• Proceedings of the PSK Conference
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• 2003.04a
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• pp.241.2-241.2
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• 2003

We report the synthesis of key intermediates for the development novel flavonoid derivatives with potential antiinflammatory activity and propose a mechanism of the one-pot reaction. The various amines (1) for this work were commercially available. Secondary amines (2) were formed by nucleophilic attraction using ethyl benzoylacetate. The C-N bond formation proceeded at refluxing in toluene with catalytic amount of p-toluenesulfonic acid and a removal of water was important in this reaction. (omitted)

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.183.2-183.2
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• 2003

We report the synthesis of 3,4-dihydro-2-oxo-4-quinolines 5a-e for the development novel flavonoid derivatives with potential antiinflammatory activity and propose a mechanism of the one-pot reaction. The various amines (la-e) for this work were commercially available. We isolated that ester (2a-e) were formed by nucleophilic attraction using ethyl benzoylacetate. The C-N bond formation proceeded at refluxing in toluene with catalytic amount of p-toluenesulfonic acid and a removal of water and ethanol was important in this reaction. (omitted)

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.188.3-189
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• 2003

Nonsteriodal antiinflammatory drugs(NSAIDs) are widely used to treat pain, fever, and inflammatory conditions including osteoarthritis. But chronic patients suffer from gastrointestinal disturbances such as discomfort, nausea, peptic ulcer and severe bleeding because NSAIDs inhibit not only COX-2 associated with anti-inflammatory activity, but also COX-l accompanied with side effects in the stomach and kidney. Therefore, in this study, we designed a new 2-thiohydantoin derivatives as selective COX-2 inhibitors is that the 5-membered heterocycle ring is substituted with two aryl groups. (omitted)

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.320.1-320.1
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• 2002

We investigated the effect of various triterpenoids isolated from the Cussonia bancoensis. such as ursolic acid. 23-hydroxyursolic acid. 3-O-${\alpha}$-L -arabinopyranosyl-23 -hydroxyursolic acid. 3-O-${\beta}$-D-glucopyranosyl-23-hydroxy-ursolic acid and 28-O-${\alpha}$-L -rhamnopyranosyl(1-4)-${\beta}$-D-glucopyranosyl( 1-6)-${\beta}$-D-glucopyranosylester of 23-hydroxyursolic acid. have been evaluated on lipopolysaccharide (LPS)-induced nitric oxide (NO) and prostaglandin E2 (PGE2) release by the macrophage cell line RAW 264.7. (omitted)

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.339.1-339.1
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• 2002

Since two selective COX-2 inhibitors. celecoxib and rofecoxib, showed good biological activity as antiinflammatory agents. many medicinal chemists are interested in specific COX-2 inhibitors. The distinguished feature of these drugs is that the 5-membered heterocycle ring is substituted with two aryl groups. Therefore, in this study, we designed a new hydantoin derivatives via the reaction of unnatural amino acids as selective COX-2 inhibitors, In systematically steps. 5-phenyl-1 (or substituted) hydantoin derivatives were prepared through esterification. bromination, C-N bond formation, cyclization from phenyl acetic acid. Particularly. a novel hydantoin ring was converted from unnatural amino acids with potassium isoyanate. In last step. the final analogs were synthesized the substitution at 3-position with alkyl reagents.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.343.1-343.1
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• 2002

Nonsteroidal antiinflammatory drugs(NSAIDs) are widely used to treat pain. fever and inflammatory condition. But chronic-disease patients suffer from gastro-intestinal disturbances such as discomfort. nausea. peptic ulcer and severe bleeding because NSAIDs inhibit not only COX-2 associated with anti-inflammatory activity but also COX-1 associated with adverse gastro-intestinal effects. On the basis of this fact. specific COX-2 inhibitors such as celecoxib and rofecoxib are introduced in the drug market. (omitted)

• Advances in Traditional Medicine
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• v.3 no.2
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• pp.90-99
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• 2003

There are several data in the literature indicating a great variety of pharmacological activities of Polypodium genus, which exhibit antiinflammatory and immunomodulatory activities. Since one of our main interests is to obtain natural immunoregulatory agents devoid of pharmacological adverse effects, we used flow cytometry analysis to highlight relative contributions of a water-soluble fraction of different concentrations of Polypodium rhizome extracts on lymphocyte subpopulations, NK and LAK activity. To measure their potential immunoregulatory activity a T cell proliferation assay in response to phytohemaglutinin (PHA) and mixed lymphocyte reactions were chosen. As a confirmatory bioassay we studied the effect of our extracts on CD45RO and CD95 antigen expressions. The results indicate that CD95 expression dramatically increases after peripheral blood lymphocyte activation and treatment with Polypodium leucotomus, cambricum and vulgare extracts, suggesting a powerful intrinsic pro-apoptotic effect.

• Bulletin of the Korean Chemical Society
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• v.28 no.4
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• pp.561-566
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• 2007

Adenosine kinase (AK) is a ubiquitous intracellular enzyme, which catalyzes the phosphorylation of adenosine (ADO) to adenosine monophosphate (AMP). AK inhibitors have therapeutic potential as analgesic and antiinflammatory agents. A chemical feature based pharmacophore model has been generated from known AK inhibitors (26 training set compounds) by HypoGen module implemented in CATALYST software. The top ranked hypothesis (Hypo1) contained four features of two hydrogen-bond acceptors (HBA) and two hydrophobic aromatics (Z). Hypo1 was validated by 124 test set molecules with a correlation coefficient of 0.905 between experimental and estimated activity. It was also validated by CatScramble method. Thus, the Hypo1 was exploited for searching new lead compounds over 238,819 chemical compounds in NCI database and then the selected compounds were screened based on restriction estimated activity and Lipinski's rules to evaluate their drug-like properties. Finally we could obtain 72 new lead candidates and the two best compound structures from them were posted.

• Archives of Pharmacal Research
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• v.27 no.6
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• pp.628-632
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• 2004

The chloroform and the ethyl acetate fractions from the roots of Acanthopanax chiisanensis exhibited a significant inhibition of prostaglandin E$_2$ (PGE$_2$）production in rat peritoneal macrophages stimulated by the protein kinase C activator, 12-O-tetradecanoylphorbol 13-acetate （TPA）. Hyperin was isolated as an active principle from the ethyl acetate fraction. It sup-pressed not only $PGE_2$ production but also nitric oxide （NO） production in vitro in a concentration dependent manner. their $IC_{50}$, being 24.3 and $32.9{\;}{\mu}M$, respectively. Hyperin also caused a significant inhibition of increase in acetic acid-induced vascular permeability in mice in vivo.

• Korean Journal of Pharmacognosy
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• v.43 no.1
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• pp.85-93
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• 2012

181 kinds of local native plants were selected by its anti-inflammatorial folk medicinal uses and evaluated it antioxidative and inhibitory activity of nitric oxide (NO) production in lipopolysaccharide (LPS)-induced 264.7 macrophage cells. Among the 181 kinds of plants, 99 species showed potent antioxidative activities and 20 extracts showed inhibitory activity towards nitric oxide production by more than 70% at a concentration of $100{\mu}g/mL$. Therefore, these plants should be considered promising candidates for the treatment of inflammatory diseases accompanying overproduction of NO.