• Title/Summary/Keyword: $PGE_{2}$

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CJ-11668, A new selective and potent COX-2 inhibitor, reduces inflamation, fever and pain in animal models

  • Kim, Seong-Woo;Park, Hyun-Jung;Kim, Young-Gi;Yeon, Kyu-Jeong;Ryu, Hyung-Chul;Park, Sang-Wook;Kim, Jong-Hoon;Ko, Dong-Hyun;Chae, Myeong-Yun
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.94.2-94.2
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    • 2003
  • CJ-11668 is a new potent and selective COX-2 inhibitor. CJ-11668 showed COX-2 inhibition (IC50) of 65nM and selectivity ratio (COX-l/COX-2) of 770 in the cell based assay. In the human whole blood assay, CJ-11668 showed COX-2 inhibition (IC50) of 370nM and selectivity ratio (COX-l/COX-2), 135. The treatment of CJ-11668 (5 mg/kg, p.o) produced a significant inhibition (35%) of inflamed rat paw volume in the carrageenan-induced acute inflammation. CJ-11668 also suppressed the PGE2 level (69% inhibition, 1 mg/kg, p.o) in the zymosan-induced mouse air pouch model after 3 hrs. (omitted)

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ET-18-O-$CH_3$ INDUCED APOPTOSIS IN H-RAS TRANSFORMED HUMAN BREAST EPITHELIAL CELLS THROUGH UP-REGULATION OF CYCLOOXYGENASE-2

  • Na, Hye-Kyung;Surh, Young-Joon
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2002.05a
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    • pp.80-80
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    • 2002
  • Cyclooxygenase-2 (COX-2) is an inducible enzyme expressed in response to a variety of cytokines. The presence of oncogenic ras has been associated with sustained induction of COX-2, which confers resistance to apoptosis. Contrary to the above notion, we found that MCF10A-ras cells treated with an anti-tumor agent, ET-18-O-$CH_3$, underwent apoptosis as revealed by proteolytic cleavage of poly(ADP-ribose)polymerase, pro-caspase 3 activity, and TUNEL staining, while the same treatment caused an increased expression of COX-2 as well as the elevated production of prostaglandin E$_2$(PGE$_2$).(omitted)

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Anti-angiogenic and anti-tumor activity of 2′ -hYdroxy-4′ -methoxychalcone

  • Jung, Sang-Hoon;Lee, Yeon-Sil;Lee, Sang-Hyun;Lim, Soon-Sung;Kim, Yeong-Shik;Shin, Kuk-Hyun
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.359.2-359.2
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    • 2002
  • In the previous study, we reported that 2'-hydroxy-4'-methxoychalcone, synthetic chalcone inhibited PGE2 production in TPA- stimulated rat peritoneal macrophages by inhibiting the induction of COX-2 protein. The present study was carried out to clarify whether 2'-hydroxy-4'-methoxychalcone inhibit angiogenesis by the experimental methods in vitro and in vivo. 2'-Hydroxy-4'-methoxychalcone decreased angiogenesis of both chick embryos in the chorioallantoic membrane assay and basic fibroblast growth factor-induced vessel formation inthe mouse Martigel plug assay. (omitted)

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GENISTEIN INHIBITS $NF-_kB-DEPENDENT$ COX-2 INDUCTION IN HUMAN BREAST EPITHELIAL CELLS BY MODULATING THE ACTIVATION OF TATA-BINDING PROTEIN

  • Chung, Myung-Hoon;Kim, Jung-Hwan;Keum, Joo-Seob;Lee, Seung-Sei;Surh, Young-Joon
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.230.2-231
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    • 2002
  • Genistein has been shown to possess chemopreventive potential. but its underlying molecular mechanisms are largely unclear. In the present study, 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 mediating inflammation. 12-Ο-Tetradecanoylphorbol-13-acetate(TPA) caused transient increases in cox-2 expression and prostaglandin E$_2$(PGE$_2$) production in MCF 10A cells, which was inhibited by genistein pretreatment. (omitted)

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INHIBITORY EFFECTS OF THE SOY ISOFLAVONE GENISTEIN ON INDUCTION OF COX-2 AND ACTIVATION OF ERK1/2 IN CULTURED MCF10A CELLS

  • Chung, Myung-Hoon;Kim, Jung-Hwan;Keum, Joo-Seob;Lee, Seung-Sei;Surh, Young-Joon
    • 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)

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ROLES OF PGE$_2$ AND 15-DEOXY-${\delta}^{12.14}$ PROSTAGLANDIN J$_2$ IN ET -18-O-$CH_3$-INDUCED INFLAMMATORY CELL DEATH

