• Natural Product Sciences
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• 제2권2호
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• pp.119-122
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• 1996

The antiinflammatory activity of the methanol extract of Leucas lavandulaefolia Rees was evaluated on different experimental models of inflammation in rats. The extract has been found to possess significant, inhibitory activity against carrageenin, histamine, serotonin, and dextran induced hind paw oedema in rats. The effect produced by extract was comparable to that of phenylbutazone and a prototype, nonsteroidal antiinflammatory agent.

• Journal of Pharmaceutical Investigation
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• 제24권1호
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• pp.17-24
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• 1994

The antiinflammatory and antirheumatic activities of a 3% ketoprofen gel (ID-GEL) were evaluated using carrageenan-induced paw edema method and adjuvant-induced arthritis method, respectively, after its transdermal administration of 50 mg on rat paws in reference to existing transdermal preparations containing 3% ketoprofen and other nonsteroidal antiinflammatory drugs (NSAIDs). The % inhibition of carrageenan-induced edema by ID-GEL was 56.2-65.0%, close to the maximum inhibition obtainable with this model, while the % inhibition by existing 3% ketoprofen gels and other NSAID transdermal preparations were 33.8-47.7% and 18.7-29.2%, respectively. ID-GEL had a pronounced antirheumatic activity in both preventive and curative studies with adjuvant-induced arthritis in rats in respect with the inhibition of edema, arthritis score and weight gain, in reference to existing 3% ketoprofen gel.

• 약학회지
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• 제38권5호
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• pp.525-529
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• 1994

Antiinflammatory activity of an 1% flurbiprofen transdermal gel was evaluated using the carrageenan-Induced rat paw edema method. The application of 50 mg of the gel on the rat hind paw, at various time intervals from 0 to 24 hrs before the carrageenan injection, significantly inhibited edema formation in all groups of dosed rats, indicating that the antiinflammatory activitv was maintained up to 24 hrs after the transdermal application of the 1% flurbiprofen gel. The topical $ED_{50}$ of flurbiprofen in the gel was 1.0 mg/kg, whereas the oral $ED_{50}$ of the drug in a suspension was 1.7 mg/kg.

• Archives of Pharmacal Research
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• 제16권1호
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• pp.29-31
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• 1993

A methanol extract of the roots of bupleurum longiradiatum (Umbelliferar) showed antiinflammatory activity in rats. Hexane, chloroform, butanol, and aqueous fractions from the methanol extract were tested with the result that only the hexane fraction exhibited positive activity. Fractionation of the hexane extract resulted in isolation of arborinone as an active principle.

• Biomolecules & Therapeutics
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• 제6권1호
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• pp.45-49
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• 1998

The pharmacokinetic properties and antiinflammatory activity of 3% ketoprofen lotion (ID-lotion), formulated with poloxamer 407, were evaluated using rats. For the pharmacokinetic study, the lotion, at the dose of 4.5 mg/kg, was applied on the dorsal skin of rats and the drug concentration in plasma was determined using an HPLC method. As references, ketoprofen suspended in saline was administered orally, and E-lotion, which is a 3% ketoprofen lotion in the Japanese market was applied transdermally. Following the transdermal application of ID-lotion and E-lotion, $C_{max}$ were 316 $\pm$22.3 ng/ml and 163 $\pm$ 12.2 ng/ml, respectively, at the same Tma of 2 hours postdose, while $C_{max}$ and $T_{max}$ after oral administration of the drug were 1,030$\pm$89.1 ng/ml and 0.25 hours, respectively. Relative bioavailabilities of ID-lotion and I-lotion were 69.3% and 34.2%, respectively. The antiinflammatory activity of the two 3% ketoprofen lotions was evaluated with carrageeneninduced edema method after 50 mg of the lotions was applied on the paw of rats. ID-lotion showed 67.6% inhibition of the edema formation, while I-lotion showed 34.\\\\`r%. The calculated ED5o after transdermal application of ID-lotion was 2.5 mg/kg, while that after oral administration was 7.0 mg/kg. Based on these results, the relative equiponderal availability of ID-lotion was 296% compared to the oral administration of ketoprofen.n.n.n.

• 약학회지
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• 제44권3호
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• pp.272-278
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• 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.

• Archives of Pharmacal Research
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• 제11권1호
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• pp.41-44
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• 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
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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.

• Journal of Ginseng Research
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• 제44권1호
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• pp.145-153
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• 2020

Background: Panax ginseng Meyer (Araliaceae) is a highly valued medicinal plant in Asian regions, especially in Korea, China, and Japan. Chemical and biological studies on P. ginseng have focused primarily on its roots, whereas the seeds remain poorly understood. This study explores the phytochemical and biological properties of compounds from P. ginseng seeds. Methods: P. ginseng seeds were extracted with methanol, and 16 compounds were isolated using various chromatographic methods. The chemical structures of the isolates were determined by spectroscopic data. Antiinflammatory activities were evaluated for triterpene and steroidal saponins using lipopolysaccharide-stimulated RAW264.7 macrophages and THP-1 monocyte leukemia cells. Results: Phytochemical investigation of P. ginseng seeds led to the isolation of a novel triterpene saponin, pseudoginsenoside RT₈, along with 15 known compounds. Pseudoginsenoside RT₈ exhibited more potent antiinflammatory activity than the other saponins, attenuating lipopolysaccharide-mediated induction of proinflammatory genes such as interleukin-1β, interleukin-6, inducible nitric oxide synthase, cyclooxygenase-2, and matrix metalloproteinase-9, and suppressed reactive oxygen species and nitric oxide generation in a dose-dependent manner. Conclusion: These findings indicate that pseudoginsenoside RT₈ has a pharmaceutical potential as an antiinflammatory agent and that P. ginseng seeds are a good natural source for discovering novel bioactive molecules.

• 약학회지
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• 제58권1호
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• pp.12-15
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• 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.