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

검색결과 306건 처리시간 0.025초

약용곤충 무당벌레류 추출물의 항산화활성과 Cyclooxygenase-2 Promoter 억제활성 비교 (Comparison of In Vitro Antioxidant Activity and Cyclooxygenase-2 Promoter Inhibitory Activity in Harmonia axyridis Pallas and Coccinella septempunctata $Linn\dot{e}$)

  • 허진철;박자영;황재삼;박해철;강석우;황석조;윤치영;권택규;이상한
    • 한국식품저장유통학회지
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    • 제13권4호
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    • pp.513-518
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    • 2006
  • 최근 곤충자원은 약용 및 식용으로 활용하려고 많은 연구가 되고 있으며 미래의 자원으로 발전할 수 있는 가능성은 충분하다. 본 연구는 곤충자원 중 칠성무당벌레와 무당벌레를 이용하여 생물학적 활성과 함께 약용 및 식용으로의 활용가능성을 알아보고자 하였다. 생물학적 활성을 알아보기 위하여 이들 추출물을 이용하여 항산화관련 실험인 DPPH, FRAP, linoleic acid 산화 억제실험을 하였으며, 분자 염증에 관련된 유전자인 Cyclooxygenase-2(Cox-2)의 promoter의 유전자 발현의 억제 유무를 알아보았다. 항산화 효과에 있어서는 무당벌레의 DW추출물에서 높은 활성을 나타내었으며, Cox-2의 promoter 활성을 조사한 결과 DW 추출물에서 Cox-2의 promoter 활성을 약 25% 정도 억제하는 무당벌레의 DW추출물을 발견하였는데 추출물의 산업적인 활용가능성을 확인하기 위하여 보다 많은 연구가 필요하다.

석곡(石斛), 석류(石榴)의 항산화, 항염증, 주름, 미백에 미치는 영향 (Effects of Dendrobii herba and Punica granatum Extract on the Anti-oxidant, Anti-inflammatory, Anti-wrinkle and Whitening)

  • 황보민;노석선;서형식
    • 한방안이비인후피부과학회지
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    • 제23권3호
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    • pp.11-32
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    • 2010
  • Objective : The aim of this study is to determine the effects of Dendrobii herba extract and Punica granatum extract on skin disease and skin beauty. Methods : To investigate in vitro anti-oxidant activity assay, ethanol extracts of medicinal plants tested by DPPH radical, xanthine oxidase activity. In the next experiment, to investigate anti-inflammatory activity assay, examined by relations in NO synthesis, IL-$1{\beta}$, IL-6, TNF-${\alpha}$, NF-${\kappa}B$, COX-2, MAP kinase. To study Skin wrinkle formation effect, we were examined by tyrosinase activities, melanin synthesis in MNT-1 cell. Results : 1. In an anti-oxidant test, Dendrobii and Punica granatum extract showed high radical scavenging activity. 2. In an anti-inflammatory test, Dendrobii herba and Punica granatum extract weakly inhibited the lipopolysaccharide(LPS)-induced nitric oxide(NO) release from RAW 246.7 macrophage cells. Dendrobii herba and Punica granatum extract also inhibited LPS-induced IL-$1{\beta}$ and COX-2 expressions. The inhibitory effect of Dendrobii herba and Punica granatum extract on macrophage activation were via the inhibition of NF-${\kappa}B$, evidenced by transient transfection assay. however, Dendrobii herba and Punica granatum extract did not have any effects about activation of Jun-N-terminal kinase(JNK) and inhibition of p38 MAP kinase in RAW 264.7 cells. 3. In the skin wrinkle formation assay, Dendrobii herba and Punica granatum extract weakly inhibited collagenase and elastase, however it was not statistically significant. 4. In the skin whitening assay, Dendrobii herba and Punica granatum extract weakly inhibited tyrosinase activity, however, it was not statistically significant. They did not have any effect on melanin synthesis, indicating that they could not be applicable for skin whitening. Conclusion : Dendrobii herba extract and Punica granatum extract may play a significant role in skin disease and skin beauty.

