• YAKHAK HOEJI
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• v.25 no.1
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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.

• Archives of Pharmacal Research
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• v.24 no.3
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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 .

• Natural Product Sciences
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• v.2 no.2
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• pp.96-101
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• 1996

A new natural product, 3,4,8-trihydroxybenzopyranopyran-6,9-dione was isolated from the aqueous ethanolic gall extract of Tamarix aphylla (Tamaricaceae) along with the known phenolics, monodecarboxyellagic acid and brevifolin carboxylic acid as well. The structures have been established by ESI-MS, $^1H$ and $^{13}C$ NMR spectral analysis. Antiinflammatory, antipyretic and ulcerogenic activities determination for both plant (Tamarix aphylla and Phragmites australis) were carried out on aq. ethanolic of extracts.

• Archives of Pharmacal Research
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• v.24 no.3
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• pp.180-189
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• 2001

A new series of pyridazine, pyrazoles, pyrazolidine-3,5-dione, Semicarbazide, thiosemicarbazides, hydantoin, thiohydantoins, 1,2,4-triazoles, S-triazolo[3,4-b]-1,3,4-thiadiazoles incorporated indirectly into salicylamide moiety at position 2 were synthesized. Also the synthesis of novel series of 3-salicylamido-2-hydroxypropyl-amino derivatives were prepared. Several of these compounds were screened for antiinflammatory, analgesic, antipyretic and ulcerogenic activities.

• Journal of Pharmaceutical Investigation
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• v.21 no.2
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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.

• Advances in Traditional Medicine
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• v.7 no.2
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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.

• Journal of the East Asian Society of Dietary Life
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• v.16 no.2
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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.

• Korean Journal of Food Science and Technology
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• v.31 no.3
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• pp.764-770
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• 1999

Antimicrobial activities were assayed through the hot-water extracts from 41 species of medicinal plants against Helicobacter pylori which is known as the ulcerogenic phathogen. Opuntia ficus-indica, Houttuynia cordata, Sinomenium acutum, and Coptis japonica showed the MIC at the concentrations less than 100 ppm, Pulsatilla koreana, Forsythia koreana, Rheum undulatum, and Perilla frutescens less than 200 ppm, Belamcanda chinensis, Arctium lappa, Cassia tora, Citrus tachibana, Siegesbeckia orientalis, and Caesalpinia sappan less than 300 ppm by the 2-fold dilution method. In disc method only three of them were confirmed to have antimicrobial activities which were increased in the order Perilla frutescens, Coptis japonica, Caesalpinia sappan. Three extracts were partitioned with chloroform, ethyl acetate and butanol in sequence and examined for the activity to inhibit H. pylori. The major ativities were observed in ethyl acetate fraction of Caesalpinia sappan, butanol fraction of Perilla frutescens, butanol and chloroform fraction of Coptis japonica. The partitioned fractions were found to have increased antimicrobial activities in all extracts. The experiments in which the extracts were added into urea R broth containing the crude urease derived from H. pylori resulted in the increase of pH and optical density at 560 nm to 8.15 and 1.7 respectively. Urease activity of H. pylori was inhibited over 80% by Caesalpinia sappan, Perilla frutescens, and Coptis japonica, of which Caesalpinia sappan suppressed up to 95%.

• Archives of Pharmacal Research
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• v.29 no.7
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• pp.591-597
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• 2006

Aerial parts of Artemisia asiatica (Compositae) have been traditionally used as an oriental medicine for the treatment of inflammatory and ulcerogenic diseases. In the present study, artemisolide was isolated as a nuclear factor $(NF)-{\kappa}B$ inhibitor from A. asiatica by activity-guided fractionation. Artemisolide inhibited $NF-{\kappa}B$ transcriptional activity in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7 with an $IC_{50}$ value of $5.8\;{\mu}M$. The compound was also effective in blocking $NF-{\kappa}B$ transcriptional activities elicited by the expression vector encoding the $NF-{\kappa}B$ p65 or p50 subunits bypassing the inhibitory kB degradation signaling $NF-{\kappa}B$ activation. The macrophages markedly increased their $PGE_2$ and NO production upon exposure to LPS alone. Artemisolide inhibited LPS-induced $PGE_2$ and NO production with $IC_{50}$ values of $8.7\;{\mu}M$ and $6.4\;{\mu}M$, respectively, but also suppressed LPS-induced synthesis of cyclooxygenase (COX)-2 or inducible NO synthase (iNOS). Taken together, artemisolide is a $NF-{\kappa}B$ inhibitor that attenuates LPS-induced production of $PGE_2$ or NO via down-regulation of COX-2 or iNOS expression in macrophages RAW 264.7. Therefore, artemisolide could represent and provide the anti-inflammatory principle associated with the traditional medicine, A. asiatica.