Avaliação da atividade biológica do eugenol frente cepas de Penicillium citrinum
Autor(a) principal: | |
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Data de Publicação: | 2023 |
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/123456789/30245 |
Resumo: | Fungi of the genus Penicillium have a wide distribution and are frequently isolated in environments ranging from crops to hospitals. Its species are implicated in several pathologies, such as penicilliosis, which mainly affects immunocompromised individuals. Considering this, and the high fungal resistance to current antifungals, the search for new antifungal agents has been encouraged. For this, medicinal plants and their phytoconstituents have been investigated. Based on this, the objective was to evaluate the biological activity of eugenol against strains of Penicillium citrinum. For this, tests were carried out to determine the Minimum Inhibitory Concentration (MIC); Minimum Fungicide Concentration (CFM); effect of the association between eugenol and the standard antifungal amphotericin B; action of products on the fungal cell wall: test with sorbitol and action of products on the cell membrane: interaction with ergosterol. Furthermore, the in vitro cytotoxic effect of eugenol on human erythrocytes was evaluated. Moreover, eugenol was submitted to online software (pkCSM and Osiris) to preview druggability and toxicity parameters. Likewise, molecular docking was performed in AutoDock 4.2 with the proteins involved in the synthesis and maintenance of the P. citrinum cell membrane. Therefore, strong antifungal activity was observed on all strains of Penicillium citrinum evaluated, since the MIC determined was 1 μg/mL and the CFM was 1 μg/mL, demonstrating fungicidal action. Furthermore, the persistence of the MIC of eugenol in the presence of sorbitol and ergosterol revealed that this molecule possibly does not directly affect the integrity of the wall and plasma membrane of Penicillium citrinum. In the association study between eugenol and amphotericin B, it was found that they had an indifferent effect. In silico studies, eugenol presented important oral bioavailability and mutagenic risk, however it was not cytotoxic in the evaluation of the hemolytic potential in human erythrocytes. Molecular docking proposes the predictive hypothesis that eugenol possibly binds to the active site of CYP51, the enzyme responsible for the biosynthesis of ergosterol, thus suggesting that the tested product acts directly on the formation of ergosterol in the fungal cytoplasmic membrane. Therefore, the evidence from this research indicates that eugenol is a promising and possible option for the treatment of fungal infections caused by Penicillium citrinum, and also in the processes of contamination by the fungus in vegetable crops. |
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Avaliação da atividade biológica do eugenol frente cepas de Penicillium citrinumProdutos naturaisEugenolAtividade antifúngicaPenicillium citrinumNatural productsAntifungal activityCNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIAFungi of the genus Penicillium have a wide distribution and are frequently isolated in environments ranging from crops to hospitals. Its species are implicated in several pathologies, such as penicilliosis, which mainly affects immunocompromised individuals. Considering this, and the high fungal resistance to current antifungals, the search for new antifungal agents has been encouraged. For this, medicinal plants and their phytoconstituents have been investigated. Based on this, the objective was to evaluate the biological activity of eugenol against strains of Penicillium citrinum. For this, tests were carried out to determine the Minimum Inhibitory Concentration (MIC); Minimum Fungicide Concentration (CFM); effect of the association between eugenol and the standard antifungal amphotericin B; action of products on the fungal cell wall: test with sorbitol and action of products on the cell membrane: interaction with ergosterol. Furthermore, the in vitro cytotoxic effect of eugenol on human erythrocytes was evaluated. Moreover, eugenol was submitted to online software (pkCSM and Osiris) to preview druggability and toxicity parameters. Likewise, molecular docking was performed in AutoDock 4.2 with the proteins involved in the synthesis and maintenance of the P. citrinum cell membrane. Therefore, strong antifungal activity was observed on all strains of Penicillium citrinum evaluated, since the MIC determined was 1 μg/mL and the CFM was 1 μg/mL, demonstrating fungicidal action. Furthermore, the persistence of the MIC of eugenol in the presence of sorbitol and ergosterol revealed that this molecule possibly does not directly affect the integrity of the wall and plasma membrane of Penicillium citrinum. In the