Cochlospermum regium (Mart. ex Schrank) Pilg. : perfil fitoquímico e avaliação da atividade e mecanismo de ação gastroprotetor do extrato hidroetanólico do xilopódio em modelos experimentais agudo e crônico

Detalhes bibliográficos
Autor(a) principal: Oliveira, Darley Maria
Data de Publicação: 2019
Tipo de documento: Tese
Idioma: por
Título da fonte: Repositório Institucional da UFMT
Texto Completo: http://ri.ufmt.br/handle/1/2499
Resumo: Cochlospermum regium (Bixaceae) is a native subshrub of Brazil and its xylopodium (infusion/decoction) is being used for the treatment of gastritis, ulcers, arthritis, infections, skin diseases, among others. The aim of the present study was to evaluate the gastroprotective/antiulcer activity and the mechanism of action of hydroethanolic extract of C. regium xylopodium (HECr), using in vitro and in vivo models. Additionally, phytochemical constituents were identified by high performance liquid chromatography (HPLC). C. regium xylopodium was macerated with ethanol/water to obtain the HECr. The phytochemical characterisation was carried out by HPLC. The antiulcer efficacy of HECr was evaluated using acute acidified ethanol (HCl/EtOH), piroxicam and water immersion-induced experimental ulcer models. Chronic gastric ulcer healing activity of HECr was evaluated through acetic acid induced model. Histological analysis and myeloperoxidase (MPO), glutathione (GSH), catalase (CAT) activities were also evaluated in chronic ulcer induced gastric tissues. The plausible mode of action of the HECr was assessed by estimation of gastric wall mucus production and the role of gastric secretion in pylorus ligature. The animals were also pre-treated with various inhibitors which includes indomethacin (10 mg/kg, p.o.), L-NAME (10 mg/kg, ip.), glibenclamide (5 mg/kg, p.o.) or yohimbine (2 mg/kg, ip.). In vitro, Helicobacter pylori action was done by broth microdilution method. The HPLC analysis data revealed the presence of gallic acid, rutin, myricetin, morin and kaempferol. HECr promoted protective effect against acute ulcers induced by HCl/EtOH with inhibitions of 47.52% (p < 0.01) and 62.69% (p < 0.001) at 100 and 400 mg/kg, and in piroxicam by 34.11% (p < 0.05), 49.14% (p < 0.01) and 61.34% (p < 0.001), at 25, 100 or 400 mg/kg, respectively, and in water restraint stress by 78.26% inhibition, p < 0.001, at the dose of 400 mg/kg when compared to the vehicle control group respectively. In the chronic gastric ulcer model, HECr significantly decreased the injured area. Histological examination indicated that oral treatment of HECr promoted healing of gastric lesions by regenerating gastric mucosa layer with less inflammatory cells. HECr reduced MPO and augmented the CAT activity and augmented GSH level. The pre-treatment with HECr increased and the gastric wall mucus production. It also significantly altered the gastric secretion parameters by causing the reduction in the gastric juice volume and the total acidity and elevated the pH level when compared with the vehicle group. Pre-treatment with inhibitors abolished the gastroprotective effect of HECr at the dose of 100 mg/kg. In microdilution assay, the HECr showed good antiHelicobacter pylori effect with MIC=100 µg/mL. The HECr presented preventive and curative effects in the experimental gastric ulcer models, besides good anti-Helicobacter pylori activity, which supports the traditional medicinal use of the xylopodium of this plant for gastrointestinal diseases. The underlying mechanisms of this antiulcerogenic/antiulcer action involve, at least, augmentation of mucus production, inhibition of gastric secretion, stimulation of PGs and NO synthesis. And that it involves activation of K + ATP channels and α2-adrenergic receptors, in addition to an antioxidant activity, probably due to the presence of gallic acid and flavonoids in HECr.
