Avaliação da atividade biológica de β- Citronelol sobre Candida albicans

Detalhes bibliográficos
Autor(a) principal: Silva, Daniele de Figueredo
Data de Publicação: 2016
Tipo de documento: Dissertação
Idioma: por
Título da fonte: Biblioteca Digital de Teses e Dissertações da UFPB
Texto Completo: https://repositorio.ufpb.br/jspui/handle/123456789/12330
Resumo: Candida albicans is the main yeast provider of opportunistic fungal infections in healthy humans and immunossupressed. The high frequency candidiasis, linked to increased therapeutic failure by reflection of resistance to antifungal agents commonly used therapy leads to search for alternative sources for obtaining new antifungal drugs. Highlighted, natural herbal products are excellent precursors for diversity of active molecular compounds. Among them, the monoterpenes are holders of a huge biological potential of human interest. Given these premises, we evaluated the biological activity of β - citronellol on Candida albicans, by microbiological tests performed in vitro by determining the minimum inhibitory concentration (MIC), followed by the Fungicide Concentration Minimum (CFM) and disk diffusion testing solid medium, for comparative study of the susceptibility profile to azole antifungals (ketoconazole, clotrimazole, fluconazole, itraconazole and miconazole) and polyenes (amphotericin B and nystatin) isolated or as association with β -.citronellol. In addition, studies were also made of ADMET parameters by in silico analysis. In studies of antifungal activity, β - citronellol obtained a MIC of 128 mg / mL (strong activity) and CFM 512 ug / mL respectively for 75% of the population of the tested fungal strains. The association study, synergism was prevalent for all antifungals. In highlighted, the combination of β- citronellol to fluconazol, itraconazole, miconazole, were found to change the sensitivity of the resistance profile for some specimens of C. albicans. In the in silico analysis, β - citronellol showed good oral bioavailability, however, irritation potential and damage to the reproductive system have been disclosed as possible severe toxicological effects to this monoterpene. In conclusion, the β- citronellol monoterpene has to have anti-Candida albicans activity of fungicide nature, besides being a great modifier of the antifungal activity when combined. And although it presented good theoretical oral bioavailability, varied toxicological profile suggests the need to assess the risk-benefit of this compound in the production of new antifungal medicine for conducting preclinical and clinical trials of nature.
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spelling Avaliação da atividade biológica de β- Citronelol sobre Candida albicansCandida albicansCandidíaseResistência antifúngicaβ- citronelolAssociaçãoSinergismoAnálise in silicoCandida albicansCandidiasisAntifungal resistanceβ- citronellolAssociationSynergismIn silico analysisCNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIACandida albicans is the main yeast provider of opportunistic fungal infections in healthy humans and immunossupressed. The high frequency candidiasis, linked to increased therapeutic failure by reflection of resistance to antifungal agents commonly used therapy leads to search for alternative sources for obtaining new antifungal drugs. Highlighted, natural herbal products are excellent precursors for diversity of active molecular compounds. Among them, the monoterpenes are holders of a huge biological potential of human interest. Given these premises, we evaluated the biological activity of β - citronellol on Candida albicans, by microbiological tests performed in vitro by determining the minimum inhibitory concentration (MIC), followed by the Fungicide Concentration Minimum (CFM) and disk diffusion testing solid medium, for comparative study of the susceptibility profile to azole antifungals (ketoconazole, clotrimazole, fluconazole, itraconazole and miconazole) and polyenes (amphotericin B and nystatin) isolated or as association with β -.citronellol. In addition, studies were also made of ADMET parameters by in silico analysis. In studies of antifungal activity, β - citronellol obtained a MIC of 128 mg / mL (strong activity) and CFM 512 ug / mL respectively for 75% of the population of the tested fungal strains. The association study, synergism was prevalent for all antifungals. In highlighted, the combination of β- citronellol to fluconazol, itraconazole, miconazole, were found to change the sensitivity of the resistance profile for some specimens of C. albicans. In the in silico analysis, β - citronellol showed good oral bioavailability, however, irritation potential and damage to the reproductive system have