• Title/Summary/Keyword: Cyclooxygenase-2 저해

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Inhibitory Activities of Natural Products on Lipopolysaccharide Induced Prostaglandin Production in Mouse Macrophages (리포폴리사카라이드에 의해 유도되는 대식세포의 프로스타글란딘 생합성을 저해하는 천연물의 탐색)

  • Noh, Min-Soo;Ha, Jun-Yong;Lee, Chang-Hoon;Lee, Woo-Young;Lee, Soo-Hwan;Lee, Jung-Joon
    • YAKHAK HOEJI
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    • v.42 no.6
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    • pp.558-566
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    • 1998
  • Two isoforms of cyclooxygenase (COX) have been identified - COX-1, which is constitlitively expressed in most tissues, and the inducible form, COX-2, of which expression is induced by inflammatory signals and mitogens. It has been considered that the beneficial effects of NSAIDs are due to the inhibition of COX-2 activity and the side effects are from the inhibition of COX-1 activity. Therefore, it is essential to develop selective COX-2 inhibitor for developing new GI-tolerable NSAIDS. To discover new leads for developing selective COX-2 inhibitors, three-hundred extracts of natural products were primarily screened with the system of prostaglandin accumulation in LPS-stimulated mouse peritoneal macrophages. To identify whether these inhibitory activities of crude extracts on the accumulation of Prostaglandins were derived from direct action against COX-2, the effects of selected extracts on exogenous arachidonic acid-derived production of prostaglandins by LPS-stimulated macrophages were determined. Among them, 5 methanol extracts of natural products, such as Zingiberis Rhizoma, Alpinae Officinarum Rhizoma, Caryophilli Flos, Scutellariae Radix, Dalbergia ordorifera. inhibited more than 70% of the prostaglandin production in LPS-stimulated mouse peritoneal macrophages at a con-centration of 1${\mu}$g/ml.

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Antioxidant and Anti-inflammatory Effects of Bletilla striata Reichenbach fil. Fractions as Cosmetic (백급(Bletilla striata Reichenbach fil.) 분획물의 항산화, 항염증 효과와 화장품소재로서의 연구)

  • Yoon, Ji-Hun;Park, Seong-Geun;Lee, Mi-Ji;Park, Jin-Young;Seo, Kyo-Seong;Woo, Kyung-Chul;Lee, Chang-Eon
    • Journal of Life Science
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    • v.23 no.9
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    • pp.1073-1078
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    • 2013
  • The antioxidant and anti-inflammatory effects of active ingredients in cosmetics are very important. The effects are closely related to the prevention of skin aging. Among medicinal plants, Bletilla striata Reichenbach fil. has well-known pharmacological activity. Extracted samples were prepared using sequential fractionation of ethyl acetate, butanol, and water. The antioxidant effect of the fractions was confirmed by DPPH and ABTS+ radical scavenging. Among the various fractions of B. striata Reichenbach fil., ethyl acetate was associated with a reduction in nitric oxide production, which was induced by LPS (lipopolysaccharide) treatment in a dose-dependent manner. In addition, the production of iNOS (inducible nitric oxide synthase) and COX-2 (cyclooxygenase-2), which are upstream regulators of nitric oxide production, was also inhibited. Thus, the ethyl acetate fraction of B. striata Reichenbach fil. appears to be a potential active ingredient for use in cosmetics.

Study of Anti-inflammatory Effect of CopA3 Peptide Derived from Copris tripartitus (애기뿔소똥구리 유래 CopA3합성 펩타이드의 항염증 효능에 관한 연구)

