• Title/Summary/Keyword: COX-2 inhibitory activity

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Experimental study of Gagam-Cheongsang BangPungTang on the anti-inflammatory effects (가감청상방풍탕(加減淸上防風湯)의 항염증 효과에 대한 실험적 연구)

  • Seo, Eun-Sung;Hwang, Chung-Yeon;Kim, Nam-Kwen
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.21 no.2
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    • pp.54-70
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    • 2008
  • Background and Object : This study was carried out to investigate the effects of GCSBPT (Gagam-Cheongsang BangPungTang) on the in vitro and in vivo anti-inflammatory reactions. Methods : Vascular permeability and Cyclooxygenase inhibition assay are examined in vitro and nitric oxide inhibition assay, radical scavenging activity test, $TNF-{\alpha}$, COX-2 inhibition test are examined in vivo. Results : GCSBPT showed inhibitory effects on vascular permeability and leukocyte migration in animal test. In cyclooxygenase 2 inhibition assay, an ethanol extract of GCSBPT inhibited prostaglandin E2 generation at a concentration of $10{\mu}g/ml$. Among the herbal ingredients of GCSBPT, ethanol extracts of Nepetae Spica exhibited potent inhibitory activities. Ethanol extract of GCSBPT inhibited the release of nitric oxide and the gene expression of inducible nitric oxide synthase in RAW 246.7 cells stimulated by lipopolysaccharide. Ethanol extract of GCSBPT exhibited radical scavenging activity of 54% at $100{\mu}g/ml$. Among the herbal ingredients of GCSBPT. Conclusions : According to the above results, I expected that GCSBPT was a potent anti-inflammatory prescription.

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Chemical Constituents of the Root of Dystaenia takeshimana and Their Anti-Inflammatory Activity

  • Kim, Ju-Sun;Kim, Jin-Cheul;Shim, Sang-Hee;Lee, Eun-Ju;Jin, Wen-Yi;Bae, Ki-Hwan;Son, Kun-Ho;Kim, Hyun-Pyo;Kang, Sam-Sik;Chang, Hyeun-Wook
    • Archives of Pharmacal Research
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    • v.29 no.8
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    • pp.617-623
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    • 2006
  • In our ongoing search for bioactive compounds originating from the endemic species in Korea, we found that the hexane and EtOAc fractions of the MeOH extract from the root of Dystaenia takeshimana (Nakai) Kitagawa (Umbelliferae) showed cyclooxygenase-2 (COX-2) and 5- lipoxygenase (5-LOX) dual inhibitory activity by assessing their effects on the production of prostaglandin $D_2\;(PGD_2)$ and leukotriene $C_4\;(LTC_4)$ in mouse bone marrow-derived mast cells. By activity-guided fractionation, five coumarins, viz. psoralen (2), xanthotoxin (3), scopoletin (4), umbelliferone (5), and (+)-marmesin (6), together with ${\beta}-sitosterol$ (1), were isolated from the hexane fraction, and two phenethyl alcohol derivatives, viz. 2-methoxy-2-(4'-hydroxyphenyl)ethanol (7) and 2-hydroxy-2-(4'-hydroxyphenyl)ethanol (8), three flavonoids, viz. apigenin (9), luteolin (10), and cynaroside (11), as well as daucosterol (12) were isolated from the EtOAc fraction using silica gel column chromatography. In addition, D-mannitol (13) was isolated from the BuOH fraction by recrystallization. Two of the coumarins, scopoletin (4) and (+)- marmesin (6), the two phenethyl alcohol derivatives (7, 8) and the three flavonoids (9-11) were isolated for the first time from this plant. Among the compounds isolated from this plant, the five coumarins as well as the three flavonoids showed COX-2/5-LOX dual inhibitory activity. These results suggest that the anti-inflammatory activity of D. takeshimana might in part occur via the inhibition of the generation of eicosanoids.

