• Title/Summary/Keyword: COX-1

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Lonicerae Flos Inhibited COX-2 and MMP-9 in LPS Induced Arthritis of Mouse through Regulation of MIF (LPS 유도 생쥐 관절염에서 금은화의 MIF 활성 조절이 COX-2와 MMP-9 생성 억제에 미치는 영향)

  • Ahn, Sang-Hyun;Kim, Ho-Hyun
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.24 no.2
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    • pp.242-248
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    • 2010
  • The present study was designed in order to determine whether Lonicerae flos (LF) could mitigate rheumatoid arthritis through inhibition of cyclooxygenase (COX)-2 and matrix metalloproteinase (MMP)-9 by regulation of macrophage migration inhibitory factor (MIF). We found that MIF mRNA expression in synoviocytes stimulated with phorbol-12-myristate-13-acetate dose-dependantly decreased by LF extract treatment (0.4 - 1.0 mg/$m{\ell}$). The distribution of MIF, COX-2 and MMP-9 positive reacted cells in LPS induced arthritis of mice were decreased by LF (45 mg/kg/day) treatment for 28 days. These data likely indicate that LF may act as MIF inhibitor and may be possible to develop useful agent for rheumatoid arthritis.

Inhibitory Effect of Glycoprotein Isolated from Cudrania tricuspidata Bureau on Histamine Release and COX-2 Activity in RBL-2H3 Cells (RBL-2H3 세포에 있어서 꾸지뽕 당단백질에 의한 히스타민 방출 및 COX-2 활성 억제 효과)

  • Oh, Phil-Sun;Lee, Hye-Jin;Lim, Kye-Taek
    • Korean Journal of Food Science and Technology
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    • v.41 no.4
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    • pp.405-412
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    • 2009
  • The purpose of this study was to determine the inhibitory effect of a glycoprotein isolated from Cudrania tricuspidata Bureau (CTB glycoprotein, 75 kDa) on immunoglobulin E (IgE)-induced allergic inflammation in RBL-2H3 cells. This experiment evaluated the production of intracellular reactive oxygen species (ROS), the activities of mitogenactivated protein kinase (MAPK), transcription factor (c-jun), and cyclooxygenase (COX)-2, and histamine release in cells. The results showed that the CTB glycoprotein inhibited histamine release and COX-2 expression induced by IgE in the cells. The CTB glycoprotein also had suppressive effects on the expressions of ERK1/2, p38 MAPK, c-jun, and the production of intracellular ROS in IgE-treated RBL-2H3 cells. The activities of c-jun and COX-2 were collectively blocked by ERK1/2 inhibitor (PD98059) and p38 MAPK inhibitor (SKF86002), respectively. Hence, we speculate that CTB glycoprotein might be a component with potential use in the preparation of health supplements for the prevention of allergic diseases.

Cyclooxygenase-2 Expression in Benign and Malignant Chondroid Tumors (양성 및 악성 연골 종양의 Cyclooxygenase-2 발현)

  • Park, Hye-Rim;Min, Kwang-Seon;Park, Yong-Koo
    • The Journal of the Korean bone and joint tumor society
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    • v.13 no.2
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    • pp.105-112
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    • 2007
  • Purpose: Recent studies have shown increased levels of cyclooxygenase-2 (COX-2) in various human malignancies to include various bone and soft tissue tumors. However, little is known with regard to COX-2 expression patterns in chondroid tumors. Materials and Methods: Immunohistochemistry assays were performed for COX-2 in enchondromas (n=10), chondroblastomas (n=11), chondromyxoid fibromas (n=5), conventional chondrosarcomas (n=17), clear cell chondrosarcomas (n=7), and mesenchymal chondrosarcomas (n=6). Results: Among the benign chondroid tumors, chondroblastomas revealed characteristic strong positivity in 6 of 11 cases(54.5%). All enchondromas and chondromyxoid fibromas were negative except in one case. In conventional chondrosarcomas, three cases(17.6%) were strongly reactive with COX-2 and all positive cases represented grade III chondrosarcomas. Clear cell chondrosarcomas were found to be focally positive in two cases(28.5%), while all mesenchymal chondrosarcomas were negative. Conclusions: These findings suggest that COX-2 overexpression in conventional chondrosarcoma may represent an advanced histologic grade. Interestingly, expression of COX-2 in chondroblastomas could be an important factor for inducing peritumoral inflammatory changes in these specific tumors.

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Orexin-A inhibits capsaicin-induced changes in cyclooxygenase-2 and brain-derived neurotrophic factor expression in trigeminal nucleus caudalis of rats

  • Kooshki, Razieh;Abbasnejad, Mehdi;Mahani, Saeed Esmaeili;Raoof, Maryam;Aghtaei, Mohammad Mehdi Moeini;Dabiri, Shahriar
    • The Korean Journal of Pain
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    • v.31 no.3
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    • pp.174-182
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    • 2018
  • Background: The trigeminal nucleus caudalis (Vc) is a primary central site for trigeminal transmitting. Noxious stimulation of the trigeminal nociceptors alters the central synaptic releases and neural expression of some inflammatory and trophic agents. Orexin-A and the orexin 1 receptor (OX1R) are expressed in pain pathways including trigeminal pain transmission. However, the the mechanism(s) underling orexin-A effects on trigeminal pain modulation have not been fully clarified. Methods: Trigeminal pain was induced by subcutaneous injection of capsaicin in the upper lip in rats. The effect of trigeminal pain on cyclooxygenase-2 (COX-2) and brain-derived neurotrophic factor (BDNF) expression in the Vc of animals was determined by immunofluorescence. Subsequently, OX1R agonist (orexin-A) and antagonist (SB-334867-A) was administrated in the Vc to investigate the possible roles of the Vc OX1R on changes in COX-2 and BDNF levels following pain induction. Results: The data indicated an increase in COX-2 and decrease in BDNF immuno-reactivity in the Vc of capsaicin, and capsaicin- pretreated with SB-334867-A (80 nM), groups of rat. However, the effect of capsaicin on COX-2 and BDNF expressions was reversed by a Vc microinjection of orexin-A (100 pM). Conclusions: Overall, the present data reveals that orexin-A can attenuate capsaicin-induced trigeminal pain through the modulation of pain effects on COX-2 and BDNF expressions in the Vc of rats.