  • Kim, Hyeon-Jeong;Kim, Dong-Hee;Lee, Jin-Young;Hwang, Jae-Sam;Lee, Joon-Ha;Lee, Seul-Gi;Jeong, Hyeon-Guk;An, Bong-Jeun
    • Journal of Life Science
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    • v.23 no.1
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    • pp.38-43
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    • 2013
  • The objective of this study was to evaluate the effect of the synthetic CopA3 peptide of Copris tripartitus on skin inflammation. Regulatory mechanisms of cytokines and nitric oxide (NO) are involved in the immunological activity of RAW 264.7 cells. Tested cells were treated with different concentrations of CopA3 and further cultured for an appropriate time after lipopolyssacharide (LPS) addition. During the entire experimental period, 5, 25, 50, and 100 ${\mu}g/ml$ of CopA3 had no cytotoxicity. At these concentrations, CopA3 inhibited tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$), interleukin-$1{\beta}$ (IL-$1{\beta}$), and interleukin-6 (IL-6). CopA3 also inhibited the expression of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2). CopA3 inhibited the activity of iNOS and COX-2 by 41% and 59%, respectively, at 100 ${\mu}g/ml$. In addition, CopA3 reduced the release of inflammatory cytokines including TNF-${\alpha}$, IL-$1{\beta}$, and IL-6. These results suggest that CopA3 may have significant effects on inflammatory factors and that it may be a potential anti-inflammatory therapeutic agent.

Anti-inflammatory effect of soil blue-green algae Nostoc commune isolated from Daejeon National Cemetery (국립대전현충원에서 분리한 남조류 구슬말(Nostoc commune)의 항염증 효과)

  • Hong, Hyehyun;Bae, Eun Hee;Park, Tae-Jin;Kang, Min-Sung;Kang, Jae Shin;Chi, Won-Jae;Kim, Seung-Young
    • Journal of Applied Biological Chemistry
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    • v.65 no.2
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    • pp.113-120
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    • 2022
  • We examined the anti-inflammatory properties of Nostoc commune HCW0811 in lipopolysaccharide-stimulated RAW264.7 macrophage cells. The anti-inflammatory activity of HCW0811 on viability of treated cells was assessed by measuring the level of expression of NO, prostaglandin E2 and pro-inflammatory cytokines, namely interleukin-1β, interleukin-6, and tumor necrosis factor-α in HCW0811 treated RAW 264.7 macrophages. HCW0811 was non-toxic to cells and inhibited the production of cytokines in a concentration-dependent manner. In addition its treatment suppressed the production of pro-inflammatory cytokines in a dose-dependent manner, and concomitantly decreased the protein expressions of inducible NO synthase and cyclooxygenase-2. Moreover, the levels of the phosphorylation of mitogen-activated protein kinase family proteins such as extracellular signal-regulated kinase, c-Jun N-terminal kinase, p38, and nuclear factor kappa B were reduced by HCW0811. These findings suggest that the HCW0811 collected from Daejeon National Cemetery have anti-inflammatory effects, and demonstrated its efficacy in cell-based in vitro assays.

Antioxidative and Antiallergic Effects of Aronia (Aronia melanocarpa) Extract (아로니아(Aronia melanocarpa)로부터 유래한 추출물의 항산화 및 항알레르기 효능)

  • Jeong, Jong-Moon
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.37 no.9
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    • pp.1109-1113
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    • 2008
  • The purpose of this study was to investigate the antioxidative and antiallergic effects of aronia extract. The aronia extract was tested for various antioxidative potentials (scavenging activity of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and superoxide anion radical) and inhibitory effect of 5-lipoxygenase (5-LO) and cyclooxygenase (COX). In aronia extract, polyphenol content was $81.6{\pm}3.3\;mg/g$ and flavonoid content was $5.15{\pm}0.16\;mg/g$. DPPH radical-scavenging activity ($SC_{50}$) of aronia extract was $6.15{\pm}0.343\;ppm$. $SC_{50}$ value of aronia extract against superoxide anion radical was $6.99{\pm}1.28\;ppm$. In addition, $IC\_{50}$ values of aronia extract against 5-LO, COX-1, and COX-2 were $42.07{\pm}0.15\;ppm$, $24{\pm}4.29\;ppm$, and $24.3{\pm}3.5\;ppm$, respectively. These results suggest that aronia extract may be useful for the prevention or treatment of allergic disease.

