• 제목/요약/키워드: cyclooxygenase inhibitory activity

검색결과 205건 처리시간 0.031초

상황버섯 균사체를 이용한 발효주의 추출물이 염증관련 단백질의 발현과 세포내 활성산소 생성에 미치는 영향 (Effect of the Evaporating Extract from Liquor of Fermentation Using Mycelium of Phellinus linteus on the Expression of Inflammatory Proteins and the Generation of Reactive Oxygen Species)

  • 이준혁;최영현;이용태;최성희;정경태;정영기;최병태
    • 동의생리병리학회지
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    • 제18권6호
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    • pp.1825-1831
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    • 2004
  • Phellinus linteus is known as a medicinal mushroom, which has the pharmaceutical activity on tumors and inflammatory diseases in traditional Oriental medicine. However, despite extensive pharmacological studies on P. linteus, the liquor of fermentation using mycelium of P. linteus(LFMP) has not been investigated. In the present study, it was examined the effect of the evaporating extract from LFMP(E-LFMP) on the expression of inflammatory proteins and the generation of reactive oxygen species in human hepatocarcinoma HepG2 cells. E-LFMP inhibited acetaldehyde-induced morphological change in HepG2 cells. Also, E-LFMP inhibits expression of inflammatory proteins including cyclooxygenase(COX)-1 and COX-2 through suppressing nuclear translocation of nuclear factor κB(NF-κB) and degradation of inhibitory κBα(IκBα). In addition, E-LFMP inhibits generation of reactive oxygen species(ROS) by hydrogen peroxide(H₂O₂) in HepG2 cells. These results suggest that LFMP has the pharmaceutical, especially anti-inflammatory, activity similar to P. linteus mushroom.

대추의 궤양성 대장염에 대한 개선 효과 (The improving effect of Zizyphus jujube on dextran sulfate sodium-induced colitis in mice)

  • 명노일
    • 대한본초학회지
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    • 제30권3호
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    • pp.35-40
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    • 2015
  • Objectives : Zizyphus jujube (ZJ) has been used as a traditional medicine for various diseases. However, the inhibitory effect of ZJ on intestinal inflammation has not been fully understood, yet. The aim of this study is to investigate anti-colitis activity of ZJ in dextran sulfate sodium (DSS)-induced colitis mouse model. Methods : To investigate the protective effects of ZJ,the colitis mice were induced by drinking water containing 5% DSS for 7 days. Mice were randomized into groups receiving ZJ (500 mg/kg), sulfasalazine (SFZ) (150 mg/kg) as a positive control, or water as a negative control. We assayed the effects of ZJ on DSS-induced the clinical signs, measuring weight loss, colon length and disease activity index (DAI). Additionally, to find a possible explanation for the anti-inflammatory effects of ZJ, we evaluated the effects of ZJ on the production of prostaglandin $E_2$ ($PGE_2$) and expression of cyclooxygenase (COX)-2 in colitis tissue. Results : The results showed that mice treated with DSS showed considerable clinical signs, including weight loss, and reduced colon length. However, administration of ZJ significantly reduced the weight loss, shortens colon length, and improved DAI as clinical symptoms. Moreover, ZJ inhibited the $PGE_2$ production and COX-2 expression levels in DSS-treated colon tissues. Conclusions : Collectively, the findings of this study provide us with novel insights into the pharmacological actions of ZJ as a potential molecule for use in the treatment of intestinal inflammation including ulcerative colitis.

Effects of Root Extracts from Angelica gigas and Angelica acutiloba on Inflammatory Mediators in Mouse Macrophages

  • Yoon, Tae-Sook;Cheon, Myeoung-Sook;Lee, Do-Yeon;Moon, Byeong-Cheol;Lee, Hye-Won;Choo, Byung-Kil;Kim, Ho-Kyoung
    • Journal of Applied Biological Chemistry
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    • 제50권4호
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    • pp.264-269
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    • 2007
  • Root extracts of Angelica gigas and A. acutiloba have been used traditionally for the treatment of gynecological diseases, as well as anemia, blood stasis, and inflammatory pain, as blood tonics in Oriental medicine. In the present study, we investigated the effects of A. gigas and A. acutiloba on inflammatory mediators in mouse macrophages and compared their activities. Many studies suggest that prostaglandin $E_2$ ($PGE_2$) biosynthesis and nitric oxide (NO) production play important roles in the processes of both inflammation and carcinogenesis. Ethanolic extracts from the roots of both species exhibited significant inhibitory effects on $PGE_2$ generation in lipopolysaccharide-stimulated RAW 264.7 cells. In particular, the extract from A. gigas was more effective than that from A. acutiloba. Although neither inhibited NO generation, the extract from A. acutiloba stimulated NO generation. Our results suggest that the roots of A. gigas might possess more anti-inflammatory and/or cancer chemopreventative activity than that of A. acutiloba due to the suppression of cyclooxygenase-2 (COX2)-mediated $PGE_2$ production. In addition, A. acutiloba might exert anti-tumor activity through an increase in macrophage-produced NO.