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spelling Cochlospermum regium (Mart. ex Schrank) Pilg. : perfil fitoquímico e avaliação da atividade e mecanismo de ação gastroprotetor do extrato hidroetanólico do xilopódio em modelos experimentais agudo e crônicoCochlospermum regiumMedicina tradicionalXilopódioAntiúlceraCompostos fenólicosCNPQ::CIENCIAS DA SAUDE::MEDICINACochlospermum regiumTraditional medicineXylopodiumAntiulcerPhenolic compoundsCochlospermum regium (Bixaceae) is a native subshrub of Brazil and its xylopodium (infusion/decoction) is being used for the treatment of gastritis, ulcers, arthritis, infections, skin diseases, among others. The aim of the present study was to evaluate the gastroprotective/antiulcer activity and the mechanism of action of hydroethanolic extract of C. regium xylopodium (HECr), using in vitro and in vivo models. Additionally, phytochemical constituents were identified by high performance liquid chromatography (HPLC). C. regium xylopodium was macerated with ethanol/water to obtain the HECr. The phytochemical characterisation was carried out by HPLC. The antiulcer efficacy of HECr was evaluated using acute acidified ethanol (HCl/EtOH), piroxicam and water immersion-induced experimental ulcer models. Chronic gastric ulcer healing activity of HECr was evaluated through acetic acid induced model. Histological analysis and myeloperoxidase (MPO), glutathione (GSH), catalase (CAT) activities were also evaluated in chronic ulcer induced gastric tissues. The plausible mode of action of the HECr was assessed by estimation of gastric wall mucus production and the role of gastric secretion in pylorus ligature. The animals were also pre-treated with various inhibitors which includes indomethacin (10 mg/kg, p.o.), L-NAME (10 mg/kg, ip.), glibenclamide (5 mg/kg, p.o.) or yohimbine (2 mg/kg, ip.). In vitro, Helicobacter pylori action was done by broth microdilution method. The HPLC analysis data revealed the presence of gallic acid, rutin, myricetin, morin and kaempferol. HECr promoted protective effect against acute ulcers induced by HCl/EtOH with inhibitions of 47.52% (p < 0.01) and 62.69% (p < 0.001) at 100 and 400 mg/kg, and in piroxicam by 34.11% (p < 0.05), 49.14% (p < 0.01) and 61.34% (p < 0.001), at 25, 100 or 400 mg/kg, respectively, and in water restraint stress by 78.26% inhibition, p < 0.001, at the dose of 400 mg/kg when compared to the vehicle control group respectively. In the chronic gastric ulcer model, HECr significantly decreased the injured area. Histological examination indicated that oral treatment of HECr promoted healing of gastric lesions by regenerating gastric mucosa layer with less inflammatory cells. HECr reduced MPO and augmented the CAT activity and augmented GSH level. The pre-treatment with HECr increased and the gastric wall mucus production. It also significantly altered the gastric secretion parameters by causing the reduction in the gastric juice volume and the total acidity and elevated the pH level when compared with the vehicle group. Pre-treatment with inhibitors abolished the gastroprotective effect of HECr at the dose of 100 mg/kg. In microdilution assay, the HECr showed good antiHelicobacter pylori effect with MIC=100 µg/mL. The HECr presented preventive and curative effects in the experimental gastric ulcer models, besides good anti-Helicobacter pylori activity, which supports the traditional medicinal use of the xylopodium of this plant for gastrointestinal diseases. The underlying mechanisms of this antiulcerogenic/antiulcer action involve, at least, augmentation of mucus production, inhibition of gastric secretion, stimulation of PGs and NO synthesis. And that it involves activation of K + ATP channels and α2-adrenergic receptors, in addition to an antioxidant activity, probably due to the presence of gallic acid and flavonoids in HECr.FAPEMATCochlospermum regium (Bixaceae) é um subarbusto nativo do Brasil e cujo xilopódio (infusão/decocção) é utilizado para o tratamento de gastrite, úlceras, artrites, infecções, doenças de pele, entre outras. O estudo objetiva avaliar a atividade antiulcerogênica/antiúlcera e o mecanismo de ação do extrato hidroetanólico do xilopódio de C. regium (EHCr), utilizando modelos in vivo e in vitro. O xilopódio de C. regium foi macerado com etanol/água para obtenção do EHCr. A caracterização