Atividade antiulcerogênica e anti-inflamatória intestinal do estragol em modelos animais

Detalhes bibliográficos
Autor(a) principal: Alves Júnior, Edvaldo Balbino
Data de Publicação: 2023
Tipo de documento: Tese
Idioma: por
Título da fonte: Biblioteca Digital de Teses e Dissertações da UFPB
Texto Completo: https://repositorio.ufpb.br/jspui/handle/123456789/29643
Resumo: Phenylpropanoids are a class of compounds produced by medicinal plants and are biosynthesized from phenylalanine via cinnamic acid. Estravole is a phenylpropanoid that is present as a constituent of essential oils of many plant species, such as Ravensara anisata (Madeira), Ocimum basilicum (Basil) and Croton zehntneri (Cinnamon). Pharmacological activities such as antioxidant, antimicrobial, anxiolytic, skeletal muscle contractile, visceral muscle relaxant, anti-inflammatory and gastroprotective are described. The present work has the general objective to evaluate the intestinal antiulcerogenic and anti-inflammatory activity of trazol in animal models. In the cysteamine-induced duodenal ulcer model, oral (v.o) administration of trazol at doses of 31; 62; 125 and 250 mg/kg) reduced (p<0.001) the ulcerative lesion area (ALU) in rat duodenum. From the gastric ulcer protocol induced by acetic acid, the toxicity was investigated by repeated doses for 14 days. The results showed that the treatment (v.o) with 250 mg/kg of trazol reduced (p<0.001) the ALU, when compared to the control group. This effect was related to an increase in the levels of GSH, SOD, IL-10 and TGFβ (p<0.001) and a reduction (p<0.001) in the levels of MDA, MPO, IL-1β, TNF-α and NFκB. The administration of trazol for 14 days did not change the weight of the organs (heart, liver, spleen and kidneys), nor the biochemical and hematological parameters evaluated. In addition, the test substance protects the animals from reduced water and feed consumption. In the acute induction model of TNBS-induced intestinal inflammation, trazol reduced (p<0.05) the macroscopic lesion score, ALU, weight/length ratio, and diarrheal index at all doses evaluated. In the sub-chronic protocol of ulcerative colitis with relapse, the most effective dose of trazol (250 mg/kg) reduced (p<0.01) the macroscopic lesion score, the ALU and the colonic weight/length ratio. From the acute and sub-chronic colitis protocols, it was observed that trazol (250 mg/kg) reduced (p<0.001) MDA and MPO levels and restored GSH and SOD levels. In addition, it reduced (p<0.001) levels of IL-1β, TNF-α and NFκB, as well as increased TGFβ levels (p<0.001) and restored (p<0.01) IL-10 levels. In the evaluation of the epithelial barrier function, an increase (p<0.001) of the immunostaining for zone of occlusion-1 (ZO-1) was shown. Based on the data analyzed, it can be suggested that trazol has anti-duodenal ulcer activity, gastric healing activity is related to the induction of re-epithelialization of the lesion and low toxicity by repeated doses. And intestinal anti-inflammatory activity in the acute and sub-chronic phase, being related to the cytoprotection of the intestinal barrier through the preservation of gap junctions, antioxidant system and immunomodulation.
