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

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Study on the anti-inflammatory effects of Cannabis sativa L. seed oil complex (햄프(Cannabis sativa L.)씨드오일 복합물의 항염증 효과에 관한 연구)

  • Chae-Hyun Kim;Se Gie Kim;Young-Ah Jang;Yong-Jin Kwon
    • Journal of the Korean Applied Science and Technology
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    • v.41 no.2
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    • pp.251-259
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    • 2024
  • This study evaluated the potential of hemp seed oil (Cannabis sativa L. seed oil, CSO) and hemp seed oil complex (Cannabis sativa L. seed oil complex, CSOC) as an anti-inflammatory material through comparative analysis. Anti-inflammatory effects of CSO and CSOC were confirmed through lipopolysaccharide (LPS)-induced RAW264.7 model. As a result of confirming the inhibition of lipid oxidation through lipoxygenase inhibitory activity, CSO was not inhibited, but COSC was inhibited by more than 70%. As a result of confirming cytotoxicity through MTT analysis, CSO did not show cytotoxicity, but CSOC showed cytotoxicity at over 200 ㎍/ml. In LPS-induced RAW264.7, the expression of inducible nitric oxide synthase (iNOS) and the production of nitric oxide (NO) were significantly inhibited by CSOC compared to CSO. Additionally, CSOC significantly inhibited the expression of cyclooxygenase (COX)-2 and the production of prostaglandin E2 (PGE2). Through this study, we confirmed that CSOC has superior anti-inflammatory effects than CSO and has the potential to be used as an anti-inflammatory material.

Inhibition of Inflammatory-cytokines Production and Prostaglandin E2 Activity by Puerariae Radix Extracts (갈근 추출물에 의한 염증성 Cytokine 생성 억제 및 Prostaglandin E2 활성 저해에 관한 연구)

  • Kim, Si-Na;Kim, Hee-Seok;Nam, Gyeong-Sug;Hwang, Sung-Wan;Hwang, Sung-Yeoun
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.35 no.1
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    • pp.28-34
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    • 2006
  • The ethanol extracts of Puerariae Radix inhibited cyclooxygenase-2 (COX-2) activity in bone marrow derived mast cells (BMMC). COX-2 is responsible for the production of large amounts of proinflammatory prostaglandins (PGs) at the inflammatory site. We have investigated the anti-inflammatory effect of ethyl acetate fraction from $70\%$ ethanol extract of Puerariae Radix (EPR), and attempted acetic acid induced writhing to verify the analgesic effect. Inflammation was induced by interleukin-1 (IL-1), tumor necrosis factor-a (TNF-a), $inteferon-\gamma$ $(IFN-\gamma)$ and lipopolysaccharide (LPS). EPR showed strong inhibitory efficacy against cytokine-induced proteoglycan degradation, prostaglandin $E_2\;(PGE_2)$ production, nitric oxide (NO) production, and matrix-metalloproteinases (MMPs) expression in mouse macrophage and rabbit articular chondrocyte. In the writhing test, EPR $(200\~400\;mg/kg)$ exhibited a dose-dependent inhibition of writhing. The results indicate that EPR have anti-inflammatory and analgesic activities, and could be a good herbal medicine candidate for treating of osteoarthritis (OA).

Artemisolide from Artemisia asiatica: Nuclear $Factor-{\kappa}B\;(NF-{\kappa}B)$ Inhibitor Suppressing Prostaglandin $E_2$ and Nitric Oxide Production in Macrophages

  • Reddy, Alavala Matta;Lee, Jun-Young;Seo, Jee-Hee;Kim, Byung-Hak;Chung, Eun-Yong;Ryu, Shi-Yong;Kim, Young-Sup;Lee, Chong-Kil;Min, Kyung-Rak;Kim, Young-Soo
    • Archives of Pharmacal Research
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    • v.29 no.7
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    • pp.591-597
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    • 2006
  • Aerial parts of Artemisia asiatica (Compositae) have been traditionally used as an oriental medicine for the treatment of inflammatory and ulcerogenic diseases. In the present study, artemisolide was isolated as a nuclear factor $(NF)-{\kappa}B$ inhibitor from A. asiatica by activity-guided fractionation. Artemisolide inhibited $NF-{\kappa}B$ transcriptional activity in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7 with an $IC_{50}$ value of $5.8\;{\mu}M$. The compound was also effective in blocking $NF-{\kappa}B$ transcriptional activities elicited by the expression vector encoding the $NF-{\kappa}B$ p65 or p50 subunits bypassing the inhibitory kB degradation signaling $NF-{\kappa}B$ activation. The macrophages markedly increased their $PGE_2$ and NO production upon exposure to LPS alone. Artemisolide inhibited LPS-induced $PGE_2$ and NO production with $IC_{50}$ values of $8.7\;{\mu}M$ and $6.4\;{\mu}M$, respectively, but also suppressed LPS-induced synthesis of cyclooxygenase (COX)-2 or inducible NO synthase (iNOS). Taken together, artemisolide is a $NF-{\kappa}B$ inhibitor that attenuates LPS-induced production of $PGE_2$ or NO via down-regulation of COX-2 or iNOS expression in macrophages RAW 264.7. Therefore, artemisolide could represent and provide the anti-inflammatory principle associated with the traditional medicine, A. asiatica.

