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
Autor(a) principal: | |
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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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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 |
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por |
language |
por |
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info:eu-repo/semantics/openAccess |
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openAccess |
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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 |
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Universidade Federal de Mato Grosso (UFMT) |
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UFMT |
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UFMT |
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Repositório Institucional da UFMT |
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Repositório Institucional da UFMT - Universidade Federal de Mato Grosso (UFMT) |
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jordanbiblio@gmail.com |
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1804648507634614272 |