Effects of KB-5492, a New Anti-Ulcer Agent with a Selective Affinity for the Sigma-Receptor, on Aspirin-Induced Disruption of the Rat Gastric Mucosal Barrier

Morimoto, Yasuo; Shimohara, Koichi; Oshima, Shinya; Hara, Hideaki; Sukamoto, Takayuki

doi:10.1254/jjp.64.49

Cited by 9 publications

(8 citation statements)

References 20 publications

(18 reference statements)

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“…Another interesting point was that ethanol-induced ulcers are inhibited by agents that enhance mucosal defensive factors such as carbenoxolone or prostaglandin E 2 but not by antisecretory agents such as cimetidine [31]. Therefore, our results suggest that the diethyl ether extract exerts a gastroprotective action related to cytoprotection and antisecretory activity.…”

Section: Resultsmentioning

confidence: 65%

Gastroprotective and antisecretory effects of Ailanthus excelsa (Roxb)

et al. 2009

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Ailanthus excelsa (Roxb), an Egyptian medicinal species highly important for treating numerous diseases, was investigated against experimentally induced gastric ulcer in rodents. We evaluated the gastroprotective effect of four extracts (petroleum ether, diethyl ether, chloroform, and methanol) of A. excelsa bark by using the ethanol-induced gastric lesion model. The pretreatment of animals with methanolic, petroleum ether, and chloroformic extracts (100 mg/kg, oral (p.o.)) from A. excelsa significantly reduced gastric lesion induced by ulcerogenic agent (56, 47, and 70%, respectively) when compared with animals pretreated with vehicle. However, the diethyl ether pretreatment led to the least gastric lesion damage (83%), similar to the standard antiulcer drug, cimetidine, at the same dose (100 mg/kg, p.o.). The lower effective dose of diethyl ether extract, as well as cimetidine, given by intraduodenal route, significantly increased the pH values and reduced the acid output of gastric juice. Sterols, triterpenes,and quassinoids are present in the diethyl ether extract of A. excelsa stem bark, which presented the best gastroprotective action among the studied extracts. Our study confirmed the traditional indications of A. excelsa for the treatment of gastric ulcer.

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Section: Resultsmentioning

confidence: 65%

Gastroprotective and antisecretory effects of Ailanthus excelsa (Roxb)

et al. 2009

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“…Gastric hemorrhagic lesions were induced by intragastric administration (0.1 ml/20 g) of an HCl/ethanol mixture, containing 150 mM HCl in 98% ethanol [17-19]. The KRGCD dissolved in CMC (0.5% carboxymethylcellulose solution dissolved in distilled water) was administered at oral doses of 30, 100, and 300 mg/kg, 1 hr before HCl/ethanol application.…”

Section: Methodsmentioning

confidence: 99%

Protective effects of a gastrointestinal agent containing Korean red ginseng on gastric ulcer models in mice

Oyagi

Ogawa

Kakino

et al. 2010

BMC Complement Altern Med

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BackgroundKorean red ginseng (KRG) is a ginseng that has been cultivated and aged for 4-6 years or more, and goes through an extensive cleaning, steaming and drying process. KRG contains more than 30 kinds of saponin components and has been reported as having various biological properties, such as anti-fatigue action, immune restoration, and neurovegetative effect. The purpose of this study was to assess the effects of a KRG-containing drug (KRGCD) on gastric ulcer models in mice.MethodsStomach ulcers were induced by oral ingestion of hydrochloride (HCl)/ethanol or indomethacin. Treatment with KRGCD (30, 100, and 300 mg/kg, p.o.) occurred 1 hr before the ulcer induction. Effect of KRGCD on anti-oxidant activity and gastric mucosal blood flow with a laser Doppler flowmeter in mice stomach tissue was evaluated.ResultsKRGCD (100 and 300 mg/kg, p.o.) significantly decreased ethanol- and indomethacin-induced gastric ulcer compared with the vehicle-treated (control) group. KRGCD (100 and 300 mg/kg) also decreased the level of thiobarbituric acid reactive substance (TBARS) and increased gastric mucosal blood flow compared with the control group.ConclusionsThese results suggest that the gastroprotective effects of KRGCD on mice ulcer models can be attributed to its ameliorating effect on oxidative damage and improving effect of gastric mucosal blood flow.

