Efeito gastroprotetor da baicaleína na mucosa gástrica de camundongos

Detalhes bibliográficos
Autor(a) principal: Ribeiro, Ana Roseli Silva
Data de Publicação: 2017
Tipo de documento: Tese
Idioma: por
Título da fonte: Repositório Institucional da UFS
Texto Completo: https://ri.ufs.br/handle/riufs/3964
Resumo: Gastric ulcer is a disease characterized by bleeding, stenosis and perforations of the gastric mucosa that can lead the patient to death. Many flavonoids have been shown to be promising for the treatment of these gastric lesions. Baicalein, a flavonoid present in Scutellaria baicalensis Georgi root (Lamiaceae), a medicinal plant widely used by Chinese medicine to treat peptic ulcers, has pharmacological properties, such as anti-inflammatory, antinociceptive, anticancer, antioxidant and antimicrobial. However, the effect of baicalein on gastric mucosa has not yet been reported. The objective of this study was to evaluate the protective and antisecretory properties of baicalein on the gastric mucosa of mice. The ethanol/HCl-induced ulcer model (60% ethanol/0.3 M HCl) was used to evaluate the protective effect of baicalein (10, 30 and 100 mg/kg) on the gastric mucosa. The participation of α2-adrenoreceptors, nonprotein sulfhydryl compounds (NP-SH), nitric oxide (NO), prostaglandin (PG), ATP-sensitive K+ channels in the gastroprotective effect of baicalein (30 mg/kg), levels of glutathione (GSH) and myeloperoxidase (MPO) activity in gastric tissue were also evaluated through the acidified ethanol induced ulcer model. The antisecretory effect of gastric acid of baicalein (10-100 mg/kg) was evaluated through the pylorus ligation model, in which the parameters of gastric secretion (volume, [H+] and pH) were evaluated in the presence or absence of the secretagogue agent histamine and mucus in the gastric contents. The in vitro activity of H+, K+-ATPase (proton pump) was also determined. Baicalein (10-100 mg/kg) presented a dose-dependent gastroprotective effect (p <0.001) against gastric lesions induced by acidified ethanol. Pretreatment by the intraperitoneal route with an α2 -adrenoreceptor antagonist (yohimbine, 2 mg/kg), a non-protein sulfide compounds blocker (N-ethylmaleimide, NEM, 10 mg/kg), a nonselective inhibitor of the NO synthase (Nw-nitro-L-arginine, L-NAME, 10 mg/kg), a nonselective cyclooxygenase inhibitor (indomethacin, 10 mg/kg) or an ATP-dependent potassium channel blocker (glibenclamide, 10 mg/kg) inhibited the gastroprotective response caused by baicalein (30 mg/kg) (p<0.001). Baicalein (30 mg/kg, p<0.05) was able to increase GSH levels and decrease MPO activity in stomach tissue exposed to the deleterious effect of acidified ethanol. Treatment with baicalein (30 and 100 mg/kg) significantly increased (p<0.05) gastric mucus secretion. In addition, treatment with baicalein reduced the volume of secretion and total acid secretion (30 and 100 mg/kg, p<0.05) and also increased (10, 30 and 100 mg/kg, p<0.001) the value of pH. Baicalein (30 mg/kg) was also effective to inhibi the effects of histamine on gastric secretion (volume, [H+] and pH, p<0.001). Baicalein 10 and 30 μg/mL demonstrated anti-H+, K+-ATPase activity. The present results provide convincing evidence that baicalein can be used as a cytoprotective agent (preventive effect) and anti-ulcer (antisecretory effect) in gastric ulcers treatment.
