Melão-de-são-caetano do Nordeste do Brasil (Momordica charantia l.): estudo farmacognóstico e microbiológico integrado ao estudo químico

Detalhes bibliográficos
Autor(a) principal: Guarniz, William Antonio Sagastegui
Data de Publicação: 2020
Tipo de documento: Tese
Idioma: por
Título da fonte: Repositório Institucional da Universidade Federal do Ceará (UFC)
Texto Completo: http://www.repositorio.ufc.br/handle/riufc/50049
Resumo: Momordica charanthia L., Curcubitaceae, is a plant used as food and in traditional medicine. The plant is included in the official list of Brazilian medicinal plants of interest to the Unified Health System. The objective of the present work is to carry out the pharmacognostic evaluation of Momordica charanthia of the macrocarp and microcarp varieties, and microbiological studies and modulator in the action of antimicrobials, with extracts and fractions of M. charanthia microcarpa variety ―melão-de-são-caetano‖ from Northeastern Brazil, including the chemical characterization of the active extracts by UPLC-QToF-ESI-MS. For pharmacognostic evaluation, fresh leaves of M. charantia L., of the microcarpa and macrocarpa varieties were used. Antimicrobial activity was evaluated with hydroalcoholic (EF) and acetone (FA) extracts from leaves, fruits (FrE; FrA) and seeds (SE; SA) of M. charantia microcarpa from northeastern Brazil, using the microdilution technique, in selected clinical bacterial and fungal strains. The extracts with significant antimicrobial activity were submitted to phytochemical profile evaluation using UPLC-QToF-ESI-MS. In addition, the most active extract was partitioned with solvents of increasing polarity, and the antimicrobial and synergistic effect, associated with conventional antibiotics by the Checkerboard technique, was evaluated again, against the microorganisms that showed greater sensitivity. The macromorphological and micromorphological results, respectively, demonstrated that the leaves of the macrocarpa variety are larger and the trichomes less frequent. The phytochemical approach of the two varieties has in common alkaloids, steroids, triterpenoids, flavonoids, saponins, phenolic compounds, condensed tannins and flavonoids. Momordicin II (C36H58O9) was isolated and identified, in the microcarpa variety, by NMR1H and NMR13C and 2D, a structure similar to that found in the variety of Asian origin. Leaf extracts showed a potent antibacterial effect against strains of Staphylococcus aureus and Staphylococcus epidermidis and weak antifungal activity against Candida albicans. Two fractions of the acetone extract showed an important synergistic effect, compared to all the antimicrobials tested except for vancomycin. Fourteen compounds were identified in the hydroalcoholic extract, while 12 were found in the acetone extract, among them kaempferol, quercertin and 7 cucurbitan type triterpenoids. Potential antibacterial activity has been demonstrated, particularly against microorganisms of clinical importance and resistant strains, in addition to having a synergistic activity when associated with antibiotics, against multi-resistant bacteria such as ORSA strains and in associations with antifungals against C. albicans, reducing their MIC up to sixteen times, which is important in inhibiting the development of bacterial resistance and in decreasing the adverse effects of these antimicrobials, especially aminoglycosides and fluoroquinolones. The phytochemical profile by UPLC-MS, showed important pharmacologically active metabolites, in the Brazilian variety, and is reported here for the first time. Further biological and pharmacological studies are needed to support the medicinal uses of this important plant. The Brazilian variety of M. Charantia can be a potential therapeutic agent in the treatment of clinically important infections.
