• Journal of Food Hygiene and Safety
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• v.14 no.4
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• pp.358-364
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• 1999

Propolis, a natural resinous compound collected from honey bees, contains many biochemical constituents and has been used in traditional medicines as early as 300 B.C. Recently, it has been reported to possess many biological activities such as antibacterial, antiviral, fungicidal, local anaesthetic, immunostimulating, antiinflammatory and free radical scavenging properties. This study was performed to investigate the pharmacological effects of the propolis extract and fractions on the gastric lesion and ulcer. The ethanol extract was fractionated with hexane, toluene and ethyl acetate. Followed by bioassay on antigastric and antiulcer activity. Propolis ethanol extracts(500, 750, 1,000, 1,500 and 2,000 mg/kg) showed the protective effect on HCl·ethanol-induced gastric lesion and the antisecretory effect against Shay’s gastric secretion in pylorus-ligated rats in a dose related manner. In the animal models of HCl·ethanol, aspirin-induced gastric lesion and Shay’s gastric secretion, the hexane and toluene fraction of propolis significantly reduced the length of gastric lesion and the acid secretion. These data showed that the gastric protective effects of propolis might result from reduction of acid secretion through the inactivation of H+/K+ATPase activity.

• Biomolecules & Therapeutics
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• v.4 no.3
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• pp.285-290
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• 1996

This study was designed to determine the effect of newly synthesized antiulcer agent, 5-pyrrolyl-6-halo-2-(pyridyl-2-methylthio)benzimidazole derivatives (IY-81233), on various experimental ulcers and on the secretion of prostaglandin $E_2(PGE_2)$ into the gastric lumen of rat. IY-81233 was previously reported to have a strong inhibitory effect on $H^+/K^$-ATPase and on gastric acid secretion in rats. Oral administration of IY-81233 at concentrations of 0.2, 2.0, and 20 mg/kg inhibited gastric lesions and duodenal ulcer induced by indomethacin, HCI-ethanol, water-immersion stress, cysteamine, and acetic acid in a dose dependent manner. Their IC$IC_{50}$ values were 3.4, 1.4, 0.8, 1.3, and 1.2 mg/kg, respectively. These results indicate that IY-81233 is a potent antiulcer agent although it is slightly less potent than omeprazole in healing of gastritis and ulcers. The secretion of $PGE_2$ into gastric lumen was also investigated in relation to the cytoprotective effect by IY-81233 in rats. The $PGE_2$ level was not changed significantly by an oral administration of IY-81233, suggesting that IY-81233 has little effect on the gastric protection. Therefore, it can be concluded that IY-81233 exerts prominent antiulcer activity by suppressing gastric acid secretion via an inhibition of a proton pump and not by protecting the gastrointestinal mucosa against various ulcerative stimuli.

• Biomolecules & Therapeutics
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• v.5 no.4
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• pp.331-335
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• 1997

In a preliminary screening of plant extracts for the antigastritic and antiulcer actions in rats, the methanol extracts of Taheebo showed positive activity in HCI . ethanol-induced gastric lesion. Among the systematic fractions of hexane, chloroform, butanol and water, the most potent $H_2O$ fraction reduced significantly HCI . ethanol-induced gastric lesion at the oral dose of 300 mg/kg. In pylorus ligated rats chloroform and butanol fraction showed decreases in the volume of gastric secretion and acid output of which effects were stronger in chloroform fraction. Further assays with hexane butanol and $H_2O$ fraction disclosed that it significantly suppressed the aspirin-induced ulcer. The butanol fraction reduced significantly acetic acid induced ulcer at the dose of 400 mg/kg. The butanol and $H_2O$ fraction reduced the malondialdehyde level in HCI . ethanol-induced gastric lesion. In pylorus ligated rats, chloroform and butanol fraction reduced the malondialdehyde level and in aspirin-induced ulcer, chloroform fraction reduced that levle. These results might suggest that the butanol and $H_2O$ fraction of Taheebo had inhibitory action in gastric lesion and ulceration through inhibition of gastric acid secretion and the decrease malondialdehyde level.

• Archives of Pharmacal Research
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• v.23 no.1
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• pp.72-78
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• 2000

The general pharmacological properties of YJA20379-1 2-dimethylamino-4,5-dihydrothiazolo[4,5:3,4]pyridol[1,2-a]benzoimidazole, a novel proton pump inhibitor with antiulcer activities were investigated in mice, rats, guinea pigs and rabbits. YJA20379-2 at oral doses of 50, 100 and 200 mg/kg did not affect the general behaviour, hexobarbital hypnosis and motor coordination in mice. The drug did not have analgesic or anticonvulsant action at 200 mg/kg. Locomotor activity and body temperature were not influenced at 100 mg/kg. At a concentration up to 2{\times}10^{-4} g/ml$, YJA20379-2 did not produce any contraction or relaxation of isolated preparations, such as the rat fundus, the guinea pig ileum and the rat uterus, and did not antagonize the contractile response to several spasmogens, such as histamine, acetylcholine, serotonin and oxytocin. At dosages up to 200 mg/kg p.o. YJA20379-2 did not affect the pupil size of mice. Intestinal propulsion of mice was not affected up to 200 mg/kg p.o. and the drug did not affect urinary excretion at 100 mg/kg p.o. These results indicate that at dosages up to 100 gm/kg p.o. YJA20379-2 was found not to affect this pharmacological profile. However, at 200 mg/kg the drug lowered body temperature and showed decreased in locomotor activity and urine volume.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.258.1-258.1
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• 2002

