• 제목/요약/키워드: cyclooxygenase-2 inhibitory activity

검색결과 204건 처리시간 0.037초

발효옻 추출물의 헬리코박터파이로리 생장억제 및 항염증 활성 (Anti-inflammatory activities of fermented Rhus verniciflua stem bark extract and its growth inhibitory effect on Helicobacter pylori)

  • 최은영;석기태;최한석;김명곤;권용수;김명조
    • 한국식품과학회지
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    • 제48권5호
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    • pp.502-507
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    • 2016
  • 본 연구는 장수버섯(Fomitella fraxinea)을 이용하여 발효처리 한무독화 옻나무 추출물의 위장기능 개선능을 확인하고자 발효옻추출물을 이용하여 H. pylori 생장억제활성, 위암세포 생장억제활성과 항염증 활성을 평가하였다. H. pylori를 접종한 배지에 발효옻 추출물을 농도별로 첨가하였을 때 2.0 mg의 농도에서 4.0 mm의 생장억제환을 확인하였으며, 발효옻 추출물을 배지에 1.0-5.0 mg 농도로 혼합한 후 H. pylori을 접종한 경우에도 생장억제능이 확인되었다. 이를 바탕으로 세포 수준에서 H. pylori에 의해 유발된다고 알려진 위암과 위염 개선능을 평가하고자 세포독성을 나타내지 않은 0.1-1.0 mg/mL의 농도범위로 AGS 위암세포 생장억제활성 및 NO 생성 저해율을 확인하였다. 실험결과 0.25 mg/mL 이상의 농도에서 20% 이상의 위암세포 생장억제활성을 확인하였으며, LPS로 염증을 유도한 RAW 264.7 세포에서 추출물 0.25 mg/mL처리시 90%의 높은 NO 생성 저해율을 확인하였다. 염증유발인자인 iNOS와 COX-2의 발현 억제율은 0.50 mg/mL 농도에서 각각 50, 10%의 억제율을 보여 NO 생성저해율은 iNOS에 의한 영향인 것으로 사료된다. 상기 결과로 발효옻 추출물은 H. pylori 생장억제능 및 높은 NO 생성저해 활성이 확인됨으로서 간접적인 위암발생 억제제 및 항염증제로서의 이용가능성을 확인하였다. 따라서 발효옻 추출물을 이용한 위장개선 식의약 소재로서의 개발 가능성이 매우 높은 것으로 생각되며 이를 위해 추가적인 연구가 진행되어야 할 것으로 사료된다.

구창(口瘡)의 외용약(外用藥)으로 다용(多用)되는 황백(黃柏), 청대(靑黛), 백반(白礬) 및 오배자(五倍子)의 항염작용(抗炎作用)에 관한 연구(硏究) (The study on the anti-inflammatory effects of Phellodendri Cortex, Indigo Naturalis, Alumen, and Chinensis Galla, most frequently used for the external theraphy of Gu-Chang)

  • 최관호;김용국;강성구;정순영;정재호;서형식;유진곤
    • 한방안이비인후피부과학회지
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    • 제18권1호
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    • pp.183-198
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    • 2005
  • This experimental study was performed to investigate the anti-inflammatory effects of Phellodendri Cortex(PC), Indigo Naturalis(IN). Alumen(AM), and Chinensis Galla(CG). These four prescriptions most frequently have been used in of oriental medicine for the external the theraphy of Gu-Chang. This study was done to evaluate the activity of superoxide dismutase(SOD) and the inhibitory effects of the formation of cyclooxygenase-2(COX-2), tumor necrosis $factor-{\alpha}(TNF-{\alpha}),\;interlenkin-1{\beta}(IL-1{\beta})$, prostaglandin-E2(PGE2) on the monocyte and neutrophil. The results were summerized as follows. 1. IN has no cytotoxicity but PC, AM, CG have a little cytotoxicity by the increase of concentrations. 2. PC, IN, AM and CG all inhibited the formation of COX-2 in the human neutrophil. 3. $1000{\mu}g/m{\ell}$ of PC increased the formation of SOD in the human monocyte. 4. $1000{\mu}g/m{\ell}$ of PC, $100{\mu}g/m{\ell}$ and $1000{\mu}g/m{\ell}$ of IN, $100{\mu}g/m{\ell}$ of CG inhibited the formation of $TNF-{\alpha}$ in the human monocyte. 5. $10{\mu}g/m{\ell}$ of PC, $1000{\mu}g/m{\ell}$ of IN inhibited the formation of $IL-1\;{\beta}$ in the human monocyte. 6. PC, IN, AM and CG all did not inhibit the production of PGE2 in the human monocyte In addition, the results show that PC, IN, AM and CG all have anti-inflammatory effects and can be used fer the external theraphy of Cu-Chang.

