Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0038358 (gastric ulcer)
 5,179 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

trans-Dehydrocrotonin (DHC), the major diterpene isolated from Croton cajucara Benth, was assayed for antiulcerogenic activity in four induced gastric ulcer models in the rat. At an oral dose of 100 mg/kg DHC showed a significant antiulcerogenic effect on ulcers induced by hypothermic restraint stress, ethanol, and pylorus ligature. No significant changes in indomethacin-induced gastric lesions or modifications in gastric parameters such as wall mucus, secretion rate, pH, and total acid content were found after DHC treatment. The acute toxicological effects of DHC were assessed in mice. The LD50 values were 876 mg/kg and 47.2 mg/kg for oral and intraperitoneal administrations, respectively. The cytotoxicity of DHC was also studied. A dose-dependent inhibition of cell viability was observed in V-79 fibroblast cell cultures with an IC50 of 240 microM. The high yields of DHC obtained from dried C. cajucara barks as well as its good antiulcerogenic activity and low toxicity support the pharmacological study of this compound as a potential new antiulcerogenic drug.
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PMID:Antiulcerogenic activity of trans-dehydrocrotonin from Croton cajucara. 952 3

Anchusa strigosa Banks et Sol (Boraginaceae) root extracts (ASRE) were prepared by soaking the dry material in boiling water. The clear soluble extract was dried and found to be 0.238 g/g dry roots. A gastric ulcer was induced in fastened animals by oral ingestion of ethanol. Administration of 0.080 g of ASRE prior to ethanol ingestion protected the stomach of the rat from ulcer formation. The ulcer index values, expressed as a percentage of total stomach surface area affected by the ulcer, were lowered from 34.0+/-4.0 to 6.0+/-0.7 and 32.5+/-9.4 to 2.2+/-1.4 by the morphometric and the planimetric methods, respectively. Treatment of the induced ulcer in guinea pigs was achieved by oral administration of ASRE at the therapeutic dose of extract of 0.286 g/kg body weight/day for 24 days. The intraperitoneal LD50 of ASRE in mice was 0.080 g extract/kg body weight. Replacing water intake by ASRE at 75 ml of variable extract concentrations of 2.865, 3.57 and 4.284 g/l per animal per day for 90 days showed no histopathological changes in all organs of the rat. However, a clear depression effect on the central nervous system and anemia were observed particularly with extract of 3.57 g/l or more.
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PMID:Effects of Anchusa strigosa root aqueous extract on gastric ethanol-induced ulcer in laboratory animals. 961 32

Ethanol-induced injury of digestive organs closely linked to the GI bleeding. The gastric or esophageal mucosal hemorrhage evoked by extra-amounts of alcohols is initiated by the microcirculatory damage of gastrointestinal mucosa. Many investigators focused on the ethanol-induced gastric ulcer formation as well as the ethanol-induced gastroesophageal reflux injury. Although the most important treatment for such a damage is of course to stop the drinking, it is also important to protect the gastrointestinal mucosa by potentiate the mucosal defense systems.
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PMID:[Ethanol-induced injury and GI bleeding]. 978 Jul 4

When free radical-scavenging activities of quercetin, alpha-tocopherol, nifedipine and tetracycline were measured by an electron spin resonance technique, all test compounds (10(-5) to 10(-3) M) scavenged both superoxide anions and hydroxyl radicals. The oral administration of quercetin (50 and 100 mg/kg), alpha-tocopherol (8 and 16 mg/kg), nifedipine (20 and 40 mg/kg) or tetracycline (10 and 20 mg/kg) markedly prevented the HCl plus ethanol-induced gastric mucosal injury and the increase in the content of thiobarbituric acid-reactive substances in the injured mucosa in rats. In addition, quercetin (25, 50 and 100 mg/kg), alpha-tocopherol (4, 8 and 16 mg/kg), nifedipine (10, 20 and 40 mg/kg) and tetracycline (5, 10 and 20 mg/kg), given orally, twice daily for 14 consecutive days from the day after acetic acid injection, dose-dependently promoted the ulcer healing and inhibited the increase in the content of thiobarbituric acid-reactive substances in the ulcerated mucosa. These results indicate that quercetin, alpha-tocopherol, nifedipine and tetracycline possess gastric cytoprotective and gastric ulcer healing-promoting actions. In addition, the free radical-scavenging properties of these compounds may be partly related to their anti-ulcer effects.
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PMID:Anti-ulcer effects of antioxidants, quercetin, alpha-tocopherol, nifedipine and tetracycline in rats. 992 Feb