been disclosed as possible severe toxicological effects to this monoterpene. In conclusion, the β- citronellol monoterpene has to have anti-Candida albicans activity of fungicide nature, besides being a great modifier of the antifungal activity when combined. And although it presented good theoretical oral bioavailability, varied toxicological profile suggests the need to assess the risk-benefit of this compound in the production of new antifungal medicine for conducting preclinical and clinical trials of nature.Conselho Nacional de Pesquisa e Desenvolvimento Científico e Tecnológico - CNPqCandida albicans é a principal levedura provedora de infecções fúngicas oportunistas em humanos sadios e imunodebilitados. A alta frequência de candidíase, vinculada ao aumento de falha terapêutica, por reflexo a resistência aos agentes antifúngicos de uso comum a terapia, leva a busca de fontes alternativas para obtenção de novas drogas antifúngicas. Em destaque, os produtos naturais à base de plantas, são ótimos precursores pela diversidade de compostos moleculares ativos. Dentre eles, os monoterpenos são detentores de um enorme potencial biológico de interesse humano. Diante dessas premissas, foi avaliada a atividade biológica de β - citronelol sobre Candida albicans, através de ensaios microbiológicos realizados in vitro, por determinação da Concentração Inibitória Mínima (CIM), seguido da Concentração Fungicida Mínima (CFM) e ensaios em difusão em disco em meio sólido, para estudo comparativo do perfil de suscetibilidade aos antifúngicos azólicos (cetoconazol, clotrimazol, fluconazol, itraconazol e miconazol) e polienos (anfotericina B e nistatina) isolados e em associação ao β- citronelol. Em adição, também foram efetuados estudos dos parâmetros de ADMET por análise in silico. Nos estudos de atividade antifúngica, β - citronelol obteve uma CIM de 128 μg/mL (forte atividade) e uma CFM de 512 μg/mL respectivamente para 75% da população das cepas fúngicas testadas. Ao estudo de associação, o sinergismo foi prevalente para todos os antifúngicos. Em destaque, a combinação de β- citronelol ao fluconazol, itraconazol e miconazol, foi constatado a modificação do perfil de resistência à sensibilidade para alguns exemplares de C. albicans. Na análise in silico, β- citronelol apresentou ter boa biodisponibilidade oral, no entanto, potencial irritante e danos ao sistema reprodutor foram revelados como possíveis efeitos toxicológicos severos a este monoterpeno. Em conclusão, o β- citronelol monoterpenoide possui ter atividade anti-Candida albicans de natureza fungicida, além de ser um ótimo modificador de atividade aos agentes antifúngicos quando combinados. E muito embora tenha apresentado boa biodisponibilidade oral teórica, o perfil de toxicológico variado sugere a necessidade em avaliar o risco-benefício desse composto na produção de novo medicamento antifúngico, por realização de ensaios pré- clínicos e clínicos.Universidade Federal da ParaíbaBrasilFarmacologiaPrograma de Pós-Graduação em Produtos Naturais e Sintéticos BioativosUFPBLima, Edeltrudes de Oliveirahttp://lattes.cnpq.br/94065728701670Silva, Daniele de Figueredo2018-11-16T14:32:30Z2018-11-162018-11-16T14:32:30Z2016-02-19info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesishttps://repositorio.ufpb.br/jspui/handle/123456789/12330porAttribution-NonCommercial-NoDerivs 3.0 Brazilhttp://creativecommons.org/licenses/by-nc-nd/3.0/br/info:eu-repo/semantics/openAccessreponame:Biblioteca Digital de Teses e Dissertações da UFPBinstname:Universidade Federal da Paraíba (UFPB)instacron:UFPB2018-11-16T14:32:30Zoai:repositorio.ufpb.br:123456789/12330Biblioteca Digital de Teses e Dissertaçõeshttps://repositorio.ufpb.br/PUBhttp://tede.biblioteca.ufpb.br:8080/oai/requestdiretoria@ufpb.br|| diretoria@ufpb.bropendoar:2018-11-16T14:32:30Biblioteca Digital de Teses e Dissertações da UFPB - Universidade Federal da Paraíba (UFPB)false
dc.title.none.fl_str_mv Avaliação da atividade biológica de β- Citronelol sobre Candida albicans
title Avaliação da atividade biológica de β- Citronelol sobre Candida albicans
spellingShingle Avaliação da atividade biológica de β- Citronelol sobre Candida albicans
Silva, Daniele de Figueredo
Candida albicans
Candidíase
Resistência antifúngica
β- citronelol
Associação
Sinergismo
Análise in silico
Candida albicans
Candidiasis
Antifungal resistance
β- citronellol
Association
Synergism
In silico analysis
CNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIA
title_short Avaliação da atividade biológica de β- Citronelol sobre Candida albicans
title_full Avaliação da atividade biológica de β- Citronelol sobre Candida albicans
title_fullStr Avaliação da atividade biológica de β- Citronelol sobre Candida albicans