Inhibition of Phorbol 12-myristate-13-acetate Induced Cyclooxygenase-2 Activity by Three-step Fermented Soybeans (PMA에 의해 유도된 cycooxygenase-2 활성에 대한 새로운 발효법에 의한 대두산물의 억제 효능)

  • Park, Cheol;Lee, Jeong-Ok;Ryu, Chung-Ho;Choi, Yung-Hyun
    • Journal of Life Science
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    • v.18 no.2
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    • pp.180-186
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    • 2008
  • In this study, we examined the effects of the fermented soybeans by Bacillus subtilis (FSB) and the novel three-step fermented soybeans (TFS) on the expression and activity of COX-2 in human leukemic U937 cell model. Treatment of phorbol 12-myristate 13-acetate (PMA) significantly induced pro-inflammatory mediators such as COX-2 expression and prostaglandin $E_2\;(PGE_2)$ production, whereas the levels of COX-1 remained unchanged. However, pre-treatment with FSB and TFS significantly attenuated the PMA-induced COX-2 protein as well as mRNA, which was associated with inhibition of $PGE_2$ production. Moreover, TFS exerts a much better inhibitory activity than FSB against PMA-induced activation of COX-2 and production of $PGE_2$ in U937 cells. Taken together, these findings provide important new insights into the possible molecular mechanisms of the anti-inflammatory activity of FSB and TFS.

Inhibitory Effect of Eurya emarginata on the Production of Pro-inflammatory Cytokines in Murine Macrophage RAW264.7 (Murine Macrophage RAW 264.7 세포에서 우묵사스레피에 의한 염증성 사이토카인 억제효과)

  • 박수영;이혜자;현은아;문지영;앙홍철;이남호;김세재;강희경;유은숙
    • YAKHAK HOEJI
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    • v.47 no.5
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    • pp.311-318
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    • 2003
  • Eurya emarginata (Thunb.) Makino (Theaceae) is distributed in coastal areas of island. The leaves of Eurya are used in the traditional medicine of the coastal areas of jeju island with the aim of diuresis or to treat ulcers. Nevertheless, there are few reports on the biological activity and constituents of E. emarginata. In this study, we investigated the pharmacological activity of the solvent extracts of E. emarginata on the several inflammatory markers (TNF-$\alpha$, IL-1$\beta$, IL-6, NO, iNOS and COX-2). Also we examined the antioxidizing effect of the solvent extracts by determination of DPPH radical-scavenging activity. Among the solvent fractions, EtOAc and BuOH extracts showed potent radical scavenging activity (RC$_{50}$=10.9 and 12.7 respectively). The subtractions of EF 5-4-6-3-2 and BF 1 potentially inhibited the mRNA expression of pro-inflammatory cytokines (IL-1$\beta$, IL-6 and TNF-$\alpha$) at the concentration of 100 $\mu\textrm{g}$/mι. Also the fractions inhibited the mRNA expression of pro-inflammatory cytokines (IL-1$\beta$, IL-6 and TNF-$\alpha$) and protein expression of iNOS and COX-2 at the concentration of 100 $\mu\textrm{g}$/mι. And then, the inhibition of iNOS was correlated with the decrease of nitrite level. These results suggest that E. emarginata may have anti-inflammatory activity through the inhibition of pro-inflammatory cytokines, iNOS and COX-2.2.

Antioxidant and Anti-inflammatory Activities of the Halophyte Cyrtomium falcatum (염생식물 도깨비고비의 항산화 및 항염증 효과)

  • Kim, Hyunmo;Kim, Hojun;Kong, Chang-Suk;Lee, Bong Ho;Sim, Hyun-Bo;Seo, Youngwan
    • Ocean and Polar Research
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    • v.43 no.3
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    • pp.113-126
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    • 2021
  • In the present study, the halophyte C. falcatum extract and its solvent fractions (n-hexane, 85% aqueous methanol, n-butanol, and water) were evaluated for antioxidant and anti-inflammatory activities. Antioxidative ability was measured by DPPH radical, intracellular reactive oxygen species (ROS) and peroxynitrite scavenging, DNA oxidation inhibition, and ferric reducing antioxidant power (FRAP). For DPPH radical and peroxynitrite scavenging, DNA oxidation inhibition, and FRAP, 85% aq.MeOH and n-BuOH fractions showed significant scavenging activity. For production of intracellular ROS in HT-1080 cells, 85% aq.MeOH fraction showed the highest scavenging activity. In addition, anti-inflammatory activity was also assessed by measuring the inhibitory effect against mRNA expression of pro-inflammatory factors (NO, IL-1β, IL-6 and COX-2) in LPS-stimulated Raw 264.7 macrophages. For NO production, crude extract exhibited a strong inhibitory effect at a concentration of 100 ㎍/ml. For mRNA expression of pro-inflammatory cytokines (IL-1β, IL-6, and COX-2), n-BuOH greatly suppressed expression levels of IL-1β and IL-6 at 100 ㎍/ml concentration while 85% aq. MeOH fraction significantly inhibited that of COX-2 even at 100 ㎍/ml. These results suggest that C. falcatum may be used as a potential source for the development of a natural antioxidant or anti-inflammatory agent.

