazenido complexado com íon ouro (I)
Evaluation of cytotoxic and antibacterial activity of a compound triazenide complexed with gold ion (I)
title Avaliação da atividade citotóxica e antibacteriana de um composto triazenido complexado com íon ouro (I)
spellingShingle Avaliação da atividade citotóxica e antibacteriana de um composto triazenido complexado com íon ouro (I)
Nunes, Melise Silveira
Triazenos
Íon ouro
Resistência bacteriana
Citotoxicidade
Triazenes
Ion gold
Bacterial resistance
Cytotoxicity
CNPQ::CIENCIAS DA SAUDE::FARMACIA
title_short Avaliação da atividade citotóxica e antibacteriana de um composto triazenido complexado com íon ouro (I)
title_full Avaliação da atividade citotóxica e antibacteriana de um composto triazenido complexado com íon ouro (I)
title_fullStr Avaliação da atividade citotóxica e antibacteriana de um composto triazenido complexado com íon ouro (I)
title_full_unstemmed Avaliação da atividade citotóxica e antibacteriana de um composto triazenido complexado com íon ouro (I)
title_sort Avaliação da atividade citotóxica e antibacteriana de um composto triazenido complexado com íon ouro (I)
author Nunes, Melise Silveira
author_facet Nunes, Melise Silveira
author_role author
dc.contributor.none.fl_str_mv Horner, Rosmari
http://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4707613Z5
Krause, Luciana Maria Fontanari
http://lattes.cnpq.br/9844890896121847
Cóser, Virgínia Maria
http://lattes.cnpq.br/4601008307298787
dc.contributor.author.fl_str_mv Nunes, Melise Silveira
dc.subject.por.fl_str_mv Triazenos
Íon ouro
Resistência bacteriana
Citotoxicidade
Triazenes
Ion gold
Bacterial resistance
Cytotoxicity
CNPQ::CIENCIAS DA SAUDE::FARMACIA
topic Triazenos
Íon ouro
Resistência bacteriana
Citotoxicidade
Triazenes
Ion gold
Bacterial resistance
Cytotoxicity
CNPQ::CIENCIAS DA SAUDE::FARMACIA
description Cancer represents one of the leading causes of death worldwide and efforts to discover more effective anticancer therapies have led to the synthesis of a wide diversity of molecular species. Another major challenge is the anti-infective treatment, because despite the large arsenal of active substances available, many show inefficiency due to the rapid emergence of resistant bacterial strains. As a result, arises the necessity of finding new active substances, more effective and targeted properties in both treatments of neoplasms as microbial resistance. Notably, the Triazenes compounds (TZCs) have been asserting itself as a promising class of metallodrugs with relevant antimicrobial and antiproliferative activity. Moreover, the association of pharmacophoric radical TZC with metal ions, such as gold, leads to a significant increase in biological activity. Because of this wide pharmacological versatility, this study aimed the evaluating in vitro of the biological activity of a compound TZC complexed with ion gold (I). The antibacterial activity was carried out by the conventional method of broth microdilution, through the technique of the minimum inhibitory concentration (MIC), against bacterial strains reference standard American Type Culture Collection (ATCC), clinical isolates with multidrug resistance (MDR) and clinical isolates biofilm producers. Cytotoxicity was evaluated by colorimetric assay based on the reduction of bromide of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) (MTT) against the standard cell line K562 (Chronic Myeloid Leukemia). The results obtained demonstrate that the compound in study present a narrow spectrum of action, being active only against microorganisms classified as Gram positive, moreover, proved to be active against all isolates producing biofilm when compared to non-producing strains of biofilm. Also showed remarkable cytotoxic activity, with IC50 4.96 μM. Thus, these results demonstrate an alternative to the design of a new class of antibacterial and antitumor metallodrugs with activity.
publishDate 2015
dc.date.none.fl_str_mv 2015-12-01
2015-12-01
2015-05-15
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 NUNES, Melise Silveira. EVALUATION OF CYTOTOXIC AND ANTIBACTERIAL ACTIVITY OF A COMPOUND TRIAZENIDE COMPLEXED WITH GOLD ION (I). 2015. 69 f. Dissertação (Mestrado em Farmacologia) - Universidade Federal de Santa Maria, Santa Maria, 2015.
http://repositorio.ufsm.br/handle/1/6029
dc.identifier.dark.fl_str_mv ark:/26339/001300000pjfk
identifier_str_mv NUNES, Melise Silveira. EVALUATION OF CYTOTOXIC AND ANTIBACTERIAL ACTIVITY OF A COMPOUND TRIAZENIDE COMPLEXED WITH GOLD ION (I). 2015. 69 f. Dissertação (Mestrado em Farmacologia) - Universidade Federal de Santa Maria, Santa Maria, 2015.
ark:/26339/001300000pjfk
url http://repositorio.ufsm.br/handle/1/6029
dc.language.iso.fl_str_mv por
language por
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Universidade Federal de Santa Maria
BR
Análises Clínicas e Toxicológicas
UFSM
Programa de Pós-Graduação em Ciências Farmacêuticas
publisher.none.fl_str_mv Universidade Federal de Santa Maria
BR
Análises Clínicas e Toxicológicas
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
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