LPS로 유도된 RAW264.7 염증모델에서 미후등의 항염증효과 (Anti-Inflammatory Effect of Bower Actinidia in LPS-Stimulated RAW264.7 Cells)

  • 김영준;송춘호
    • Korean Journal of Acupuncture
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    • 제30권4호
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    • pp.243-251
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    • 2013
  • Objectives : Bower Actinidia has been widely used for treatment of inflammatory diseases, such as jaundice, cystolithiasis. However, the mechanism of its anti-inflammatory activity has not been clarified. In this study, we investigated the inhibitory effect of Bower Actinidia pharmacopuncture extract(BA) on LPS-induced inflammation. Methods : The effect of BA was analyzed by ELISA, RT-PCR and Western blotting in LPS-stimulated RAW264.7 cells. Results : We found that BA suppressed not only the mRNA expression of pre-inflammatory cytokines, cyclooxygenase-2(COX-2) and inducible nitric oxide synthase(iNOS), but also the phosphorylation of ERK, JNK and p38. Conclusions : These results suggest that BA exerts an anti-inflammatory effect through the regulation of the mitogen-activated protein kinase(MAPK) pathway, thereby decreasing production of pre-inflammatory cytokines.

한국 자생식물로부터 아라키돈산 대사계 효소 저해제 검색 (2) (Screening of Arachidonic Acid Cascade Related Enzymes Inhibitors from Korean Indigenous Plants (2))

  • 정혜진;문태철;이은경;손건호;김현표;강삼식;배기환;안인파;권동렬
    • 약학회지
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    • 제47권2호
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    • pp.69-77
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    • 2003
  • Arachidonic acid (AA), which is stored in membrane glycerophospholipids, is liberated by phospholipase $A_2$ (PLA$_2$) enzymes and is sequentially converted to cyclooxygenases (COXs) and lipoxygenases (LOXs) then to various bioactive PGs, and LTs. In order to find the specific inhibitors of AA metabolism especially PLA$_2$, COX-2, 5-LO and lyso PAF acetyltransferase, 120 Korean residential plants extracts were evaluated for their inhibitory activity on PGD$_2$, LTC$_4$ production from cytokine-induced mouse bone marrow-derived mast cells (BMMC) and arachidonic acid released from phospholipid and PAF production from lyso PAF. From this screening procedure, methanol extract of ten indigenous plant such as Salix gracilistyla, Sedum kamtschaticum, Cirsium chanroenicum, Hypericum ascyron, Astilbe chinensis, Agrimonia pilosa, Aristolochia manshuriensis, Vodia daniellii, Pyrola japonica, Styrax obassia were found to inhibit production of inflammatory mediators in vitro assay system.

Inhibitory Effect of Probenecid on Osteoclast Formation via JNK, ROS and COX-2

  • Cheng, Mi Hyun;Kim, Sung-Jin
    • Biomolecules & Therapeutics
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    • 제28권1호
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    • pp.104-109
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    • 2020
  • Probenecid is a representative drug used in the treatment of gout. A recent study showed that probenecid effectively inhibits oxidative stress in neural cells. In the present study, we investigated whether probenecid can affect osteoclast formation through the inhibition of reactive oxygen species (ROS) formation in RAW264.7 cells. Lipopolysaccharide (LPS)-induced ROS levels were dose-dependently reduced by probenecid. Fluorescence microscopy analysis clearly showed that probenecid inhibits the generation of ROS. Western blot analysis indicated that probenecid affects two downstream signaling molecules of ROS, cyclooxygenase 2 (COX-2) and c-Jun N-terminal kinase (JNK). These results indicate that probenecid inhibits ROS generation and exerts antiosteoclastogenic activity by inhibiting the COX-2 and JNK pathways. These results suggest that probenecid could potentially be used as a therapeutic agent to prevent bone resorption.