Inhibitory Effect of Taraxci Herba Methanol Extract on Pro-inflammatory Mediator in Lipopolysaccharide;Activated Raw 264.7 cells

  • Jo, Mi-Jeong;Chu, Yan-Hui;Back, Young-Doo;Lee, Byung-Wook;Shin, Soon-Shik;Kwon, Young-Kyu;Kim, Sang-Chan
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.22 no.4
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    • pp.907-913
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    • 2008
  • Taraxci Herba (TH; Pogongyoung in Korean) has been used in traditional oriental medicine for the treatment of various ailments. The biological activity of this plant is not yet evaluated systematically. This study was conducted to evaluate the inhibitory effects of TH on the production of nitric oxide (NO) and the expression of inducible nitric oxide synthase (iNOS) in lipopolysaccharide (LPS)-activated Raw264.7 cells. The aim of the present work is to investigate a potential anti-inflammatory activity of TH. The Raw264.7 cells were cultured in DMEM medium for 24 h. After serum starvation for 12 h, the cells were treated with TH for 1 h, followed by stimulating NO production with LPS ($2{\mu}g/ml$). As result of this study, TH inhibited the levels of NO, PGE2, $TNF-{\alpha}$, IL-6 and $IL-1{\beta}$, and the expressions of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) activated by LPS. These inhibitory effects were mediated though the inhibition of phosphorylation of inhibitory kappa B ($I{\kappa}B$). These findings showed that TH could have some anti-inflammatory effects.

Anti-inflammatory and Anti-Atopic Effects of Crude Extracts and Solvent Fractions of Phormium tenax leaf (신서란(Phormium tenax) 잎 조추출물 및 용매 분획물의 항염증 및 항아토피 효과)

  • Yang, Kwon Min;Song, Sang mok;Lee, Doseung;Yoon, Weon-Jong;Kim, Chan-Shick;Kim, Chang Sook
    • Korean Journal of Plant Resources
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    • v.32 no.5
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    • pp.433-441
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    • 2019
  • This study describes a preliminary evaluation of the anti-inflammatory activity and anti-atopic activity of Phormium tenax leaf extracts. P. tenax leaf was extracted using 70% ethanol and then fractionated sequentially with n-hexane, methylene chloride, ethyl acetate, n-butanol. In order to effectively screen for anti-inflammatory agents, we first investigated the inhibitory effects of P. tenax leaf crude extracts and solvent fractions on production of pro-inflammatory factors[nitric oxide(NO), prostaglandin $E_2(PGE_2)$, inducible nitric oxide synthase(iNOS) and cyclooxygenase-2(COX-2)] and pro-inflammatory cytokines [tumor necrosis $factor-{\alpha}(TNF-{\alpha})$, interleukin-6(IL-6) and $interleukin-1{\beta}(IL-1{\beta})$] in lipopolysaccharide(LPS)-stimulated RAW 264.7 cells. In addition, we also evaluated of their inhibitory effect on the atopic dermatitis-like inflammatory markers such as macrophage-derived chemokine(MDC) and thymus and activation-regulated chemokine(TARC) in HaCaT cells. Among the five solvent fractions of P. tenax, methylene chloride and ethyl acetate fractions inhibited production of pro-inflammatory factors and pro-inflammatory cytokines in a dose dependent manner, respectively. These fractions were also showed inhibitory activity for MDC and TARC expression levels in $IFN-{\gamma}-stimulated$ HaCaT cells, respectively. These results suggest that P. tenax have significantly effects of anti-inflammatory activity and anti-atopic activity that might be beneficial for the topical treatment of inflammatory skin disorders.