fitoquímica foi realizada por CLAE. A atividade antiulcerogênica do EHCr foi avaliada usando modelos agudos de úlceras gástricas induzidas por etanol acidificado (etanol/HCl), piroxicam e estresse por imersão em água e crônico induzida pela aplicação tópica de ácido acético na camada serosa do estômago de camundongos. A análise histológica e as atividades da mieloperoxidase (MPO) e catalase (CAT) e níveis de glutationa (GSH) também foram avaliados em tecidos gástricos de animais ulcerados por ácido acético. Para elucidar possíveis mecanismos de ação antiúlcerogênica do EHCr foram determinados a produção de muco, pelo método de alcian blue. E o volume, acidez livre e total da secreção gástrica, em modelo de ligação pilórica. Noutros experimentos, os camundongos foram pré-tratados com vários inibidores que incluíram indometacina (10 mg/kg, v.o.), L-NAME (10 mg/kg, ip.), glibenclamida (5 mg/kg, v.o.) e ioimbina (2 mg/kg, ip.). A atividade anti-Helicobacter pylori in vitro do EHCr foi determinada em ensaio de microdiluição em caldo. As análises por CLAE do EHCr revelaram as presenças de ácido gálico, rutina, miricetina, morina e kaempferol. Nos modelos de úlceras gástricas agudas, o pré-tratamento com EHCr (100 e 400 mg/kg) reduziu (p < 0,01) as lesões ulcerosas induzidas por etanol/HCl em 47,52% e 62,69%; por piroxicam em 34,11% (p < 0,05), 49,14% (p < 0,01) e 61,34% (p < 0,001) com 25; 100 e 400 mg/kg, respectivamente; por estresse em 78.26% (p < 0,001) com 400 mg/kg, quando comparadas ao grupo veículo. No modelo de úlcera gástrica crônica, o pós-tratamento com EHCr diminuiu a área lesada e o exame histológico do tecido gástrico mostrou redução do edema, infiltrado celular e regeneração da mucosa gástrica. O EHCr reduziu a atividade da MPO, aumentou a atividade da CAT e os níveis de GSH. O pré-tratamento com EHCr reverteu em a redução do muco pelo etanol/HCl. A administração intraduodenal de EHCr reduziu o volume da secreção gástrica e a acidez total e aumentou o pH gástrico. O pré-tratamento com inibidores aboliu o efeito gastroprotetor do EHCr (100 mg/kg). No ensaio de microdiluição, o EHCr apresentou boa atividade anti-Helicobacter pylori in vitro com CIM= 100 µg/mL. O EHCr apresentou efeitos preventivos e curativos nos modelos experimentais de úlcera gástrica, além de boa atividade anti-Helicobacter pylori, que sustenta o uso medicinal tradicional do xilopódio desta planta para doenças gastrintestinais Os mecanismos subjacentes desta ação gastroprotetora envolvem, pelo menos em parte, aumento da produção de muco, inibição da secreção gástrica, estimulação de PG e síntese de NO, ativação de canais de K + ATP e receptores α2-adrenérgicos, além de atividade antioxidante, provavelmente devido à presença de ácido gálico e flavonoides em HECr.Universidade Federal de Mato GrossoBrasilFaculdade de Medicina (FM)UFMT CUC - CuiabáPrograma de Pós-Graduação em Ciências da SaúdeMartins, Domingos Tabajara de OliveiraKaruppusamy, Arunachalamhttp://lattes.cnpq.br/8737379045278143http://lattes.cnpq.br/3794477872946546Martins, Domingos Tabajara de Oliveira109.726.923-04http://lattes.cnpq.br/3794477872946546Lima, Joaquim Corsino da Silva148.059.011-87http://lattes.cnpq.br/4242124025195243109.726.923-04706.801.091-10Lemos, Larissa Maria Scalon517.801.946-68http://lattes.cnpq.br/9276020258429877Beserra, Angela Marcia Selhorst e Silva626.480.552-15http://lattes.cnpq.br/1359644931327470Gazoni, Vanessa Fátima812.348.300-78http://lattes.cnpq.br/9900136032713640Silva Junior, Iberê Ferreira da919.373.611-87http://lattes.cnpq.br/0290268585006188Oliveira, Darley Maria2021-05-13T19:00:53Z2019-06-282021-05-13T19:00:53Z2019-06-27info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/doctoralThesisOLIVEIRA, Darley Maria. Cochlospermum regium (Mart. ex Schrank) Pilg.: perfil fitoquímico e avaliação da atividade e mecanismo de ação gastroprotetor do extrato hidroetanólico do xilopódio em modelos experimentais agudo e crônico. 2019. 78 f. Tese (Doutorado em Ciências da Saúde) - Universidade Federal de Mato Grosso, Faculdade de Medicina, Cuiabá, 2019.http://ri.ufmt.br/handle/1/2499porinfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da UFMTinstname:Universidade Federal de Mato Grosso (UFMT)instacron:UFMT2021-05-19T07:03:05Zoai:localhost:1/2499Repositório InstitucionalPUBhttp://ri.ufmt.br/oai/requestjordanbiblio@gmail.comopendoar:2021-05-19T07:03:05Repositório Institucional da UFMT - Universidade Federal de Mato Grosso (UFMT)false
