• Biomolecules & Therapeutics
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• v.18 no.2
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• pp.159-165
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• 2010

Alpinia katsumadai has been widely used in traditional Chinese and Korean medicine to treat a variety of conditions including emesis and gastric disorders such as gastric pain and distended abdomen. To investigate the antinociceptive potential and mechanism of A. katsumadai, ethanolic extracts of A. katsumadai were assayed on cyclooxygenase-2 and evaluated for analgesic activity based on phenylbenzoquinone (PBQ)-induced writhing and carrageenan-induced hyperalgesia tests. A. katsumadai extracts inhibited the cyclooxygenase-2 enzyme activity in a dose-dependent fashion at an $IC_{50}$ value of 0.044 ${\mu}g$/ml. A. katsumadai extract (30-300 mg/kg, orally (p.o.) administered) significantly inhibited PBQ-induced writhing. This inhibition was judged not to be a false positive because a Rota-rod test revealed no difference in muscular coordination when compared to the controls. With regard to the carrageenan-induced hyperalgesia, A. katsumadai extract (30-300 mg/kg, p.o.) produced a significant, dose-dependent increase in the withdrawal response latencies. Naloxone did not reverse the analgesic effect of A. katsumadai extract in the carrageenan-induced hyperalgesia. Taken together, these results suggest that the antinociceptive activity of A. katsumadai is not related to the opioid receptor. A. katsumadai extract has remarkable, non-opioidreceptor-mediated analgesic effects on PBQ-induced writhing and carrageenan-induced hyperalgesia that occur via cyclooxygenase-2 inhibition.

• Journal of Food Hygiene and Safety
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• v.8 no.3
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• pp.157-161
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• 1993

In order to get infonnations on the development of alcohol induced cardiovascular disorders, primary cultured vascular smooth muscle cells (PVSMC) were treated with acetaldehyde, one of the most reactive metabolites of ethanol. Acetaldehyde caused the striking release of lactate dehydrogenase (LDH) from PVSMC and it stimulated the prostaglandin synthesis in the same system. But it didn't induce cyclooxygenase activity. lipoxygenase inhibitors-propyl gallate and nordihydroguaiaretic acid could reverse the effect of acetaldehyde, but dexamethasone, a phospholipase $A_2\;(PIA_2)$ inhibitor and cyclooxygenase inhibitors except indomethacin could not protect the cells from acetaldehyde toxicity. These results indicate that enhanced prostaglandin synthesis by acetaldehyde is not a direct cause of cell death, but secondary effect due to the activation of PIAl and also, the roles of the lipoxygenase metabolites and/or $PIA_2$ activity itself might be more important in the cytotoxicity of acetaldehyde.

• Journal of Physiology & Pathology in Korean Medicine
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• v.20 no.2
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• pp.455-459
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• 2006

The inhibitors of prostaglandin $E_2\;(PGE_2)$ production and cyclooxygenase-2 (COX-2) activity have been considered as potential anti-inflammatory agents. In this study, we evaluated 9 compounds isolated from 5 Korean phytomedicinal plants (Spirea prunifolia, Paeonia suffruticosa, Salvia miltiorrhiza, Scutellaria baicalensis, and Artemisia capillaris) for the inhibition of $PGE_2$production and COX-2 expession in lipopolysaccharide (LPS)-stimulated human macrophages U937 cells. As a result, several compound such as prunioside A, penta-O-galloyl-beta-D-glucose, tanshinone IIA, baicalin, baicalein, wogonin, scopolatin, scoparone and decursinol showed potent inhibition of $PGE_2$production (50-70% inhibition at the test concentration of $10\;{\mu}M$). In addition, these compounds were also considered as potential inhibitors of COX-2 activity (45-73% inhibition at the test concentration of $10\;{\mu}M$). These active compound mediating COX-2 inhibitory activities are warranted for further elucidation of active principles for development of anti-inflammatory agents and these properties may contribute to the anti-atopic dermatitis activity.

• Journal of Physiology & Pathology in Korean Medicine
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• v.19 no.5
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• pp.1419-1426
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• 2005

This study was carried out to investigate the effects of herbal extracts on the skin inflammatory reactions which use the makeup preparations. In experiment 1, among the herbal ingredients of herbal extracts, ethanol extracts and 1,3-BG(Butylene Glycol) extracts of Galla Rhois showed potent radical scavenging activity, more than 91% at all concentrations, tested by DPPH (1,1-diphenyl-2-picryl-hyrazyl) method. In experiment 2, ethanol extracts of Chrysanthemi Flos, Gardenias Flos, Galla Rhois showed potent inhibitory activity of the lipopolysaccharide-induced nitric oxide(NO) production, more than 87% at $10{\mu}g/m{\ell}$, by the macrophage RAW 246.7 cells. And 1,3-BG extracts of Taraxaci Herbs, Corm Fructus, Galla Rhois showed potent inhibitory activity of nitric oxide production, more than 89% at $10{\mu}g/m{\ell}$. In experiment 3, ethanol extracts of Chrysanthemi Flos, Gardeniae Flos, Galla Rhois showed potent inhibitory effects of cyclooxygenase-II activity, more than 78% at $10{\mu}g/m{\ell}$, by using ELISA kit. And 1,3-BG extracts of Galla Rhois, Carthami Flos, Chrysanthemi Flos, Taraxaci Herba, Corm Fructus showed potent inhibitory effects of cyclooxygenase-II(COX-II) activity, more than 80% at $10{\mu}g/m{\ell}$. Therefore, 1 expect that herbal extracts, especially Galla Rhois may be used as a drug for treatment on skin inflammation and a material of the makeup preparations.

