• Archives of Pharmacal Research
• /
• 제11권1호
• /
• 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.

• Journal of Pharmaceutical Investigation
• /
• 제14권3호
• /
• pp.136-143
• /
• 1984

Inclusion complex formation of fenbufen with ${\beta}-cyclodextrin$ in water and in solid state was comfirmed by solubility method, ultra violet absorption, circular dichroism and infra-red spectroscopies, differential thermal analysis, and X-ray diffractometry. A solid complex of fenbufen with ${\beta}-cyclodextrin$ in 1 : 1 molar ratio was prepared by the freeze-drying method, its dissolution characteristics in water and its analgesic and antiinflammatory effect in mouse or rat were examined. The apparent release of fenbufen from the inclusion complex was significantly improved, hut no significant difference in its analgesic and antiinflammatory effect was found.

• 생약학회지
• /
• 제29권1호
• /
• pp.1-7
• /
• 1998

Aqueous extract of Morus alba L. blocked the toxic effect of paraquat on E. coli growth. The active components in the extract may be capable of crossing the cell membranes and protect against superoxide toxicity in E. coli, The extract inhibited $FeSO_4/H_2O_2$ induced lipid peroxidation in rat liver homogenate and protected against t-butyl hydroperoxide caused Ac2F cell damage. Moreover, the extract showed inhibitory effect on phospholipase $A_2$ activity in a dose dependent manner. Antiinflammatory effect of the extract was further investigated using the carrageenin-induced oedema model. A single adminstration of the extract (3g/kg body, p.o.) was more effective than indomethacin. These results suggest that the isolation and identification of the active components would have significant therapeutic application to inflammation associated with oxygen radicals.

• Archives of Pharmacal Research
• /
• 제20권5호
• /
• pp.414-419
• /
• 1997

Gastrointestinal irritation is the most frequent adverse effect in patients chronically taking nonsteroidal antiinflammatory drugs (NSAIDs) for the treatment of arthritic conditions. Gastroprotective effect of DA-9601, a new antiulcer agent from Artemisiae Herba extract, against NSAID was evaluated in a rat model of arthritis that is similar in many aspects to human rheumatoid arthritis. Daily oral dosing of naproxen (30 mg/kg), one of the most commonly used NSAID, induced apparent gastric lesions as well as a significant decrease in mucosal prostagiandin $E_2;(PGE_2)$ and prostagiandin F_${1{\alpha}}$$(PGF_{1{\alpha}})$ levels. Coadministration of DA-9601 prevents naproxen-induced mucosal injury and depletion of prostaglandins, in a dose-related manner. DA-9601 did not alter the antiinflammatory or analgesic effect of naproxen. The present results suggest that DA-9601 may be useful as a mucoprotectant against NSAIDs in clinical practice.

• 약학회지
• /
• 제44권3호
• /
• 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.

• Natural Product Sciences
• /
• 제2권1호
• /
• 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.

• 생약학회지
• /
• 제10권2호
• /
• 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.

• 약학회지
• /
• 제25권3호
• /
• 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.

• 대한약학회:학술대회논문집
• /
• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
• /
• 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)

• 약학회지
• /
• 제23권2호
• /
• pp.119-124
• /
• 1979

Eight derivatives of arylpropionic acid, arylcarbonylpropicnic acid, and arylhydroxybutyric acid were synthesized and their structures were elucidated on the basis of elemental analysis and spectral data. Also their antiinflammatory activities were evaluated by the method of the inhibitory effect on the carrageenin-induced rat paw edema and compared with phenylbutazone. Compound (I) exhibited 59% edema inhibition vs control when 100 mg/kg, was orally administered, whereas phenylbutazone showed 57.8% for 50mg/kg.