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RAW 264.7 세포에서 담배잎산말의 TLR4/MAPKs/NF-κB 신호전달체계 조절을 통한 항염증 효과 (Desmarestia tabacoides Ameliorates Lipopolysaccharide-induced Inflammatory Responses via Attenuated TLR4/MAPKs/NF-κB Signaling Cascade in RAW264.7 Cells)

  • 윤현서;안현;박충무
    • 생명과학회지
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    • 제33권6호
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    • pp.463-470
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    • 2023
  • Desmarestia tabacoides Okamura는 전 세계적으로 널리 분포하는 갈조류 중 하나이다. 몇몇 산말류의 항종양, 멜라닌 생성 억제 및 광보호 활성에 대한 연구는 있었으나 D. tabacoides Okamura의 항염증 기전에 대해서는 보고되지 않아 본 연구에서는 LPS (lipopolysaccharide)로 자극된 RAW 264.7 세포에서 D. tabacoides Okamura 에탄올 추출물(DTEE)의 항염증 기전을 inducible nitric oxide synthase (iNOS)와 cyclooxygenase (COX)-2의 발현 및 이들의 상위신호전달물질인 nuclear factor (NF)-κB, mitogen-activated protein kinase (MAPK) 그리고 phosphoinositide-3-kinase (PI3K)/Akt의 인산화 조절 정도를 통해 분석하였다. DTEE의 처리는 세포 독성 없이 LPS로 유도된 NO와 prostaglandin (PG) E2의 생성과 이들의 생성 효소인 iNOS 및 COX-2의 발현을 유의하게 억제하였다. 그리고 LPS에 의해 활성화된 NF-κB 및 상위 신호 전달 물질인 extracellular signal-regulated kinase (ERK), c-Jun NH2-terminal kinase (JNK) 및 p38은 DTEE 처리에 의해 유의적으로 억제되었다. DTEE의 처리는 RAW 264.7 세포에서 LPS에 의해 활성화되는 adaptor molecule인 Toll-like receptor (TLR) 4 및 myeloid differentiation primary response (MyD) 88 또한 유의적으로 억제하였다. 이 결과를 통해 DTEE는 LPS에 의해 유도된 TLR4와 NF-κB 및 MAPK의 활성을 억제함으로써 염증 매개인자의 발현을 조절하였고, 이는 DTEE가 염증을 완화할 수 있는 기능성 식품의 소재로써 유용하게 사용될 수 있음을 시사한다.

Estragole Exhibits Anti-inflammatory Activity with the Regulation of NF-κB and Nrf-2 Signaling Pathways in LPS-induced RAW 264.7 cells

  • Roy, Anupom;Park, Hee-Juhn;Jung, Hyun Ah;Choi, Jae Sue
    • Natural Product Sciences
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    • 제24권1호
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    • pp.13-20
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    • 2018
  • Estragole is a naturally occurring phenylpropanoid obtained from essential oils found in a broad diversity of plants. Although the phenylpropanoids show many biological activities, clear regulation of the inflammatory signaling pathways has not yet been determined. Here, we scrutinized the anti-inflammatory effect of estragole. The anti-inflammatory effect of estragole was determined through the inhibitory mechanisms of inducible nitric oxide synthase (iNOS), cyclooxygenase (COX-2), nuclear factor kappa B ($NF-{\kappa}B$), and mitogen-activated protein kinases (MAPK) pathways and the activation of nuclear factor erythroid 2-related factor 2 (Nrf-2)/heme oxygenase (HO)-1 pathways in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. Estragole significantly inhibited NO production, iNOS and COX-2 expression as well as LPS-induced $NF-{\kappa}B$ and MAPK activation. Furthermore, estragole suppressed LPS-induced intracellular ROS production but up-regulated the stress response gene HO-1 via the activation of transcription factor Nrf-2. These findings demonstrate that estragole inhibits the LPS-induced expression of inflammatory mediators via the down-regulation of iNOS, COX-2, $NF-{\kappa}B$, and MAPK pathways, as well as the up-regulation of the Nrf-2/HO-1 pathway, indicating that this phenylpropanoid has potential therapeutic and preventive applications in various inflammatory diseases.

