• Archives of Pharmacal Research
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• v.15 no.3
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• pp.251-255
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• 1992

A number of 4-hydroxy-2H (or alkyl)-N-(3-aralkyl-2-thio-1-hydantoinyl)-1, 2-benzothiazine3-carboxamide 1, 1-dioxides were synthesized through the reaction of 4-hydroxy-2H (or alkyl)1, 2-benzothiazine-3-carboxylic methyl ester 1, 1-dioxide and 1-amino-2-thio-3-aralkyl-4-imidazolones in xylene. The compounds synthesized were screened for antinflammatory effect on carrageenin-induced edema in rat and for analgesic effect on acetic acid-induced Writhing syndrome in mice. Most compounds were inhibots of carrageenin-induced rat foot edema and some showed significant antinflammatory activity comparable to that of indomethacin and significant analgesic activity comparable to that of indomethacin and aspirin.

• Bulletin of the Korean Chemical Society
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• v.26 no.12
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• pp.1975-1980
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• 2005

A series of substituted rutaecarpines were prepared by employing Fischer indole synthesis as key step and their inhibitory activities on COX-1 and 2 as well as selectivity on COX-2 were evaluated. The compounds with a methanesulfonyl and a bromo group at C10 showed promising inhibitory activity ($IC_{50}$ = 0.27, 0.35 $\mu$M, respectively) with selectivity.

• Microbiology and Biotechnology Letters
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• v.23 no.5
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• pp.526-530
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• 1995

Phospholipase A$_{2}$ (PLA$_{2}$) is lipolytic enzyme that has known to be involved in inflammation. In the course of our screening for antiinflammatory compounds from natural products, a compound having PLA$_{2}$ inhibitory activities was isolated from the methanol extract of Umbilicaria esculenta. The compound was identified as lecanoric acid based on various NMR studies including DEPT, HETERO-COSY and HMBC experiments. Lecanoric acid inhibited human rheumatoid synovial PLA$_{2}$ activity with IC$_{50}$ of 0.17 mM and also exhibited antitumor activity (ED$_{50}$=2.7 $\mu $g/ml) against skin tumor cell line (LOX-IMVI).

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.371.3-372
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• 2002

We have reported cytotoxicities based on several types of sugar linkage in saponins in addition to antitumor and antiinflammatory effects. In order to find further structure-activity relationship on the cytotoxicity of saponins. we intended to isolate oleanane disaccharides Irom the saponin-containing extract of Akebia Quinata (Lardizabalaceae). (omitted)

• Archives of Pharmacal Research
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• v.17 no.5
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• pp.304-308
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• 1994

Among the new series of phenylacetamides, one of capsaicin derivatives, KR-25018 was found to have a very potent analgesic activity. Thus, the phamacological properties of KR-25018 were compared with those of morphine, capsaicin, and nonsteroidal antiinflammatory drugs (NSAIDs). The analgesic activities were evaluated in several animal models, using different stimuli, such as phenylbenzoquinone(PBQ)-induced weithing test, tail-filck test in mice and adjuvant arthritic flexion test in rat. The relationship of phamacological properties of KR-25018 to that of centrally acting opioids was assessed by the blocking test using naloxone. The analgesic potency of the KR-25018 $(MPED_{50}=0.89{\;}p.o.{\;}in{\;}PBQ-induced{\;}weithing{\;}test, {\;}MPED_{50}$=0.61$ s.c. in tail-flick test in mice0, with different action mechanism from morphine and NSAIDs, was comparable to that of morphine.

• Natural Product Sciences
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• v.15 no.2
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• pp.55-59
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• 2009

This study for developing a new anti-inflammatory medicine was sought by investigating the antiinflammatory properties of C. indicum L. extract. Rats were treated with either saline (control) or C. indicum L. extract and then injected with LPS. We found that the plasma concentration of IL-1${\beta}$ IL-6, TNF-${\alpha}$and IL-10 peaked at 5h after LPS injection, and the plasma concentration of IL-6 and TNF-${\alpha}$ showed a tendency to decrease, and IL-10 concentration showed a tendency to increase with increasing levels of C. indicum L. extract. In the liver concentration of cytokines at 5 h post LPS injection, IL-1${\alpha}$ and IL-6 decreased with increasing concentration of C. indicum L. extract, however TNF-${\alpha}$ and IL-10 did not differ significantly the treatment groups.

• Archives of Pharmacal Research
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• v.13 no.2
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• pp.161-165
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• 1990

For evaluating the cytolytic effects on the mouse thymocytes, four typical antiinflammatory steroids (dexamethasone, triamcinolone acetonide, prednisolone, hydrocortisone) were selected in this study. When steroids were treated to the mouse thymocytes in vitro cytolysis occurred with dose-dependent fashion and the activities were found to be paralle with the known local anti-inflammatory activities. In vivo thymus atrophogenic activities appeared by the treatment of topical and subcutaneous applications of the derivatives were also found to dose-dependent, but not coincided with the thymocyte cytolytic activities in vitro and local anti-inflammaatory activity in the case of triamcinolone acetonide. Triamicinolone acetonide induced potent thymocyte cytolysis in vitro, but showed less thymus atrophy.

• Korean Journal of Pharmacognosy
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• v.28 no.4
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• pp.275-279
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• 1997

Fruits of Arctium lappa L. (Compositae), which has been used as the antiinflammatory, detoxifying and diuretic agents in the folk remedies, was examined on the in vitro oxidation of human low density lipoprotein (LDL). Several lines of evidence indicate that oxidized LDL (Ox-LDL) may promote atherogenesis. Hence. The role of antioxidants in the prevention of LDL oxidation needs to be determined. The activity of fractions of Arctii Fructus treated with oxidized LDL which was incubated with $16\;{\mu}M$ of $Cu^{2+}$ for metal catalyzed oxidation was investigated. The BuOH fraction (4\;ppm) inhibited the oxidative modification of LDL as evidenced by a decrease in the lipid peroxide content (thiobarbituric acid reacting substances activity), the negative charge of LDL (electrophoretic mobility) and increase of the vitamine E content.

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.147.1-147.1
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• 2003

As an attempt to search for bioactive natural products exerting antiinflammatory activity, we have evaluated the anti-inflammatory and antinociceptive activities of the methanol extract from the Fomes fomentarius (MEFF). MEFF (50, 100 mg/kg/day, p.o.) significantly reduced an acute paw edema induced by carrageenan in rats. When analgesic activity was measured by acetic acid-induced writhing test and hot plate test, MEFF showed a dose-dependent inhibition in animal models. In addition, MEFF potently inhibited the LPS-induced production of NO, $PGE_2$ and TNF-$\alpha$production of macrophages. (omitted)

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.161.3-162
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• 2003

Ginseng (the root of Panax ginseng C.A $M_{EYER}$, family Araliaceae) is frequently used as a crude substance in Asian countries as a traditional medicine. The major components of ginseng are ginsenosides, which have been reported to show various biological activities including antiinflammatory activity and antitumor effect. In addition, Sugiyama et al. reported that ginsenoside Rg3 suppresses histamine release from mast cells due to stimulation with compound 48/80 in vitro. However, the antiallergic effects of ginsenoside Rh2, which is metabolized by human intestinal bacteria to ginsenoside Rg3, have not been studied. (omitted)