Since endogenous vasopressin has been reported to be an aggressor in the gastric mucosa and a vasoconstrictor in the gastric circulation, we investigated the gastric cytoprotective effects of OPC-21268, a newly developed, nonpeptide, orally active vasopressin-1 receptor antagonist, on ethanol-induced gastric injury in rats. The rats were treated with OPC-21268 or placebo 2 hr before ethanol administration, and the gastric mucosa was evaluated macroscopically for ulcer damage, and histologically for gastric mucosal injury. Gastric mucosal blood flow, erythrocyte volume, and erythrocyte velocity were also measured in groups given saline, ethanol alone, and ethanol after OPC-21268. To investigate the role of systemic or locally secreted vasopressin, we measured plasma and tissue (gastric mucosa) vasopressin concentrations after ethanol or vehicle administration. Prophylactic OPC-21268 treatment improved the gastric ulcer score in a dose-dependent manner, and histological examination demonstrated that the drug significantly ameliorated the gastric injury induced by ethanol. The hemodynamic values obtained in the OPC-21268-treated and ethanol-treated group were similar to those in the saline control group, but values were significantly (P < 0.05) higher for gastric mucosal blood flow and erythrocyte velocity and lower for erythrocyte volume compared to the group given ethanol alone. Plasma vasopressin concentrations were not significantly different in the control group and at 15, 30, and 60 min after administration of ethanol. However, ethanol administration caused a threefold increase in gastric tissue vasopressin level (P < 0.05) compared to the control group. These results suggested that OPC-21268 relieved congestive hyperemia in the gastric mucosa and ameliorated the mucosal injury caused by ethanol, probably as a result of inhibition of vasopressin-mediated actions on the stomach. The vasopressin involved was probably generated locally in the gastric mucosa after ethanol administration.
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PMID:Protective effect of a vasopressin-1 selective antagonist, OPC-21268, against ethanol-induced damage of the rat gastric wall. 1008 Jan 41

Croton cajucara Benth. (Euphorbiaceae) is widely used in Amazonian folk medicine for the treatment of a wide range of gastrointestinal symptoms. The essential oil from its bark was investigated for acute toxicity in mice and for its ability to prevent the formation of ulceration of the gastric mucosa in different models of experimentally induced gastric ulcer in mice and rats. When previously administered orally at a dose of 100 mg kg(-1), the essential oil significantly reduced (P < 0.01) the gastric injury induced by hypothermic restraint stress (48%), indomethacin (47%), ethanol (86%) and pylorus ligature models (87%) in rats. In the HCl/ethanol-induced gastric ulcer model in mice, at oral doses of 100 and 200 mg kg(-1), the essential oil from C. cajucara significantly reduced (P < 0.01) the formation of gastric lesions by 52% and 67%, respectively, when compared with the control group. In rats submitted to pylorus ligature, the essential oil given orally increased the volume of gastric juice when compared with the control group (P < 0.01). When the essential oil (100 mg kg(-1)) was administered intraduodenally to mice, significant modifications were found in gastric parameters such as pH and total acid content after oil treatment. We observed significant changes (P < 0.01) in gastric juice parameters such as an increase in volume and a decrease in gastric acidity (pH and total acid content). The acute toxicologic effects of the essential oil from C. cajucara were assessed in mice. The LD50 values were 9.3 g kg(-1) by the oral route and 680 mg kg(-1) by the intraperitoneal route. The good yield of essential oil obtained from dried C. cajucara bark (1%) as well as its anti-ulcerogenic activity and low toxicity suggest that pharmacological studies of this substance as a potential new anti-ulcerogenic drug are warranted.
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PMID:Effects of an essential oil from the bark of Croton cajucara Benth. on experimental gastric ulcer models in rats and mice. 1034 36

The decoction of Dalbergia monetaria L. is popularly used in Brazil for the treatment of gastric ulcer and the lyophilized aqueous extract (LAE) of D. monetaria has significant anti-ulcerogenic activity and inhibits gastric ulcer lesions induced by pylorus-ligature, ethanol and hypothermic-restraint stress. This work was conducted to identify the antiulcerogenic mechanisms of action of the LAE of D. monetaria. We analysed the effect of the LAE on prostaglandin E2 (PGE2) synthesis and on the characteristics (pH, volume and total acid content) of gastric juice. The antagonism between the LAE and histamine or carbachol was also analysed. The LAE increased gastric mucosal PGE2 synthesis compared with control (89.7+/-21.5 and 52.6+/-11.8 pg mg(-1), respectively) as assayed by enzyme immunoassay in the rat stomach. The LAE reduced the total acid content of gastric juice, but did not modify pH or gastric volume significantly, in Shay rats. Dose-response curves to histamine were shifted to the right in guinea-pig isolated right atria (pD2 values were 5.77+/-0.2 and 5.42+/-0.3, respectively, in the absence and presence of the LAE), with a significant reduction in maximum response (140+/-15.1 and 98+/-13.0, respectively). The same effect was observed when the agonist was isoprenaline. The LAE had no effect on the dose-response curve to carbachol in rat fundus strips. Thus, the protective effect of the LAE on induced gastric lesions might be because of synergistic effects, e.g. increased PGE2 synthesis and antagonism of H2 histamine and beta-adrenergic receptors, reducing gastric acid secretion. Increased PGE2 synthesis results in increased protection, and antagonism of H2 histamine and beta-adrenergic receptors reduces aggressive factors against the gastric mucosa.
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PMID:Anti-ulcerogenic mechanisms of a lyophilized aqueous extract of Dalbergia monetaria L. in rats, mice and guinea-pigs. 1045 52