Piperine (piperinoyl-piperidine) is a nitrogenous pungent substance contained in black pepper. the well know spice obtained from Piper nigrum L. (Piperaceae). Pharmacological studies have shown that piperine reduces inflammation and pain. possesses anticonvulsant and antiulcer activity. protects the liver and has deleterious effects on testis function. Prostaglandins(PGs) are a family of intercellular and intracellular messengers derived from arachidonic acid(AA) by phospholipase(PL) and cyclooxygenase(COX). (omitted)

• Biomolecules & Therapeutics
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• v.4 no.1
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• pp.84-88
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• 1996

Alnus japonica cortex has been used as antidiarrhea, antihemorrhage and the remedy of indigestion. This study was performed to investigate the effectiveness of the methanol extracts of the Alnus japonica cortex on the gastric lesion and ulcer. The methanol extract was fractionated with hexane, chloroform and butanol, followed by bioassay on antigastritic and antiulcer activity. The methanol extract showed low acute toxicity with minimum lethal dose of more than 5000 mg/kg, p.o. in mice. The chloroform and the butanol fraction reduced gastric lesion in HCI. ethanol induced gastritic model. On gastric secretion in pylorus ligated rat, the hexane and chloroform fraction decreased the volume and acidity. The butanol fraction had significant inhibitory effects on aspirin and Shay's ulcer. The butanol fraction showed a tendency to inhibit the decrease of mucin secretion due to ingestion of absolute ethanol.

• Proceedings of the KAIS Fall Conference
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• 2009.05a
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• pp.607-611
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• 2009

Stomach ulcer is the sickness with high frequency of occurrence at the digestive organs and is usually induced by a disproportion of an aggressive factor and a defense factor. To find the medicines having comparative effect to $Stillen^{(R)}$ currently on sale, we screened SHI-7004 and carried out following experiments; Effects of HCl-EtOH induced gastric lesions measuring test, Acid-Neutralizing Capacity, DPPH antioxidation activity, effect of stomach glands secrection. We can suggest that this herbal medicines could be a promising drug for the treatment of gastrc ulcers.

• Archives of Pharmacal Research
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• v.25 no.1
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• pp.67-70
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• 2002

The effects of the dried stem powder of Opuntia ficus-indica var. saboten (OF-s) were investigated on gastric lesion and ulcer models in rats. It showed significant inhibition in HCl·ethanolinduced gastric lesion at the doses of 200 and 600 mg/kg p.o. and in HCl·aspirin-induced gastric lesion at 600 mg/kg p.o. OF-s also showed significant inhibition in indomethacin-induced gastric lesion at the doses of 200 and 600 mg/kg, p.o. However, it did not affect both the aspirin-induced and Shay ulcers in rats. It also did not affect gastric juice secretion, acid output and pH. These data indicate that OF-s only possesses pronounced inhibitory action on gastric lesion without antiulcer activity in rats.

• Journal of the Korean Chemical Society
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• v.57 no.2
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• pp.227-233
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• 2013

A series of newer substituted-imidazolidine derivatives 3a-k were synthesized and assayed in vivo to investigate their anti-inflammatory, analgesic and antiulcer activity. The results of biological evaluation revealed that the three compounds, 4-[1,3-bis(4-hydroxy-3-methoxybenzyl)-2-imidazolidinyl]phenyldiethylamine (3g), 4-[1,3-bis(3-Ethoxy-4-hydroxybenzyl)-2-imidazolidinyl] phenyldiethylamine (3h) and 4-(1,3-bis(benzo[d][1,3]dioxol-5-ylmethyl)-4-methylimidazolidin-2-yl)-N,N-diethylbenzenamine (3j) were good in their anti-inflammatory and analgesic actions. Additionally these derivatives showed superior GI safety profile as compared to that of the standard drug in terms of low severity index. The results are statistically treated for its significance.

• Korean Journal of Pharmacognosy
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• v.43 no.1
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• pp.72-78
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• 2012

Alnus japonica Steud (A. japonica) have long been used in the traditional medicine for gastric disorder, hepatitis and fatty liver in Korea. Antiulcer effects of A. japonica hot water extract (AJ ext) were evaluated by in vitro antibacterial activity against H. pylori, by the inhibitory action against the in vitro gastric $H^+/K^+$-ATPase and using rat models of gastric mucosal damage and gastric ulcer induced by HCl-ethanol, indomethacin, and restraint and water-immersion stress. For the determination of antibacterial activity of AJ ext against H. pylori, the activity of urease which released from H. pylori was measured in culture. AJ ext showed weak antibacterial activity against H. pylori with the growth inhibitions of 37% and 61% by adding final concentrations of 500 and $1000{\mu}g/ml$ culture, respectively at 24 h. To observe the inhibitory activity of AJ ext against the $H^+/K^+$-ATPase in hog gastric membrane vesicle, $IC_{50}$ value of AJ ext was $806.3{\mu}g/ml$. Pretreatment of AJ ext (200, 500 mg/kg, p.o.) prevented in a dose-dependent manner the acute gastritis in HCl-ethanol model and the formation of gastric ulcer in indomethacin model and restraint and water-immersion stress model. These results suggest that the AJ ext can be used for prevention and treatment of gastric mucosal damage and ulcers induced by various stress.