Acemannan과 aloesin의 혼합 비율에 따른 대식세포에서의 항염증 효과 (Anti-inflammatory effect in macrophages according to the mixing ratio of acemannan and aloesin)

  • 김효민;김정환;유단희;전세영;김현진;도선길;이인철;강정욱
    • 한국식품저장유통학회지
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    • 제31권2호
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    • pp.315-323
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    • 2024
  • 현재 항염증 활성에 대한 효능이 검증된 acemannan과 aloesin을 다양한 비율로 혼합하여 비율에 따른 항염증 효능을 확인하고자 본 연구를 진행하였다. 항염증 활성은 NO, PGE2, TNF-α 및 IL-6 생성량 및 염증 관련 단백질인 iNOS, COX-2의 발현량에 대한 효능을 검증하였다. Acemannan과 aloesin 각각의 NO 생성 저해 활성 결과와 혼합 시료인 AA-1, AA-2, AA-3, AA-4, AA-5의 NO 생성 저해 활성 결과를 비교하였을 때, 혼합 시료가 더 우수한 NO 생성 저해 활성을 나타내는 것을 확인하였다. 이후 최적의 배합 비율을 찾기 위해 PGE2, TNF-α 및 IL-6 생성량에 대해 측정하였다. 그 결과, 시료 5종 모두 최종농도인 100 ㎍/mL 농도에서 LPS 단독 처리군 대비 저해 효과가 나타났으며, 이 중 AA-2의 저해 효과가 가장 높은 것을 확인하여 western blot을 통한 염증 관련 단백질 발현량은 AA-2를 이용하여 실험을 진행하였다. 염증 관련 단백질인 iNOS 및 COX-2의 발현량을 측정 결과, AA-2는 농도 의존적으로 감소하였으며, 최종 농도인 100 ㎍/mL 농도에서 LPS 단독 처리군 대비 각각 25% 이상의 억제 효과가 나타나는 것을 확인하였다. 이러한 결과들을 토대로 acemannan과 aloesin을 다양한 비율로 배합하였을 때, 항염증 활성을 가진 것을 확인하였으며, 이 중 acemannan과 aloesin이 1:2의 비율로 혼합되었을 때 가장 높은 항염증 활성을 나타내었다. 결론적으로 acemannan과 aloesin을 혼합한 시료는 다양한 기능성 소재로써 활용이 가능하며, 이후 항염증 활성 실험들의 기초자료로도 활용이 가능한 것을 확인하였다.

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.

Molecular Mechanisms of Cell Cycle Arrest and Apoptosis by Dideoxypetrosynol A, a Polyacetylene from the Sponge Petrosia sp., in Human Monocytic Leukemia Cells

  • Choi, Yung Hyun
    • 한국해양바이오학회지
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    • 제1권4호
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    • pp.243-251
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    • 2006
  • Dideoxypetrosynol A, a polyacetylene from the marine sponge Petrosia sp., is known to exhibit significant selective cytotoxic activity against a small panel of human tumor cell lines, however, the mechanisms of which are poorly understood. In the present study, it was investigated the further possible mechanisms by which dideoxytetrosynol A exerts its anti-proliferative action in cultured human leukemia cell line U937. We observed that the proliferation-inhibitory effect of dideoxypetrosynol A was due to the induction of G1 arrest of the cell cycle and apoptosis, which effects were associated with up-regulation of cyclin D1 and down-regulation of cyclin E without any change in cyclin-dependent-kinases (Cdks) expression. Dideoxypetrosynol A markedly induced the levels of Cdk inhibitor p16/INK4a expression. Furthermore, down-regulation of phosphorylation of retinoblastoma protein (pRB) by this compound was associated with enhanced binding of pRB and the transcription factor E2F-1. The increase in apoptosis was associated with a dose-dependent up-regulation in pro-apoptotic Bax expression and activation of caspase-3 and caspase-9. Dideoxytetrosynol A decreased the levels of cyclooxygenase (COX)-2 mRNA and protein expression without significant changes in the levels of COX-1, which was correlated with a decrease in prostaglandin E2 (PGE2) synthesis. Furthermore, dideoxytetrosynol A treatment markedly inhibited the activity of telomerase, and the expression of human telomerase reverse transcriptase (hTERT), a main determinant of the telomerase enzymatic activity, was progressively down-regulated by dideoxytetrosynol A treatment in a dose-dependent fashion. Taken together, these findings provide important new insights into the possible molecular mechanisms of the anti-cancer activity of dideoxytetrosynol A.

