Análise fitoquímicas e avaliação da atividade e do mecanismo de ação antiúlcera do extrato hidroetanólico das folhas de Helicteres sacarolha A. St. – Hil. et al.
Autor(a) principal: | |
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Data de Publicação: | 2014 |
Tipo de documento: | Tese |
Idioma: | por |
Título da fonte: | Repositório Institucional da UFMT |
Texto Completo: | http://ri.ufmt.br/handle/1/3332 |
Resumo: | Helicteres sacarolha Kunth. (Malvaceae) is a plant found in the Amazon region of Brazil and widely used in folk medicine of several countries for the treatment of gastric disorders, inflammation and infections. The aim of this study was to evaluate the acute and chronic toxicity, the preventive activities (gastroprotective) and curative (anti-ulcer) of hydroethanolic extract of Helicteres sacarolha (EHHs) and to elucidate the possible mechanisms involved in these activities. Additionally, phytochemical analyzes were carried out on EHHs. The leaves of Helicteres sacarolha were macerated in 75% hydroethanol (1:3 w / v) to obtain HEHs. Cytotoxicity of EHHs was evaluated in CHO-K1 and RAW 264.7 cells by the method of Alamar blue and acute animal toxicity in Swiss-Webster mice by Hippocratic test. The subchronic toxicity was evaluated in Wistar rats treated for 30 days with fixed doses of HEHs. Secondary metabolites were analyzed and confirmed by thin layer chromatography (TLC), spectrophotometry and high performance liquid chromatography (HPLC). The gastroprotective activity was assessed using gastric ulcer models of acidified ethanol, piroxicam, water restraint stress (acute models) and acetic acid (chronic) in rodents. The anti-Helicobacter pylori potential of HEHs was evaluated by broth microdilution method studies, determining the minimum inhibitory concentration (MIC). Antioxidant studies in vitro (DPPH, FRAP, chelating iron and linoleic acid tests) and in vivo (catalase and myeloperoxidase) were evaluated. The antisecretory activity of HEHs was assessed by the pylorus ligation in rats the likely mechanism of action of HEHs was evaluated ulcerated animals with acidified ethanol and pretreated with yohimbine, glibenclamide, indomethacin and L-NAME. The profile of proinflammatory and anti-inflammatory cytokines was evaluated in acetic acid ulcerated animals. HEHs presented low cytotoxicity in CHO-K1 and RAW 264.7, with IC50> 200 /mL. When administered orally at doses up to 2000 mg / kg in male mice and 4000 mg / kg in female mice, caused no change HEHs in signs and symptoms evaluated. In the subchronic toxicity test no significant changes were observed by treatment with HEHs in the parameters observed, except elevation of leukocytes (28%), basophils (ca.4 times) and decrease of neutrophils (18%), monocytes (65%) , hemoglobin (3.6%) and hematocrit (6.5%) that were not followed by clinical and hsitopatológicas changes. Total phenols and flavonoids were 19.9% and 14.4% respectively. The major compounds detected in HEHs were ellagic acid (6%) and morin (0.3%). HEHs demonstrated antiulcer activitis in the acute and chronic ulcer models. The antiulcer activity of HEHs involved the participation of NO, α-receptor, prostaglandins, K+ - ATP channels and antioxidant mechanisms and is dependent only on inhibition of gastric volume but not the acid secretion mechanisms. The ulcer healing action of HEHs involved attenuation of pro-inflammatory cytokines. HEHs was inactive against Helicobacter pylori. The results of this study confirm the popular use of the leaves of Helicteres sacarolha in gastric ulcers and that HEHs has low toxicity and a multitargeted action. The main metabolic constituents are the phenols and flavonoids, with ellagic acid and morin being the major classes of compounds. Ellagic acid is possibly involved in the gastroprotective antiulcer action of HEHs. Further experiments are required to advance preclinical validation of HEHs with the aim of developing an anti-ulcer phytotherapy. |