Citrus platymamma inhibits the expression of pro-inflammatory cytokines, inducible nitric oxide synthase, and cyclooxygenase-2 in RAW264.7 macrophage (RAW264.7 대식세포에서 Citrus platymamma의 iNOS, COX-2, 염증성 사이토카인 발현 억제 효과)

  • Kim, Sang Suk;Park, Kyung Jin;An, Hyun Joo;Choi, Young Hun
    • Food Science and Preservation
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    • v.23 no.7
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    • pp.1026-1032
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    • 2016
  • Citrus platymamma hort. ex Tanaka is widely used in traditional Korean medicine because of its medicinal benefits including an anti-inflammatory effect. This study aimed to evaluate changes in the flavonoid content and anti-inflammatory activities of C. platymamma during its harvest period. Fruit peel samples were obtained between September 2015 and February 2016. The results indicate that C. platymamma peel extract (CPE) was an effective inhibitor of lipopolysaccharide (LPS)-induced NO production in RAW264.7 cells. The inhibitory effects of CPE at $100{\mu}g/mL$ concentration included dose-dependent decreases in the expression of iNOS and COX-2 proteins. In addition, CPE decreased the expression of pro-inflammatory cytokines TNF-${\alpha}$, IL-$1{\beta}$, and IL-6. The highest anti-inflammatory activity and flavonoid content were observed in CPE of C. platymamma peel harvested during the immature fruit period in September. Further, to assess the suitability of CPE for cosmetic use, we performed MTT assays using HaCaT keratinocytes and observed that CPE did not exhibit any cytotoxicity. To test the potential application of CPE as a cosmetic material, we also performed primary skin irritation tests on normal skin of 30 volunteers and no adverse reactions were observed. The results of this study indicate that CPE may be considered as an anti-inflammatory candidate for inclusion in cosmetic materials.

Inhibitory Effect of Kamisopunghwalhyeol-tang (Jiaweishufenghuoxie-tang) on Inflammatory Cytokine Production and $NF-{\kappa}B$ and AP-1 Activation in Cultured Humau Fibroblast-like Synoviocytes (가미속풍활형탕이 human fibroblast-like synoviocytes 내 염증 유발 cytokine과 전사인자에 미치는 영향)

  • 양동원;오민석;김동희
    • The Journal of Korean Medicine
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    • v.24 no.3
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    • pp.84-95
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    • 2003
  • Objective : This study was carried out to investigate the effects of Kamisopunghwalhyeol-tang (Jiaweishujenghuoxie-tang; Kami-SPHHT) on the immunity responses of the Synoviocytes isolated from the patients on rheumatoid arthritis. Methods : Cells were stimulated by $Interleukin-1{\beta}$ and Tumor Necrosis $Factor-{\alpha}$ in the presence or absence of Kami-SPHHT, and then induced cytokine mRNA levels were determined by RT-PCR and real-time quantitative RT-PCR. Results : Levels of $IL-1{\beta},{\;}IL-6,{\;}TNF-{\alpha}$, COX-2, and NOS II mRNA expressions significantly decreased in Kami-SPHHT treated cells compared to non-treated control cells. Also, DNA-binding activity of $NF-{\kappa}B$ and AP-l decreased in Kami- SPHHT treated hFLSs. Conclusion : These results suggest that Kami-SPHHT may be involved in anti-inflammatory reactions by inducing cytokine gene expression in synoviocytes, and further in vivo examination on its efficacy can provide potential application for the treatment of rheumatoid arthritis.