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“…Os animais foram distribuídos randomicamente em sete grupos. A úlcera foi induzida por administração intragástrica de solução 150 mM de ácido clorídrico (HCl) em etanol (EtOH) 95%, sendo usado o volume de 5mL/kg (Mizui et al, 1987;Morimoto et al, 1994;Shujaa et al, 2009;Oyagi et al, 2010). Os animais do grupo 1 (controle positivo, n = 6) sofreram indução de úlcera e após 1 hora foram eutanasiados com tiopental.…”

Section: Ensaio Gastroprotetorunclassified

Atividade gastroprotetora do extrato etanólico de Pavonia alnifolia A.St.-Hil.

Ewald

Loyolla

Pereira

et al. 2015

Rev. bras. plantas med.

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RESUMO:No Brasil, a família Malvaceae está representada por aproximadamente 200 espécies e algumas foram descritas como gastroproteroras. Pavonia alnifolia A.St.-Hil. (Malvaceae) foi selecionada após uma abordagem quimiossistemática, considerando-se sua potencial capacidade em prevenir lesões gástricas. Assim, a atividade gastroprotetora do extrato etanólico de caules de P. alnifolia foi avaliada utilizando o modelo de indução aguda da lesão gástrica por etanol acidificado em camundongos. Além disso, foram quantificados o teor de flavonóides, pelo método de cloreto de alumínio, e de polifenóis, pelo método Folin-Ciocalteu, uma vez que a relação desses componentes com a proteção gástrica foi evidenciada. Os ensaios apontaram redução acentuada das lesões gástricas em camundongos tratados com o extrato da planta em todas as doses ensaiadas (10, 100 e 300 mg/kg). Esse efeito pode estar relacionado com a presença de polifenóis, cujo teor encontrado foi 74,3 ± 7,5 µg equivalente de pirogalol/mg do material vegetal examinado e 82,7 ± 7,1 µg equivalente de pirogalol /mg da amostra no extrato preparado por percolação e teor de flavonoides totais, que por sua vez apresentou um resultado de 17,1 ± 1,4 µg/mg de extrato. O extrato apresentou proteção da mucosa gástrica e este efeito pode estar relacionado à presença dos polifenóis e flavonóides encontrados. Palavras-chave:Pavonia, Malvaceae, gastroproteção, flavonóides, polifenóis.ABSTRACT: Gastro protective activity of the Pavonia alnifolia A.St.-Hil. extract. In Brazil, the Malvaceae family is represented by at about 200 species. Some of those species are known as gastro protective ones. The Pavonia alnifolia A.St.-Hil (Malvaceae) was selected after a chemosystematic approach. The gastro preventive activity of the ethanol extract of stems Pavonia alnifolia was evaluated through the use of the Ethanol:chlroridric acid model on mice. The quantification of the total flavonoids (aluminum chloride method) and total polyphenols (Folin-Ciocalteu method) was also performed since the relation of those components with gastric protection has been previously highlighted. The tests showed a significant reduction of the ulcer formation in the mice treated with the plant extract (10, 100 and 300 mg/kg). This effect may be related to the presence of polyphenols whose content was found to be 74.3 ± 7.5 µg/mg of vegetal material and 82.7 ± 7.1 µg/mg of crude extract and flavonoids, which in turn showed a content of 17.1 ± 1.4 µg/mg dry extract.

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Effects of KB-5492, a New Anti-Ulcer Agent with a Selective Affinity for the Sigma-Receptor, on Aspirin-Induced Disruption of the Rat Gastric Mucosal Barrier

Cited by 9 publications

References 20 publications

Gastroprotective and antisecretory effects of Ailanthus excelsa (Roxb)

Gastroprotective and antisecretory effects of Ailanthus excelsa (Roxb)

Protective effects of a gastrointestinal agent containing Korean red ginseng on gastric ulcer models in mice

Atividade gastroprotetora do extrato etanólico de Pavonia alnifolia A.St.-Hil.

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