Avaliação da inibição da prolil oligopeptidase, dipeptidil peptidase e acetilcolinesterase por constituintes de plantas nativas do bioma Pampa- RS. Parâmetros bioquímicos e comportamentais de Phyllanthus tenellus.
Autor(a) principal: | |
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Data de Publicação: | 2016 |
Tipo de documento: | Tese |
Idioma: | por |
Título da fonte: | Manancial - Repositório Digital da UFSM |
Texto Completo: | http://repositorio.ufsm.br/handle/1/17779 |
Resumo: | In this work six native species of Biome Pampa- RS were selected: Spermacoce poaya, Borreria verticillata, Galianthe fastigiata (Rubiaceae), two species of Hypericum: Hypericum brasiliense e H.connatum e Phyllanthus tenellus in order to assess the species with the highest inhibitory potential against POP. Therefore, we performed the phytochemical study of the CE and fractions of the species Hypericumbrasiliense, Hypericum connatum and Phyllanthus tenellus. The fractionation of the species resulted in the isolation of the following compounds: chlorogenic acid (1), quercetrin (2), rutin (3), quercetin (4) and isoquercetrina (5). From the specie P. tenellus the main constituent of ethyl acetate fraction the ellagitannin corilagin was isolated (6) and the flavonoids rutin (7) and (8) vitexin 2 "-O-rhamnoside. The structures of the isolated metabolites were elucidated by 1H and 13C NMR, mass spectrometry and HPLC. The extracts, fractions and isolated compounds were evaluated as inhibitors of prolyl oligopeptidase (POP), dipeptidyl peptidase (DPP IV) and acetylcholinesterase (AChE). All the tested samples of the genus Hypericum showed inhibitory activity of POP. In contrast, the DPP IV inhibitor effect was not significant for all extracts and tested substances. In relation to Phyllanthus tenellus, all fractions and corilagin demonstrated inhibitory potential against POP, except the aqueous fraction that showed less potential for inhibition. Against AChE and DPP IV it was found that only the dichloromethane fraction presented inhibitory potential. The permeability assay (PAMPA) of the hydroalcoholic extract of H. brasiliense showed that the quercetin features moderate permeability 2,19x10-7cm. The analysis of hydroalcoholic extract of P. tenellus showed that the POP inhibitor corilagin is able to pass through the phospholipid membrane by passive diffusion showing moderate permeability 1,26x10-7cm. The plant extract significantly decreased the time of stererotypy in mice, mainly at the dose of 5mg/Kg of CE, such effect was observed both in the acute treatments and in the subchronic treatment. In addition, the CE reduced reactive oxygen species in the striatum and hippocampus. |
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Avaliação da inibição da prolil oligopeptidase, dipeptidil peptidase e acetilcolinesterase por constituintes de plantas nativas do bioma Pampa- RS. Parâmetros bioquímicos e comportamentais de Phyllanthus tenellus.Evaluation of the inhibition of prolyl oligopeptidase, dipeptidyl peptidase and acetylcholinesterase of constituents of native plants of the bioma Pampa-RS. Biochemical and behavioral parameters of Phyllanthus tenellus.Prolil oligopeptidadesDipeptidil peptidaseHypericum brasilienseHypericum connatumPhyllanthus tenellusProlyl oligopeptidaseDipeptidyl peptidaseHypericum brasilienseHypericum connatumCNPQ::CIENCIAS DA SAUDE::FARMACIAIn this work six native species of Biome Pampa- RS were selected: Spermacoce poaya, Borreria verticillata, Galianthe fastigiata (Rubiaceae), two species of Hypericum: Hypericum brasiliense e H.connatum e Phyllanthus tenellus in order to assess the species with the highest inhibitory potential against POP. Therefore, we performed the phytochemical study of the CE and fractions of the species Hypericumbrasiliense, Hypericum connatum and Phyllanthus tenellus. The fractionation of the species resulted in the isolation of the following compounds: chlorogenic acid (1), quercetrin (2), rutin (3), quercetin (4) and isoquercetrina (5). From the specie P. tenellus the main constituent of ethyl acetate fraction the ellagitannin corilagin was isolated (6) and the flavonoids rutin (7) and (8) vitexin 2 "-O-rhamnoside. The structures of the isolated metabolites were elucidated by 1H and 13C NMR, mass spectrometry and HPLC. The extracts, fractions and isolated compounds were evaluated as inhibitors of prolyl oligopeptidase (POP), dipeptidyl peptidase (DPP IV) and acetylcholinesterase (AChE). All the tested samples of the genus Hypericum showed inhibitory activity of POP. In contrast, the DPP IV inhibitor effect was not significant for all extracts and tested substances. In relation to Phyllanthus tenellus, all fractions and corilagin demonstrated inhibitory potential against POP, except the aqueous fraction that showed less potential for inhibition. Against AChE and DPP IV it was found that only the dichloromethane fraction presented inhibitory potential. The permeability assay (PAMPA) of the hydroalcoholic extract of H. brasiliense showed that the quercetin features moderate permeability 2,19x10-7cm. The analysis of hydroalcoholic extract of P. tenellus showed that the POP inhibitor corilagin is able to pass through the phospholipid membrane by passive diffusion showing moderate permeability 1,26x10-7cm. The plant extract significantly decreased the time of stererotypy in mice, mainly at the dose of 5mg/Kg of CE, such effect was observed both in the acute treatments and in the subchronic treatment. In addition, the CE reduced reactive oxygen species in the striatum and hippocampus.Conselho Nacional de Pesquisa e Desenvolvimento Científico e Tecnológico - CNPqNeste trabalho foram selecionadas para prospecção seis espécies nativas do Bioma Pampa- RS: Spermacoce poaya, Borreria verticillata, Galianthe fastigiata (Rubiaceae), Hypericum brasiliense e H. connatum (Hypericaceae) e Phyllanthus tenellus (Euphorbiaceae), com o intuito de avaliar as espécies com maior potencial inibitório frente a prolil oligopeptidase (POP). Foram destacadas para o estudo fitoquímico os extratos brutos e frações das espécies Hypericum brasiliense, Hypericum connatum e Phyllanthus tenellus. O fracionamento das espécies H. connatum e H.brasilinese resultou no isolamento dos seguintes compostos: ácido clorogênico (1), quercetrina (2), rutina (3), quercetina (4) e isoquercetrina (5). A partir deP. tenellus foi isolado como constituinte principal da fração acetato de etila o elagitanino corilagina (6) e foram identificados os flavonoides rutina (7) e vitexina 2”-O-raminosideo(8). As estruturas dos metabólitos isolados foram elucidadas através de RMN 1H e 13C, espectrometria de massas e CLAE. Os extratos, frações e compostos isolados foram avaliados como inibidores das enzimas prolil oligopeptidase (POP), dipeptidil peptidase (DPP IV) e acetilcolinesterase (AChE). Todas as amostras testadas do gênero Hypericum apresentaram atividade inibidora da POP. Em contraste, o efeito inibidor da DPP IV não foi significativo para todos os extratos e substâncias testadas. Em relação à espécie Phyllanthus tenellus, todas as frações e a corilagina demonstraram alto potencial inibitório frente a POP, exceto a fração aquosa. Frente a DPP IV e AChE somente a fração diclorometano apresentou potencial inibitório significativo. O ensaio de permeabilidade (PAMPA), do extrato hidroalcoólico da espécie H. brasiliense mostrou que o metabólito quercetina (4) apresenta moderada permeabilidade 2,19x10-7cm. A análise do extrato hidroalcoólico de P.tenellus mostrou que o inibidor da POP corilagina foi o único constituinte capaz de atravessar o modelo de certificação mostrando uma moderada permeabilidade 1,26x10-7cm.O extrato da planta diminuiu significativamente o tempo de estereotipia nos animais testados, principalmente na dose de 5 mg / Kg, sendo o efeito observado tanto nos tratamentos agudos quanto no tratamento