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Análise fitoquímicas e avaliação da atividade e do mecanismo de ação antiúlcera do extrato hidroetanólico das folhas de Helicteres sacarolha A. St. – Hil. et al.Helicteres sacarolhaÚlcera gástricaCicatrizanteToxicidadeAntioxidanteCompostos fenólicosCNPQ::CIENCIAS DA SAUDEHelicteres sacarolhaGastric ulcerUlcer healingToxicityAntioxidantPhenolic compoundsHelicteres sacarolha Kunth. (Malvaceae) is a plant found in the Amazon region of Brazil and widely used in folk medicine of several countries for the treatment of gastric disorders, inflammation and infections. The aim of this study was to evaluate the acute and chronic toxicity, the preventive activities (gastroprotective) and curative (anti-ulcer) of hydroethanolic extract of Helicteres sacarolha (EHHs) and to elucidate the possible mechanisms involved in these activities. Additionally, phytochemical analyzes were carried out on EHHs. The leaves of Helicteres sacarolha were macerated in 75% hydroethanol (1:3 w / v) to obtain HEHs. Cytotoxicity of EHHs was evaluated in CHO-K1 and RAW 264.7 cells by the method of Alamar blue and acute animal toxicity in Swiss-Webster mice by Hippocratic test. The subchronic toxicity was evaluated in Wistar rats treated for 30 days with fixed doses of HEHs. Secondary metabolites were analyzed and confirmed by thin layer chromatography (TLC), spectrophotometry and high performance liquid chromatography (HPLC). The gastroprotective activity was assessed using gastric ulcer models of acidified ethanol, piroxicam, water restraint stress (acute models) and acetic acid (chronic) in rodents. The anti-Helicobacter pylori potential of HEHs was evaluated by broth microdilution method studies, determining the minimum inhibitory concentration (MIC). Antioxidant studies in vitro (DPPH, FRAP, chelating iron and linoleic acid tests) and in vivo (catalase and myeloperoxidase) were evaluated. The antisecretory activity of HEHs was assessed by the pylorus ligation in rats the likely mechanism of action of HEHs was evaluated ulcerated animals with acidified ethanol and pretreated with yohimbine, glibenclamide, indomethacin and L-NAME. The profile of proinflammatory and anti-inflammatory cytokines was evaluated in acetic acid ulcerated animals. HEHs presented low cytotoxicity in CHO-K1 and RAW 264.7, with IC50> 200 /mL. When administered orally at doses up to 2000 mg / kg in male mice and 4000 mg / kg in female mice, caused no change HEHs in signs and symptoms evaluated. In the subchronic toxicity test no significant changes were observed by treatment with HEHs in the parameters observed, except elevation of leukocytes (28%), basophils (ca.4 times) and decrease of neutrophils (18%), monocytes (65%) , hemoglobin (3.6%) and hematocrit (6.5%) that were not followed by clinical and hsitopatológicas changes. Total phenols and flavonoids were 19.9% and 14.4% respectively. The major compounds detected in HEHs were ellagic acid (6%) and morin (0.3%). HEHs demonstrated antiulcer activitis in the acute and chronic ulcer models. The antiulcer activity of HEHs involved the participation of NO, α-receptor, prostaglandins, K+ - ATP channels and antioxidant mechanisms and is dependent only on inhibition of gastric volume but not the acid secretion mechanisms. The ulcer healing action of HEHs involved attenuation of pro-inflammatory cytokines. HEHs was inactive against Helicobacter pylori. The results of this study confirm the popular use of the leaves of Helicteres sacarolha in gastric ulcers and that HEHs has low toxicity and a multitargeted action. The main metabolic constituents are the phenols and flavonoids, with ellagic acid and morin being the major classes of compounds. Ellagic acid is possibly involved in the gastroprotective antiulcer action of HEHs. Further experiments are required to advance preclinical validation of HEHs with the aim of developing an anti-ulcer phytotherapy.Helicteres sacarolha A. St. - Hil (Malvaceae) é uma planta encontrada na região Amazônica do Brasil e amplamente empregada na medicina popular de Brasil e Bolivia para o tratamento de distúrbios gástricos, inflamação e infecções. O objetivo deste estudo foi avaliar a toxicidade aguda e crônica, as atividades preventiva (gastroprotetora) e curativa (antiúlcera) do extrato hidroetanólico das folhas de Helicteres