• Title/Summary/Keyword: cyclooxygenase

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Cyclooxygenase Inhibitory Activity of Ginsenosides from Panax ginseng

  • Yoo, Hye-Hyun;Kang, Ki-Sung;Lee, Yang-Beom;Kim, Bak-Kwang;Park, Man-Ki;Park, Jeong-Hill
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.216.1-216.1
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    • 2003
  • P. ginseng C.A. Meyer is one of the most widely used herbal medicine in Asia. It has been used for the treatment of many disorders. Its major constituent is known to be ginsenosides, and there are many documents about bioactivities of ginsenosides such as anti-oxidant, anti-tumorigenic, anti-fatigue, and anti-inflammatory activities. Some of these activities are supposed to have some correlation with inhibitory action of cyclooxygenase (COX). Ginsenosides from P. ginseng and sapogenins were evaluated for their inhibitory effects against both cyclooxygenase-1 and -2 (COX-1 and -2). Inhibitory activity was evaluated by measuring prostaglandin E$_2$ (PGE$_2$) production from arachidonic acid with an ELISA reader. (omitted)

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Effects of Cyclooxygenase Inhibitors on Vascular Reactivity and Alterations of Cyclooxygenase Expression (혈관 반응성에 대한 Cyclooxygenase 억제제 효과와 Cyclooxygenase 발현 변화)

  • Lee, Ki-Young;Park, Jin-Woo;Eum, Eun-A;Kang, Young-Jin;Lee, Kwang-Youn;Choi, Hyoung-Chul
    • Journal of Yeungnam Medical Science
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    • v.23 no.1
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    • pp.36-44
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    • 2006
  • Background: There is controversy regarding whether COX-2 specific inhibitors are associated with elevation of blood pressure. We compared the effects of aspirin, indomethacin, and celecoxib for vascular reactivity induced by phenylephrine. We also tested the effects of indomethacin and NO donor on COX-1 and COX-2 protein expression, as well as nitrite production in culture medium of vascular smooth muscle cells. Materials and Methods: In this experiment, we used the isometric tension study for vascular reactivity. After 45 minutes of pretreatment with aspirin, indomethacin, celecoxib, and phenylephrine induced contractions were tested. COX-1 and COX-2 protein expressions were analyzed by Western blot and nitrite production by the Griess reaction. Results: Although celecoxib pretreatment caused enhanced arterial contraction, aspirin pretreatment induced more potent arterial contraction than celecoxib in the isometric tension study of rabbit femoral artery. COX-1 protein expression was unchanged by indomethacin, SNP and NOR-3; COX-2 protein expression was increased by the addition of indomethacin, SNP, and NOR-3. Especially, NOR-3, a NO donor, significantly increased COX-2 protein expression with unstimulated conditions as well as LPS stimulation. Induction of nitrite production was higher with NOR-3 treatment than SNP treatment with LPS stimulation. Conclusion: These results suggest that aspirin caused more potent vascular contraction than celecoxib and indomethacin. COX-2 expression in VSMC depended on the types of NO donor and LPS stimulation.

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Evaluation of cyclooxygenase (COX) inhibition in rosemary extract (로즈마리 추출물의 cyclooxygenase (COX) 효소 및 유전자 발현에 미치는 영향)

  • Sehee Lee;Soo-yeon Park;Kyeong Jin Kim;Sonwoo Kim;Yanghoon P. Jung;Ji Yeon Kim
    • 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.

Synthesis and cyclooxygenase-2 inhibitory activity of tetrahydroaminoacridine and their analogues

  • Shin, H.S.;Kang, J.Y.;Park, M.S.;Kwon, S.K.
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.248.3-249
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    • 2003
  • A series of tetrahydroaminoacridine and their analogues were synthesized. Tetrahydroaminoacridine(tacrine) is an anticholinesterase agent used in the treatment of Alzheimer's disease. Introduction of piperidine group at the para position enhanced anti-inflamatory activity for Alzheimer's disease. We investigated their ability to inhibit cyclooxygenase-1 and 2 isoforms. (omitted)

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Anti-inflammatory Flavonoids: Modulators of Proinflammatory Gene Expression

  • Kim, Hyun-Pyo;Son, Kun-Ho;Chang, Hyeun-Wook;Kang, Sam-Sik
    • Natural Product Sciences
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    • v.10 no.1
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    • pp.1-10
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    • 2004
  • Plant flavonoids possess anti-inflammatory activity in vitro and in vivo. Although the action mechanisms are not fully understood, recent studies have clearly shown that certain flavonoids, especially flavone derivatives, express their anti-inflammatory activity at least in part by modulation of proinflammatory gene expression such as cyclooxygenase-2, inducible nitric oxide synthase and various cytokines. This review summarizes the recent findings of flavonoids modulating expression of proinflammatory molecules.

CELECOXB (CELEBREX) INHIBITS PHORBOL ESTER-INDUCED COX-2 EXPRESSION AND $PGE_2$ PRODUCTION IN MOUSE SKIN: AP-1 AND C/EBP AS POSSIBLE MOLECULAR TARGETS

  • Chun, Kyung-Soo;Surh, Young-Joon
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2002.05a
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    • pp.103-104
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    • 2002
  • Cyclooxygenase (COX), an important enzyme involved in mediating the inflammation, catalyzes the rate-limiting step in the formation of prostaglandins from arachidonic acid. There are two isoforms of COX, designated as COX-1 and COX-2. While COX-1 is constitutively expressed in most tissues, COX-2 can be induced transiently by proinflammatory cytokines, endotoxins, growth factors, oncogenes, UV and mitogens.(omitted)

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CELECOXIB INHIBITS PHORBOL ESTER-INDUCED EXPRESSION OF CYCLOOXYGENASE-2 AND ACTIVATION OF ERKl/2 IN MOUSE SKIN IN VIVO

  • Chun, Kyung-Soo;Surh, Young-Joon
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2001.10a
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    • pp.137-138
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    • 2001
  • There has been accumulating evidence for the association of inflammatory tissue damage with the process of cancer development. Cyclooxygenase (COX), an important enzyme involved in mediating the inflammation, catalyzes the formation of prostaglandins (PGs) from arachidonic acid. There are two isoforms of COX, designated as COX-l and COX-2. COX-l is a housekeeping enzyme which is constitutively expressed and is thought to be involved in maintaining physiological functions.(omitted)

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EFFECTS OF NATURALLY OCCURRING DIARYHEPTANOIDS ON CYCLOOXYGENASE-2 EXPRESSION AND NF- $\textsc{k}$B ACTIVATION IN HUMAN BREAST EPITHELIAL CELLS

  • Kim, Jung-Hwan;Surh, Young-Joan
    • 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)

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Recent Advances in Anti-inflammatory Flavonoid Research since 2004

  • Kim Hyun-Pyo
    • 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.