• Journal of Applied Biological Chemistry
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• v.66
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• pp.114-121
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• 2023

Selective cyclooxygenase (COX)-2 inhibition is a novel strategy to reduce the risk of gastrointestinal side effects caused by conventional nonsteroidal anti-inflammatory drugs. However, some selective COX-2 inhibitors have become apparent to increase the risk of severe cardiovascular disease. The aim of this study was to examine the anti-inflammatory effect of rosemary extract (RE) and confirm the safety of cardiovascular side effects. Inhibition of COX enzyme activity was assessed, and the levels of COX-2 and prostaglandin E₂ (PGE₂) and COX-1 and thromboxane B₂ (TXB₂) were evaluated in lipopolysaccharide (LPS)-induced RAW 264.7 cells. The 40% RE group showed increased COX-2 inhibition activity in a dose-dependent manner, whereas the 50% RE group only exhibited at 100 ㎍/mL. In a cell-based study, COX-2 mRNA expression was similar in both RE groups and PGE₂ levels tended to decrease in the 40% RE group compared to the LPS group in the LPS pretreatment condition. In the LPS posttreatment condition, the COX-2 mRNA expression decreased in the 40% RE group, and PGE₂ levels were increased in the 40 and 50% RE groups. In both conditions, there was no significant difference in COX-1 and TXB₂ levels. In conclusion, 40 and 50% RE showed significant COX-2 inhibition, similar to the positive control group. It was confirmed that the inhibition of the COX-2 expression, but the effect did not affect the balance between prostacyclin and TXB₂. These results indicate that rosemary showed COX-2 inhibition activity with a low risk of cardiovascular diseases.

• Journal of Microbiology and Biotechnology
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• v.17 no.9
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• pp.1546-1549
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• 2007

Chitosan oligosaccharide (COS, 3 kDa

• Archives of Pharmacal Research
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• v.27 no.4
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• pp.442-448
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• 2004

Wogonin (5,7-dihydroxy-8-methoxyflavone) is a down-regulator of cyclooxygenase-2 and inducible nitric oxide synthase expression, contributing to anti-inflammatory activity in vivo. For further characterization of modulatory activity on ploinflammatory gene expression in vivo, the effect of wogonin was examined in this experiment using animal models of skin inflammation. By topical application, wogonin inhibited an edematic response as well as ploinflammatory gene expression against contact dermatitis In mice. Wogonin inhibited ear edema ($19.4-22.6\%$) at doses of $50-200\;{\mu}g$/ear and down-regulated interleukin-$1{\beta}$ induction ($23.1\%$) at $200{\mu}g$/ear in phenol-induced simple irritation. Wogonin ($2{\times}50-2{\times}200{\mu}g$/ear) also inhibited edematic response ($51.2-43.9\%$) and down-regulated ploinflammatory gene expression of cyclooxygenase-2, interleukin-$1{\beta}$, interferon-$\gamma$, intercellular adhesion molecule-1 and inducible nitric oxide synthase with some different sensitivity against picryl chloride-induced delayed hypersensitivity reaction. All these results clearly demonstrate that wogonin is a down-regulator of ploinflammatory gene expression in animal models of skin inflammation. Therefore, wogonin may have potential for a new anti-inflammatory agent against skin inflammation.

• Archives of Pharmacal Research
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• v.25 no.3
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• pp.329-335
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• 2002

Previously, several prenylated flavonoids having a C-8 lavandulyl moiety were found to inhibit cyclooxygenase-1 (COX-1) as well as 5-lipoxygenase (5-LOX), and sophoraflavanone G was the most potent inhibitor against these eicosanoid generating enzymes among 19 prenylated flavonoids tested. In this investigation, effects of sophoraflavanone G on COX-2 induction from RAW 264.7 cells and in vivo inflammatory response were studied. Sophoraflavanone G inhibited prostaglandin $E_2{\;}(PGE_2)$ production from lipopolysaccharide (LPS)-treated RAW cells by COX-2 down-regulation at 1-50 uM. Other prenylated flavonoids including kuraridin and sanggenon D also down-regulated COX-2 induction at 10-25 uM, while kurarinone and echinoisoflavanone did not. In addition, sophoraflavanone G showed in vivo anti-inflammatory activity against mouse croton oil-induced ear edema and rat carrageenan paw edema via oral (2-250 mg/kg) or topical administration (10-250 ug/ear). Although the potencies of inhibition were far less than that of a reference drug, prednisolone, this compound showed higher anti-inflammatory activity when applied topically, suggesting a potential use for several eicosanoidrelated skin inflammation such as atopic dermatitis.

• Proceedings of the Korean Society of Toxicology Conference
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• 2001.10a
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• pp.133-134
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• 2001

Abnormal regulation of the inducible form of cyclooxygenase (COX-2) has been often observed in various types of cancerous and transformed cells. Recently, targeted inhibition of COX-2 is recognized as one of the promising strategies for the prevention or treatment of cancer as well as inflammation, As part of a program to evaluate the cancer chemopreventive potential of anti-inflammatory phytochemicals, we initially determined the COX-2 inhibitory activity of some naturally occurring diarylheptanoids structurally related to curcumin.(omitted)

• Biomolecules & Therapeutics
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• v.14 no.1
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• pp.11-18
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• 2006

Certain flavonoids possess anti-inflammatory activity. Besides their antioxidative property, the cellular action mechanisms of flavonoids include an inhibition of arachidonate metabolizing enzymes such as cyclooxygenases and lipoxygenases, and a down-regulation of proinflammatory gene expression such as cyclooxygenase-2, inducible nitric oxide synthase and tumor necrosis factor-$\alpha$. In this review, the recent findings of anti-inflammatory flavonoid research since 2004 were summarized. And the cellular mechanisms on signal transduction pathways were also discussed.