dc.title.none.fl_str_mv Cochlospermum regium (Mart. ex Schrank) Pilg. : perfil fitoquímico e avaliação da atividade e mecanismo de ação gastroprotetor do extrato hidroetanólico do xilopódio em modelos experimentais agudo e crônico
title Cochlospermum regium (Mart. ex Schrank) Pilg. : perfil fitoquímico e avaliação da atividade e mecanismo de ação gastroprotetor do extrato hidroetanólico do xilopódio em modelos experimentais agudo e crônico
spellingShingle Cochlospermum regium (Mart. ex Schrank) Pilg. : perfil fitoquímico e avaliação da atividade e mecanismo de ação gastroprotetor do extrato hidroetanólico do xilopódio em modelos experimentais agudo e crônico
Oliveira, Darley Maria
Cochlospermum regium
Medicina tradicional
Xilopódio
Antiúlcera
Compostos fenólicos
CNPQ::CIENCIAS DA SAUDE::MEDICINA
Cochlospermum regium
Traditional medicine
Xylopodium
Antiulcer
Phenolic compounds
title_short Cochlospermum regium (Mart. ex Schrank) Pilg. : perfil fitoquímico e avaliação da atividade e mecanismo de ação gastroprotetor do extrato hidroetanólico do xilopódio em modelos experimentais agudo e crônico
title_full Cochlospermum regium (Mart. ex Schrank) Pilg. : perfil fitoquímico e avaliação da atividade e mecanismo de ação gastroprotetor do extrato hidroetanólico do xilopódio em modelos experimentais agudo e crônico
title_fullStr Cochlospermum regium (Mart. ex Schrank) Pilg. : perfil fitoquímico e avaliação da atividade e mecanismo de ação gastroprotetor do extrato hidroetanólico do xilopódio em modelos experimentais agudo e crônico
title_full_unstemmed Cochlospermum regium (Mart. ex Schrank) Pilg. : perfil fitoquímico e avaliação da atividade e mecanismo de ação gastroprotetor do extrato hidroetanólico do xilopódio em modelos experimentais agudo e crônico
title_sort Cochlospermum regium (Mart. ex Schrank) Pilg. : perfil fitoquímico e avaliação da atividade e mecanismo de ação gastroprotetor do extrato hidroetanólico do xilopódio em modelos experimentais agudo e crônico
author Oliveira, Darley Maria
author_facet Oliveira, Darley Maria
author_role author
dc.contributor.none.fl_str_mv Martins, Domingos Tabajara de Oliveira
Karuppusamy, Arunachalam
http://lattes.cnpq.br/8737379045278143
http://lattes.cnpq.br/3794477872946546
Martins, Domingos Tabajara de Oliveira
109.726.923-04
http://lattes.cnpq.br/3794477872946546
Lima, Joaquim Corsino da Silva
148.059.011-87
http://lattes.cnpq.br/4242124025195243
109.726.923-04
706.801.091-10
Lemos, Larissa Maria Scalon
517.801.946-68
http://lattes.cnpq.br/9276020258429877
Beserra, Angela Marcia Selhorst e Silva
626.480.552-15
http://lattes.cnpq.br/1359644931327470
Gazoni, Vanessa Fátima
812.348.300-78
http://lattes.cnpq.br/9900136032713640
Silva Junior, Iberê Ferreira da
919.373.611-87
http://lattes.cnpq.br/0290268585006188
dc.contributor.author.fl_str_mv Oliveira, Darley Maria
dc.subject.por.fl_str_mv Cochlospermum regium
Medicina tradicional
Xilopódio
Antiúlcera
Compostos fenólicos
CNPQ::CIENCIAS DA SAUDE::MEDICINA
Cochlospermum regium
Traditional medicine
Xylopodium
Antiulcer
Phenolic compounds
topic Cochlospermum regium
Medicina tradicional
Xilopódio
Antiúlcera
Compostos fenólicos
CNPQ::CIENCIAS DA SAUDE::MEDICINA
Cochlospermum regium
Traditional medicine
Xylopodium
Antiulcer
Phenolic compounds
description Cochlospermum regium (Bixaceae) is a native subshrub of Brazil and its xylopodium (infusion/decoction) is being used for the treatment of gastritis, ulcers, arthritis, infections, skin diseases, among others. The aim of the present study was to evaluate the gastroprotective/antiulcer activity and the mechanism of action of hydroethanolic extract of C. regium xylopodium (HECr), using in vitro and in vivo models. Additionally, phytochemical constituents were identified by high performance liquid chromatography (HPLC). C. regium xylopodium was macerated with ethanol/water to obtain the HECr. The phytochemical characterisation was carried out by HPLC. The antiulcer efficacy of HECr was evaluated using acute acidified ethanol (HCl/EtOH), piroxicam and water immersion-induced experimental ulcer models. Chronic gastric ulcer healing activity of HECr was evaluated through acetic acid induced model. Histological analysis and myeloperoxidase (MPO), glutathione (GSH), catalase (CAT) activities were also evaluated in chronic ulcer induced gastric tissues. The plausible mode of action of the HECr was assessed by estimation of gastric wall mucus production and the role of gastric secretion in pylorus ligature. The animals were also pre-treated with various inhibitors which includes indomethacin (10 mg/kg, p.o.), L-NAME (10 mg/kg, ip.), glibenclamide (5 mg/kg, p.o.) or yohimbine (2 mg/kg, ip.). In vitro, Helicobacter pylori action was done by broth microdilution method. The HPLC analysis data revealed the presence of gallic acid, rutin, myricetin, morin and kaempferol. HECr promoted protective effect against acute ulcers induced by HCl/EtOH with inhibitions of 47.52% (p < 0.01) and 62.69% (p < 0.001) at 100 and 400 mg/kg, and in piroxicam by 34.11% (p < 0.05), 49.14% (p < 0.01) and 61.34% (p < 0.001), at 25, 100 or 400 mg/kg, respectively, and in water restraint stress by 78.26% inhibition, p < 0.001, at the dose of 400 mg/kg when compared to the vehicle control group respectively. In the chronic gastric ulcer model, HECr significantly decreased the injured area. Histological examination indicated that oral treatment of HECr promoted healing of gastric lesions by regenerating gastric mucosa layer with less inflammatory cells. HECr reduced MPO and augmented the CAT activity and augmented GSH level. The pre-treatment with HECr increased and the gastric wall mucus production. It also significantly altered the gastric secretion parameters by causing the reduction in the gastric juice volume and the total acidity and elevated the pH level when compared with the vehicle group. Pre-treatment with inhibitors abolished the gastroprotective effect of HECr at the dose of 100 mg/kg. In microdilution assay, the HECr showed good antiHelicobacter pylori effect with MIC=100 µg/mL. The HECr presented preventive and curative effects in the experimental gastric ulcer models, besides good anti-Helicobacter pylori activity, which supports the traditional medicinal use of the xylopodium of this plant for gastrointestinal diseases. The underlying mechanisms of this antiulcerogenic/antiulcer action involve, at least, augmentation of mucus production, inhibition of gastric secretion, stimulation of PGs and NO synthesis. And that it involves activation of K + ATP channels and α2-adrenergic receptors, in addition to an antioxidant activity, probably due to the presence of gallic acid and flavonoids in HECr.
publishDate 2019
dc.date.none.fl_str_mv 2019-06-28
2019-06-27
2021-05-13T19:00:53Z
2021-05-13T19:00:53Z
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 OLIVEIRA, Darley Maria. Cochlospermum regium (Mart. ex Schrank) Pilg.: perfil fitoquímico e avaliação da atividade e mecanismo de ação gastroprotetor do extrato hidroetanólico do xilopódio em modelos experimentais agudo e crônico. 2019. 78 f. Tese (Doutorado em Ciências da Saúde) - Universidade Federal de Mato Grosso, Faculdade de Medicina, Cuiabá, 2019.
http://ri.ufmt.br/handle/1/2499
identifier_str_mv OLIVEIRA, Darley Maria. Cochlospermum regium (Mart. ex Schrank) Pilg.: perfil fitoquímico e avaliação da atividade e mecanismo de ação gastroprotetor do extrato hidroetanólico do xilopódio em modelos experimentais agudo e crônico. 2019. 78 f. Tese (Doutorado em Ciências da Saúde) - Universidade Federal de Mato Grosso, Faculdade de Medicina, Cuiabá, 2019.
url http://ri.ufmt.br/handle/1/2499
dc.language.iso.fl_str_mv por
language por
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.publisher.none.fl_str_mv Universidade Federal de Mato Grosso
Brasil
Faculdade de Medicina (FM)
UFMT CUC - Cuiabá
Programa de Pós-Graduação em Ciências da Saúde
publisher.none.fl_str_mv Universidade Federal de Mato Grosso
Brasil
Faculdade de Medicina (FM)
UFMT CUC - Cuiabá
Programa de Pós-Graduação em Ciências da Saúde
dc.source.none.fl_str_mv reponame:Repositório Institucional da UFMT
instname:Universidade Federal de Mato Grosso (UFMT)
instacron:UFMT
instname_str Universidade Federal de Mato Grosso (UFMT)
instacron_str UFMT
institution UFMT
reponame_str Repositório Institucional da UFMT
collection Repositório Institucional da UFMT
repository.name.fl_str_mv Repositório Institucional da UFMT - Universidade Federal de Mato Grosso (UFMT)
repository.mail.fl_str_mv jordanbiblio@gmail.com
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