• 제목/요약/키워드: cyclooxygenase inhibitory activity

검색결과 207건 처리시간 0.036초

원지(遠志)의 항염증 작용에 대한 연구 (Anti-inflammatory activity of the water extract of Polygala tenuifolia Willd)

  • 오현석;김병우
    • 대한한방내과학회지
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    • 제34권2호
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    • pp.204-214
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    • 2013
  • Objectives : This study was designed to investigate the cellular and molecular mechanisms of anti-inflammatory activity of the water extract of Polygala tenuifolia Willd. (Pt-WE). Methods : Using lipopolysaccharide (LPS)-stimulated murine RAW264.7 cells, we examined inflammatory mediators such as nitric oxide (NO), inducible NO synthase (iNOS), cyclooxygenase (COX)-2 and prostaglandin $E_2$ ($PGE_2$). Also, the inhibitory effect of Pt-WE on the activity of activator protein 1 (AP-1) and upstream signaling molecules was evaluated. To assess the protective effect of Pt-WE on hydrochloride/ethanol (HCl/EtOH)-induced gastric ulcer in mice, we compared Pt-WE (200 mg/kg) with ranitidine (50 mg/kg) treated mice's gastric mucosa, based on gross observations. Results : Pt-WE inhibited LPS-induced production of NO, $PGE_2$ in a dose-dependent manner, without causing cytotoxicity. Pt-WE suppressed AP-1 activation by reducing generations of both c-Jun and c-Fos. In addition, Pt-WE inhibited the p-MKK 4/7 (mitogen-activated protein kinase kinase 4/7) and p-JNK (c-Jun N-terminal kinase) 1 in LPS-stimulated RAW264.7 cells. HCl/EtOH-induced gastric ulcer lesions were inhibited by pre-treatment of Pt-WE based on gross observations. In addition, Pt-WE decreased the phosphorylation level of JNK. Conclusions : These results demonstrate that Pt-WE has anti-inflammatory and gastroprotective effects. Thus, Pt-WE may be used widely in treatment of not only neurodegenerative diseases but also inflammatory diseases.

Inhibitory Effects of Ginsenoside Rb1,Rg3, and Panax ginseng Head Butanol Fraction on Inflammatory Mediators from LPS-Stimulated RAW 264.7 Cells

  • Lee, Je-Hyuk;Jeong, Choon-Sik
    • Biomolecules & Therapeutics
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    • 제16권3호
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    • pp.277-285
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    • 2008
  • Panax ginseng C.A. Mayer (Araliaceae, P. ginseng) has been used for the enhancement of vascular and immune functions in Korea and Japan for a long time. Ginsenoside $Rb_1$ and $Rg_3$ isolated from P. ginseng head-part butanolic extract (PGHB) were investigated for anti-inflammatory activity. Ginsenosides and PGHB did not affect the cell viability within $0\;-\;100\;{\mu}g/ml$ concentration to RAW 264.7 murine macrophage cells. Ginsenosides and PGHB inhibited partly lipopolysaccharide (LPS)-induced nitrite production in a dose-dependent manner. The ginsenosides and PGHB showed partially chemical nitric oxide (NO) quenching (maximum 40%) in the cell-free system. Also, ginsenoside $Rb_1$ and $Rg_3$ inhibited markedly approximately 74 and 54% of inducible nitric oxide synthase (iNOS) mRNA transcription from LPS-induced RAW 264.7 cells. Taken together, the inhibitory effect of ginsenosides and PGHB on NO production did not occur as a result of cell viability, but was caused by both the chemical NO quenching and the regulation of iNOS. Additionally, the ginsenoside $Rb_1$ and PGHB inhibited prostaglandin $E_2$ ($PGE_2$) synthesis in a concentration-dependent manner, showed approximately 70-98% inhibition at $100\;{\mu}g/ml$ concentration. And the treatment with ginsenosides and PGHB attenuated partially LPS-upregulated cyclooxygenase-2 (COX-2) gene transcription. Ginsenoside $Rg_3$ suppressed LPS-stimulated interleukin-6 (IL-6) level to the basal in RAW 264.7 cells. From these results, ginsenoside $Rb_1,\;Rg_3$, and PGHB may be useful for the relief and retardation of immunological inflammatory responses and its action may occur through the reduction of inflammatory mediators, including NO, $PGE_2$, and IL-6 production.

