• Archives of Pharmacal Research
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• 제16권1호
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• pp.71-74
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• 1993

The protective effect of adenosine triphosphate (ATP) on gastic ulcer induced in rats has been studied. Gastic ulceration was induced by hypothemic restraint stress or dicolofenac sodium. Gastic acid secretion and mucosal injury produced by the hypothemic restraint stress was greater as compared with those produced by diclofenac sodifum. ATP significantly reduced area of injury, however, increased cyclic adenosine monophosphate (cATP) content. Administration of dipyridamole along with ATP did not change the total lesion area in both models when compared to ATP alone. Aminophyline antagonized antagonized the protective effect of ATP on the injured area. Famotidine was found to be effective in reducing gastric acid output as well as the total injured area without any change in cAMP content when given along with ATP.

• Journal of Pharmaceutical Investigation
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• 제17권2호
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• pp.79-88
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• 1987

In order to reduce gastric irritation of iron preparations, one prodrug, glycine complex of ferrous fumarate, was synthesized, identified, examined for physico-chemical properties and compared with ferrous fumarate, ferrous sulfate and ferroglycine sulfate. That novel ferroglycine fumarate (FGF) resulted in higher dissolution rate in water, artificial gastric and intestinal juice. The absorption rate constants $(K_a)$ in rat of FGF was greater and ulcerogenic dose on stomach was increased remarkably than those of iron parent materials and ferroglycine sulfate.

• Journal of Plant Biotechnology
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• 제37권1호
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• pp.47-56
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• 2010

Sea buckthorn (Hippophae rhamnoides L.) is deciduous shrubs in the genus Hippophae, mainly cultivated in Europe and Asia. Sea buckthorn berries have a high vitamin C, vitamin E, carotenoids, carbohydrates, protein, organic acids, dietary minerals, triterpenoids, polyphenolic acids and amino acids. Extracts of sea buckthorn berries have anti- obesity, anti-oxidantive, anti-microbial, anti-ulcerogenic, anti-diabetic and nutritional effects. Sea buckthorn used as a traditional medicine for the treatment of cough, aid digestion, invigorate blood circulation and alleviate pain. Extracts of sea buckthorn branches and leaves was administered to humans and animals to treat gastrointestinal distress in Mongolia. This paper briefly reviews the most relevant experimental data on the pharmacological effects and isolated component of sea buckthorn. And, we also describe the importance of sea buckthorn as the environmental-friendly crops.

• 대한화학회지
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• 제57권2호
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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.

• 약학회지
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• 제30권3호
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• pp.128-138
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• 1986

Three newly synthesized alkanol esters of d-2-(6-methoxy-2-naphthyl) propionic acid, NAPROXEN were examined for physicochemical properties and biopharmaceutical characteristics. These esters were very stable in solid state, but more than 90% of these esters were hydrolysed to the parent, naproxen in rabbit's liver hornogenates. They showed higher dissolution rate in the artificial gastric and intestinal juice, and significantly greater partition coefficient in n-octanol, when compared with naproxen. The absorption rate constants of these esters were increased, while the elimination rate constants were decreased, comparing with naproxen. The ulcerogenic doses on gastric and intestinal mucosa were increased remarkably, and the antiinflammatory dose against carrageenininduced edema on rat hind paw was decreased markedly in these esters, and thus the safety indexes of these esters were higher than that of naproxen.

• Biomolecules & Therapeutics
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• 제9권2호
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• pp.69-78
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• 2001

Cyclooxygenase (COX) is an enzyme, which catalyzes the production of prostaglandins from arachi-donic acid and exists in two isoforms (COX-1 and COX-2). COX-1 is involved in the maintenance of physiological functions such as platelet aggregation, cytoprotection in the stomach and maintenance of normal kidney function. COX-2 is induced significantly in vivo under inflammatory conditions. COX-1 and COX-2 serve different physiological and pathological functions. All commercially available nonsteroidal antiinflammatory drugs (NSAIDS) are inhibitors of both COX-1 and COX-2. Therefore, selective inhibitors of COX-2 may be effective antiinflammatory agents without the ulcerogenic effects associated with current NSAms. Since the mid 1990s, a number of reports have been appeared on the preparation and biological activity of selective COX-2 inhibitors. Recently celecoxib, and rofecoxib, the representative COX-2 inhibitors, are introduced in the drug market. In this paper the relationship of structure-activity for selective COX-2 inhibitors is reviewed.