subcrônico. Além disso, o extrato bruto reduziu as espécies reativas de oxigênio no estriado e hipocampo.Universidade Federal de Santa MariaBrasilFarmacologiaUFSMPrograma de Pós-Graduação em FarmacologiaCentro de Ciências da SaúdeDalcol, Ionara Irionhttp://lattes.cnpq.br/9769548819312192Flores, Alex Fabiani Clarohttp://lattes.cnpq.br/1159954352174167Ilha, Viniciushttp://lattes.cnpq.br/3882671719676564Loro, Vania Luciahttp://lattes.cnpq.br/6392817606416780Pavanato, Maria Amáliahttp://lattes.cnpq.br/8701892865724171Santos, Maura Zubiaurre dos2019-08-07T20:39:13Z2019-08-07T20:39:13Z2016-05-19info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/doctoralThesisapplication/pdfhttp://repositorio.ufsm.br/handle/1/17779porAttribution-NonCommercial-NoDerivatives 4.0 Internationalhttp://creativecommons.org/licenses/by-nc-nd/4.0/info:eu-repo/semantics/openAccessreponame:Manancial - Repositório Digital da UFSMinstname:Universidade Federal de Santa Maria (UFSM)instacron:UFSM2019-08-08T06:02:27Zoai:repositorio.ufsm.br:1/17779Biblioteca Digital de Teses e Dissertaçõeshttps://repositorio.ufsm.br/ONGhttps://repositorio.ufsm.br/oai/requestatendimento.sib@ufsm.br||tedebc@gmail.comopendoar:2019-08-08T06:02:27Manancial - Repositório Digital da UFSM - Universidade Federal de Santa Maria (UFSM)false |
dc.title.none.fl_str_mv |
Avaliação da inibição da prolil oligopeptidase, dipeptidil peptidase e acetilcolinesterase por constituintes de plantas nativas do bioma Pampa- RS. Parâmetros bioquímicos e comportamentais de Phyllanthus tenellus. Evaluation of the inhibition of prolyl oligopeptidase, dipeptidyl peptidase and acetylcholinesterase of constituents of native plants of the bioma Pampa-RS. Biochemical and behavioral parameters of Phyllanthus tenellus. |
title |
Avaliação da inibição da prolil oligopeptidase, dipeptidil peptidase e acetilcolinesterase por constituintes de plantas nativas do bioma Pampa- RS. Parâmetros bioquímicos e comportamentais de Phyllanthus tenellus. |
spellingShingle |
Avaliação da inibição da prolil oligopeptidase, dipeptidil peptidase e acetilcolinesterase por constituintes de plantas nativas do bioma Pampa- RS. Parâmetros bioquímicos e comportamentais de Phyllanthus tenellus. Santos, Maura Zubiaurre dos Prolil oligopeptidades Dipeptidil peptidase Hypericum brasiliense Hypericum connatum Phyllanthus tenellus Prolyl oligopeptidase Dipeptidyl peptidase Hypericum brasiliense Hypericum connatum CNPQ::CIENCIAS DA SAUDE::FARMACIA |
title_short |
Avaliação da inibição da prolil oligopeptidase, dipeptidil peptidase e acetilcolinesterase por constituintes de plantas nativas do bioma Pampa- RS. Parâmetros bioquímicos e comportamentais de Phyllanthus tenellus. |
title_full |
Avaliação da inibição da prolil oligopeptidase, dipeptidil peptidase e acetilcolinesterase por constituintes de plantas nativas do bioma Pampa- RS. Parâmetros bioquímicos e comportamentais de Phyllanthus tenellus. |
title_fullStr |
Avaliação da inibição da prolil oligopeptidase, dipeptidil peptidase e acetilcolinesterase por constituintes de plantas nativas do bioma Pampa- RS. Parâmetros bioquímicos e comportamentais de Phyllanthus tenellus. |
title_full_unstemmed |
Avaliação da inibição da prolil oligopeptidase, dipeptidil peptidase e acetilcolinesterase por constituintes de plantas nativas do bioma Pampa- RS. Parâmetros bioquímicos e comportamentais de Phyllanthus tenellus. |
title_sort |
Avaliação da inibição da prolil oligopeptidase, dipeptidil peptidase e acetilcolinesterase por constituintes de plantas nativas do bioma Pampa- RS. Parâmetros bioquímicos e comportamentais de Phyllanthus tenellus. |
author |
Santos, Maura Zubiaurre dos |
author_facet |
Santos, Maura Zubiaurre dos |
author_role |
author |
dc.contributor.none.fl_str_mv |
Dalcol, Ionara Irion http://lattes.cnpq.br/9769548819312192 Flores, Alex Fabiani Claro http://lattes.cnpq.br/1159954352174167 Ilha, Vinicius http://lattes.cnpq.br/3882671719676564 Loro, Vania Lucia http://lattes.cnpq.br/6392817606416780 Pavanato, Maria Amália http://lattes.cnpq.br/8701892865724171 |