Effects of Herbal Acupuncture of Clematis Mandshurica Maxim. at Sinsu-hyul (BL 23) on Adjuvant Arthritis in Rats.

  • Kim, Kap-Sung;Lee, Seung-Deok;Lee, Chang-Hwan
    • 대한한의학회지
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    • 제27권4호
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    • pp.174-181
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    • 2006
  • Objective : Based on the immunological dysfunction in RA and the immunological feature of Clematis mandshurica Maxim. herbal acupuncture solution (CM-HAS), this study examined whether subcutaneous (s.c.) administration of CM-HAS has anti-inflammatory effects on adjuvant arthritis (AA) in the rat. Methods : Complete Freund's adjuvant was used to induce AA in rats. Secondary paw swelling of AA rats was measured, and polyarthritis index was scored. The administration of CM-HAS (2, 5, 10 mg/kg) to the Sinsu-hyul (BL 23) acupuncture point subcutaneously (s.c.) inhibited the inflammatory response and restored the weight of body and immune organs of AA rats. In this study. inhibitory effect of CM-HAS on cyclooxygenase-2 (COX-2) was evaluated. The plant material selected for this study has been used in Korean medicine for the treatment of various diseases that are considered as inflammatory in nature, e.g. asthma, arthritis, rheumatism, fever, edema, infections, snakebite and related inflammatory diseases. Results : There were significant secondary inflammatory reactions in AA rats, accompanied with the simultaneous decrease of body and immune organs weight. The administration of CM-HAS (2, 5, 10 mg/kg, s.c.) improved the above changes significantly. CM-HAS showed inhibitory activity against COX-2, which supports their traditional uses. In this study, aspirin and indomethacin were used to contrast with CM-HAS as the COX-2 inhibitors. Conclusion: The findings of this study may explain at least in part why CM-HAS has been traditionally used for the treatment of inflammatory conditions in traditional Korean and Chinese medicine.

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LPS로 유도한 RAW 264.7 세포의 염증반응에서 뚝새풀 에탄올 추출물의 억제 효과 (Inhibitory Effect of Alopecurus aequalis Sobol Ethanol Extracts on LPS-induced Inflammatory Response in RAW 264.7 Cells)

  • 정호경;강병만;장지훈;안병관;여준환;정원석;조정희;국용인;현규환;조현우
    • 한국약용작물학회지
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    • 제22권2호
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    • pp.98-104
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    • 2014
  • In the present study, we investigated the anti-inflammatory effects by Alopecurus aequalis Sobol on the lipopolysaccharide (LPS)-induced nitric oxide (NO) production by RAW 264.7 cell line. Consistent with these observations, DS reduced the LPS-induced expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) at the protein levels in a concentration-dependent manner. In addition, the release of tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$) and interleukin-6 (IL-6) were also reduced by DS. Moreover, LPS increased expression phosphorylation of $I{\kappa}B{\alpha}$, but DS showed inhibitory effect by reducing LPS-inducible p-$I{\kappa}B{\alpha}$ expression level. These results suggest that the down regulation of iNOS, COX-2, TNF-${\alpha}$, and IL-6 expression by DS are achieved by the downregulation of NF-${\kappa}B$ activity, a transcription factor necessary for pro-inflammatory mediators, and that is also responsible for its anti-inflammatory effects.

