• YAKHAK HOEJI
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• v.48 no.2
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• pp.141-146
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• 2004

Selective COX-2 inhibitors were expected to retain anti-inflammatory activity by inhibition of prostaglandin production with reduction of gastric and renal side effect associated with non-steroidal anti-inflammatory drugs. This study reported the syntheses of novel 2-thiohydantoin and hydantoin derivatives which have the structure of 5-membered heterocyclic ring substituted with two aryl groups, phenyl group at 5-position and p-sulfamylphenyl or p-methoxyphenyl group at 1-position. These synthetic compounds showed significant COX-2 activities in vitro screening. Among them, 5-phenyl-2-thiohydantoin and hydantoin substituted with benzyl group at 3-position, compounds 5 and 8, could be considered as lead compounds with $IC_{50}$/=13.13∼18.78 $\mu\textrm{g}$/$m\ell$ for the development of COX-2 inhibitors.

• Proceedings of the Korean Society of Toxicology Conference
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• 2002.05a
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• pp.95-95
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• 2002

Cyclooxygenases (COXs) are key enzymes in the conversion of arachidonic acid into prostanoids, which are involved in cell proliferation and inflammation. Two distinct COXS have been identified: COX-l which is constitutively expressed and COX-2 which is induced by different products such as tumor promoters or growth factors.(omitted)

• Proceedings of the Korean Society of Toxicology Conference
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• 2002.05a
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• pp.87-87
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• 2002

We have investigated the effects of genistein on induction of cyclooxygenase-2 (COX-2) that plays an important role in the pathophysiology of carcinogenesis as well as in cellular response to inflammatory stimuli. Treatment of MCF10A cells with 12-O-Tetradecanoylphorbol-13-acetate (TPA) or TNF-$\alpha$ resulted in increased COX-2 expression and PGE$_2$ production, which was inhibited by genistein.(omitted)

• Advances in Traditional Medicine
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• v.7 no.3
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• pp.229-234
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• 2007

In macrophages, nitric oxide (NO) is released as an inflammatory mediator and has been proposed to be an important modulator of many pathophysiological conditions including inflammation. In this study, we have examined the inhibition effects of NO production by 85% methanol extract of the flower of Pueraria thunbergiana (PF) in mouse macrophages. Extract of PF (1, 10, 100 ${\mu}g/ml$) inhibited NO production, inducible NO synthase and cyclooxygenase-2 expression in interferon-g and lipopolysaccharide-stimulated mouse peritoneal macrophages and it had no cytotoxicity. These data suggest that 85% methanol extract of PF might be useful in controlling macrophages mediated inflammatory disease.

• Proceedings of the Korean Society of Life Science Conference
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• 2005.04a
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• pp.226-226
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• 2005

• Proceedings of the Korean Society of Toxicology Conference
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• 2001.10a
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• pp.31-32
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• 2001

A wide array of phenolic substances, particularly those present in dietary and medicinal plants, have been reported to possess substantial anticarcinogenic and antimutagenic activities. The majority of naturally occurring phenolics retain antioxidative and anti-inflammatory properties which appear to contribute to their chemopreventive or chemoprotective activity. Inducible cyclooxygenase (COX-2) and nitric oxide synthase (iNOS) are important enzymes that mediate inflammatory processes.(omitted)

• Archives of Pharmacal Research
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• v.27 no.5
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• pp.467-470
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• 2004

Comparative molecular field analysis and comparative molecular similarity indices analysis were performed on twenty five analogues of pimarane COX-2 inhibitor to optimize their cyclooxygenase-2 (COX-2) selective anti-inflammatory activities.

• YAKHAK HOEJI
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• v.55 no.4
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• pp.295-300
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• 2011

We investigated the effects of butanol fraction of Asterias amurensis (BFA) on the anti-allergic activity. BFA inhibited both cyclooxygenase-2 dependent prostaglandin $D_2$ and 5-lipoxygenase dependent leukotriene $C_4$ generation in a concentration-dependent manner with $IC_{50}$ values of 174.6 and 22.2 ${\mu}g$/ml, respectively. In addition, BFA also inhibited the degranulation in a dose dependent manner. Furthermore, oral administration of BFA inhibited IgE-mediated passive cutaneous anaphylaxis in mice. These results suggested that BFA may be useful in regulating mast cell-mediated allergic diseases.

• YAKHAK HOEJI
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• v.43 no.1
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• pp.117-123
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• 1999

Because of the potent effects of lipid mediators such as prostaglandins (PGs), leukotriens (LTs) and platelet activating factor (PAF) on a variety of cells and tissues, they are considered as major contributors to the process leading to inflammation and allergy. To pursue the mechanism of anti-inflammatory activity of Lonicera japonica, we tested inhibitory effects of 7 flavonoids from Lonicera japonica on arachidonic acid cascade related enzymes, such as inflammatory phospholipase $A_2$, cyclooxygenase-1 and 2, 5-lipoxygenase, in bone marrow derived mast cell (BMMC), and lyso PAF-acetyltransferase in rat spleen microsomes. Anti-inflammatory activities of lonicera japonica are thought to be attributed at least in part to the inhibition of arachidonic acid cascade releated enzymes by flavonoids such as apigenin, luteolin quercetin.

• Journal of Acupuncture Research
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• v.22 no.2
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• pp.111-121
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• 2005

Human placental extract (HPE), which is prepared from the placenta of healthy pregnant females, has been widely used in clinical field. HPE is known to possess anti-inflammatory, anti-viral, anti-oxidative, anti-mutagenic, and analgesic properties. In this study, the effect of HPE against lipopolysaccharide (LPS)-induced inflammation was investigated. From the present results, HPE was shown to suppress prostaglandin E2 synthesis (PGE2) and nitric oxide (NO) production by inhibition on the LPS-stimulated enhancement of the cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) expressions in mouse BV2 microglial cells. These results suggest that HPE may offer a valuable mean of therapy for the treatment of brain inflammatory diseases by attenuating LPS-induced PGE2 and NO production.