Inhibitory Effect of Chan-Su on the Secretion of PGE2 and NO in LPS-stimulated BV2 Microglial Cells

  • Kim, Min-Hee;Lyu, Ji-Hyo;Lyu, Sun-Ae;Hong, Sang-Hoon;Kim, Won-Il;Yoon, Hwa-Jung;Ko, Woo-Shin
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.22 no.5
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    • pp.1315-1321
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    • 2008
  • Chan-Su (Venenum bufonis) has long been for a variety of other purposes including treatment of inflammation in the folk medicine recipe. Since nitric oxide (NO) is one of the major inflammatory parameters, we first studied the effects of Chan-Su on NO production in lipopolysaccharide (LPS)-stimulated BV2 microglial cells, Chan-Su inhibited the secretion of NO in BV2 microglial cells, without affecting cell viability, The protein level of inducible nitric oxide synthase (iNOS) was decreased by Chan-Su, And Chan-Su also inhibited production of prostaglandin E2 (PGE2) and expression of cyclooxygenase (COX)-2. Proinflammatory cytokines, such as tumor necrosis factor $(TNF)-{\alpha}$, interleukin $(IL)-1{\beta}$ and IL-12, were inhibited by Chan-Su in a dose-dependent manner. And Chan-Su inhibited the degradation of ${IkB-\alpha}$, which was considered to be inhibitor of nuclear factor $(NF)-{\kappa}B$, one of a potential transcription factor for the expression of iNOS, COX-2 and proinflammatory cytokines. These results suggest that Chan-Su could exert its anti-inflammatory actions by suppressing the synthesis of NO through inhibition of $I{\kappa}B-{\alpha}$ degradation.

Inhibitory effect of broccoli leaf extract on PGE2 production by NF-κB inhibition (NF-κB 저해를 통한 브로콜리 잎 추출물의 PGE2 저해효과)

  • Park, Sook Jahr;An, Iseul;Noh, Gyu Pyo;Yoo, Byung Hyuk;Lee, Jong Rok
    • The Korea Journal of Herbology
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    • v.34 no.6
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    • pp.117-124
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    • 2019
  • Objective : Broccoli is edible green plant that has a wide variety of health benefits including cancer prevention and cholesterol reduction. However, leaves of broccoli are not eaten and are mostly left as waste. This study was conducted to evaluate the effects of the broccoli leaf extract (BLE) on prostaglandin E2 (PGE2) production related to nuclear factor kappa B (NF-κB) signaling in lipopolysaccharide (LPS)-activated macrophages. Methods : BLE was prepared by extracting dried leaf with ethanol. Cell viability was determined by 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. PGE2 and inflammatory cytokines were detected by enzyme-linked immunosorbent assay (ELISA). Expression level of each protein was monitored by Western blot analysis. Results : In LPS-activated Raw264.7 cells, PGE2 release into culture medium was dramatically enhanced compared to control cells. However, increased PGE2 was attenuated dose-dependently by treatment with BLE. Inhibition of PGE2 production by BLE was due to the suppression of cyclooxygenase-2 (COX-2) expression determined by Western blot analysis. BLE also inhibited the production of inflammatory cytokines such as interleukin-6 (IL-6) and tumor necrosis factor-alpha (TNF-α). Inhibition at PGE2 and cytokine was mediated from inhibition of nuclear translocation of NF-κB due to the repression of inhibitory kappa B alpha (IκBα) phosphorylation and degradation. Conclusion : This study showed that BLE exerted inhibitory activities against PGE2, which is critical for the initiation and resolution of inflammatory responses, and that inhibition of PGE2 was mediated by suppression of NF-κB signaling. These results suggest that the waste broccoli leaves could be used for controlling inflammation.

Induction of Cdk inhibitor p21 and inhibition of cyclooxygenase-2 by resveratrol in human lung carcinoma A549 cells. (Resveratrol에 의한 A549 인체 폐암세포의 증식억제 및 apoptosis 유발에 관한 연구)