생지황음자(生地黃飮子) 추출물이 단핵세포에서 당화종말산물로 유도된 염증반응에 미치는 효과 (Effects of Saengjihwangeum-ja Extracts on the Expression of Inflammatory Response in Human Monocyte Cells Induced by Advanced Glycation End Product)

  • 이광규;한웅;정한솔
    • 동의생리병리학회지
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    • 제23권6호
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    • pp.1305-1313
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    • 2009
  • Saengjihwangeum-ja (SJHEJ) was recorded in DongEuiBoGam as being able to be used for treatment of Sogal whose concept had been applied to Diabetes Mellitus (DM). Modification of proteins by long term circulation of glucose leads to the formation of advanced glycation end product(AGE). Recent immunological studies demonstrated that ligation of AGE play an important role in the development of diabetic complications including atherosclerosis, which includes activation, adhesion, and migration of monocytes. Also, AGE and Maillard reaction product(MRP) could augment monocyte inflammatory responses via ligation of AGE receptor. In this study, the effects of SJHEJ extracts on the expression of inflammatory response-related genes such as tumor necrosis factor-$\alpha$, monocyte chemoattractant protein-1, interferon-g-inducible protein-10, and cyclooxygenase-2 in the human monocyte cell line, THP-1 cells. Reverse transcriptase-polymerase chain reaction revealed that SJHEJ had inhibitory effects on the expression of the TNF-a, MCP-1, IP-10, COX2, IL-1b genes in MRP-induced THP-1 cells. Treatment with SJHEJ had reduced reactive oxygen production in THP-1 cells stimulated by MRP. These inhibitory effects might be exerted via prevention of oxidative stress in activated monocytes. In addition, radical scavenging activity of SJHEJ was increased. These results suggest that SJHEJ has a beneficial effects for improve diabetic vascular complication.

Monascus sp. BHN-MK로 발효생산한 홍국 에탄올 추출물의 Raw 264.7 대식세포에 있어 친-염증성 iNOS와 COX-2 단백질 발현 억제 효과 (Inhibitory Effect of Ethanol Extract of Monascus-fermented Red Yeast Rice on Proinflammatory iNOS and COX-2 Protein Expression in LPS-stimulated RAW 264.7 Macrophage Cells)

  • 김기현;이준형;권기석;서을원;이중복
    • 생명과학회지
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    • 제30권4호
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    • pp.352-358
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    • 2020
  • 홍국은 한국에서 오랫동안 음식과 전통의학 소재로 사용되어 왔다. Monascus sp.의 생장과 2차 대사과정을 통해 Monascus 색소, monacolins, γ-aminobutyric acid 등을 생산할 수 있다. Monascus 종의 대사산물인 monacolin K, γ-aminobutyric acid과 dimerumic acid는 특정 항산화 효과로 인해 콜레스테롤과 혈압을 낮춘다고 알려져 있다. 이 연구는 Monascus sp.로 발효된 홍국쌀 에탄올 추출물의 항염증 활성을 조사하였다. 홍국 에탄올 추출물의 총 폴리페놀 함량을 측정하였고, 항염증 효과는 LPS가 유도된 Raw 264.7 cell에서 NO 생성, iNOS 및 사이클로옥시게나아제-2(cyclooxygenase-2 (COX-2)) 단백질 활성을 측정하였다. 총 폴리페놀 함량은 발효되지 않은 일반쌀보다 높은 함량을 나타내었다. NO 생성 저해활성 평가는 400 ㎍/ml 농도에서 LPS를 처리하지 않은 음성대조군의 NO 생성량과 유사한 결과를 나타내었다. iNOS 및 COX-2 단백질 발현 저해활성은 400 및 800 ㎍/ml에서 iNOS의 발현을 상당부분 억제하였다. 홍국 에탄올 추출물은 높은 항염증 효과를 확인하였으며, 기능성화장품 및 항염증소재로서 활용 가능할 것으로 사료된다.