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감귤류 과피 추출물의 항염증 효과 (Anti-Inflammatory Effect of Peel Extracts from Citrus Fruits)

  • 이숙현;서석종;이경혜;양종범;최성업;박성수
    • 한국식품위생안전성학회지
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    • 제28권4호
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    • pp.342-348
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    • 2013
  • 본 연구에서는 감귤류 중 온주밀감, 레몬, 한라봉의 과피추출물(PE)에 대한 항염증 효과를 조사하였다. 감귤류 세품종 과피추출물(PE)에 대한 murine macrophage cell line Raw 264.7세포를 배양하여 세포독성, NO생성량, 세포내 염증관련 단백질 발현 양상을 분석하였다. 그 결과 CUP, CHP, CLP 처리구의 경우 2 mg/mL 이하의 농도에서는 세포생육을 저해하지 않았다. LPS (100 ng/mL)를 처리한 세포의 NO생성량을 LPS를 처리하지 않은 대조구와 비교했을 때 상당량이 증가했음을 알 수 있었고, 추출물을 농도별로 처리했을 때 농도가 증가할수록 NO생성량은 감소하였다. 각 처리구에서 각 1 mg/mL 농도에서는 CUP > CHP > CLP 순으로 NO 저해활성이 강하게 나타났다. Western blot의 결과상으로는 CUP와 CHP의 iNOS 단백질 저해활성이 비슷한 강도로 나타남을 확인하였다. COX-2 효소의 저해활성은 CUP > CHP > CLP의 순으로 나타났다. 따라서 CUP, CHP, CLP 처리구는 모두 항염증 작용을 가지고 있으며, 또한 CUP 처리구가 세 개의 추출물 중에서 가장 저해활성이 강하였다.

Inhibitory Effect of Carnosol on Phthalic Anhydride-Induced Atopic Dermatitis via Inhibition of STAT3

  • Lee, Do Yeon;Hwang, Chul Ju;Choi, Ji Yeon;Park, Mi Hee;Song, Min Ji;Oh, Ki Wan;Son, Dong Ju;Lee, Seung Hwa;Han, Sang Bae;Hong, Jin Tae
    • Biomolecules & Therapeutics
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    • 제25권5호
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    • pp.535-544
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    • 2017
  • Carnosol is a phenolic antioxidant present in rosemary (Rosmarinus officinalis). It is known for anti-inflammatory effects, analgesic activity and anti-cancer effects. However, no study has been dedicated yet to its effect on atopic dermatitis (AD). Here, we show that carnosol effectively inhibited LPS-induced nitric oxide (NO) generation and expression of inflammatory marker proteins (iNOS and COX-2) in RAW 264.7 cells. In addition, carnosol effectively inhibits the phosphorylation of STAT3 and DNA binding activity in RAW 264.7 cells. Pull down assay and docking model analysis showed that carnosol directly binds to the DNA binding domain (DBD) of STAT3. We next examined the anti-atopic activity of carnosol ($0.05{\mu}g/cm^2$) using 5% Phthalic anhydride (PA)-induced AD model in HR1 mice. Carnosol treatment significantly reduced 5% PA-induced AD like skin inflammation in skin tissues compared with control mice. Moreover, carnosol treatment inhibits the expression of iNOS and COX-2 in skin tissue. In addition, the levels of $TNF-{\alpha}$, $IL-1{\beta}$, and Immunoglobulin-E in blood serum was significantly decreased in carnosol treated mice compared with those of 5% PA treated group. Furthermore, the activation of STAT3 in skin tissue was decreased in carnosol treated mice compared with control mice. In conclusion, these findings suggest that carnosol exhibited a potential anti-AD activity by inhibiting pro-inflammatory mediators through suppression of STAT3 activation via direct binding to DBD of STAT3.