In the rat stomach, evidence has been provided that capsaicin-sensitive sensory nerves (CSSN) are involved in a local defense mechanism against gastric ulcer. In the present study capsaicin or resiniferatoxin (RTX), a more potent capsaicin analogue, was used to elucidate the role of these sensory nerves in gastric mucosal protection, mucosal permeability, gastric acid secretion and gastrointestinal blood flow in the rat. In the rat stomach and jejunum, intravenous RTX or topical capsaicin or RTX effected a pronounced and long-lasting enhancement of the microcirculation at these sites, measured by laser Doppler flowmetry technique. Introduction of capsaicin into the rat stomach in very low concentrations of ng-microg x mL(-1) range protected the gastric mucosa against damage produced by topical acidified aspirin, indomethacin, ethanol or 0.6 N HCl. Resiniferatoxin exhibited acute gastroprotective effect similar to that of capsaicin and exerted marked protective action on the exogenous HCl, or the secretagogue-induced enhancement of the indomethacin injury. The ulcer preventive effect of both agents was not prevented by atropine or cimetidine treatment. Capsaicin given into the stomach in higher desensitizing concentrations of 6.5 mM markedly enhanced the susceptibility of the gastric mucosa and invariably aggravated gastric mucosal damage evoked by later noxious challenge. Such high desensitizing concentrations of capsaicin, however, did not reduce the cytoprotective effect of prostacyclin (PGI2) or beta-carotene. Capsaicin or RTX had an additive protective effect to that of atropine or cimetidine. In rats pretreated with cysteamine to deplete tissue somatostatin, capsaicin protected against the indomethacin-induced mucosal injury. Gastric acid secretion of the pylorus-ligated rats was inhibited with capsaicin or RTX given in low non-desensitizing concentrations, with the inhibition being most marked in the first hour following pylorus-ligation. Low intragastric concentrations of RTX reduced gastric hydrogen ion back-diffusion evoked by topical acidified salicylates. It is concluded that the gastropotective effect of capsaicin-type agents involves primarily an enhancement of the microcirculation effected through local release of mediator peptides from the sensory nerve terminals. A reduction in gastric acidity may contribute to some degree in the gastric protective action of capsaicin-type agents. The vasodilator and gastroprotective effects of capsaicin-type agents do not depend on vagal efferents or sympathetic neurons, involve prostanoids, histaminergic or cholinergic pathways.
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PMID:Capsaicin-sensitive afferent sensory nerves in modulating gastric mucosal defense against noxious agents. 1067 23

The prevalence of gastric ulcers in patients with liver cirrhosis is increased compared with that in the general population, and portal hypertension may contribute to the increased risk of gastric ulcer in cirrhosis patients. Aggressive factors involved in the pathogenesis of gastric ulcer are diminished in association with portal hypertension. In contrast, most of the important gastric mucosal defense mechanisms are shown to be impaired in portal hypertension; many of these mechanisms are also found to be altered in patients with liver cirrhosis. Portal hypotensive treatment with propranolol reduces ethanol-induced gastric mucosal damage in portal hypertensive rats and improves endoscopic signs of portal hypertensive gastropathy in cirrhosis patients. Together, these findings suggest portal hypertension-induced impairment of the gastric mucosal defenses to be an important factor in the pathogenesis of gastric ulcer in patients with liver cirrhosis. Prospective studies of portal pressure-reducing procedures, such as pharmacotherapy with propranolol, and their effect on the incidence of gastric ulcer in cirrhosis patients are needed to confirm this suggestion.
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PMID:Does portal hypertension contribute to the pathogenesis of gastric ulcer associated with liver cirrhosis? 1068 Jun 61

The gastroprotective activity of the essential oil from the bark of Croton cajucara Benth (Euphorbiaceae) was assessed in three different models of experimentally induced gastric ulcer in mice. At oral dose of 100 mg/kg the essential oil reduced gastric lesions induced by hypothermic restraint stress and HCl/ethanol significantly. In the HCl/ethanol model a dose-dependent gastroprotective effect was found. Moreover, significant changes in gastric parameters such as pH, secretion rate and total gastric acid were found after intraduodenal administration of essential oil under ligated pylorus (Shay) conditions. The acute toxicity of essential oil was assessed in mice. The LD50 values were 9.3 and 680 mg/kg for oral and intraperitoneal administrations, respectively. The cytotoxicity of essential oil was studied also. A dose-dependent cell viability inhibition was found in V79 fibroblast cell cultures with an IC50 of 22.9 microg/ml. Our results support the pharmacological study of this essential oil.
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PMID:Gastroprotective effect of essential oil from Croton cajucara Benth. (Euphorbiaceae). 1072 4


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