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In Vitro Anti-Inflammatory and Skin Protective Effects of Codium fragile Extract on Macrophages and Human Keratinocytes in Atopic Dermatitis

  • A-yeong Jang;JeongUn Choi;Weerawan Rod-in;Ki Young Choi;Dae-Hee Lee;Woo Jung Park
    • Journal of Microbiology and Biotechnology
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    • v.34 no.4
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    • pp.940-948
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    • 2024
  • Codium fragile has been traditionally used in oriental medicine to treat enterobiasis, dropsy, and dysuria, and it has been shown to possess many biological properties. Atopic dermatitis (AD) is one of the types of skin inflammation and barrier disruption, which leads to chronic inflammatory skin diseases. In the current investigation, the protective effects of C. fragile extract (CFE) on anti-inflammation and skin barrier improvement were investigated. In LPS-stimulated RAW 264.7 cells, nitric oxide generation and the expression levels of interleukin (IL)-1β, IL-4, IL-6, iNOS, COX-2, and tumor necrosis factor-alpha (TNF)-α were reduced by CFE. CFE also inhibited the phosphorylation of NF-κB-p65, ERK, p-38, and JNK. Additionally, CFE showed inhibitory activity on TSLP and IL-4 expression in HaCaT cells stimulated with TNF-α/interferon- gamma (IFN-γ). Enhanced expression of factors related to skin barrier function, FLG, IVL, and LOR, was confirmed. These findings implied that CFE may be used as a therapeutic agent against AD due to its skin barrier-strengthening and anti-inflammatory activities, which are derived from natural marine products.

Acacia ferruginea Inhibits Tumor Progression by Regulating Inflammatory Mediators-(TNF-α, iNOS, COX-2, IL-1β, IL-6, IFN-γ, IL-2, GM-CSF) and Pro-Angiogenic Growth Factor-VEGF

  • Sakthivel, Kunnathur Murugesan;Guruvayoorappan, Chandrasekaran
    • Asian Pacific Journal of Cancer Prevention
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    • v.14 no.6
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    • pp.3909-3919
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    • 2013
  • The aim of the present investigation was to evaluate the effect of A ferruginea extract on Dalton's lymphoma ascites (DLA) induced tumours in BALB/c mice. Experimental animals received A ferruginea extract (10 mg/kg.b.wt) intraperitoneally for 14 consecutive days after DLA tumor challenge. Treatment with extract significantly increased the life span, total white blood cell (WBC) count and haemoglobin (Hb) content and decreased the level of serum aspartate transaminase (AST), alanine transaminase (ALT), alkaline phosphatase (ALP), gamma glutamyl transferase (${\gamma}$-GT) and nitric oxide (NO) in DLA bearing ascites tumor models. In addition, administration of extract significantly decreased the tumour volume and body weight in a DLA bearing solid tumor model. The levels of pro-inflammatory cytokines such as tumor necrosis factor-alpha (TNF-${\alpha}$), interleukin-1 beta (IL-$1{\beta}$), interleukin-6 (IL-6) and granulocyte monocyte-colony stimulating factor (GM-CSF), as well as pro-angiogenic growth factors such as vascular endothelial growth factor (VEGF) and inducible nitric oxide synthase (iNOS) were elevated in solid tumour controls, but significantly reduced by A ferruginea administration. On the other hand, the extract stimulated the production of interleukin-2 (IL-2) and interferon-gamma (IFN-${\gamma}$) in animals with DLA induced solid tumours. Increase in $CD4^+$ T-cell population suggested strong immunostimulant activity for this extract. GC/MS and LC/MS analysis showed quinone, quinoline, imidazolidine, pyrrolidine, cyclopentenone, thiazole, pyrazole, catechin and coumarin derivatives as major compounds present in the A ferruginea methanolic extract. Thus, the outcome of the present study suggests that A ferruginea extract has immunomodulatory and tumor inhibitory activities and has the potential to be developed as a natural anticancer agent.

Anti-inflammatory Activity of Extracts from Ultra-Fine Ground Saururus chinensis Leaves in Lipopolysaccharide-Stimulated Raw 264.7 Cells

  • Kim, Dong-Hee;Cho, Jun-Hyo;Cho, Young-Je
    • Journal of Applied Biological Chemistry
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    • v.59 no.1
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    • pp.37-43
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    • 2016
  • Bioactive components of ultra-fine ground Saururus, the extraction yield increases when the leaves are ultra-fine ground. Comparison of normal-ground and ultra-fine ground Saururus chinensis leaves showed that the solid content and antiinflammatory activity of ultra-fine ground extracts was higher than that of normal-ground extracts. Lipopolysaccharide (LPS)-stimulated Raw 264.7 cells were treated with different concentrations of Saururus chinensis extract and the amount of nitric oxide (NO) was determined; LPS-treated cells produced 2 times more NO than cells that were not treated with LPS. Moreover, the NO production in cells treated with Saururus chinensis extract was inhibited in a concentration-dependent manner. Because the stimulant-induced NO production is regulated by the inducible nitric oxide synthase (iNOS), we measured the iNOS protein level to elucidate the mechanism by which the NO production was inhibited. We found that the amount of iNOS decreased dose-dependently. It was reduced by 53% at a Saururus chinensis extract concentration of $100{\mu}g/mL$. The protein expression of cyclooxygenase-2 (COX-2) in LPS-treated Raw 264.7 cells was inhibited by 31% at $100{\mu}g/mL$ of Saururus chinensis extract. Gel shift of the nuclear factor kappa B-DNA complex occurred in LPS-treated cells and the intensity of the band decreased gradually in a concentration-dependent manner. Ultra-fine ground Saururus chinensis extract had a concentration-dependent inhibitory effect on the production of prostaglandin $E_2$, tumor necrosis factor ${\alpha}$, interleukin $1{\beta}$ (IL-$1{\beta}$), IL-6, and IL-8 in LPS-treated Raw 264.7 cells, i.e., at $50{\mu}g/mL$ of Saururus chinensis extract, their levels were decreased by 53, 67, 52, 37, and 21% respectively.