Effects of Electroacupuncture on the Expression of Cyclooxygenase in the Spinal Cord of Carrageenan-injected Rat (전침이 carrageenan유발 동통모델의 척수배각내 cyclooxygenase 발현에 미치는 영향)

  • Choi, Yung-Hyun;Lee, Yong-Tae;Choi, Byung-Tae
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.19 no.3
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    • pp.749-752
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    • 2005
  • We investigated the effects of electroacupuncture (EA) on the expression of cyclooxygenase in the spinal cord of acute inflammatory pain model. Inflammation was induced by an intraplantar injection of 1% carrageenan into the right hind paw of Sprague-Dawley. Bilateral 2 Hz EA stimulation with 0.5 mA, 1 mA and 3 mA were delivered at those acupoints corresponding to Zusanli and Sanyinjiao in man via the needles in carrageenan-injected rats. Three hours after carrageenan injection, effects of EA on cyclooxygenase (COX) expression were observed in the dorsal horn of the spinal cord using immunohistochemical method. The immunoreaction of COX-1 tended to increase in the superficial laminae and the neck of the dorsal horn as compared with normal. The COX-2 immunoreaction in the carrageenan-injected rat was also significantly increased in the all regions of the dorsal horn as compared with normal one. However, COX-1 immunoreaction in carrageenan-injected rat were decreased in the superficial laminae and neck of the dorsal horn by low intensity of EA stimulation. Except high intensity of EA stimulation in the superficial laminae, COX-2 expression was attenuated in all regions of the dorsal horn by all types of EA treatment. It is concluded that EA treatment may attenuate inflammatory pain in carrageenan-injected rat through modulating expression of COX-2 in the dorsal horn of the spinal cord.

Piceatannol-Induced G1 Arrest of the Cell Cycle is Associated with Inhibition of Prostaglandin E2 Production in Human Gastric Cancer AGS Cells (Piceatannol에 의한 AGS 인체 위암세포의 G1 Arrest 및 Prostaglandin E2 생성의 억제)

  • Choi, Yung-Hyun
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.41 no.7
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    • pp.907-913
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    • 2012
  • Piceatannol (trans-3,4,3',5'-tetrahydroxystilbene) is a polyphenol detected in grapes, rhubarb, and sugarcane. Although recent experimental data revealed that this compound is known to exhibit immunosuppressive and antitumorigenic activities in several cell lines, the molecular mechanisms underlying anticancer activity are poorly understood. In the present study, we investigated possible further mechanisms by which piceatannol exerts its anti-proliferative action in cultured human gastric cancer AGS cells. Piceatannol treatment resulted in the inhibition of growth and G1 arrest of the cell cycle in a concentration-dependent manner, as determined by MTT assay and flow cytometry analysis. The induction of G1 arrest by piceatannol was associated with the modulation of cyclin-dependent kinases (Cdks) and cyclins, up-regulation of the expression of Cdk inhibitor p21 (WAF1/CIP1) in both transcriptional and translational levels, and the inhibition of phosphorylation of retinoblastoma proteins and E2F1 expression. In addition, piceatannol treatment caused a progressive decrease in the expression levels of cyclooxygenase (COX)-2 without significant changes in the levels of COX-1, which was correlated with a decrease in prostaglandin $E_2$ synthesis.

Isolation of COX-2 Inhibitors from Alpinia officinarum (양강으로부터 COX-2 억제활성물질의 분리)

  • Kim, Ju-Sun;Son, Kun-Ho;Kim, Hyun-Pyo;Chang, Hyeun-Wook;Kang, Sam-Sik
    • Korean Journal of Pharmacognosy
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    • v.31 no.1
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    • pp.57-62
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    • 2000
  • By bioassay-guided fractionation followed by chromatographic separation of the MeOH extract of Alpinia Rhizome, five COX-2 inhibitors were isolated and characterized as pinocembrin, galangin 3-methyl ether, galangin, kaempferid, and 5-hydroxy-7-(4'-hydroxy-3'-methoxyphenyl)-1-phenyl-3-heptanone.

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Synthesis and Antiinflammatory Activity of 1.5- and 4.5-Disubstituted Imidazoles

  • Tuyen, Truong-Ngoc;Sin, Kwan-Seog;Kim, Hyun-Pyo;Park, Hae-Il
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.347.4-348
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    • 2002
  • Recently it has been demonstrated that selective cyclooxygenase-2 (COX-2) inhibitors retain the antiinflammatory effect but with markedly reduced GI toxicity compared to non selective inhibitors such as traditional NSAIDs. As a consequence, intense efforts have been made to develop selective COX-2 inhibtors during the last decade. Two compounds in this class. celecoxib and rofecoxib. are already in the market and are proved as potent and selective COX-2 inhibitors with much better gastric tolerance. However. there are still strong domands for a COX-2 inhibitor with improved efficacy and safety profiles. Here we report the synthesis and biological profiles of 1.5- and 4.5-disubstituted imidazole analogues as structural equivalents of cefecoxib and refecoxib. The imidazole analogues are overlapped well whth the 3D srructures of celecoxib and rofecoxib.

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