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spelling Atividade antiulcerogênica e anti-inflamatória intestinal do estragol em modelos animaisProdutos naturaisFenilpropanoides - EstragolAtividade cicatrizante gástricaAtividade antiúlcera duodenalAtividade anti-inflamatória intestinalNatural productsPhenylpropanoids - EstragoleGastric healing activityDuodenal antiulcer activityIntestinal anti-inflammatory activityCNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIAPhenylpropanoids are a class of compounds produced by medicinal plants and are biosynthesized from phenylalanine via cinnamic acid. Estravole is a phenylpropanoid that is present as a constituent of essential oils of many plant species, such as Ravensara anisata (Madeira), Ocimum basilicum (Basil) and Croton zehntneri (Cinnamon). Pharmacological activities such as antioxidant, antimicrobial, anxiolytic, skeletal muscle contractile, visceral muscle relaxant, anti-inflammatory and gastroprotective are described. The present work has the general objective to evaluate the intestinal antiulcerogenic and anti-inflammatory activity of trazol in animal models. In the cysteamine-induced duodenal ulcer model, oral (v.o) administration of trazol at doses of 31; 62; 125 and 250 mg/kg) reduced (p<0.001) the ulcerative lesion area (ALU) in rat duodenum. From the gastric ulcer protocol induced by acetic acid, the toxicity was investigated by repeated doses for 14 days. The results showed that the treatment (v.o) with 250 mg/kg of trazol reduced (p<0.001) the ALU, when compared to the control group. This effect was related to an increase in the levels of GSH, SOD, IL-10 and TGFβ (p<0.001) and a reduction (p<0.001) in the levels of MDA, MPO, IL-1β, TNF-α and NFκB. The administration of trazol for 14 days did not change the weight of the organs (heart, liver, spleen and kidneys), nor the biochemical and hematological parameters evaluated. In addition, the test substance protects the animals from reduced water and feed consumption. In the acute induction model of TNBS-induced intestinal inflammation, trazol reduced (p<0.05) the macroscopic lesion score, ALU, weight/length ratio, and diarrheal index at all doses evaluated. In the sub-chronic protocol of ulcerative colitis with relapse, the most effective dose of trazol (250 mg/kg) reduced (p<0.01) the macroscopic lesion score, the ALU and the colonic weight/length ratio. From the acute and sub-chronic colitis protocols, it was observed that trazol (250 mg/kg) reduced (p<0.001) MDA and MPO levels and restored GSH and SOD levels. In addition, it reduced (p<0.001) levels of IL-1β, TNF-α and NFκB, as well as increased TGFβ levels (p<0.001) and restored (p<0.01) IL-10 levels. In the evaluation of the epithelial barrier function, an increase (p<0.001) of the immunostaining for zone of occlusion-1 (ZO-1) was shown. Based on the data analyzed, it can be suggested that trazol has anti-duodenal ulcer activity, gastric healing activity is related to the induction of re-epithelialization of the lesion and low toxicity by repeated doses. And intestinal anti-inflammatory activity in the acute and sub-chronic phase, being related to the cytoprotection of the intestinal barrier through the preservation of gap junctions, antioxidant system and immunomodulation.Conselho Nacional de Pesquisa e Desenvolvimento Científico e Tecnológico - CNPqOs fenilpropanóides são uma classe de compostos produzidos pelas plantas medicinais e são biossintetizados a partir da fenilalanina via ácido cinâmico. O estragol é um fenilpropanoide que está presente como constituinte de óleos essenciais de muitas espécies vegetais, como Ravensara anisata (Madeira), Ocimum basilicum (Manjericão) e Croton zehntneri (Canelinha). Atividades farmacológicas como antioxidante, antimicrobiana, ansiolítica, contrátil do músculo esquelético, relaxante do músculo visceral, anti-inflamatória e gastroprotetora são descritas. O presente trabalho tem como objetivo geral avaliar a atividade antiulcerogênica e anti-inflamatória intestinal do estragol em modelos animais. No modelo de úlcera duodenal induzida por cisteamina a administração oral (v.o) de estragol nas doses de 31; 62; 125 e 250 mg/kg) reduziu (p<0,001) a área de lesão ulcerativa (ALU) em duodenos de ratos. A