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spelling Melão-de-são-caetano do Nordeste do Brasil (Momordica charantia l.): estudo farmacognóstico e microbiológico integrado ao estudo químicoMomordica charantiaAntibacterianosProdutos BiológicosAntifúngicosSinergismo FarmacológicoMomordica charanthia L., Curcubitaceae, is a plant used as food and in traditional medicine. The plant is included in the official list of Brazilian medicinal plants of interest to the Unified Health System. The objective of the present work is to carry out the pharmacognostic evaluation of Momordica charanthia of the macrocarp and microcarp varieties, and microbiological studies and modulator in the action of antimicrobials, with extracts and fractions of M. charanthia microcarpa variety ―melão-de-são-caetano‖ from Northeastern Brazil, including the chemical characterization of the active extracts by UPLC-QToF-ESI-MS. For pharmacognostic evaluation, fresh leaves of M. charantia L., of the microcarpa and macrocarpa varieties were used. Antimicrobial activity was evaluated with hydroalcoholic (EF) and acetone (FA) extracts from leaves, fruits (FrE; FrA) and seeds (SE; SA) of M. charantia microcarpa from northeastern Brazil, using the microdilution technique, in selected clinical bacterial and fungal strains. The extracts with significant antimicrobial activity were submitted to phytochemical profile evaluation using UPLC-QToF-ESI-MS. In addition, the most active extract was partitioned with solvents of increasing polarity, and the antimicrobial and synergistic effect, associated with conventional antibiotics by the Checkerboard technique, was evaluated again, against the microorganisms that showed greater sensitivity. The macromorphological and micromorphological results, respectively, demonstrated that the leaves of the macrocarpa variety are larger and the trichomes less frequent. The phytochemical approach of the two varieties has in common alkaloids, steroids, triterpenoids, flavonoids, saponins, phenolic compounds, condensed tannins and flavonoids. Momordicin II (C36H58O9) was isolated and identified, in the microcarpa variety, by NMR1H and NMR13C and 2D, a structure similar to that found in the variety of Asian origin. Leaf extracts showed a potent antibacterial effect against strains of Staphylococcus aureus and Staphylococcus epidermidis and weak antifungal activity against Candida albicans. Two fractions of the acetone extract showed an important synergistic effect, compared to all the antimicrobials tested except for vancomycin. Fourteen compounds were identified in the hydroalcoholic extract, while 12 were found in the acetone extract, among them kaempferol, quercertin and 7 cucurbitan type triterpenoids. Potential antibacterial activity has been demonstrated, particularly against microorganisms of clinical importance and resistant strains, in addition to having a synergistic activity when associated with antibiotics, against multi-resistant bacteria such as ORSA strains and in associations with antifungals against C. albicans, reducing their MIC up to sixteen times, which is important in inhibiting the development of bacterial resistance and in decreasing the adverse effects of these antimicrobials, especially aminoglycosides and fluoroquinolones. The phytochemical profile by UPLC-MS, showed important pharmacologically active metabolites, in the Brazilian variety, and is reported here for the first time. Further biological and pharmacological studies are needed to support the medicinal uses of this important plant. The Brazilian variety of M. Charantia can be a potential therapeutic agent in the treatment of clinically important infections.Momordica charanthia L., Curcubitaceae, é uma planta usada como alimento e na medicina tradicional. A planta está incluída na lista oficial de plantas medicinais brasileiras de interesse para o Sistema Único de Saúde. O objetivo do presente trabalho é realizar a avaliação farmacognóstica de Momordica charanthia das variedades macrocarcarpa e microcarpa, e estudos microbiológicos e modulador na ação de antimicrobianos, com extratos e frações de M. charanthia variedade microcarpa ―melão-de-são-caetano‖ do Nordeste do Brasil, incluindo a caracterização química dos extratos ativos por UPLC-QToF-ESI-MS. Para avaliação farmacognóstica, foram utilizadas folhas frescas de M. charantia L., das variedades microcarpa e macrocarpa. A atividade antimicrobiana foi avaliada com os extratos hidroalcoólico (FE) e acetona (FA) de folhas, frutos (FrE; FrA) e sementes (SE; SA) de M. charantia microcarpa do nordeste do Brasil, utilizando a técnica de microdiluição, nas linhagens bacterianas e fúngicas clínicas selecionadas. Os extratos com atividade antimicrobiana significativa foram submetidos à avaliação de perfil fitoquímico usando UPLC-QToF-ESI-MS. Além, o extrato mais ativo foi