• 약학회지
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• 제25권1호
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• pp.9-14
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• 1981

Anti-infammatory, analgesic and ulcerogenic activities of fentiazac were investigated in comparison with those of acetylsalicylic acid, fenbufen, naproxen and phenylbutazone. On the anti-inflammatory activity in carrageenin-induced rat paw edema and the analgesic activity on writhing syndrome induced with acetic acid in mice, fentiazac displayed more potent effect than acetylsalicylic acid, fenbufen and pbenylbutazone. But the ulcerogenic action of fentiazac on gastrointestinal tract in fasting rats was less than that of reference drugs. From these investigation, fentiazac seemed to indicate a poor correlation between the extent of anti-inflammatory activity and ulcerogenic action.

• Journal of Pharmaceutical Investigation
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• 제24권2호
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• pp.105-108
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• 1994

The ulcerogenic activity of a 3% ketoprofen gel (ID-GEL) after its transdermal application in rats was determined with the Litchfield and Wilcoxon method in reference to the oral administration of ketoprofen in a suspension. The $UD_{50}$ (dose producing ulcers in 50%, of the rats tested) of ID-GEL after its transdermal application was approximately 4 times greater than that after the oral administration of the drug, indicating that the ulcerogenic activity of ketoprofen was much lowered with its transdermal application.

• Journal of Pharmaceutical Investigation
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• 제17권2호
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• pp.61-65
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• 1987

4-Pivaloyloxy, 4-benzenesulfonyloxy and 4-p-toluenesulfonyloxy compounds of piroxicam (2a, 2b and 2c) and isoxicam(4a, 4b and 4c) were synthesized in fairly good yield. Antiinflammatory and ulcerogenic effects of the 6 compounds were determined. Antiinflammatory effect of 2a was comparable to that of piroxicam and ulcerogenic effect of 2a was less than that of piroxicam.

• Natural Product Sciences
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• 제15권1호
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• pp.22-26
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• 2009

Phytochemical investigation of the roots of Echiochilon fruticosum resulted in the isolation of two naphthoquinone derivatives. Compound 1 was identified as anhydroalkanin while compound 2 was identified as a new derivative 5-hydroxy 8-methoxy 2-(4-methylpent-1,3-dienyl) naphthalene-1,4-dione named as echiochiloquinone. In addition, caffeic acid 3, caffeic acid methyl ester 4 were isolated. The structures were determined by physical, chemical and spectral methods. The anti-inflammatory activity of the root extracts and compound 2 was evaluated utilizing both cotton pellet-induced and carragenin-induced rat paw edema. The ulcerogenic effect was also studied.

• Natural Product Sciences
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• 제15권3호
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• pp.134-138
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• 2009

In an attempt to establish anti-ulcerogenic activity of potato tubers, inhibitory activity against ethanol- and indomethacin-induced gastric ulcer models in rats was evaluated for the first time. From several varieties of potato tubers including Solanum tuberosum L. cv. Superior (white skin and fresh potato) and two new varieties of (Bora valley and Gogu valley), raw potato juice was prepared and the starch was obtained from each juice by filtration and drying. Upon oral administration to rats, raw potato juice showed more or less inhibitory activity. The starch showed higher and dose-dependent inhibitory activity, suggesting that the active ingredient in raw potato juice may be the starch. Particularly, the starch obtained from the tubers of new potato variety, "Bora valley," with purple color, showed the highest inhibitory activity (62.4% and 37.1% inhibition of ulcer index at 500 mg/kg), while omeprazole (proton pump inhibitor) used as a reference drug showed 74.4% and 75.7% inhibition at 20 mg/kg against ethanol- and indomethacin-induced ulcer formation, respectively. The present study provides a first evidence of anti-ulcerogenicity of raw potato juice and the starch. Especially, the starch from "Bora valley" strongly inhibited ulcer formation in rats. Considering that these are food components, they may be safely used for anti-ulcerogenic nutraceuticals.

• Advances in Traditional Medicine
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• 제7권2호
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• pp.141-149
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• 2007

Madhuca indica has been used ethnomedically in Indian folks. In the present study we have investigated anti-inflammatory, anti-ulcer and hypoglycaemic effect of ethanolic extract (EE) and crude alkaloid extract of Madhuca indica seed cake on albino rats. The study showed that the EE had a significant, dose dependent anti-edematogenic, anti-ulcerogenic and hypoglycaemic activity, whereas the crude alkaloid extract exhibited a significant only. Both the extracts possess dose dependent inhibitory activity on carrageenan-induced edema, inhibiting prostaglandins or mediators involved in prostaglandin synthesis, the second phase of inflammation. The EE was significantly effective in protecting pylorus-ligation-induced gastric ulcers at a higher dose level. The active principle of EE seems to be a selective inhibitor of the COX II (prostaglandin synthesis) without important effect on COX I since, EE exhibited both anti-edematogenic and anti-ulcerogenic effect. The EE was effective in reducing the plasma glucose level in normal albino rats in a dose dependent manner, producing hypoglycaemic effect by stimulating the release of insulin from the ${\beta}-cells$ and/or increasing the uptake of glucose from the plasma.

• Archives of Pharmacal Research
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• 제24권3호
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• pp.171-179
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• 2001

The present investigation deals with the synthesis of some new salicylamidoacetyl sulfonamides 3a,b, salicylamido ethylacetate 4, salicylamido acetic acid hydrazide 5, which is considered as the key intermediate for the synthesis of several series of new compounds such as salicylamido pyrazol 6 and pyrazolone 1. N-imido-derivatives 9, 10, 11, thiadiazole 13, oxadiazole 14, 15, Schiffs bases 16a-f. Cyclocondensation of Schiffs bases with thioglycolic acid gave thiazolidinone 18a-c while with acetylchloride afforded azitidinones 19a-c and with acetic anhydride gave 1,4-benzoxazepine-3,5-dione. Some of the compounds were tested for their analgesic and antiinflammatory activities as well as ulcerogenic effects. Some derivatives were more effective than salicylamide and ulcerogenic activity was variably lowered .

• Journal of Pharmaceutical Investigation
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• 제21권2호
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• pp.103-110
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• 1991

Two new prodrugs of lonazolac, lonazolac acetic acid ester and lonazolac argininate, were prepared and examined for physicochemical properties and biopharmaceutical characteristics. The prodrugs were stable in solid state and lonazolac argininate showed higher dissolution rate than lonazolacca in both artificial gastric and intestinal juices. These prodrugs have higher analgegic effect than that of lonazolac-Ca in mice, and increased anti-inflammatory activities in rats. In addition, ulcerogenic effects and acute toxicity of these prodrugs were lower than those of lonaaolac-Ca. Lonazolac acetic acid ester showed larger area under the plasma concentration-time curves (AUC) than that of lonazolac. Therefore, it was suggested that these prodrugs of lonazolac have advantages over lonzolac-Ca for not only enhanced bioavailability but also decreased ulcerogenic and toxic effects.

• 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.

• 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.