partir do protocolo de úlcera gástrica induzida por ácido acético foi investigada a toxicidade por doses repetidas durante 14 dias. Os resultados demostraram que o tratamento (v.o) com estragol na dose de 250 mg/kg reduziu (p<0,001) a ALU, quando comparado ao grupo controle. Esse efeito foi relacionado a um aumento dos níveis de GSH, SOD, IL-10 e TGFβ (p<0,001) e uma redução (p<0,001) dos níveis de MDA, MPO, IL-1β, TNF-α e NFκB. A administração de estragol durante 14 dias não alterou o peso dos órgãos (coração, fígado, baço e rins), nem os parâmetros bioquímicos e hematológicos avaliados. Além disso, a substância teste protege os animais da redução do consumo de água e de ração. No modelo de indução aguda de inflamação intestinal induzida por TNBS, o estragol reduziu (p<0,05) o escore de lesão macroscópica, a ALU, a relação peso/comprimento e o índice diarreico em todas as doses avaliadas. No protocolo sub-crônico de colite ulcerativa com recidiva, o estragol em sua dose mais efetiva (250 mg/kg) reduziu (p<0,01) o escore de lesão macroscópica, a ALU e a relação peso/comprimento do cólon. A partir dos protocolos agudo e subcrônico de colite, foi observado que o estragol (250 mg/kg) reduziu (p<0,001) os níveis de MDA e MPO e restaurou os níveis de GSH e SOD. Em adição, reduziu (p<0,001) os níveis de IL-1β, TNF-α e e NFκB, bem como, aumentou os níveis de TGFβ (p<0,001) e restaurou (p<0,01) os de IL-10. Na avaliação de função da barreira epitelial foi mostrado um aumento (p<0,001) da imunomarcação para zona de oclusão-1 (ZO-1). A partir dos dados analisados, pode-se sugerir que o estragol apresenta atividade antiúlcera duodenal, atividade cicatrizante gástrica está relacionada à indução da reepitelização da lesão e baixa toxicidade por doses repetidas. E atividade anti-inflamatória intestinal na fase aguda e sub-crônica, sendo relacionada à citoproteção da barreira intestinal por meio da preservação das junções comunicantes, sistema antioxidante e da imunomodulação.Universidade Federal da ParaíbaBrasilFarmacologiaPrograma de Pós-Graduação em Produtos Naturais e Sintéticos BioativosUFPBBatista, Leônia Mariahttp://lattes.cnpq.br/0601720493634706Alves Júnior, Edvaldo Balbino2024-02-26T14:06:43Z2023-05-302024-02-26T14:06:43Z2023-03-29info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/doctoralThesishttps://repositorio.ufpb.br/jspui/handle/123456789/29643porAttribution-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:UFPB2024-02-27T06:06:33Zoai:repositorio.ufpb.br:123456789/29643Biblioteca Digital de Teses e Dissertaçõeshttps://repositorio.ufpb.br/PUBhttp://tede.biblioteca.ufpb.br:8080/oai/requestdiretoria@ufpb.br|| diretoria@ufpb.bropendoar:2024-02-27T06:06:33Biblioteca Digital de Teses e Dissertações da UFPB - Universidade Federal da Paraíba (UFPB)false
dc.title.none.fl_str_mv Atividade antiulcerogênica e anti-inflamatória intestinal do estragol em modelos animais
title Atividade antiulcerogênica e anti-inflamatória intestinal do estragol em modelos animais
spellingShingle Atividade antiulcerogênica e anti-inflamatória intestinal do estragol em modelos animais
Alves Júnior, Edvaldo Balbino
Produtos naturais
Fenilpropanoides - Estragol
Atividade cicatrizante gástrica
Atividade antiúlcera duodenal
Atividade anti-inflamatória intestinal
Natural products
Phenylpropanoids - Estragole
Gastric healing activity
Duodenal antiulcer activity
Intestinal anti-inflammatory activity
CNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIA
title_short Atividade antiulcerogênica e anti-inflamatória intestinal do estragol em modelos animais
title_full Atividade antiulcerogênica e anti-inflamatória intestinal do estragol em modelos animais
title_fullStr Atividade antiulcerogênica e anti-inflamatória intestinal do estragol em modelos animais
title_full_unstemmed Atividade antiulcerogênica e anti-inflamatória intestinal do estragol em modelos animais
title_sort Atividade antiulcerogênica e anti-inflamatória intestinal do estragol em modelos animais
author Alves Júnior, Edvaldo Balbino
author_facet Alves Júnior, Edvaldo Balbino
author_role author
dc.contributor.none.fl_str_mv Batista, Leônia Maria
http://lattes.cnpq.br/0601720493634706
dc.contributor.author.fl_str_mv Alves Júnior, Edvaldo Balbino
dc.subject.por.fl_str_mv Produtos naturais