  • 김영애;임선영;이숙희;박건영;이원호;최영현
    • Journal of Life Science
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    • v.14 no.5
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    • pp.800-808
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    • 2004
  • Resveratrol, a phytoalexin found at high levels in grapes and in grape products such as red wine, has been reported to possess a wide range of biological and pharmacological activities including antioxident, anti-inflammatory, anti-mutagenic, and anti-carcinogenic effects. According to recent studies, this compound is an effective inhibitor of cell growth in general, triggers partial arrest of the cell cycle and induce apoptosis. In this study, the anti-proliferative effects of resveratrol in A549 human lung carcinoma cells were investigated. It is shown that resveratrol induced the growth inhibition in a time-dependent manner and morphological changes of A549 cells, which were associated with induction of S phase arrest of the cell cycle and apoptotic cell death. The Bcl-$X_L$levels were markedly down-regulated in resveratrol treated cells, however, Bax and Bcl-2 were remained unchanged. Resveratrol treatment induced the proteolytic degradation of Sp-l and proliferating cell nuclear antigen protein, and inhibited the expression of $\beta$-catenin protein. Resveratrol treatment also induced a marked up-regulation of cyclin-dependent kinase (Cdk) inhibitor p21 and inhibited the kinase activities of Cdk2 and Cdk4. In addition, resveratrol treatment inhibited the levels of cyclooxygenase (COX)-2 mRNA and protein, and the release of prostagladin E2 without alteration of COX-1 expression. Taken together, these findings suggest that resveratrol may be a potential chemotherapeutic agent for the control of human lung carcinorma cells.

Regulation of Bcl-2 Family and Cyclooxygenases by Furanoterpenoids Isolated from a Marine Sponge Swcotragus nt. in Human Lung Cancer A549 Cells. (인체폐암세포의 Bcl-2 family 및 cyclooxygenases의 발현에 미치는 해면동물 Sarcotragus sp. 유래 furanoterpenoids의 영향)

  • 최영현;최혜정;김남득;정지형
    • Journal of Life Science
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    • v.14 no.3
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    • pp.445-452
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    • 2004
  • We investigated the cytotoxic effects of seven furanoterpenoids 〔sarcotin A, epi-sarcotin A, ircinin-1, epi-sarcotrine B, sarcotin I, (8E, l3Z, 20Z)-strobilinin/(7E,l3Z, 20Z)-felixinin and (7E,12E,18R,20Z)-variabilin〕 isolated from the sponge Sarcotragus sp. (the order Dictyoceratida) on the growth of A549 human lung carcinoma cells. MTT data revealed that sarcotin A and (7E,12E,18R,20Z)-variabilin exhibited higher potencies on the anti-proliferative activities than the other compounds in A549 cells. The growth inhibition by treatment with compounds (especially epi-sarcotin A, ircinin-1 and epi-sarcotrine B) were associated with the induction of apoptotic cell death through the concentration-dependent increase of Bax/Bcl-2 ratio in a p53-dependent or independent pathway Additionally, epi-sarcotin A and ircinin-1 strongly inhibited the levels of cyclooxygenase (COX)-2 expression without alteration of COX-1. Taken together, the results suggest that the furanoterpenoids from the marine sponge have strong potentials as candidates for anti-cancer drugs.

Inhibitory Effect of Mixture of Ethanol Extracts in Agastachis Herba and Pueraria Radix on the Proliferation and $PGE_2$ Production of HT-29 Human Colon Cancer Cell Line (곽향과 갈근 복합제제의 대장암 세포주 HT-29 증식 저해효과 및 $PGE_2$ 생성 억제효과)

  • Lee, Seung-Youn;Kim, Hee-Seok;Kim, Jeoung-Ok;Hwang, Sung-Wan;Hwang, Sung-Yeoun
    • Korean Journal of Pharmacognosy
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    • v.37 no.4 s.147
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    • pp.283-289
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    • 2006
  • Ethanol extracts of the whole herb of Agastachis Herba (A) and of Pueraria Radix (P) alone and of their mixture (A+P) downregulated the cell growth, cyclooxygenase-2 (COX-2) expression, prostaglandin $E_2\;(PGE_2)$, and cGMP production. A, P, and A + P inhibited the cell growth of HT-29 colon cancer cells in a concentration- and time-dependent manner but not the growth of normal colon cell, CCD-112CoN. In addition, they markedly inhibited the productions of $PGE_2$ and cGMP as well as the mRNA expression of COX-2. These data suggest that non-toxic concentration of A, P, and A + P have a significant effect on the in vitro growth of HT-29 cells, specifically through the inhibition of the $PGE_2$ production via COX-2.