• 동아시아식생활학회지
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• 제16권2호
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• pp.199-206
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• 2006

This study was designed to investigate the effect of medicinal herb extract on the antioxidant and antimicrobial activities against Helicobacter pylori, which is known as a ulcerogenic pathogen. The concentration of total phenolic compound of Scutellaria baicalensis(13.14%) was highest among water extracts and that of Ulmus parvifolia(15.12%) was highest among the ethanol extracts. The antioxidant activity of the water extract of Scutellaria baicalensis and of the ethanol extract of Ulmus parvifolia were 91.00% and 65.03%, respectively, in DPPH assay. The antioxidant activity of the water extract of Scutellaria baicalensis and of the ethanol extract of Ulmus parvifolia were 32.90% and 27.70%, respectively, in SOD assay. The antioxidant activity of the water extract of Ulmus parvifolia and of the ethanol extract of Glycyrrhiza uralensis Fischer was 2.15 and 2.17, respectively, in TBARS assay. In disc method, Scutellaria baicalensis showed the highest anti-microbial activity against H. pylori, followed by Glycyrrhiza uralensis Fischer among the water extracts and Glycyrrhiza uralensis Fischer showed the highest anti-microbial activity followed by Radix puerariae among ethanol extract.

• Advances in Traditional Medicine
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• 제4권4호
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• pp.253-260
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• 2004

Zosterin is a pectin from a seagrasses of the family Zosteraceae. Zosterin was given to rats intragastrically once 1h before the emotional stress or injection of indomethacin, or administration of 2, 4-D solution daily for seven days at dose of 100 mg/kg. The data obtained demonstrate that zosterin enhances resistance of the stomach tissue to various ulcerogenic factors (emotional stress, indomethacin, pesticide 2, 4-D). It was shown to possess a gastroprotective effect, which is accompanied by diminution of the number and sizes of destructive regions in the gastric mucosa during the ulcer affection, as well as reduction of ATP and glycogen deficit, decrease of lactate excess, and normalization of the energy balance in the gastric mucosa. According to its antiulcer effect, zosterin may be recommended for application in prevention and treatment of stomach diseases together with the basic therapy.

• 약학회지
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• 제48권6호
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• pp.317-322
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• 2004

The use of nonsteroidal anti-inflammatory drugs (NSAIDs) is limited by their ability to induce gastrointestinal injury. It has been shown that nitric oxide (NO), similar to pro staglandins (PGs), appears to play an important role in gastric mucosal defence. We hypothesized that NSAIDs contained NO group would be less acutely toxic to the gastric mucosa, but would not interfere with their ability to suppress inflammatory process in rats. We have compared the ulcerogenic and anti-inflammatory effect of CW-501029 (NO-NSAIDs), CW-501027 (NSAIDs) and indomethacin. Both did not change mean blood pressure and heart rates, indicating that they had no side effect on cardiovascular system. We found that CW-501029 increased nitrite/nitrate levels without changing of blood pressure and heart rates. We suggest that it may help gastric mucosal blood flow, the which helps reducing the discomfort in astrointestinal system. Carrageenan-induced PGE2 increase was reduced in a similar tendency when compared CW-501027 or CW-501027 with control in back exudate of rats, but CW-501029 less reduced PGE2 than CW-502027 or indomethacin in gastric tissues. CW-501027 or CW-501029 reduced platelet aggregation. From these results we suggest that CW-501029 may improve the side effect by reduction of short-term gastric injury and less inhibition of PGs synthesis.

• 셀메드
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• 제6권2호
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• pp.11.1-11.7
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• 2016

The aimed of the presence study was to determine the antiulcer potential of virgin coconut oil (VCO), either extracted by wet process (VCO_A) or fermentation process (VCO_B), and to compare their effectiveness against the copra oil (CO) using the HCl/ethanol-induced gastric ulcer model. Earlier, the oils underwent chemical analysis to determine the free fatty acids composition, physicochemical properties and anti-oxidant capability. In the antiulcer study, rats (n=6) were pre-treated orally for 7 consecutive days with distilled water (vehicle), 100 mg/kg ranitidine (positive group) or the respective oils (10, 50, and 100% concentration). One hour after the last test solutions administration on Day 7^th, the animals were subjected to the gastric ulcer assay. Macroscopic and microscopic analyses were performed on the collected rat's stomachs. From the results obtained, the chemical analysis revealed i) the presence of high content of lauric acid followed by myristic acid and palmitic acid in all oils and; ii) the significant (^*p< 0.05) different in anisidine- and peroxide-value, percentage of free fatty acid, total phenolic content and total antioxidant activity among the oils. The animal study demonstrated that all oil possess significant (^*p< 0.05) antiulcer activity with VCO_B being the most effective oil followed by VCO_A and CO. The macroscopic observations were supported by the microscopic findings. Interestingly, all oils were more effective than 100 mg/kg ranitidine (reference drug). In conclusion, coconut oils exert remarkable antiulcer activity depending on their methods of extraction, possibly via the modulation of its antioxidant and anti-inflammatory activity.