Fenilpropanoides - Estragol
Atividade cicatrizante gástrica
Atividade antiúlcera duodenal
Atividade anti-inflamatória intestinal
Natural products
Phenylpropanoids - Estragole
Gastric healing activity
Duodenal antiulcer activity
Intestinal anti-inflammatory activity
CNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIA
topic Produtos naturais
Fenilpropanoides - Estragol
Atividade cicatrizante gástrica
Atividade antiúlcera duodenal
Atividade anti-inflamatória intestinal
Natural products
Phenylpropanoids - Estragole
Gastric healing activity
Duodenal antiulcer activity
Intestinal anti-inflammatory activity
CNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIA
description Phenylpropanoids are a class of compounds produced by medicinal plants and are biosynthesized from phenylalanine via cinnamic acid. Estravole is a phenylpropanoid that is present as a constituent of essential oils of many plant species, such as Ravensara anisata (Madeira), Ocimum basilicum (Basil) and Croton zehntneri (Cinnamon). Pharmacological activities such as antioxidant, antimicrobial, anxiolytic, skeletal muscle contractile, visceral muscle relaxant, anti-inflammatory and gastroprotective are described. The present work has the general objective to evaluate the intestinal antiulcerogenic and anti-inflammatory activity of trazol in animal models. In the cysteamine-induced duodenal ulcer model, oral (v.o) administration of trazol at doses of 31; 62; 125 and 250 mg/kg) reduced (p<0.001) the ulcerative lesion area (ALU) in rat duodenum. From the gastric ulcer protocol induced by acetic acid, the toxicity was investigated by repeated doses for 14 days. The results showed that the treatment (v.o) with 250 mg/kg of trazol reduced (p<0.001) the ALU, when compared to the control group. This effect was related to an increase in the levels of GSH, SOD, IL-10 and TGFβ (p<0.001) and a reduction (p<0.001) in the levels of MDA, MPO, IL-1β, TNF-α and NFκB. The administration of trazol for 14 days did not change the weight of the organs (heart, liver, spleen and kidneys), nor the biochemical and hematological parameters evaluated. In addition, the test substance protects the animals from reduced water and feed consumption. In the acute induction model of TNBS-induced intestinal inflammation, trazol reduced (p<0.05) the macroscopic lesion score, ALU, weight/length ratio, and diarrheal index at all doses evaluated. In the sub-chronic protocol of ulcerative colitis with relapse, the most effective dose of trazol (250 mg/kg) reduced (p<0.01) the macroscopic lesion score, the ALU and the colonic weight/length ratio. From the acute and sub-chronic colitis protocols, it was observed that trazol (250 mg/kg) reduced (p<0.001) MDA and MPO levels and restored GSH and SOD levels. In addition, it reduced (p<0.001) levels of IL-1β, TNF-α and NFκB, as well as increased TGFβ levels (p<0.001) and restored (p<0.01) IL-10 levels. In the evaluation of the epithelial barrier function, an increase (p<0.001) of the immunostaining for zone of occlusion-1 (ZO-1) was shown. Based on the data analyzed, it can be suggested that trazol has anti-duodenal ulcer activity, gastric healing activity is related to the induction of re-epithelialization of the lesion and low toxicity by repeated doses. And intestinal anti-inflammatory activity in the acute and sub-chronic phase, being related to the cytoprotection of the intestinal barrier through the preservation of gap junctions, antioxidant system and immunomodulation.
publishDate 2023
dc.date.none.fl_str_mv 2023-05-30
2023-03-29
2024-02-26T14:06:43Z
2024-02-26T14:06:43Z
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 https://repositorio.ufpb.br/jspui/handle/123456789/29643
url https://repositorio.ufpb.br/jspui/handle/123456789/29643
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
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instname_str Universidade Federal da Paraíba (UFPB)
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reponame_str Biblioteca Digital de Teses e Dissertações da UFPB
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repository.name.fl_str_mv Biblioteca Digital de Teses e Dissertações da UFPB - Universidade Federal da Paraíba (UFPB)
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