sacarolha (EHHs) e elucidar os possíveis mecanismos de ação envolvidos nestas atividades. Adicionalmente, foram realizadas as análises químicas do EHHs. As folhas de Helicteres sacarolha foram maceradas em solução hidroetanólica 75% (1:3 p/v) para obter o EHHs. A citotoxicidade do EHHs foi avaliada em células CHOk1 e RAW 264.7 pelo método de azul de Alamar e a toxicidade aguda animal em camundos Swiss-Webster através do teste Hipocrático. A toxicidade subcrônica foi avaliada em ratos Wistar tratados por 30 dias com doses fixas do EHHs. Os metabólitos secundários foram analisados e confirmados por cromatografia em camada delgada (CCD), espectrofotometria e cromatografia líquida de alta eficiência (CLAE). A atividade gastroprotetora foi avaliada usando os modelos de úlcera gástrica por etanol acidificado, piroxicam, estresse por contenção em água (modelos agudos) e ácido acético (crônico) em roedores. O potencial anti-Helicobacter pylori do EHHS foi avaliado pelo método de microdiluição em caldo, determinando a concentração inibitória mínima (CIM). Estudos antioxidantes in vivo (catalase e MPO) e in vitro (DPPH, FRAP, quelante de ferro e ácido linoleico) foram realizados. A atividade antissecretória do EHHs foi avaliada pela ligadura do piloro de ratos O provável mecanismo de ação do EHHs foi avaliado em animais ulcerados por etanol acidificado e pré-tratados com ioimbina, glibenclamida, indometacina, L-NAME e muco gástrico. O perfil de citocinas pró-inflamatórias e anti-inflamatória foi auferido em animais ulceradso por ácido acético. O EHHs apresentou baixa citotoxicidade em CHO-k1 e RAW 264.7, com CI50>200 μg/mL. Quando administrado oralmente, em doses até 2000 mg/kg em camundongos machos e 4000 mg/kg em camundogos fêmeas, o EHHs não causou alterações dos sinais e sintomas analisados. No teste de toxicidade subrônica não foram verificadas alterações relevantes ao tratamento com EHHs nos parâmetros observados, a não ser elevação de leucócitos (28%), basófilos (ca.4 vezes) e redução de neutrófilos (18%), monócitos (65%), hemoglobina (3,6%) e hematócrito (6,5%) que não foram seguidas de allterações clínicas e hsitopatológicas. O EHHs apresentou 19,9% de fenois totais e 14,4% de flavonoides. Os compostos majoritários presentes no EHHs foram o ácido elágico (6%) e morina (0,3%). O EHHs apresentou atividade antiúlcera aguda e crônica. Participam na ação gastroprotetora do EHHs, NO, α2-adrenoceptores, prostaglandinas, canais de K+ ATP e mecanismos antioxidantes, sem o envolvimento de mecanismos antissecretórios. Na ação cicatrizante da úlcera pelo EHHs, estão envolvidos a inibição de citocinas pró-inflamatórias. O EHHs foi inativo frente ao Helicobacter pylori. Os resultados desse estudo comprovam o uso popular das folhas de Helicteres sacarolha em úlceras gástricas e que o EHHs tem baixa toxicidade e ação multialvo, tendo como principais classes metabólicas os fenois e flavonoides e como compostos majoritários possivelmente envolvidos na ação gastroprotetora e antiúlcera o ácido elágico. Mais ensaios são necesários para avançar na validação pré-clínica do EHHs, visando o desenvolvimento de um fitoterápico antiúlcera.Universidade Federal de Mato GrossoBrasilFaculdade de Medicina (FM)UFMT CUC - CuiabáPrograma de Pós-Graduação em Ciências da SaúdeMartins, Domingos Tabajara de Oliveirahttp://lattes.cnpq.br/3794477872946546Martins, Domingos Tabajara de Oliveira109.726.923-04http://lattes.cnpq.br/3794477872946546Lopes, Lousã879.675.298-04http://lattes.cnpq.br/8843725522665416109.726.923-04Adzu, Bulus705.985.581-52http://lattes.cnpq.br/5877616611156488Jesus, Neyres Zínia Taveira de469.179.851-04http://lattes.cnpq.br/2760653304094924Cechinel Filho, Valdir443.476.009-25http://lattes.cnpq.br/8521384605324445Balogun, Sikiru Olaitan2022-06-10T19:03:18Z2015-08-212022-06-10T19:03:18Z2014-10-09info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/doctoralThesisBALOGUN, Sikiru Olaitan. Análise fitoquímicas e avaliação da atividade e do mecanismo de ação antiúlcera do extrato hidroetanólico das folhas de Helicteres sacarolha A. St. – Hil. et al. 2014. 117 f. Tese (Doutorado em Ciências da Saúde) - Universidade Federal de Mato Grosso, Faculdade de Medicina, Cuiabá, 2014.http://ri.ufmt.br/handle/1/3332porinfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da UFMTinstname:Universidade Federal de Mato Grosso (UFMT)instacron:UFMT2022-06-14T07:03:00Zoai:localhost:1/3332Repositório InstitucionalPUBhttp://ri.ufmt.br/oai/requestjordanbiblio@gmail.comopendoar:2022-06-14T07:03Repositório Institucional da UFMT - Universidade Federal de Mato Grosso (UFMT)false |