  • Na, Hye-Kyung;Surh, Young-Joon
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.313.3-314
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    • 2002
  • Cyclooxygenase-2 (COX-2) is an inducible enzyme expressed in response to a variety of cytokines and other proinflammatory stimuli. It has been known that aberrant up-regulation of COX-2 is associated with resistance to apoptosis. Contrary to the above notion. treatment of MCF10A-ras cells with the anti-tumor agent ET -18-O-$CH_3$ caused increased expression of COX-2 and its mRNA transcript. while inducing apoptosis as revealed by proteolytic cleavage of poly(ADP-ribose)polymerase. caspase-3 activation, and positive TUNEL staining. (omitted)

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EFFECT OF CAPSAICIN ON LPS-INDUCED PROSTAGLANDIN E2 PRODUCTION BY MURINE PERITONEAL MACROPHAGES

  • Kim, Chu-Sook;Kim, Byung-Sam;Han, In-Seob;Chei, Suck-Young;Kwon, Byung-Se;Rina Yu
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2001.10a
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    • pp.132-132
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    • 2001
  • Proinflamamtory mediators such as prostaglandins (PGs), cyclooxygenase-2 (COX-2), and inducible nitric oxide synthase (iNOS) are known to be key mediators in pathogenesis of inflammatory diseases. Capsaicin, the major ingredient of hot pepper, is considered to elicit anti-inflammatory property. In this study, the effect of capsaicin on the prostaglandin E$_2$(PGE$_2$) production was investigated in murine peritoneal macrophages.(omitted)

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In vitro Antiinflammatory Activity of the Essential oil Extracted from Chrysanthemum sibiricum in Murine Macrophage RAW 264.7 Cells

  • Lee, Kyung-Tae;Kim, Pyung-Kyu;Ji, Sa-Young;Shin, Kyoung-Min;Park, Jong-Won;Jung, Hyun-Ju;Park, Hee-Juhn
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.384.2-384.2
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    • 2002
  • This research was undertaken to find the in vitro anti-inflammatory action of the essenetial oil (CS-oil) extracted from Chrysanthemum sibiricum (Compositae) herbs. We investigated the effects of the CS-oil not only on the formation NO and $PGE_2$ and TNF-$\alpha$ but also on inducible nitric oxide synthase and cyclooxygenase-2 (COX-2) in lipopolysaccharide (LPS)-induced murine macrophage 264.7. The data obtained were consistent with the modulation of iNOS enzyme expression. (omitted)

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Protective Effect of Fermented Brassica Puree on HCl/Ethanol-Induced Acute Gastritis via Prevention of Gastric Mucosal Injury (염산/에탄올로 유도된 급성 위염 동물모델에서 십자화과 생즙 발효물의 위점막 보호 효과)

  • Park, Yang-Gyu;Cho, Jeong-Hwi;Choi, Jinyoung;Kim, Youngpil;Lee, Sang-yeob;Park, Ju-Hun;Oh, Hong-Geun
    • The Korean Journal of Food And Nutrition
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    • v.34 no.5
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    • pp.468-476
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    • 2021
  • In recent years, there has been an increase in the morbidity of gastritis in Korea due to lifestyle factors mostly changes in eating habits and stress. Gastritis is more likely to progress to gastric cancer, and therefore it is important to prevent and manage gastritis through lifestyle adjustment and treatment at an early stage. In this study, cabbage, which was found to be effective in gastritis, was mixed and fermented with other crucifer plants such as kale and broccoli to evaluate the overall efficacy of fermented brassica puree on alcoholic acute gastritis. Based on our results, fermented brassica puree alleviated gastric injury induced by 150 mM HCl/60% ethanol. In addition, it was confirmed that PGE2, a gastric mucosal protective factor, was increased, and other positive effects such as an increase of MUC1 and regulation of PKC were observed. The results of this study suggest that fermented brassica puree can relieve acute alcoholic gastritis by regulating PGE and the expression of MUC1, a gene related to mucus secretion, and activating PKC, which is related to mucosal cell activity.

Inhibitory effects of natural products on lipopolysaccharide-stimulated PGE2 and nitric oxide production in RAW 264.7 cells

  • Park, Hye-Jin;Min, Hye-Young;Park, Dong-Ki;Lee, Sang-Kook
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.268.2-269
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    • 2003
  • Prostaglandins (PGs) and NO (nitric oxide) are important elements to keep homeostasis and host defense system in human beings. When PGs and NO are overproduced by cyclooxygenase-2(COX-2) and inducible nitric oxide synthase (iNOS), respectively, they can cause chronic inflammation, tissue damage, and carcinogenesis. On this line, we are interested in finding agents that can inhibit the production of PGs and NO from natural products for devloping anti-inflammatory and cancer chemopreventive agents. (omitted)

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