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Type: Dissertação
Title: Investigação dos efeitos inibitórios de Eryngium foetidum, (E)-2-dodecenal e arbutina frente a mecanismos oxidativos e enzimas digestivas
Author: Xavier, Julianna Oliveira de Lucas
First Advisor: Sousa, Orlando Vieira de
Referee Member: Valverde, Simone Sacramento
Referee Member: Araújo, Ana Lúcia Santos de Matos
Resumo: O processo digestivo dos alimentos compreende um conjunto de transformações físicas e químicas com a participação de enzimas digestivas (tripsina, alfa-amilases, alfa-glicosidases e lipases) cujos produtos nutricionais podem estar relacionados a mecanismos oxidativos e diferentes distúrbios metabólicos (obesidade, diabetes e dislipidemia). Assim, a busca por agentes inibidores dessas enzimas com ação antioxidante tem sido uma das estratégias para o tratamento desses distúrbios. O objetivo do presente estudo foi investigar os efeitos inibitórios de extratos de Eryngium foetidum, (E)-2-dodecenal e arbutina frente a mecanismos oxidativos e enzimas digestivas. Os extratos das folhas frescas (EFF) e secas (EFS) de E. foetidum foram obtidos por percolação com etanol 100% e (E)-2-dodecenal e arbutina foram adquiridos comercialmente. Os teores de fenóis e flavonoides totais foram determinados por espectrofotometria. A atividade antioxidante foi avaliada pelos métodos de sequestro do radical DPPH•, poder de redução do ferro (FRAP) e co-oxidação do β-caroteno/ácido linoleico. O efeito inibitório frente as enzimas digestivas foi verificado com alfa-amilase pancreática, alfaglicosidase e lipase pancreática. Os estudos de docking molecular foram realizados entre ligantes (E-2-dodecenal e arbutina) e enzimas digestivas. Os teores de fenóis totais foram de 107,2 ± 0,73 mgEAG/g (EFS) e 118,8 ± 1,64 mgEAG/g (EFF), enquanto os flavonoides foram de 7,5 ± 0,18 mgERU/g (EFS) e 77,6 ± 0,65 mgERU/g (EFF). Usando o método do DPPH•, EFF e arbutina apresentaram IC50 de 61,54 ± 0,35 e 176,30 ± 1,71 µg/mL, respectivamente, enquanto no FRAP, esses valores foram de 545,30 ± 15,01 e 231,00 ± 2,08 µg/mL, respectivamente. EFF e arbutina com 52,69 ± 2,84 e 53,38 ± 3,15%, respectivamente, inibiram a peroxidação lipídica. Com relação ao efeito inibitório, (E)-2-dodecenal (42,86 ± 0,00%) e arbutina (53,33 ± 0,95%) foram ativos contra a alfa-amilase pancreática. EFF (79,94 ± 0,81%) inibiu a alfa-glicosidase, enquanto (E)-2-dodecenal (80,56 ± 7,35%) foi ativo contra a lipase pancreática. O docking molecular revelou que o (E)-2-dodecenal e a arbutina interagiram com os sítios catalíticos das enzimas, o que pode justificar a capacidade inibitória. Portanto, os resultados indicam que as folhas de E. foetidum, assim como o (E)-2-dodecenal e a arbutina, apresentam potencial antioxidante e inibitório das enzimas digestivas, podendo ser agentes promissores para o tratamento de distúrbios metabólicos associados a processos oxidativos.
Abstract: The digestive process of food comprises a set of physical and chemical transformations with the participation of digestive enzymes (trypsin, alpha-amylases, alpha-glucosidases and lipases) whose nutritional products may be related to oxidative mechanisms and different metabolic disorders (obesity, diabetes and dyslipidemia). Thus, the search for inhibitors of these enzymes with antioxidant action has been one of the strategies for the treatment of these disorders. The aim of the present study was to investigate the inhibitory effects of extracts of Eryngium foetidum, (E)-2-dodecenal and arbutin on oxidative mechanisms and digestive enzymes. Fresh (FLE) and dried (DLE) leaf extracts of E. foetidum were obtained by percolation with 100% ethanol and (E)-2-dodecenal and arbutin were purchased commercially. Total phenols and flavonoids contents were determined by spectrophotometry. Antioxidant activity was evaluated by DPPH• radical scavenging, ferric reducing antioxidant power (FRAP) and βcarotene/linoleic acid assays. The inhibitory effect against digestive enzymes was verified with pancreatic alpha-amylase, alpha-glucosidase and pancreatic lipase. Molecular docking studies were performed between ligands (E-2-dodecenal and arbutin) and digestive enzymes. Total phenols contents were of 107.2 ± 0.73 mgEGA/g (DLE) and 118.8 ± 1.64 mgEGA/g (FLE), while flavonoids were of 7.5 ± 0.18 mgERU/g (DLE) and 77.6 ± 0.65 mgERU/g (FLE). Using the DPPH• assay, FLE and arbutin presented IC50 of 61.54 ± 0.35 and 176.30 ± 1.71 µg/mL, respectively, while in FRAP, these values were of 545.30 ± 15.01 and 231.00 ± 2.08 µg/mL, respectively. Regarding the inhibitory effect, (E)-2-dodecenal (42.86 ± 0.00%) and arbutin (53.33 ± 0.95%) were active against pancreatic alpha-amylase. FLE (79.94 ± 0.81%) inhibited alpha-glucosidase, while (E)-2-dodecenal (80.56 ± 7.35%) was active against pancreatic lipase. Molecular docking revealed that (E)-2-dodecenal and arbutin interacted with the catalytic sites of the enzymes, which may explain the inhibitory capacity. These results indicate that E. foetidum leaves, as well as (E)-2-dodecenal and arbutin, have antioxidant potential and inhibitory capacity against digestive enzymes, and may be promising agents for the treatment of metabolic disorders associated with oxidative processes.
Keywords: Eryngium foetidum
(E)-2-dodecenal
Arbutina
Inibidores de enzimas
Antioxidantes
Docking molecular
Arbutin
Enzyme inhibitors
Antioxidants.
Molecular docking
CNPq: CNPQ::CIENCIAS DA SAUDE::FARMACIA
Language: por
Country: Brasil
Publisher: Universidade Federal de Juiz de Fora (UFJF)
Institution Initials: UFJF
Department: Faculdade de Farmácia
Program: Programa de Pós-graduação em Ciências Farmacêuticas
Access Type: Acesso Aberto
Attribution-NonCommercial-NoDerivs 3.0 Brazil
Creative Commons License: http://creativecommons.org/licenses/by-nc-nd/3.0/br/
DOI: https://doi.org/10.34019/ufjf/di/2022/00030
URI: https://repositorio.ufjf.br/jspui/handle/ufjf/13957
Issue Date: 17-Feb-2022
Appears in Collections:Mestrado em Ciências Farmacêuticas (Dissertações)



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