dc.title.none.fl_str_mv |
Análise fitoquímicas e avaliação da atividade e do mecanismo de ação antiúlcera do extrato hidroetanólico das folhas de Helicteres sacarolha A. St. – Hil. et al. |
title |
Análise fitoquímicas e avaliação da atividade e do mecanismo de ação antiúlcera do extrato hidroetanólico das folhas de Helicteres sacarolha A. St. – Hil. et al. |
spellingShingle |
Análise fitoquímicas e avaliação da atividade e do mecanismo de ação antiúlcera do extrato hidroetanólico das folhas de Helicteres sacarolha A. St. – Hil. et al. Balogun, Sikiru Olaitan Helicteres sacarolha Úlcera gástrica Cicatrizante Toxicidade Antioxidante Compostos fenólicos CNPQ::CIENCIAS DA SAUDE Helicteres sacarolha Gastric ulcer Ulcer healing Toxicity Antioxidant Phenolic compounds |
title_short |
Análise fitoquímicas e avaliação da atividade e do mecanismo de ação antiúlcera do extrato hidroetanólico das folhas de Helicteres sacarolha A. St. – Hil. et al. |
title_full |
Análise fitoquímicas e avaliação da atividade e do mecanismo de ação antiúlcera do extrato hidroetanólico das folhas de Helicteres sacarolha A. St. – Hil. et al. |
title_fullStr |
Análise fitoquímicas e avaliação da atividade e do mecanismo de ação antiúlcera do extrato hidroetanólico das folhas de Helicteres sacarolha A. St. – Hil. et al. |
title_full_unstemmed |
Análise fitoquímicas e avaliação da atividade e do mecanismo de ação antiúlcera do extrato hidroetanólico das folhas de Helicteres sacarolha A. St. – Hil. et al. |
title_sort |
Análise fitoquímicas e avaliação da atividade e do mecanismo de ação antiúlcera do extrato hidroetanólico das folhas de Helicteres sacarolha A. St. – Hil. et al. |
author |
Balogun, Sikiru Olaitan |
author_facet |
Balogun, Sikiru Olaitan |
author_role |
author |
dc.contributor.none.fl_str_mv |
Martins, Domingos Tabajara de Oliveira http://lattes.cnpq.br/3794477872946546 Martins, Domingos Tabajara de Oliveira 109.726.923-04 http://lattes.cnpq.br/3794477872946546 Lopes, Lousã 879.675.298-04 http://lattes.cnpq.br/8843725522665416 109.726.923-04 Adzu, Bulus 705.985.581-52 http://lattes.cnpq.br/5877616611156488 Jesus, Neyres Zínia Taveira de 469.179.851-04 http://lattes.cnpq.br/2760653304094924 Cechinel Filho, Valdir 443.476.009-25 http://lattes.cnpq.br/8521384605324445 |
dc.contributor.author.fl_str_mv |
Balogun, Sikiru Olaitan |
dc.subject.por.fl_str_mv |
Helicteres sacarolha Úlcera gástrica Cicatrizante Toxicidade Antioxidante Compostos fenólicos CNPQ::CIENCIAS DA SAUDE Helicteres sacarolha Gastric ulcer Ulcer healing Toxicity Antioxidant Phenolic compounds |
topic |
Helicteres sacarolha Úlcera gástrica Cicatrizante Toxicidade Antioxidante Compostos fenólicos CNPQ::CIENCIAS DA SAUDE Helicteres sacarolha Gastric ulcer Ulcer healing Toxicity Antioxidant Phenolic compounds |
description |
Helicteres sacarolha Kunth. (Malvaceae) is a plant found in the Amazon region of Brazil and widely used in folk medicine of several countries for the treatment of gastric disorders, inflammation and infections. The aim of this study was to evaluate the acute and chronic toxicity, the preventive activities (gastroprotective) and curative (anti-ulcer) of hydroethanolic extract of Helicteres sacarolha (EHHs) and to elucidate the possible mechanisms involved in these activities. Additionally, phytochemical analyzes were carried out on EHHs. The leaves of Helicteres sacarolha were macerated in 75% hydroethanol (1:3 w / v) to obtain HEHs. Cytotoxicity of EHHs was evaluated in CHO-K1 and RAW 264.7 cells by the method of Alamar blue and acute animal toxicity in Swiss-Webster mice by Hippocratic test. The subchronic toxicity was evaluated in Wistar rats treated for 30 days with fixed doses of HEHs. Secondary