노회(蘆薈)(알로에), 자화지정(紫花地丁)의 항산화, 항염증, 주름, 미백에 미치는 영향 (Effects of Aloe and Violae herba Extract on the Anti-oxidant, Anti-inflammatory, Anti-wrinkle and Whitening)

  • 김창훈;정현아;노석선;홍석훈
    • 한방안이비인후피부과학회지
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    • 제23권1호
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    • pp.23-43
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    • 2010
  • Objective : This study was performed to assess the effects of Aloe and Violae herba extracts on skin disease and skin beauty. Methods : Anti-oxidant effects were measured by the scavenging for DPPH radical, xanthine oxidase activity. Anti-inflammatory effects were examined by relations in NO synthesis, IL-$1{\beta}$, IL-6, TNF-$\alpha$, NF-kB, COX-2, MAP kinase. The skin wrinkle formation effects were measured by collagenase and elastase activities. The whitening effects were examined by tyrosinase activities, melanin synthesis in MNT-1 cell. Results : 1. In an anti-oxidant test, Aloe and Violae herba extracts showed high radical scavenging activity. 2. In an anti-inflammatory test, Aloe and Violae herba extracts strongly inhibited the lipopolysaccharide(LPS)-induced nitric oxide(NO) release from the RAW 246.7 macrophage cells. Aloe and Violae herba extracts also inhibited the LPS-induced IL-$1{\beta}$ and COX-2 expressions. The inhibitory effects of Aloe and Violae herba extracts on macrophage activation were via the inhibition of NF-kB, evidenced by transient transfection assay. Furthermore, Aloe and Violae herba extracts weakly inhibited the activation of Jun-N-terminal kinase(JNK) but they did not have any effects on p38 MAP kinase in RAW 264.7 cells. 3. In the skin wrinkle formation assay, Aloe extract strongly inhibited collagenase and elastase, whose activity are tightly related with the wrinkle formation. 4. In the skin whitening assay, Aloe and Viloae herba extracts weakly inhibited tyrosinase activity, however, it was not statistically significant. Besides they did not have any effects on melanin synthesis, indicating that they could not be applicable for skin whitening. Conclusion : This study show that Aloe and Violae herba extracts may play a significant role in skin disease and skin beauty.

쥐 대식세포에 대한 고추나무(Staphylea bumalda) 잎의 항염증 효과 검증 (Anti-inflammatory Effects of Staphylea bumalda Leaves Extracts in Murine Macrophages)

  • 김정화;이재권
    • 약학회지
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    • 제59권6호
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    • pp.251-258
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    • 2015
  • Aim of the present study was to investigate whether methanol extract from the leaves of Staphylea bumalda could be used to suppress lipopolysaccharide (LPS)-induced inflammatory responses in murine macrophage cell lines, Raw 264.7 cells. The extract reduced nitric oxide (NO), cyclooxigenase-2 (COX-2) and pro-inflammatory cytokines production from LPS-stimulated Raw 264.7 cells. These inhibitory effects were associated with decreases in the phosphorylation of MAP kinases and the activity of $NF{\kappa}B$ signal pathways. Our results indicate that Staphylea bumalda significantly inhibits the inflammatory activity of activated macrophages, suggesting that Staphylea bumalda could be a potential candidate for the treatment of inflammatory disease.

Inhibitory effect of benzoxathiol LYR-71 compound on inflammatory enzymes and cytokines

  • Kim, Min-Hee;Lee, Yong-Rok;Min, Kyung-Rak;Kim, Young-Soo
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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    • pp.146.2-147
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    • 2003
  • The benzoxathiol LYR-71 compound was discovered as an inhibitor of NF-kB transcriptional activity with an IC50 value of 5.4 uM. Furthermore, benzoxathiol LYR-71 compound inhibited the NF-kB binding activity to DNA in a dose-dependent manner, which was identified by EMSA with oligonucleotide corresponding to NF-kB consensus sequence. It is well known that NF-kB is an important transcription factor to regulate the expression of inflammatory enzymes (iNOS and COX-2) and cytokines (TNF, IL-1 and IL-6). (omitted)

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