NDRG2 Controls COX-2/PGE2-Mediated Breast Cancer Cell Migration and Invasion

  • Kim, Myung-Jin;Kim, Hak-Su;Lee, Soo-Hwan;Yang, Young;Lee, Myeong-Sok;Lim, Jong-Seok
    • Molecules and Cells
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    • v.37 no.10
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    • pp.759-765
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    • 2014
  • N-myc downstream-regulated gene 2 (NDRG2), which is known to have tumor suppressor functions, is frequently down-regulated in breast cancers and potentially involved in preventing the migration and invasion of malignant tumor cells. In the present study, we examined the inhibitory effects of NDRG2 overexpression, specifically focusing on the role of cyclooxygenase-2 (COX-2) in the migration of breast cancer cells. NDRG2 overexpression in MDA-MB-231 cells inhibited the expression of the COX-2 mRNA and protein, the transcriptional activity of COX-2, and prostaglandin $E_2$ ($PGE_2$) production, which were induced by a treatment with phorbol-12-myristate-13-acetate (PMA). Nuclear transcription factor-${\kappa}B$ (NF-${\kappa}B$) signaling attenuated by NDRG2 expression resulted in a decrease in PMA-induced COX-2 expression. Interestingly, the inhibition of COX-2 strongly suppressed PMA-stimulated migration and invasion in MDA-MB-231-NDRG2 cells. Moreover, siRNA-mediated knockdown of NDRG2 in MCF7 cells increased the COX-2 mRNA and protein expression levels and the PMA-induced COX-2 expression levels. Consistent with these results, the migration and invasion of MCF7 cells treated with NDRG2 siRNA were significantly enhanced following treatment with PMA. Taken together, our data show that the inhibition of NF-${\kappa}B$ signaling by NDRG2 expression is able to suppress cell migration and invasion through the down-regulation of COX-2 expression.

Antioxidant Activity and Physiological Function of the Anomala albopilosa Extracts (청동풍탱이(Anomala albopilosa)추출물의 항산화성 및 생리기능)

  • Yoon, Weon-Jong;Lee, Jung-A;Kim, Ji-Young;Kim, Sang-Bum;Park, Soo-Yeong
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.36 no.6
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    • pp.670-677
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    • 2007
  • We analyzed antioxidant and physiological activities to investigate the functional effects of ethanol extracts of Anomala albopilosa imago and A. albopilosa larva. In order to effectively screen for anti-inflammatory agents, we first investigated the antioxidant activities such as DPPH radical scavenging capacity, superoxide radical scavenging capacity, xanthine oxidase inhibitory activity, and nitric oxide scavenging capacity of the A. albopilosa extracts. By the screening system, we found that A. albopilosa extracts had antioxidant activity which increased with increments of the extract concentration. Moreover, we examined the inhibitory effect of the A. albopilosa extracts on the production of anti-inflammatory factors that the nitric oxide (NO), inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) and prostaglandin $E_2\;(PGE_2)$ production activated with LPS ($1{\mu}g/mL$) in murine macrophage cell line RAW 264.7. A. albopilosa extracts potentially inhibited the iNOS and COX-2 in a dose-dependent manner. The inhibition of iNOS activity was correlated with the decrease in nitrite levels. Additionally, the $PEG_2$ production is markedly inhibited after a treatment with the A. albopilosa extracts.

Anti-inflammatory Activity of Veronica peregrina

  • Jeon, Hoon
    • Natural Product Sciences
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    • v.18 no.3
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    • pp.141-146
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    • 2012
  • Veronica peregrina (Scrophylariaceae) has been widely used as a Korean traditional medicine for the treatment of various pathological conditions including infection, hemorrhage and gastric ulcer. In the current study, we investigated the inhibitory effect of methanolic extracts of V. Peregrina (VPM) on the LPS-mediated nitric oxide (NO) production in mouse (C57BL/6) peritoneal macrophages. NO production was significantly down-regulated by the treatment of VPM dose dependently. To evaluate the mechanism of the inhibitory action of VPM on NO production, we performed iNOS enzyme activity assay and checked the change of inducible nitric oxide synthase (iNOS) levels by Western blotting. Although VPM did not affect iNOS enzyme activity, iNOS protein expression was attenuated by VPM indicating VPM inhibits NO production via suppression of iNOS enzyme expression. In addition, VPM attenuated the expression of another pro-inflammatory mediator such as cyclooxygenase-2 (COX-2) in a dose dependent manner. We also found that VPM can reduce trypsin-induced paw edema in mice. Based on this study, we suggest that V. peregrina may be beneficial in diseases which related to macrophage-mediated inflammatory disorders.