particionado com solventes de crescente polaridade, e avaliado novamente o efeito antimicrobiano e sinérgico, associados com antibióticos convencionais pela técnica de Checkerboard, frente ao microorganismos que apresentaram maior sensibilidade. Os resultados macromorfológico e micromorfológico, respectivamente, demonstraram que as folhas da variedade macrocarpa são maiores e os tricomas menos frequentes. A abordagem fitoquímica das duas variedades têm em comum alcalóides, esteróides, triterpenóides, flavonóides, saponinas, compostos fenólicos, taninos condensados e flavonóides. Foi isolada e identificada a Momordicina II (C36H58O9), na variedade microcarpa, por RMN1H e RMN13C e 2D, estrutura semelhante a encontrada na variedade de origem asiática. Os extratos das folhas apresentaram potente efeito antibacteriano contra cepas de Staphylococcus aureus e do Staphylococcus epidermidis e fraca atividade antifúngica contra Candida albicans. Duas frações do extrato acetônico apresentaram efeito sinérgico importante, frente a todos os antimicrobianos testados com exceção da vancomicina. Quatorze compostos foram identificados no extrato hidroalcoólico, enquanto 12 foram encontrados no extrato acetônico, entre eles o kaempferol, quercertina e sete triterpenóides do tipo cucurbitano. Demonstrou-se a potencial atividade antibacteriana, particularmente contra microrganismos de importância clínica e cepas resistentes, além de ter uma atividade sinérgica quando é associado a antibióticos, contra bactérias multirresistentes como as cepas de ORSA e em associações com antifúngicos contra C. albicans, reduzindo seu MIC até dezesseis vezes, o que é importante na inibição do desenvolvimento de resistência bacteriana e na diminuição dos efeitos adversos destes antimicrobianos, principalmente dos aminoglicosídeos e fluoroquinolonas. O perfil fitoquímico por UPLC-MS mostrou importantes metabólitos farmacologicamente ativos, na variedade brasileira, e é relatado aqui pela primeira vez. São necessários outros estudos biológicos e farmacológicos para apoiar os usos medicinais desta planta importante. A variedade brasileira de M. Charantia pode ser um potencial agente terapêutico no tratamento de infecções clinicamente importantes.Bandeira, Mary Anne MedeirosMonteiro, Mirian ParenteGuarniz, William Antonio Sagastegui2020-02-14T11:41:15Z2020-02-14T11:41:15Z2020-02-05info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/doctoralThesisapplication/pdfGUARNIZ, W. A. S. Melão-de-são-caetano do Nordeste do Brasil (Momordica charantia l.): estudo farmacognóstico e microbiológico integrado ao estudo químico. 2020. 107 f. Tese (Doutorado em Desenvolvimento e Inovação Tecnológica em Medicamentos) - Faculdade de Farmácia, Odontologia e Enfermagem, Universidade Federal do Ceará, Fortaleza, 2020.http://www.repositorio.ufc.br/handle/riufc/50049porreponame:Repositório Institucional da Universidade Federal do Ceará (UFC)instname:Universidade Federal do Ceará (UFC)instacron:UFCinfo:eu-repo/semantics/openAccess2020-02-14T11:41:15Zoai:repositorio.ufc.br:riufc/50049Repositório InstitucionalPUBhttp://www.repositorio.ufc.br/ri-oai/requestbu@ufc.br || repositorio@ufc.bropendoar:2024-09-11T18:35:28.949348Repositório Institucional da Universidade Federal do Ceará (UFC) - Universidade Federal do Ceará (UFC)false
dc.title.none.fl_str_mv Melão-de-são-caetano do Nordeste do Brasil (Momordica charantia l.): estudo farmacognóstico e microbiológico integrado ao estudo químico
title Melão-de-são-caetano do Nordeste do Brasil (Momordica charantia l.): estudo farmacognóstico e microbiológico integrado ao estudo químico
spellingShingle Melão-de-são-caetano do Nordeste do Brasil (Momordica charantia l.): estudo farmacognóstico e microbiológico integrado ao estudo químico
Guarniz, William Antonio Sagastegui
Momordica charantia
Antibacterianos
Produtos Biológicos
Antifúngicos
Sinergismo Farmacológico
title_short Melão-de-são-caetano do Nordeste do Brasil (Momordica charantia l.): estudo farmacognóstico e microbiológico integrado ao estudo químico
title_full Melão-de-são-caetano do Nordeste do Brasil (Momordica charantia l.): estudo farmacognóstico e microbiológico integrado ao estudo químico
title_fullStr Melão-de-são-caetano do Nordeste do Brasil (Momordica charantia l.): estudo farmacognóstico e microbiológico integrado ao estudo químico
title_full_unstemmed Melão-de-são-caetano do Nordeste do Brasil (Momordica charantia l.): estudo farmacognóstico e microbiológico integrado ao estudo químico
title_sort Melão-de-são-caetano do Nordeste do Brasil (Momordica charantia l.): estudo farmacognóstico e microbiológico integrado ao estudo químico
author Guarniz, William Antonio Sagastegui
author_facet Guarniz, William Antonio Sagastegui
author_role author
dc.contributor.none.fl_str_mv Bandeira, Mary Anne Medeiros
Monteiro, Mirian Parente
