• YAKHAK HOEJI
• /
• v.44 no.3
• /
• pp.272-278
• /
• 2000

The antiinflammatory mechanism of NSAIDs is attributed to the reduction of prostaglandin synthesis by the direct inhibition of cyclooxygenase. Inhibition of prostaglandin production in organs such as stomach and kidney can result in gastric lesions, nephrotoxicity and increased bleeding. In this study, newly designed COX-2 inhibitors, synthesized 1,2-benzothiazine derivatives, were screened in vitro for selectivity of COX-1 and COX-2 inhibition properties. Lead compounds in the structure-activity relationship were studied to synthesize new highly selective COX-2 inhibitors.13 determine inhibitory effect of COX-2, synthesized 1,2-benzothiazine derivatives were screened with accumulation of prostaglandin by lipopolysaccharide (LPS) in aspirin-treated macrophages and murine macropharge cell. Some of synthesized 1,2-benzothiazine derivatives were shown to be effective as selective COX-2 inhibitory activity. Others exhibited a preferential inhibition of COX-2, although some COX-1 inhibitory activity was still present. As a conclusion, simple monomer derivatives were more active than dimer derivatives. Substitution of halogen (Br, C1) on the benzothiazine nucleus slightly enhanced inhibition activity.

• Korean Journal of Pharmacognosy
• /
• v.15 no.4
• /
• pp.203-205
• /
• 1984

The extract of Ssangkum-tang was investigated on antiinflammatory activities. The extract showed antiedematous action at a dose of 500mg/kg po in carrageenin edema test in rats. The extract also inhibited the leakage of pontamine sky blue into peritoneal cavity in mice at the doses of 300 and 500mg/kg po.

• Natural Product Sciences
• /
• v.2 no.1
• /
• pp.24-28
• /
• 1996

The antiinflammatory and analgesic activities of higenamine were evaluated by measuring edema volume and pain threshold in adjuvant arthritic rats and acetic acid-induced writhing test in mice. Higenamine, with consecutive oral administrations at doses of 10 and 50 mg/kg/day, showed significant antiedemic effect and elevation of pain threshold during the secondary lesion of adjuvant arthritis. Higenamine also showed a significant inhibition of acetic acid-induced writhing syndrome with a single oral administration (200 mg/kg). From these results, it is postulated that higenamine might possess both of centrally and peripherally mediated analgesic properties.

• Korean Journal of Pharmacognosy
• /
• v.10 no.2
• /
• pp.73-77
• /
• 1979

Antiinflammatory action of phytolaccosides B and E isolated from the roots of Phytolacca americana was investigated and compared with that of aescin. Phytolaccoside B, when it was administered intravenously, exerted a potent inhibitory effect on the transudation caused by absorptive sponge pellet implanted s.c. in rats and on carrageenin induced edema in rats. Phytolaccoside E showed a weaker action than Phytolaccoside B did. Hemolytic potency of the saponins was decreased in the order of aescin, phytolaccosides B and E showing a same tendency as in antiinflammatory action. The experimental result suggests that the mode of action of phytolaccosides is the same as that of aescin.

• YAKHAK HOEJI
• /
• v.25 no.3
• /
• pp.109-114
• /
• 1981

The authors investigated drug interaction of ibuprofen and prednisolone in antiinflammatory and antipyretic activities. We have found significant differences of the antiinflammatory and antipyretic activities between single and concurrent administration of ibuprofen and prednisolone, using Sprague-Dawley Strain rats, carrageenin as a phlogistic agent and brewer's yeast as a fever inducing agent. 1) Ibuprofen(20mg/kg) was administered to the rats orally and resulted in significant reduction of (31.70 %) the swelling of rat paw induced by carrageenin, 2) prednisolone (9mg/kg) showed significant reduction of (45.76%) the swelling, 3) concurrent administration of ibuprofen (20mg/kg) and prednisolone (9mg/kg) also reduced (57.40%) the swelling. In ibuprofen (125mg/kg) administration, the inhibition rate of edema was 39.32% and in prednisolone (1mg/kg) administration, the rate was 39.04%. In concurrent administration of ibuprofen (125mg/kg) and prednisolone (1mg/kg), the inhibition rate of edema was 63.09%. Concurrent administration of ibuprofen and prednisolone showed more anti-inflammatory effects than single administration of ibuprofen and prednisolone respectively. Prednisolone itself did not show antipyretic effect, but concurrent administration of ibuprofen and prednisolone showed more antipyretic effects than ibuprofen single administratron.

• Archives of Pharmacal Research
• /
• v.11 no.1
• /
• pp.41-44
• /
• 1988

Several 4-cyano-1-benzofuranyl-1-butanone derivatives were synthesized and screened for potential antiinflammatory and analgesic activities. The effect of structural variation of these molecules on biological activities was systematically examined. Among these compounds $V_a,\;V_c\;and\;VI_e$ were found to demonstrate a significant antiinflammatory effect. Compounds $VI_e,\;V_a,\;I_d,\;I_band\;VII_f$ were also significantly effective as analgesic ones.

• YAKHAK HOEJI
• /
• v.58 no.1
• /
• pp.12-15
• /
• 2014

Polygonum cuspidatum which is widely distributed in Korea has been used as treatments of dermatitis, gonorrhea, favus athlete's foot, hyperlipidemia and inflammation in traditional medicine. We examined anti-oxidant and antiinflammatory activity by measuring DPPH radical scavenging activity and the inhibition of IFN-${\gamma}$ and LPS-induced NO production in RAW 264.7 murine macrophage cells. We isolated and characterized resveratrol (1), trans-resveratrol 3-O-${\beta}$-Dglucopyranoside (2). Compounds 1 and 2 showed potent activities compared with L-NMMA ($N^G$-monomethyl-L-arginine). These results suggested that the stilbene compounds isolated from Polygonum cuspidatum might be used as antiinflammatory agents.

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

• YAKHAK HOEJI
• /
• v.56 no.6
• /
• pp.372-376
• /
• 2012

Militarin was isolated from Cordyceps militaris, a caterpillar-grown traditional medicinal mushroom and reported to possess anticancer activities against several tumor cells. A number of militarin derivatives bearing different numbers of ethylene glycol unit were synthesized and evaluated for their biological activities related with anticancer and antiinflammatory effects. Among militarin derivatives tested, the compounds 2 and 5 exhibited anticancer and antiinflammatory activities.

• Proceedings of the PSK Conference
• /
• 2003.10b
• /
• pp.197.4-198
• /
• 2003

As an attempt to search for bioactive natural constituents exerting antinociceptive and antiinflammatory activities, we examined the potency of the extract of R. coreanus fruits by the activity-guided fractionation. The EtOAc- and BuOH fraction and those alkaline hydrolysates showed significant antinociceptive effects as assessed by writhing-, hot plate- and tail flicks tests in mice and rats as well as antiinflammatory effect in rats with carrageenan-induced edema. BuOH extract was subjected to column chromatography to obtain a large amount of niga-ichigoside F$_1$ (1, 23-hydroxytormentic acid 28-O-glc), which was again hydrolyzed in NaOH solution to yield an aglycone 23-hydroxytormentic acid (1a). (omitted)