association study between eugenol and amphotericin B, it was found that they had an indifferent effect. In silico studies, eugenol presented important oral bioavailability and mutagenic risk, however it was not cytotoxic in the evaluation of the hemolytic potential in human erythrocytes. Molecular docking proposes the predictive hypothesis that eugenol possibly binds to the active site of CYP51, the enzyme responsible for the biosynthesis of ergosterol, thus suggesting that the tested product acts directly on the formation of ergosterol in the fungal cytoplasmic membrane. Therefore, the evidence from this research indicates that eugenol is a promising and possible option for the treatment of fungal infections caused by Penicillium citrinum, and also in the processes of contamination by the fungus in vegetable crops.NenhumaOs fungos do gênero Penicillium apresentam ampla distribuição e são frequentemente isolados em ambientes que compreende desde lavouras, até hospitais. Suas espécies estão implicadas em diversas patologias, a exemplo penicilose, que acomete principalmente indivíduos imunocomprometidos. Em vista disso, e da elevada resistência fúngica aos antifúngicos atuais, tem-se impulsionado a busca por novos agentes antifúngicos. Para isso, as plantas medicinais e seus fitoconstituintes tem sido investigadas. Com base nisso, objetivou-se avaliar a atividade biológica do eugenol frente cepas de Penicillium citrinum. Para isso, foram realizados ensaios de determinação da Concentração Inibitória Mínima (CIM); Concentração Fungicida Mínima (CFM); efeito da associação entre eugenol e o antifúngico padrão anfotericina B; ação dos produtos na parede celular fúngica: ensaio com sorbitol e ação dos produtos sobre a membrana celular: interação com ergosterol. Além disso, foi avaliado o efeito citotóxico in vitro do eugenol sobre eritrócitos humanos. Ademais, o eugenol foi submetido aos sistemas (pkCSM e Osiris) para realizar a antevisão de parâmetros de drogabilidade e toxicidade. Do mesmo modo, o docking molecular foi realizado no AutoDock 4.2 com as proteínas envolvidas com a síntese e manutenção da membrana celular de P. citrinum. Assim observou-se forte atividade antifúngica sobre todas as cepas de Penicillium citrinum avaliadas, visto que a CIM determinada foi de 1 μg/mL e a CFM de 1 μg/mL, demonstrando ação fungicida. Ademais, a permanência da CIM do eugenol na presença de sorbitol e ergosterol, revelaram que esta molécula possivelmente não afeta a integridade diretamente da parede e da membrana plasmática de Penicillium citrinum. No estudo de associação entre o eugenol e a anfotericina B, foi verificado que estes possuem um efeito indiferente. Já nos estudos in silico, o eugenol apresentou importante biodisponibilidade oral e risco mutagênico, entretanto não foi citotóxico na avaliação do potencial hemolítico em eritrócitos humanos. O docking molecular, propõe a hipótese preditiva de que o eugenol liga-se possivelmente ao sítio ativo da CYP51, enzima responsável pela biossíntese do ergosterol, sugerindo dessa forma que o produto testado atua de forma direta na formação do ergosterol da membrana citoplasmática fúngica. Assim sendo, as evidências desta pesquisa apontam que o eugenol retrata como promissor e possível opção para o tratamento de infecções fúngicas causadas por Penicillium citrinum, e também nos processos de contaminação pelo fungo nas culturais vegetais.Universidade Federal da ParaíbaBrasilFarmacologiaPrograma de Pós-Graduação em Produtos Naturais e Sintéticos BioativosUFPBLima, Edeltrudes de Oliveirahttp://lattes.cnpq.br/9406572870167006Araújo, Emmanuel Melquíades2024-05-22T09:55:56Z2023-11-232024-05-22T09:55:56Z2023-11-17info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesishttps://repositorio.ufpb.br/jspui/handle/123456789/30245porAttribution-NoDerivs 3.0 Brazilhttp://creativecommons.org/licenses/by-nd/3.0/br/info:eu-repo/semantics/openAccessreponame:Biblioteca Digital de Teses e Dissertações da UFPBinstname:Universidade Federal da Paraíba (UFPB)instacron:UFPB2024-05-23T06:09:04Zoai:repositorio.ufpb.br:123456789/30245Biblioteca Digital de Teses e Dissertaçõeshttps://repositorio.ufpb.br/PUBhttp://tede.biblioteca.ufpb.br:8080/oai/requestdiretoria@ufpb.br|| diretoria@ufpb.bropendoar:2024-05-23T06:09:04Biblioteca Digital de Teses e Dissertações da UFPB - Universidade Federal da Paraíba (UFPB)false |
dc.title.none.fl_str_mv |
Avaliação da atividade biológica do eugenol frente cepas de Penicillium citrinum |
title |
Avaliação da atividade biológica do eugenol frente cepas de Penicillium citrinum |
spellingShingle |
Avaliação da atividade biológica do eugenol frente cepas de Penicillium citrinum Araújo, Emmanuel Melquíades Produtos naturais Eugenol Atividade antifúngica Penicillium citrinum Natural products Antifungal activity CNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIA |
title_short |
Avaliação da atividade biológica do eugenol frente cepas de Penicillium citrinum |
title_full |
Avaliação da atividade biológica do eugenol frente cepas de Penicillium citrinum |
title_fullStr |
Avaliação da atividade biológica do eugenol frente cepas de Penicillium citrinum |
title_full_unstemmed |
Avaliação da atividade biológica do eugenol frente cepas de Penicillium citrinum |
title_sort |
Avaliação da atividade biológica do eugenol frente cepas de Penicillium citrinum |
author |
Araújo, Emmanuel Melquíades |
author_facet |
Araújo, Emmanuel Melquíades |
author_role |
author |
dc.contributor.none.fl_str_mv |
Lima, Edeltrudes de Oliveira http://lattes.cnpq.br/9406572870167006 |
dc.contributor.author.fl_str_mv |
Araújo, Emmanuel Melquíades |
dc.subject.por.fl_str_mv |
Produtos naturais Eugenol Atividade antifúngica Penicillium citrinum Natural products Antifungal activity CNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIA |
topic |
Produtos naturais Eugenol Atividade antifúngica Penicillium citrinum Natural products Antifungal activity CNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIA |
description |
Fungi of the genus Penicillium have a wide distribution and are frequently isolated in environments ranging from crops to hospitals. Its species are implicated in several pathologies, such as penicilliosis, which mainly affects immunocompromised individuals. Considering this, and the high fungal resistance to current antifungals, the search for new antifungal agents has been encouraged. For this, medicinal plants and their phytoconstituents have been investigated. Based on this, the objective was to evaluate the biological activity of eugenol against strains of Penicillium citrinum. For this, tests were carried out to determine the Minimum Inhibitory Concentration (MIC); Minimum Fungicide Concentration (CFM); effect of the association between eugenol and the standard antifungal amphotericin B; action of products on the fungal cell wall: test with sorbitol and action of products on the cell membrane: interaction with ergosterol. Furthermore, the in vitro cytotoxic effect of eugenol on human erythrocytes was evaluated. Moreover, eugenol was submitted to online software (pkCSM and Osiris) to preview druggability and toxicity parameters. Likewise, molecular docking was performed in AutoDock 4.2 with the proteins involved in the synthesis and maintenance of the P. citrinum cell membrane. Therefore, strong antifungal activity was observed on all strains of Penicillium citrinum evaluated, since the MIC determined was 1 μg/mL and the CFM was 1 μg/mL, demonstrating fungicidal action. Furthermore, the persistence of the MIC of eugenol in the presence of sorbitol and ergosterol revealed that this molecule possibly does not directly affect the integrity of the wall and plasma membrane of Penicillium citrinum. In the association study between eugenol and amphotericin B, it was found that they had an indifferent effect. In silico studies, eugenol presented important oral bioavailability and mutagenic risk, however it was not cytotoxic in the evaluation of the hemolytic potential in human erythrocytes. Molecular docking proposes the predictive hypothesis that eugenol possibly binds to the active site of CYP51, the enzyme responsible for the biosynthesis of ergosterol, thus suggesting that the tested product acts directly on the formation of ergosterol in the fungal cytoplasmic membrane. Therefore, the evidence from this research indicates that eugenol is a promising and possible option for the treatment of fungal infections caused by Penicillium citrinum, and also in the processes of contamination by the fungus in vegetable crops. |
publishDate |
2023 |
dc.date.none.fl_str_mv |
2023-11-23 2023-11-17 2024-05-22T09:55:56Z 2024-05-22T09:55:56Z |
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/123456789/30245 |
url |
https://repositorio.ufpb.br/jspui/handle/123456789/30245 |
dc.language.iso.fl_str_mv |
por |
language |
por |
dc.rights.driver.fl_str_mv |
Attribution-NoDerivs 3.0 Brazil http://creativecommons.org/licenses/by-nd/3.0/br/ info:eu-repo/semantics/openAccess |
rights_invalid_str_mv |
Attribution-NoDerivs 3.0 Brazil http://creativecommons.org/licenses/by-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 |
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Universidade Federal da Paraíba (UFPB) |
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UFPB |
institution |
UFPB |
reponame_str |
Biblioteca Digital de Teses e Dissertações da UFPB |
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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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diretoria@ufpb.br|| diretoria@ufpb.br |
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1809927051184963584 |