사과 과피 추출물의 염증 관련 효소 억제 효과 (Inhibitory Effects of Apple Peel Extract on Inflammatory Enzymes)

  • 김일낭
    • 한국식품과학회지
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    • 제47권4호
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    • pp.534-538
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    • 2015
  • 본 연구는 사과 과육을 이용한 잼, 음료, 소스, 통조림 등을 가공하는 과정 중 부수적으로 발생하는 사과 과피의 활용을 위해 70% 에탄올 추출물을 이용하여 생리활성을 측정하였다. 이를 위해 사과 과피 추출물의 총 페놀 및 플라보노이드 함량을 측정하고 항산화 활성과 항염 효과를 평가하였다. 사과 과피 추출물의 총 페놀 함량과 플라보노이드 함량은 각각 $6.8{\pm}0.5mgGAE/g$, 플라보노이드는 $3.3{\pm}0.3mgCE/g$으로 나타났다. 항산화 활성을 평가하기 위해 측정한 DPPH 라디칼 소거능은 추출물의 농도에 의존적으로 증가하여 0.1, 0.5 및 1.0 mg/mL의 농도에서 각각 $18.9{\pm}1.6$, $46.3{\pm}2.3$$58.1{\pm}3.9%$로 나타났다(p<0.05). 사과 과피 추출물에 의한 염증 관련 효소 활성 억제 효과를 측정한 결과 $sPLA_2$ 활성은 0.5 및 1.0 mg/mL 농도에서 각각 $26.9{\pm}1.4$$53.5{\pm}2.3%$ 유의적으로 감소하였다(p<0.05). COX-2 활성 억제 효과는 0.1, 0.5 및 1.0 mg/mL의 모든 농도에서 각각 $16.7{\pm}2.6$, $43.6{\pm}3.0$$64.8{\pm}5.4%$로 유의적이었으나 COX-1 활성은 1.0 mg/mL에서만 13.4% 유의적인 저해효과를 나타냈다(p<0.05). LOX 활성 저해 효과 또한 0.1, 0.5 및 1.0 mg/mL 농도에서 각각 $11.9{\pm}1.3$, $27.4{\pm}2.7$$44.4{\pm}4.5%$로 나타나 유의적인 항염 효과를 보였다(p<0.05). 본 연구결과는 사과 과피 추출물이 라디칼 소거능을 통한 항산화 효과를 가지고, 다양한 염증 관련 효소의 활성을 억제함으로써 염증 반응을 전반적으로 조절하고 완화시킬 수 있음을 보여주어, 사과를 이용한 제품의 가공 과정에서 부산물로 생기는 과피를 항산화 및 항염 효과를 가지는 건강기능성식품 소재로 이용할 수 있는 가능성을 시사한다.

금은화 수용성 추출물의 LPS 유도 염증매개물 억제 효과 (Inhibitory Effect of Aqueous Extract from Lonicera japonica Flower on LPS-induced Inflammatory Mediators in RAW 264.7 Macrophages.)

  • 윤용갑;김규민;이성준;유승훈;장선일
    • 대한본초학회지
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    • 제22권3호
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    • pp.117-125
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    • 2007
  • Objective : Lonicera japonica (Caprifoliaceae) has long been used for treatment of infectious diseases in oriental countries. The aim of this study was to investigative the effect by which the aqueous extract from flower of L. japonica (LJFAE) inhibited the lipopolysaccharide (LPS)-induced inflammatory mediators in murine macrophages, RAW 264.7 cells Methods : The dried flowers of L. japonica were extracted with distilled water at $100^{\circ}C$ for 7 h. The extract was filtered through 0.45 ${\mu}m$ filter, freeze-dried. The dried extract was dissolved in Hank's balanced salt solution (HBSS) and filtered through 0.22 ${\mu}m$ filter before use. Accumulated nitrite, an oxidative product of nitric oxide (NO), was measured in the culture medium by the Griess reaction. The levels of prostaglandin E2 (PGE2), tumor necrosis factor-$\alpha$ (TNF-$\alpha$), interleukin-1$\beta$ (IL-1$\beta$), and IL-6 production, inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) expression were measured by enzyme-linked immunosorbent assay and Western blot analysis. Results: LJFAE (10-400 ${\mu}g$/ml) per se had no cytotoxic effect in unstimulated macrophages, but LJFAE concentration-dependently reduced NO, PGE2, TNF-, IL-l, and IL-6 production and COX-2 activity caused by stimulation of LPS. The levels of iNOS and COX-2 protein expressions were markedly suppressed by the treatment with LJFAE in a concentration dependent manner. Conclusions : These results suggest that LJFAE suppress the NO and PGE2production in macrophages by inhibiting iNOS and COX-2 expression and these properties may contribute to the anti-inflammatory activity of Lonicera japonica.