metabolites were analyzed and confirmed by thin layer chromatography (TLC), spectrophotometry and high performance liquid chromatography (HPLC). The gastroprotective activity was assessed using gastric ulcer models of acidified ethanol, piroxicam, water restraint stress (acute models) and acetic acid (chronic) in rodents. The anti-Helicobacter pylori potential of HEHs was evaluated by broth microdilution method studies, determining the minimum inhibitory concentration (MIC). Antioxidant studies in vitro (DPPH, FRAP, chelating iron and linoleic acid tests) and in vivo (catalase and myeloperoxidase) were evaluated. The antisecretory activity of HEHs was assessed by the pylorus ligation in rats the likely mechanism of action of HEHs was evaluated ulcerated animals with acidified ethanol and pretreated with yohimbine, glibenclamide, indomethacin and L-NAME. The profile of proinflammatory and anti-inflammatory cytokines was evaluated in acetic acid ulcerated animals. HEHs presented low cytotoxicity in CHO-K1 and RAW 264.7, with IC50> 200 /mL. When administered orally at doses up to 2000 mg / kg in male mice and 4000 mg / kg in female mice, caused no change HEHs in signs and symptoms evaluated. In the subchronic toxicity test no significant changes were observed by treatment with HEHs in the parameters observed, except elevation of leukocytes (28%), basophils (ca.4 times) and decrease of neutrophils (18%), monocytes (65%) , hemoglobin (3.6%) and hematocrit (6.5%) that were not followed by clinical and hsitopatológicas changes. Total phenols and flavonoids were 19.9% and 14.4% respectively. The major compounds detected in HEHs were ellagic acid (6%) and morin (0.3%). HEHs demonstrated antiulcer activitis in the acute and chronic ulcer models. The antiulcer activity of HEHs involved the participation of NO, α-receptor, prostaglandins, K+ - ATP channels and antioxidant mechanisms and is dependent only on inhibition of gastric volume but not the acid secretion mechanisms. The ulcer healing action of HEHs involved attenuation of pro-inflammatory cytokines. HEHs was inactive against Helicobacter pylori. The results of this study confirm the popular use of the leaves of Helicteres sacarolha in gastric ulcers and that HEHs has low toxicity and a multitargeted action. The main metabolic constituents are the phenols and flavonoids, with ellagic acid and morin being the major classes of compounds. Ellagic acid is possibly involved in the gastroprotective antiulcer action of HEHs. Further experiments are required to advance preclinical validation of HEHs with the aim of developing an anti-ulcer phytotherapy. |
publishDate |
2014 |
dc.date.none.fl_str_mv |
2014-10-09 2015-08-21 2022-06-10T19:03:18Z 2022-06-10T19:03:18Z |
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 |
BALOGUN, Sikiru Olaitan. Análise fitoquímicas e avaliação da atividade e do mecanismo de ação antiúlcera do extrato hidroetanólico das folhas de Helicteres sacarolha A. St. – Hil. et al. 2014. 117 f. Tese (Doutorado em Ciências da Saúde) - Universidade Federal de Mato Grosso, Faculdade de Medicina, Cuiabá, 2014. http://ri.ufmt.br/handle/1/3332 |
identifier_str_mv |
BALOGUN, Sikiru Olaitan. Análise fitoquímicas e avaliação da atividade e do mecanismo de ação antiúlcera do extrato hidroetanólico das folhas de Helicteres sacarolha A. St. – Hil. et al. 2014. 117 f. Tese (Doutorado em Ciências da Saúde) - Universidade Federal de Mato Grosso, Faculdade de Medicina, Cuiabá, 2014. |
url |
http://ri.ufmt.br/handle/1/3332 |
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por |
language |
por |
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info:eu-repo/semantics/openAccess |
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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 |
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Universidade Federal de Mato Grosso (UFMT) |
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UFMT |
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Repositório Institucional da 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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1804648513203601408 |