Acer okamotoanum Inhibit the Hydrogen Peroxide-Induced Oxidative Stress in C6 Glial Cells

  • Choi, Soo Yeon;Kim, Ji Hyun;Quilantang, Norman G.;Lee, Sanghyun;Cho, Eun Ju
    • Natural Product Sciences
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    • 제24권3호
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    • pp.148-154
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    • 2018
  • Chronic oxidative stress due to the accumulation of reactive oxygen species (ROS) in neuronal cells ultimately leads to neurodegenerative diseases. The use of natural therapies for the prevention of ROS-induced cell damage and for the treatment of neurodegenerative disorders has shown promising results. In this study, we evaluated the neuroprotective effects of the ethyl acetate (EtOAc) fraction of A. okamotoanum against the hydrogen peroxide ($H_2O_2$)-induced oxidative stress in C6 glial cells. Results show that cell viability was decreased in cells incubated with $H_2O_2$, whereas the addition of EtOAc fraction treatments in such cells significantly increased viability. The EtOAc fraction showed the highest inhibitory activity against ROS production and it also decreased the expressions of inflammatory proteins including cyclooxygenase-2, inducible nitric oxide synthase and interleukin-$1{\beta}$. Furthermore, the EtOAc fraction inhibited apoptosis by regulating the protein expressions cleaved caspase -9, -3, poly ADP ribose polymerase, Bax and Bcl-2. Therefore, these results show that the EtOAc fraction of A. Okamotoanum exhibits neuroprotective effects against $H_2O_2$ induced oxidative damage by regulating the inflammatory reaction and apoptotic pathway.

Anti-inflammatory Effects of the Methanol Extract of Polytrichum Commune via NF-κB Inactivation in RAW 264.7 Macrophage Cells

  • Cho, Woong;Park, Seung-Jae;Shin, Ji-Sun;Noh, Young-Su;Cho, Eu-Jin;Nam, Jung-Hwan;Lee, Kyung-Tae
    • Biomolecules & Therapeutics
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    • 제16권4호
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    • pp.385-393
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    • 2008
  • As an attempt to search for bioactive natural products exerting anti-inflammatory activity, we evaluated the effects of the methanol extract of Polytrichum commune Hedw (PCM) (Polytrichaceae) on lipopolysaccharide (LPS)-induced nitric oxide (NO), prostaglandin $E_2$ ($PGE_2$) and pro-inflammatory cytokines release in murine macrophage cell line RAW 264.7. PCM potently inhibits the production of NO, $PGE_2$, tumor necrosis factor (TNF)-$\alpha$ and interleukin (IL)-6. Consistent with these results, PCM also concentration-dependently inhibited LPS-induced inducible NO synthase (iNOS) and cyclooxygase (COX)-2 at the protein levels, and iNOS, COX-2, TNF-$\alpha$ and IL-6 at the mRNA levels without an appreciable cytotoxic effect on RAW 264.7 macrophag cells. Furthermore, PCM inhibited LPS-induced nuclear factor-kappa B (NF-$\kappa$B) activation as determined by NF-$\kappa$B reporter gene assay, and this inhibition was associated with a decrease in the nuclear translocation of p65 and p50 NF-$\kappa$B. Taken together, these results suggest that PCM may play an anti-inflammatory role in LPS-stimulated RAW 264.7 macrophages through the inhibitory regulation of iNOS, COX-2, TNF-$\alpha$ and IL-6 via NF-$\kappa$B inactivation.

Peroxisome proliferator-activated receptor ${\gamma}$ agonist suppresses human telomerase reverse transcriptase expression and aromatase activity in eutopic endometrial stromal cells from endometriosis

  • Chang, Hye Jin;Lee, Jae Hoon;Hwang, Kyung Joo;Kim, Mi Ran;Yoo, Jung Hyun
    • Clinical and Experimental Reproductive Medicine
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    • 제40권2호
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    • pp.67-75
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    • 2013
  • Objective: To investigate the effect of peroxisome proliferator activated receptor ${\gamma}$(PPAR${\gamma}$) agonist on the cell proliferation properties and expression of human telomerase reverse transcriptase (hTERT) and aromatase in cultured endometrial stromal cell (ESC) from patients with endometriosis. Methods: Human endometrial tissues were obtained from women with endometriosis and healthy women (controls) using endometrial biopsy. Isolated ESCs were cultured and the cell proliferation was measured by 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide assay and expression of hTERT, aromatase, and cyclooxygenase (COX)-2 by western blotting according to the addition of rosiglitazone (PPAR${\gamma}$ agonist). Results: We demonstrate that the cultured ESCs of endometriosis showed hTERT protein overexpression and increased cellular proliferation, which was inhibited by rosiglitazone, in a dose-dependent manner. At the same time, PPAR${\gamma}$ agonist also inhibited aromatase and COX-2 expression, resulting in decreased prostaglandin $E_2$ production in the ESCs of endometriosis. Conclusion: This study suggests that PPAR${\gamma}$ agonist plays an inhibitory role in the proliferative properties of eutopic endometrium with endometriosis by down-regulation of hTERT and COX-2 expression; this could be a new treatment target for endometriosis.

