• 약학회지
• /
• 제25권1호
• /
• pp.9-14
• /
• 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
• /
• 제24권3호
• /
• pp.171-179
• /
• 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
• /
• 제2권2호
• /
• pp.96-101
• /
• 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
• /
• 제24권3호
• /
• pp.180-189
• /
• 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
• /
• 제21권2호
• /
• pp.103-110
• /
• 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
• /
• 제7권2호
• /
• pp.141-149
• /
• 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.

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

• 한국식품과학회지
• /
• 제31권3호
• /
• pp.764-770
• /
• 1999

41종의 약용식물을 열수추출하여 위궤양 원인균으로 보고된 Helicobacter pylori에 대해 항균활성을 탐색하였다. 2-fold dilution 방법에 의해서는 백련초, 어성초, 방기, 황련은 100 ppm이하, 백두옹, 연교, 종대황, 소엽은 200 ppm 이하, 사간, 우방자, 결명자, 귤피, 희침, 소목은 300 ppm 이하와 농도에서 H. pylori에 대해 항균활성을 나타냈다. 이중 3가지 추출물만이 disc 방법을 통해 항균활성이 재확인되었으며, 소목, 황련, 소엽의 순으로 강한 항균활성을 나타냈다. 항균활성이 확인된 3가지 추출물을 chloroform, ethyl acetate, butanol로 순차 분획하여 H. pylori에 대한 항균활성을 확인하였다. 소목의 경우는 ethyl acetate 분획물에서, 소엽의 경우는 butanol 분획물에서, 황련의 경우는 butanol과 chloroform 분획물에서 가장 강한 항균활성을 나타내었다. 추출물의 분획에 따른 항균활성의 상승효과는 모든 추출물에서 확인할 수 있었다. H. pylori의 crude-urease를 분리하여 urea R broth에서 흡광도와 pH를 조사한 결과, 반응 2시간 후 pH가 8.15까지, 560 nm에서의 흡광도는 1.7까지 증가하는 것으로 나타났다. H. pylori의 urease 활성은 소목, 소엽, 황련에 의해 80%이상 억제되었으며, 이중 소목은 urease 활성을 95%이상 억제시켰다.

• Archives of Pharmacal Research
• /
• 제29권7호
• /
• pp.591-597
• /
• 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.