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

  • 정종문
    • 한국식품영양과학회지
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    • 제37권9호
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    • pp.1109-1113
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    • 2008
  • 본 연구에서는 아로니아 추출물의 항산화제와 항알레르기 치료제로써의 유효성을 알아보기 위해 페놀성 화합물 및 플라보노이드 함량과 DPPH 라디칼 포착효능, superoxide 음이온 라디칼 포착효능, 5-LO억제 효능 및 COX억제효능을 측정하였다. 측정결과 아로니아는 유효성분으로 예상되는 페놀성 화합물과 플라보노이드가 각각 $745.4{\pm}3.7\;mg/g$, $74.63{\pm}2.2\;mg/g$으로 상당량 함유되어 있으며, 상당히 낮은 농도($6.15{\pm}0.343\;ppm$, $6.99{\pm}1.26\;ppm$)에서 DPPH 라디칼과 superoxide 음이온 라디칼을 50% 소거하는 것으로 나타났다. 아로니아의 항알레르기 효능에 관하여 5-LO의 $IC_{50}$값이 $47.07{\pm}0.15\;ppm$으로, EGCG의 $IC_{50}(15.83{\pm}0.98\;ppm)$보다는 높았지만 아로니아가 EGCG와 같은 단일물질이 아니라 천연혼합물임을 감안하여 다른 천연물들의 $IC_{50}$값과 비교하였을 때 5-LO를 비교적 낮은 농도에서 억제하고 있다고 볼 수 있다. 또한, COX-1과 COX-2의 저해 비율 비교를 통해 양성대조군으로 사용한 EGCG만큼 COX-2를 선택적으로 저해하고 있음을 확인하였다. 이상의 결과에 따르면 아로니아 추출물은 항산화 및 항알레르기 효능을 갖고 있으며, 따라서 알레르기성 비염이나 아토피와 같은 알레르기 관련 질병 치료에 유효하게 사용될 것이라 생각된다.

미세먼지에 의해 유발되는 인간각질형성세포 손상에 대한 신규 트리펩타이드의 보호 효과 (Protective Effects of Novel Tripeptide Against Particulate Matter-induced Damage in HaCaT Keratinocytes)

  • 이응지;강한아;황보별;이영민;정용지;김은미
    • 대한화장품학회지
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    • 제47권1호
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    • pp.75-84
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    • 2021
  • 본 연구에서는 3 개의 아미노산으로 이루어진 트리펩타이드의 미세먼지에 의한 인간각질형성세포의 손상 억제 효과에 대해 확인하였다. 실험 결과 트리펩타이드 처리 시 미세먼지에 의한 세포 사멸이 억제되어 생존율 증가가 관찰되었으며, aryl hydrocarbon receptor (AhR) 기전 활성이 억제 되어 독성 대사체 생성과 염증반응에 관여하는 하위 인자인 cytochrome P450 family 1 subfamily A member 1 (CYP1A1) 및 cyclooxygenase-2 (COX-2)의 발현이 저해되었다. 또한 미세먼지에 의한 산화적 스트레스 억제 효과를 나타내어 염증성 사이토카인의 발현을 저해하였고, 피부 구성 단백질의 분해를 유도하는 matrix metalloproteinase-1 (MMP-1)의 발현을 저해하였으며, 세포 사멸 인자의 수준을 저해하였다. 이 결과를 종합해 볼 때, 본 연구의 트리펩타이드는 미세먼지에 의한 인간각질형성세포의 사멸 및 주변 피부 조직의 손상을 유도할 수 있는 기전들을 억제하여 보호 효과를 나타내는 것으로 보인다. 트리펩타이드의 이러한 안티폴루션 효과는 신규 기능성 화장품 소재로 응용될 수 있을 것으로 기대된다.