title_full_unstemmed Avaliação da atividade biológica de β- Citronelol sobre Candida albicans
title_sort Avaliação da atividade biológica de β- Citronelol sobre Candida albicans
author Silva, Daniele de Figueredo
author_facet Silva, Daniele de Figueredo
author_role author
dc.contributor.none.fl_str_mv Lima, Edeltrudes de Oliveira
http://lattes.cnpq.br/94065728701670
dc.contributor.author.fl_str_mv Silva, Daniele de Figueredo
dc.subject.por.fl_str_mv Candida albicans
Candidíase
Resistência antifúngica
β- citronelol
Associação
Sinergismo
Análise in silico
Candida albicans
Candidiasis
Antifungal resistance
β- citronellol
Association
Synergism
In silico analysis
CNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIA
topic Candida albicans
Candidíase
Resistência antifúngica
β- citronelol
Associação
Sinergismo
Análise in silico
Candida albicans
Candidiasis
Antifungal resistance
β- citronellol
Association
Synergism
In silico analysis
CNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIA
description Candida albicans is the main yeast provider of opportunistic fungal infections in healthy humans and immunossupressed. The high frequency candidiasis, linked to increased therapeutic failure by reflection of resistance to antifungal agents commonly used therapy leads to search for alternative sources for obtaining new antifungal drugs. Highlighted, natural herbal products are excellent precursors for diversity of active molecular compounds. Among them, the monoterpenes are holders of a huge biological potential of human interest. Given these premises, we evaluated the biological activity of β - citronellol on Candida albicans, by microbiological tests performed in vitro by determining the minimum inhibitory concentration (MIC), followed by the Fungicide Concentration Minimum (CFM) and disk diffusion testing solid medium, for comparative study of the susceptibility profile to azole antifungals (ketoconazole, clotrimazole, fluconazole, itraconazole and miconazole) and polyenes (amphotericin B and nystatin) isolated or as association with β -.citronellol. In addition, studies were also made of ADMET parameters by in silico analysis. In studies of antifungal activity, β - citronellol obtained a MIC of 128 mg / mL (strong activity) and CFM 512 ug / mL respectively for 75% of the population of the tested fungal strains. The association study, synergism was prevalent for all antifungals. In highlighted, the combination of β- citronellol to fluconazol, itraconazole, miconazole, were found to change the sensitivity of the resistance profile for some specimens of C. albicans. In the in silico analysis, β - citronellol showed good oral bioavailability, however, irritation potential and damage to the reproductive system have been disclosed as possible severe toxicological effects to this monoterpene. In conclusion, the β- citronellol monoterpene has to have anti-Candida albicans activity of fungicide nature, besides being a great modifier of the antifungal activity when combined. And although it presented good theoretical oral bioavailability, varied toxicological profile suggests the need to assess the risk-benefit of this compound in the production of new antifungal medicine for conducting preclinical and clinical trials of nature.
publishDate 2016
dc.date.none.fl_str_mv 2016-02-19
2018-11-16T14:32:30Z
2018-11-16
2018-11-16T14:32:30Z
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 https://repositorio.ufpb.br/jspui/handle/123456789/12330
url https://repositorio.ufpb.br/jspui/handle/123456789/12330
dc.language.iso.fl_str_mv por
language por
dc.rights.driver.fl_str_mv Attribution-NonCommercial-NoDerivs 3.0 Brazil
http://creativecommons.org/licenses/by-nc-nd/3.0/br/
info:eu-repo/semantics/openAccess
rights_invalid_str_mv Attribution-NonCommercial-NoDerivs 3.0 Brazil
http://creativecommons.org/licenses/by-nc-nd/3.0/br/
eu_rights_str_mv openAccess
dc.publisher.none.fl_str_mv Universidade Federal da Paraíba
Brasil
Farmacologia
Programa de Pós-Graduação em Produtos Naturais e Sintéticos Bioativos
UFPB
publisher.none.fl_str_mv Universidade Federal da Paraíba
Brasil
Farmacologia
Programa de Pós-Graduação em Produtos Naturais e Sintéticos Bioativos
UFPB
dc.source.none.fl_str_mv reponame:Biblioteca Digital de Teses e Dissertações da UFPB
instname:Universidade Federal da Paraíba (UFPB)
instacron:UFPB
instname_str Universidade Federal da Paraíba (UFPB)
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reponame_str Biblioteca Digital de Teses e Dissertações da UFPB
collection Biblioteca Digital de Teses e Dissertações da UFPB
repository.name.fl_str_mv Biblioteca Digital de Teses e Dissertações da UFPB - Universidade Federal da Paraíba (UFPB)
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