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spelling Ribeiro, Ana Roseli SilvaThomazzi, Sara Mariahttp://lattes.cnpq.br/60048075542771592017-09-26T12:28:37Z2017-09-26T12:28:37Z2017-01-27RIBEIRO, Ana Roseli Silva. Efeito gastroprotetor da baicaleína na mucosa gástrica de camundongos. 2017. 83 f. Tese (Pós-Graduação em Ciências Fisiológicas) - Universidade Federal de Sergipe, São Cristóvão, 2017.https://ri.ufs.br/handle/riufs/3964Gastric ulcer is a disease characterized by bleeding, stenosis and perforations of the gastric mucosa that can lead the patient to death. Many flavonoids have been shown to be promising for the treatment of these gastric lesions. Baicalein, a flavonoid present in Scutellaria baicalensis Georgi root (Lamiaceae), a medicinal plant widely used by Chinese medicine to treat peptic ulcers, has pharmacological properties, such as anti-inflammatory, antinociceptive, anticancer, antioxidant and antimicrobial. However, the effect of baicalein on gastric mucosa has not yet been reported. The objective of this study was to evaluate the protective and antisecretory properties of baicalein on the gastric mucosa of mice. The ethanol/HCl-induced ulcer model (60% ethanol/0.3 M HCl) was used to evaluate the protective effect of baicalein (10, 30 and 100 mg/kg) on the gastric mucosa. The participation of α2-adrenoreceptors, nonprotein sulfhydryl compounds (NP-SH), nitric oxide (NO), prostaglandin (PG), ATP-sensitive K+ channels in the gastroprotective effect of baicalein (30 mg/kg), levels of glutathione (GSH) and myeloperoxidase (MPO) activity in gastric tissue were also evaluated through the acidified ethanol induced ulcer model. The antisecretory effect of gastric acid of baicalein (10-100 mg/kg) was evaluated through the pylorus ligation model, in which the parameters of gastric secretion (volume, [H+] and pH) were evaluated in the presence or absence of the secretagogue agent histamine and mucus in the gastric contents. The in vitro activity of H+, K+-ATPase (proton pump) was also determined. Baicalein (10-100 mg/kg) presented a dose-dependent gastroprotective effect (p <0.001) against gastric lesions induced by acidified ethanol. Pretreatment by the intraperitoneal route with an α2 -adrenoreceptor antagonist (yohimbine, 2 mg/kg), a non-protein sulfide compounds blocker (N-ethylmaleimide, NEM, 10 mg/kg), a nonselective inhibitor of the NO synthase (Nw-nitro-L-arginine, L-NAME, 10 mg/kg), a nonselective cyclooxygenase inhibitor (indomethacin, 10 mg/kg) or an ATP-dependent potassium channel blocker (glibenclamide, 10 mg/kg) inhibited the gastroprotective response caused by baicalein (30 mg/kg) (p<0.001). Baicalein (30 mg/kg, p<0.05) was able to increase GSH levels and decrease MPO activity in stomach tissue exposed to the deleterious effect of acidified ethanol. Treatment with baicalein (30 and 100 mg/kg) significantly increased (p<0.05) gastric mucus secretion. In addition, treatment with baicalein reduced the volume of secretion and total acid secretion (30 and 100 mg/kg, p<0.05) and also increased (10, 30 and 100 mg/kg, p<0.001) the value of pH. Baicalein (30 mg/kg) was also effective to inhibi the effects of histamine on gastric secretion (volume, [H+] and pH, p<0.001). Baicalein 10 and 30 μg/mL demonstrated anti-H+, K+-ATPase activity. The present results provide convincing evidence that baicalein can be used as a cytoprotective agent (preventive effect) and anti-ulcer (antisecretory effect) in gastric ulcers treatment.A úlcera gástrica é uma doença caracterizada por sangramentos, estenoses e perfurações da mucosa gástrica podendo levar o paciente à morte. Muitos flavonoides demonstraram ser promissores para o tratamento dessas lesões gástricas. A baicaleína, um flavonoide presente na raiz da Scutellaria baicalensis Georgi (Lamiaceae), planta medicinal bastante utilizada pela medicina chinesa para tratamento das úlceras pépticas, possui propriedades farmacológicas como anti-inflamatória, antinociceptiva, anticancerígena, antioxidante e antimicrobiana, entretanto o efeito da baicaleína sobre a mucosa gástrica ainda não foi relatado. Portanto, o objetivo deste estudo foi avaliar as propriedades protetora e antissecretória da baicaleína sobre a mucosa gástrica de camundongos. O modelo de úlcera induzida por etanol acidificado (etanol a 60%/HCl a 0,3 M) foi utilizado para avaliar o efeito protetor da baicaleína (10, 30 e 100 mg/kg) sobre a mucosa gástrica. A participação dos receptores α2-adrenérgicos, compostos sulfidrílicos não proteicos (NP-SH), óxido nítrico (NO), prostaglandina (PG), canais K+ ATP no efeito gastroprotetor da baicaleína (30 mg/kg) e os níveis de glutationa (GSH) e a atividade da enzima mieloperoxidase (MPO) no tecido gástrico também foram avaliados através do modelo de úlcera induzida por etanol acidificado. O efeito antissecretório da baicaleína sobre o ácido gástrico da baicaleína (10, 30 e 100 mg/kg) foi avaliado no modelo de ligadura do piloro, em que os parâmetros da secreção gástrica (volume, [H+] e pH) na presença ou ausência do agente secretagogo histamina, bem como muco no conteúdo gástrico foram avaliados. A atividade in vitro da H+, K+-ATPase (bomba de prótons) também foi determinada. A baicaleína (10-100 mg/kg) apresentou efeito gastroprotetor dose-dependente (p<0,001) contra as lesões gástricas induzidas pelo etanol acidificado. O pré-tratamento pela via intraperitoneal com um antagonista dos receptores α2-adrenérgicos (ioimbina, 2 mg/kg), um bloqueador dos grupamentos sulfidrílicos não proteicos (N-etilmaleimida, NEM, 10 mg/kg), um inibidor não seletivo da sintase do NO (Nw-nitro- L-arginina, L-NAME, 10 mg/kg), um inibidor não seletivo da ciclooxigenase (indometacina, 10 mg/kg) ou um bloqueador de canais para potássio sensíveis a ATP (glibenclamida, 10 mg/kg) inibiram a resposta gastroprotetora causada pela baicaleína (30 mg/kg) (p<0,001). Este flavonoide aumentou a concentração de GSH e diminuiu a atividade da MPO no tecido estomacal exposto ao efeito deletério do etanol acidificado. O tratamento com baicaleína (30 e 100 mg/kg) aumentou significativamente (p<0,05) a secreção do muco gástrico, assim como reduziu (30 e 100 mg/kg, p<0,05) o volume de secreção e secreção ácida total, e também aumentou (10, 30 e 100 mg/kg, p<0,001) o valor do pH. A baicaleína (30 mg/kg) também foi eficaz na inibição dos efeitos da histamina na secreção gástrica (volume, [H+] e pH, p<0,001). A baicaleína 10 e 30 μg/mL demonstrou atividade inibitória da H+, K+- ATPase. Os resultados apresentados fornecem evidências de que a baicaleína pode ser utilizada como um agente citoprotetor e antissecretório no tratamento das úlceras gástricas.Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - CAPESapplication/pdfporUniversidade Federal de SergipePós-Graduação em Ciências FisiológicasUFSBrasilFisiologiaUlceras gástricasFlavonóidesAntioxidantesBaicaleínaGastroproteçãoGastric ulcerGastroprotectionFlavonoidsBaicaleinCIENCIAS BIOLOGICAS::FISIOLOGIAEfeito gastroprotetor da baicaleína na mucosa gástrica de camundongosGastroprotective effects of baicalein in gastric mucosa of miceinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/doctoralThesisinfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da UFSinstname:Universidade Federal de Sergipe (UFS)instacron:UFSORIGINALANA_ROSELI_SILVA_RIBEIRO.pdfapplication/pdf2470948https://ri.ufs.br/jspui/bitstream/riufs/3964/1/ANA_ROSELI_SILVA_RIBEIRO.pdfe1ec710c964e37c9aaa64530818aaa0fMD51TEXTANA_ROSELI_SILVA_RIBEIRO.pdf.txtANA_ROSELI_SILVA_RIBEIRO.pdf.txtExtracted texttext/plain133547https://ri.ufs.br/jspui/bitstream/riufs/3964/2/ANA_ROSELI_SILVA_RIBEIRO.pdf.txtc0eb2b5e2337868268a6dfea100c63ffMD52THUMBNAILANA_ROSELI_SILVA_RIBEIRO.pdf.jpgANA_ROSELI_SILVA_RIBEIRO.pdf.jpgGenerated Thumbnailimage/jpeg1272https://ri.ufs.br/jspui/bitstream/riufs/3964/3/ANA_ROSELI_SILVA_RIBEIRO.pdf.jpgae38fd81872a7a2d61e54aa36c3e2b17MD53riufs/39642017-11-24 21:45:52.658oai:ufs.br:riufs/3964Repositório InstitucionalPUBhttps://ri.ufs.br/oai/requestrepositorio@academico.ufs.bropendoar:2017-11-25T00:45:52Repositório Institucional da UFS - Universidade Federal de Sergipe (UFS)false
dc.title.por.fl_str_mv Efeito gastroprotetor da baicaleína na mucosa gástrica de camundongos
dc.title.alternative.eng.fl_str_mv Gastroprotective effects of baicalein in gastric mucosa of mice
title Efeito gastroprotetor da baicaleína na mucosa gástrica de camundongos
spellingShingle Efeito gastroprotetor da baicaleína na mucosa gástrica de camundongos
Ribeiro, Ana Roseli Silva
Fisiologia
Ulceras gástricas
Flavonóides
Antioxidantes
Baicaleína
Gastroproteção
Gastric ulcer
Gastroprotection
Flavonoids
Baicalein
CIENCIAS BIOLOGICAS::FISIOLOGIA
title_short Efeito gastroprotetor da baicaleína na mucosa gástrica de camundongos
title_full Efeito gastroprotetor da baicaleína na mucosa gástrica de camundongos
title_fullStr Efeito gastroprotetor da baicaleína na mucosa gástrica de camundongos
title_full_unstemmed Efeito gastroprotetor da baicaleína na mucosa gástrica de camundongos
title_sort Efeito gastroprotetor da baicaleína na mucosa gástrica de camundongos
author Ribeiro, Ana Roseli Silva
author_facet Ribeiro, Ana Roseli Silva
author_role author
dc.contributor.author.fl_str_mv Ribeiro, Ana Roseli Silva
dc.contributor.advisor1.fl_str_mv Thomazzi, Sara Maria
dc.contributor.authorLattes.fl_str_mv http://lattes.cnpq.br/6004807554277159
contributor_str_mv Thomazzi, Sara Maria
dc.subject.por.fl_str_mv Fisiologia
Ulceras gástricas
Flavonóides
Antioxidantes
Baicaleína
Gastroproteção
topic Fisiologia
Ulceras gástricas
Flavonóides
Antioxidantes
Baicaleína
Gastroproteção
Gastric ulcer
Gastroprotection
Flavonoids
Baicalein
CIENCIAS BIOLOGICAS::FISIOLOGIA
dc.subject.eng.fl_str_mv Gastric ulcer
Gastroprotection
Flavonoids
Baicalein
dc.subject.cnpq.fl_str_mv CIENCIAS BIOLOGICAS::FISIOLOGIA