Inhibitory Effects of Total Saponin Korean Red Ginseng on Thromboxane A2 Production and P-Selectin Expression via Suppressing Mitogen-Activated Protein Kinases

  • Shin, Jung-Hae;Kwon, Hyuk-Woo;Rhee, Man Hee;Park, Hwa-Jin
    • 대한의생명과학회지
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    • 제23권4호
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    • pp.310-320
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    • 2017
  • Ginseng has been widely used for traditional medicine in eastern Asia and is known to have inhibitory effects on cardiovascular disease (CVD) such as thrombosis, atherosclerosis, and myocardial infarction. Because, platelet is a crucial mediator of CVD, many studies are focusing on inhibitory mechanism of platelet functions. Among platelet activating molecules, thromboxane $A_2$ ($TXA_2$) and P-selectin play a central role in CVD. $TXA_2$ leads to intracellular signaling cascades and P-selectin plays an important role in platelet-neutrophil and platelet-monocyte interactions leading to the inflammatory response. In this study, we investigated the inhibitory mechanisms of total saponin fraction from Korean red ginseng (KRG-TS) on $TXA_2$ production and P-selectin expression. Thrombin-elevated $TXA_2$ production and arachidonic acid release were decreased by KRG-TS dose (25 to $150{\mu}g/mL$)-dependently via down regulation of microsomal cyclooxygenase-1 (COX-1), $TXA_2$ synthase (TXAS) activity and dephosphorylation of cytosolic phospholipase $A_2$ ($cPLA_2$). In addition, KRG-TS suppressed thrombin-activated P-selectin expression, an indicator of granule release via dephosphorylation of mitogen-activated protein kinases (MAPK). Taken together, we revealed that KRG-TS is a beneficial novel compound inhibiting $TXA_2$ production and P-selectin expression, which may prevent platelet aggregation-mediated thrombotic disease.

식물성 일반식품 자원의 에탄올 추출물이 염증 효소계에 미치는 영향 (Inhibitory Effects on the Enzymes Involved in the Inflammation by the Ethanol Extracts of Plant Foodstuffs)

  • 권은숙;김일낭;권훈정
    • 한국식품과학회지
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    • 제39권3호
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    • pp.348-352
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    • 2007
  • 한국인이 상용하는 식물성 식품 30종의 에탄올 추출물을 이용하여 $sPLA_{2}$, COX-1, COX-2, 12-LOX 의 활성 억제 효과를 측정하여 식물 추출물이 염증 효소계에 미치는 영향을 포괄적으로 평가하였다. 그 결과 모든 식물 추출물은 적어도 한 개 이상의 염증 관련 효소의 활성을 저해하였다. 몇 가지 두류와 숙주나물, 일부 잎채소는 염증반응의 상위 단계 효소인 $sPLA_{2}$의 활성을 저해하였으며, 12-LOX 활성은 발아나물인 콩나물과 숙주나물에 의해서만 특이적으로 저해되었다. 대부분의 식품들은 COX-1과 COX-2 활성을 동시에 저해하였고, 미나리와 비름만이 COX-1 활성 저해 없이 COX-2만을 선택적으로 저해하였다. 모든 두류 유래식품과 식물 뿌리류는 COX-2에만 선택적이지는 않았으나, COX-1보다 더 낮은 농도에서 COX-2 활성을 억제하였다. 여러 식품들 중 염증반응의 상위단계 효소인 $sPLA_{2}$ 활성을 억제하는 일부 두류와 잎채소류 및 숙주나물은 염증 초기에 작용하여 염증 반응의 발전을 차단하는데 도움을 줄 수 있을 것으로 보인다. 특히, 녹두는 비교적 낮은 $IC_{50}$ 값을 보이며 $sPLA_{2}$와 COX-2를 효과적으로 저해하는 것으로 나타나 염증반응의 여러 단계에서 항염 효과를 나타낼 수 있는 유용한 식품으로 판단된다. 또한 각각의 염증 관련 효소에 대한 억제 능력이 크지는 않았지만, 염증 반응의 초기 및 후기 단계의 모든 효소를 저해 하였던 숙주나물과 12-LOX 및 COX-2를 동시에 저해한 콩나물도 여러 염증 효소를 복합적으로 억제시킴으로써 항염능을 나타낼 수 있다는 점에 주목 할 필요가 있다. 본 연구 결과 식물성 식품에 의한 염증 완화 및 예방 효과는 각기 다른 염증 효소의 활성을 다양한 정도로 저해함으로써 발현됨을 알 수 있다. 밝혀졌으며 제2형 당뇨모델인 $KK-A^{y}$ 마우스를 이용한 동물실험에서도 뚜렷한 혈당강하효과를 나타내어 인슐린 민감성 제재로 개발 할 수 있는 가능성을 보여 주었다.균은 $0.9{\sim}2.6%$이었으며, 8종류 약제에 저항성인 균도 1.7%있었다. 이상의 결과로 국내에서 분리된 M. pneumoniae 균주는 적게는 1-4 종류의 항생제에, 많게는 5-8 종류의 항생제에 저항성인 균주가 있으므로 마이코플라스마폐렴 환자를 치료할때는 macrolide계나 quinolone계의 항생제 선택에 신중을 기하여야 하며, 가급적이면 항생제 감수성 검사를 실시하여 적절한 항생제를 선택함으로써 저항성균의 출현율을 줄일 수 있고 효율적인 치료도 할 수 있도록 하여야 할 것으로 생각된다.이어트에도 도움이 되리라 생각한다. 56.3%, 엽산 81.3% 등으로 높게 나타나 근로자들의 영양 문제가 심각함을 알 수 있다.혁신지방분권위원회에서 제시한 자치경찰제도(안)을 중심으로 자치경찰제도 운용의 목적 충족과 실질적인 효과의 측면에서 분석하고 바람직한 자치경찰제도의 운용에 대해 살펴본다.rc}C$ 이내에서 높을수록, 염분은 20-35 psu 이내에서 높을수록 잠입률이 높은 경향을 나타내었다. 교수학습모형에 관련된 지식을 묻는 내용으로 주로 출제되었다. 이에 구체적인 개선방안으로 특정 교수학습모형의 이론적 토대가 되고 전체적인 교수설계를 하기 위한 기본 바탕이 될 수 있는 교수학습이론에 관한 내용, 또한 현재가정과교육에 있어서 유용한 교수학습법이라고 입증되고 있는 실천적 추론 가정과 수업에 관한 내용으로의 확대를 제안하였다. 가정과교육평가 문항의 출제는 대다수의 문항이 수행평가에 관한 문항내용으로 출제되었다. 이에 구체적인 개선방안으로 문항의 변별도 여부의 판단, 평가문항의 내용 타당도 분석, 평가결과를 해석하는 능력, 평가자의 철학적 관점과 같은 내용으로의 확대를 제안하였다.