dc.contributor.author.fl_str_mv |
Santos, Maura Zubiaurre dos |
dc.subject.por.fl_str_mv |
Prolil oligopeptidades Dipeptidil peptidase Hypericum brasiliense Hypericum connatum Phyllanthus tenellus Prolyl oligopeptidase Dipeptidyl peptidase Hypericum brasiliense Hypericum connatum CNPQ::CIENCIAS DA SAUDE::FARMACIA |
topic |
Prolil oligopeptidades Dipeptidil peptidase Hypericum brasiliense Hypericum connatum Phyllanthus tenellus Prolyl oligopeptidase Dipeptidyl peptidase Hypericum brasiliense Hypericum connatum CNPQ::CIENCIAS DA SAUDE::FARMACIA |
description |
In this work six native species of Biome Pampa- RS were selected: Spermacoce poaya, Borreria verticillata, Galianthe fastigiata (Rubiaceae), two species of Hypericum: Hypericum brasiliense e H.connatum e Phyllanthus tenellus in order to assess the species with the highest inhibitory potential against POP. Therefore, we performed the phytochemical study of the CE and fractions of the species Hypericumbrasiliense, Hypericum connatum and Phyllanthus tenellus. The fractionation of the species resulted in the isolation of the following compounds: chlorogenic acid (1), quercetrin (2), rutin (3), quercetin (4) and isoquercetrina (5). From the specie P. tenellus the main constituent of ethyl acetate fraction the ellagitannin corilagin was isolated (6) and the flavonoids rutin (7) and (8) vitexin 2 "-O-rhamnoside. The structures of the isolated metabolites were elucidated by 1H and 13C NMR, mass spectrometry and HPLC. The extracts, fractions and isolated compounds were evaluated as inhibitors of prolyl oligopeptidase (POP), dipeptidyl peptidase (DPP IV) and acetylcholinesterase (AChE). All the tested samples of the genus Hypericum showed inhibitory activity of POP. In contrast, the DPP IV inhibitor effect was not significant for all extracts and tested substances. In relation to Phyllanthus tenellus, all fractions and corilagin demonstrated inhibitory potential against POP, except the aqueous fraction that showed less potential for inhibition. Against AChE and DPP IV it was found that only the dichloromethane fraction presented inhibitory potential. The permeability assay (PAMPA) of the hydroalcoholic extract of H. brasiliense showed that the quercetin features moderate permeability 2,19x10-7cm. The analysis of hydroalcoholic extract of P. tenellus showed that the POP inhibitor corilagin is able to pass through the phospholipid membrane by passive diffusion showing moderate permeability 1,26x10-7cm. The plant extract significantly decreased the time of stererotypy in mice, mainly at the dose of 5mg/Kg of CE, such effect was observed both in the acute treatments and in the subchronic treatment. In addition, the CE reduced reactive oxygen species in the striatum and hippocampus. |
publishDate |
2016 |
dc.date.none.fl_str_mv |
2016-05-19 2019-08-07T20:39:13Z 2019-08-07T20:39:13Z |
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 |
http://repositorio.ufsm.br/handle/1/17779 |
url |
http://repositorio.ufsm.br/handle/1/17779 |
dc.language.iso.fl_str_mv |
por |
language |
por |
dc.rights.driver.fl_str_mv |
Attribution-NonCommercial-NoDerivatives 4.0 International http://creativecommons.org/licenses/by-nc-nd/4.0/ info:eu-repo/semantics/openAccess |
rights_invalid_str_mv |
Attribution-NonCommercial-NoDerivatives 4.0 International http://creativecommons.org/licenses/by-nc-nd/4.0/ |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
application/pdf |
dc.publisher.none.fl_str_mv |
Universidade Federal de Santa Maria Brasil Farmacologia UFSM Programa de Pós-Graduação em Farmacologia Centro de Ciências da Saúde |
publisher.none.fl_str_mv |
Universidade Federal de Santa Maria Brasil Farmacologia UFSM Programa de Pós-Graduação em Farmacologia Centro de Ciências da Saúde |
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 |
_version_ |
1805922014373871616 |