Screening of Useful Plants with Anti-inflammatory and Antioxidant Activity (항염증 및 항산화 활성 보유 유용 식물 탐색)

  • Lee, Seung-Eun;Choi, Jehun;Lee, Jeong-Hoon;Noh, Hyung-Jun;Kim, Geum-Sook;Kim, Jinkyung;Chung, Hae-Young;Kim, Seung-Yu
    • Korean Journal of Plant Resources
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    • v.26 no.4
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    • pp.441-449
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    • 2013
  • This study was conducted to select some useful plants as functional material candidates. A total of 38 plants were preliminarily screened for the anti-inflammatory and antioxidant activities. The preliminarily selected 8 plants were further investigated to verify the in vitro inhibitory effect on inflammation and oxidative stress. Boehmeria platanifolia (root), Carpinus coreana (branch), and Eupatorium japonicum (leaf) inhibited the expression of inducible nitric oxide synthase (iNOS) in lipopolysaccharide (LPS)-treated RAW 264.7 cells. Eupatorium japonicum (leaf) suppressed the expression of cyclooxygenase-2 (COX-2), whereas Boehmeria platanifolia (root) and Prunus yedoensis (branch) inhibited the transcription of nuclear factor-kappa B (NF-${\kappa}B$). Treatment with the extracts ($2.5{\sim}20{\mu}g/ml$) of Abutilon theophrasti (leaf, flower/seed) and Hemistepta lyrata (stem) did not show toxicity on RAW 264.7 cell proliferation, but treatment with $2.5{\mu}g/ml$ of Boehmeria platanifolia (root) exhibited cell toxicity. Carpinus coreana (branch) and Prunus yedoensis (branch) showed potent scavenging activities on peroxynitrite. Akebia quinata (flower), Carpinus coreana (branch), and Prunus yedoensis (branch) effectively inhibited reactive oxygen species (ROS). Abutilon theophrasti (leaf), Boehmeria platanifolia (root), Carpinus coreana (branch), and Eupatorium japonicum (leaf) exhibited strong inhibitory capacity with regard to nitric oxide (NO) production. The results suggested that Abutilon theophrasti (leaf) has in vitro anti-inflammatory and antioxidant activities, and that is a useful functional material candidate.

Poncirin alleviates the symptoms of dextran sulfate sodium-induced colitic mice (Poncirin의 dextran sulfate sodium 유도 마우스 궤양성 대장염 증세 감소 효과)

  • Kim, Jong-Bin;Cho, Woong;Han, Ar-Reum;Seo, Eun-kyung;Lee, Kyung-Tae
    • Korean Journal of Pharmacognosy
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    • v.39 no.2
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    • pp.104-109
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    • 2008
  • We previously reported that anti-inflammatory properties of poncirin, isolated from fruit of Poncirus trifoliata, might be the result from the inhibition of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), tumor necrosis $factor-{\acute{a}}$ ($TNF-{\alpha}$) and interlukin-6 (IL-6) expression via the down-regulation of $NF{-\kappa}B$ binding activity. In this study, we investigated whether poncirin has an inhibitory effect on the production of pro-inflammatory mediators ex vivo and whether poncirin could relieve the symptoms of dextran sulfate sodium (DSS)-induced colitis in mice model of inflammatory bowel disease. Poncirin significantly inhibited the productions of NO, IL-6 and $TNF-{\alpha}$ in lipopolysaccharide (LPS)-induced mouse peritoneal macrophage. In addition, poncirin-treated mice when compared to control mice not receiving treatment recovered better from the weight loss caused by DSS-induced colitis. Changes in disease activity index (DAI) of poncirin-treated mice were also more favorable than for control mice and were comparable with mice treated with a typical anti-inflammatory-drug, 5-aminosalichylic acid (5-ASA). In addition, suppression of plasma NO and IL-6 productions of poncirin-treated mice was also observed in DSS-induced colitis. These results suggest that poncirin has potentially useful anti-inflammatory effects mediated by suppression of inflammatory mediator productions.