description Gastric ulcer is a disease characterized by bleeding, stenosis and perforations of the gastric mucosa that can lead the patient to death. Many flavonoids have been shown to be promising for the treatment of these gastric lesions. Baicalein, a flavonoid present in Scutellaria baicalensis Georgi root (Lamiaceae), a medicinal plant widely used by Chinese medicine to treat peptic ulcers, has pharmacological properties, such as anti-inflammatory, antinociceptive, anticancer, antioxidant and antimicrobial. However, the effect of baicalein on gastric mucosa has not yet been reported. The objective of this study was to evaluate the protective and antisecretory properties of baicalein on the gastric mucosa of mice. The ethanol/HCl-induced ulcer model (60% ethanol/0.3 M HCl) was used to evaluate the protective effect of baicalein (10, 30 and 100 mg/kg) on the gastric mucosa. The participation of α2-adrenoreceptors, nonprotein sulfhydryl compounds (NP-SH), nitric oxide (NO), prostaglandin (PG), ATP-sensitive K+ channels in the gastroprotective effect of baicalein (30 mg/kg), levels of glutathione (GSH) and myeloperoxidase (MPO) activity in gastric tissue were also evaluated through the acidified ethanol induced ulcer model. The antisecretory effect of gastric acid of baicalein (10-100 mg/kg) was evaluated through the pylorus ligation model, in which the parameters of gastric secretion (volume, [H+] and pH) were evaluated in the presence or absence of the secretagogue agent histamine and mucus in the gastric contents. The in vitro activity of H+, K+-ATPase (proton pump) was also determined. Baicalein (10-100 mg/kg) presented a dose-dependent gastroprotective effect (p <0.001) against gastric lesions induced by acidified ethanol. Pretreatment by the intraperitoneal route with an α2 -adrenoreceptor antagonist (yohimbine, 2 mg/kg), a non-protein sulfide compounds blocker (N-ethylmaleimide, NEM, 10 mg/kg), a nonselective inhibitor of the NO synthase (Nw-nitro-L-arginine, L-NAME, 10 mg/kg), a nonselective cyclooxygenase inhibitor (indomethacin, 10 mg/kg) or an ATP-dependent potassium channel blocker (glibenclamide, 10 mg/kg) inhibited the gastroprotective response caused by baicalein (30 mg/kg) (p<0.001). Baicalein (30 mg/kg, p<0.05) was able to increase GSH levels and decrease MPO activity in stomach tissue exposed to the deleterious effect of acidified ethanol. Treatment with baicalein (30 and 100 mg/kg) significantly increased (p<0.05) gastric mucus secretion. In addition, treatment with baicalein reduced the volume of secretion and total acid secretion (30 and 100 mg/kg, p<0.05) and also increased (10, 30 and 100 mg/kg, p<0.001) the value of pH. Baicalein (30 mg/kg) was also effective to inhibi the effects of histamine on gastric secretion (volume, [H+] and pH, p<0.001). Baicalein 10 and 30 μg/mL demonstrated anti-H+, K+-ATPase activity. The present results provide convincing evidence that baicalein can be used as a cytoprotective agent (preventive effect) and anti-ulcer (antisecretory effect) in gastric ulcers treatment.
publishDate 2017
dc.date.accessioned.fl_str_mv 2017-09-26T12:28:37Z
dc.date.available.fl_str_mv 2017-09-26T12:28:37Z
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dc.identifier.citation.fl_str_mv RIBEIRO, Ana Roseli Silva. Efeito gastroprotetor da baicaleína na mucosa gástrica de camundongos. 2017. 83 f. Tese (Pós-Graduação em Ciências Fisiológicas) - Universidade Federal de Sergipe, São Cristóvão, 2017.
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identifier_str_mv RIBEIRO, Ana Roseli Silva. Efeito gastroprotetor da baicaleína na mucosa gástrica de camundongos. 2017. 83 f. Tese (Pós-Graduação em Ciências Fisiológicas) - Universidade Federal de Sergipe, São Cristóvão, 2017.
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