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

  • 양권민;송상목;이도승;윤원종;김찬식;김창숙
    • 한국자원식물학회지
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    • 제32권5호
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    • pp.433-441
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    • 2019
  • 본 연구는 하라케케(Harakeke)로 불리는 신서란(Phormium tenax)를 화장품 및 의약품산업의 기능성 소재로서의 이용 가능성을 확인하기 위하여 신서란 잎을 대상으로 70% 에탄올 추출물과 용매 분획물을 제조하여, 이것들의 항염증 및 항아토피의 효과를 조사하였다. LPS로 유도된 RAW 264.7 세포에서 신서란 에탄올 추출물과 용매 분획물의 항염증 효과를 조사한 결과, methylene chloride와 ethyl acetate 분획물에서 NO와 $PGE_2$ 생성 억제 활성이 가장 높게 나타났으며, 농도 의존적으로 NO와 $PGE_2$ 생성 억제 활성을 보였다. 또한, 이들 분획물에서는 iNOS 및 COX-2 발현 억제 활성을 보였다. 신서란 잎 조추출물과 용매 분획물에 의한 NO, $PGE_2$ 생성 억제 활성이 NOS 및 COX-2 발현 억제에 의한 것임을 제시한다. 더불어, $hIFN-{\gamma}$로 자극된 HaCaT 세포에 용매 분획물을 처리하여 MDC 및 TRAC 생성억제 효과를 조사한 바, methylene chloride 분획물은 MDC 및 TATC의 생성을 각각 65%, 52% 생성억제 시켰으며, ethyl acetate 분획물은 MDC 및 TATC의 생성을 각각93%, 84% 억제 효과를 보였다. 이상의 결과는 신서란 잎 조추출물과 용매 분획물을 이용한 항염증 및 항아토피 효능을 갖는 유효성분 분리 및 활용화 연구에 중요한 기초자료가 될 것이며, 기능성 화장품, 의약외품 및 의약품 소재 개발에 적용 가능성이 높다고 사료된다.

황기의 COX-2 활성 억제 효과 (Inhibitory effect of Astragali Radix on COX-2 activity)

  • 김은정;오오진;이상국;양기숙
    • 생약학회지
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    • 제32권4호통권127호
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    • pp.311-315
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    • 2001
  • The root of Astragalus membranaceus Bunge (Leguminosae), which has been used for the treatment of hypertension, chronic hepatitis, duodenal ulcers, chronic nephritis and promotion of immunity in folk remedies. Cyclooxygenase (COX-2) is responsible for the production of large amounts of proinflammatory prostaglandins (PGs) at the inflammatory site. Thus, a logical approach to the treatment of inflammatory disease should involve the inhibitors of COX-2. To develop new COX-2 inhibitors from natural products, Astragali Radix was screened by inhibiting prostaglandin $E_2(PGE_2)$ generation in the culture medium using enzyme immunometric assay. Two isoflavone glycosides, $7,2'-dihydroxy-3',4'-dimethoxyisoflavan-7-O-{\beta}-D-glucoside$ and $calycosin-7-O-{\beta}-D-glucoside$ isolated from Astragali Radix inhibited COX-2 activity.

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