dc.contributor.author.fl_str_mv Guarniz, William Antonio Sagastegui
dc.subject.por.fl_str_mv Momordica charantia
Antibacterianos
Produtos Biológicos
Antifúngicos
Sinergismo Farmacológico
topic Momordica charantia
Antibacterianos
Produtos Biológicos
Antifúngicos
Sinergismo Farmacológico
description Momordica charanthia L., Curcubitaceae, is a plant used as food and in traditional medicine. The plant is included in the official list of Brazilian medicinal plants of interest to the Unified Health System. The objective of the present work is to carry out the pharmacognostic evaluation of Momordica charanthia of the macrocarp and microcarp varieties, and microbiological studies and modulator in the action of antimicrobials, with extracts and fractions of M. charanthia microcarpa variety ―melão-de-são-caetano‖ from Northeastern Brazil, including the chemical characterization of the active extracts by UPLC-QToF-ESI-MS. For pharmacognostic evaluation, fresh leaves of M. charantia L., of the microcarpa and macrocarpa varieties were used. Antimicrobial activity was evaluated with hydroalcoholic (EF) and acetone (FA) extracts from leaves, fruits (FrE; FrA) and seeds (SE; SA) of M. charantia microcarpa from northeastern Brazil, using the microdilution technique, in selected clinical bacterial and fungal strains. The extracts with significant antimicrobial activity were submitted to phytochemical profile evaluation using UPLC-QToF-ESI-MS. In addition, the most active extract was partitioned with solvents of increasing polarity, and the antimicrobial and synergistic effect, associated with conventional antibiotics by the Checkerboard technique, was evaluated again, against the microorganisms that showed greater sensitivity. The macromorphological and micromorphological results, respectively, demonstrated that the leaves of the macrocarpa variety are larger and the trichomes less frequent. The phytochemical approach of the two varieties has in common alkaloids, steroids, triterpenoids, flavonoids, saponins, phenolic compounds, condensed tannins and flavonoids. Momordicin II (C36H58O9) was isolated and identified, in the microcarpa variety, by NMR1H and NMR13C and 2D, a structure similar to that found in the variety of Asian origin. Leaf extracts showed a potent antibacterial effect against strains of Staphylococcus aureus and Staphylococcus epidermidis and weak antifungal activity against Candida albicans. Two fractions of the acetone extract showed an important synergistic effect, compared to all the antimicrobials tested except for vancomycin. Fourteen compounds were identified in the hydroalcoholic extract, while 12 were found in the acetone extract, among them kaempferol, quercertin and 7 cucurbitan type triterpenoids. Potential antibacterial activity has been demonstrated, particularly against microorganisms of clinical importance and resistant strains, in addition to having a synergistic activity when associated with antibiotics, against multi-resistant bacteria such as ORSA strains and in associations with antifungals against C. albicans, reducing their MIC up to sixteen times, which is important in inhibiting the development of bacterial resistance and in decreasing the adverse effects of these antimicrobials, especially aminoglycosides and fluoroquinolones. The phytochemical profile by UPLC-MS, showed important pharmacologically active metabolites, in the Brazilian variety, and is reported here for the first time. Further biological and pharmacological studies are needed to support the medicinal uses of this important plant. The Brazilian variety of M. Charantia can be a potential therapeutic agent in the treatment of clinically important infections.
publishDate 2020
dc.date.none.fl_str_mv 2020-02-14T11:41:15Z
2020-02-14T11:41:15Z
2020-02-05
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/doctoralThesis
format doctoralThesis
status_str publishedVersion
dc.identifier.uri.fl_str_mv GUARNIZ, W. A. S. Melão-de-são-caetano do Nordeste do Brasil (Momordica charantia l.): estudo farmacognóstico e microbiológico integrado ao estudo químico. 2020. 107 f. Tese (Doutorado em Desenvolvimento e Inovação Tecnológica em Medicamentos) - Faculdade de Farmácia, Odontologia e Enfermagem, Universidade Federal do Ceará, Fortaleza, 2020.
http://www.repositorio.ufc.br/handle/riufc/50049
identifier_str_mv GUARNIZ, W. A. S. Melão-de-são-caetano do Nordeste do Brasil (Momordica charantia l.): estudo farmacognóstico e microbiológico integrado ao estudo químico. 2020. 107 f. Tese (Doutorado em Desenvolvimento e Inovação Tecnológica em Medicamentos) - Faculdade de Farmácia, Odontologia e Enfermagem, Universidade Federal do Ceará, Fortaleza, 2020.
url http://www.repositorio.ufc.br/handle/riufc/50049
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instname_str Universidade Federal do Ceará (UFC)
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