Curcumin Inhibits the Activation of Immunoglobulin E-Mediated Mast Cells and Passive Systemic Anaphylaxis in Mice by Reducing Serum Eicosanoid and Histamine Levels

  • Li, Xian;Lu, Yue;Jin, Ye;Son, Jong-Keun;Lee, Seung Ho;Chang, Hyeun Wook
    • Biomolecules & Therapeutics
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    • 제22권1호
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    • pp.27-34
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    • 2014
  • Curcumin is naturally occurring polyphenolic compound found in turmeric and has many pharmacological activities. The present study was undertaken to evaluate anti-allergic inflammatory activity of curcumin, and to investigate its inhibitory mechanisms in immunoglobulin E (IgE)/Ag-induced mouse bone marrow-derived mast cells (BMMCs) and in a mouse model of IgE/Ag-mediated passive systemic anaphylaxis (PSA). Curcumin inhibited cyclooxygenase-2 (COX-2) dependent prostaglandin $D_2$ ($PGD_2$) and 5-lipoxygenase (5-LO) dependent leukotriene $C_4$ ($LTC_4$) generation dose-dependently in BMMCs. To probe the mechanism involved, we assessed the effects of curcumin on the phosphorylation of Syk and its downstream signal molecules. Curcumin inhibited intracellular $Ca^{2+}$ influx via phospholipase $C{\gamma}1$ ($PLC{\gamma}1$) activation and the phosphorylation of mitogen-activated protein kinases (MAPKs) and the nuclear factor-${\kappa}B$ (NF-${\kappa}B$) pathway. Furthermore, the oral administration of curcumin significantly attenuated IgE/Ag-induced PSA, as determined by serum $LTC_4$, $PGD_2$, and histamine levels. Taken together, this study shows that curcumin offers a basis for drug development for the treatment of allergic inflammatory diseases.

Imperatorin Suppresses Degranulation and Eicosanoid Generation in Activated Bone Marrow-Derived Mast Cells

  • Jeong, Kyu-Tae;Lee, Eujin;Park, Na-Young;Kim, Sun-Gun;Park, Hyo-Hyun;Lee, Jiean;Lee, Youn Ju;Lee, Eunkyung
    • Biomolecules & Therapeutics
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    • 제23권5호
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    • pp.421-427
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    • 2015
  • Imperatorin has been known to exert many biological functions including anti-inflammatory activity. In this study, we investigated the inhibitory effects of imperatorin on the production of inflammatory mediators in mouse bone marrow-derived mast cells (BMMC). Imperatorin inhibited degranulation and the generation of eicosanoids (leukotriene $C_4$ ($LTC_4$) and prostaglandin $D_2$ ($PGD_2$) in IgE/antigen (Ag)-stimulated BMMC. To elucidate the molecular mechanism involved in this process, we investigated the effect of imperatorin on intracellular signaling in BMMC. Biochemical analyses of the IgE/Ag-mediated signaling pathway demonstrated that imperatorin dramatically attenuated degranulation and the production of 5-lipoxygenase-dependent $LTC_4$ and cyclooxygenase-2-dependent $PGD_2$ through the inhibition of intracellular calcium influx/phospholipase $C{\gamma}1$, cytosolic phospholipase $A_2$/mitogen-activated protein kinases and/or nuclear factor-${\kappa}B$ pathways in BMMC. These results suggest that the effects of imperatorin on inhibition of degranulation and eicosanoid generation through the suppression of multiple steps of IgE/Ag-mediated signaling pathways would be beneficial for the prevention of allergic inflammation.

5β-Hydroxypalisadin B isolated from red alga Laurencia snackeyi attenuates inflammatory response in lipopolysaccharide-stimulated RAW 264.7 macrophages

  • Wijesinghe, W.A.J.P.;Kang, Min-Cheol;Lee, Won-Woo;Lee, Hyi-Seung;Kamada, Takashi;Vairappan, Charles S.;Jeon, You-Jin
    • ALGAE
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    • 제29권4호
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    • pp.333-341
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    • 2014
  • In this study, four compounds isolated from the red alga Laurencia snackeyi were evaluated for their potential anti-inflammatory effect in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. These compounds were tested for their inhibitory effects on nitric oxide (NO) production in LPS-stimulated RAW 264.7 cells. Since $5{\beta}$-hydroxypalisadin B showed the best activity it was further tested for the production of prostaglandin-$E_2$ ($PGE_2$), expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), the release of pro-inflammatory cytokines tumor necrotic factor-alpha (TNF-${\alpha}$), interleukin-$1{\beta}$ (IL-$1{\beta}$), and interleukin-6 (IL-6). $5{\beta}$-Hydroxypalisadin B significantly reduced the $PGE_2$ release and suppressed the iNOS and COX-2 expression in LPS-stimulated RAW 264.7 cells. It also significantly reduced the release of pro-inflammatory cytokines TNF-${\alpha}$, IL-$1{\beta}$, and IL-6. These findings provide the first evidence of anti-inflammatory potential of $5{\beta}$-hydroxypalisadin B isolated from the red alga L. snackeyi and hence, it could be exploited as an active ingredient in pharmaceutical, nutraceutical and functional food applications.