• Advances in Traditional Medicine
• /
• 제10권1호
• /
• pp.37-43
• /
• 2010

Palmitic acid (PA) is one of free fatty acids, which is found from Gaultheria itoana Hayata and Sarcopyramis nepalensis. Although PA has a variety of pharmacological effects including mediates hypothalamic insulin resistance, induces IP-10 expression, and promote apoptotic activities, the anti-inflammatory mechanism of PA in mouse peritoneal macrophages remains unclear. In this study, we showed that PA exerted an anti-inflammatory action through suppression the production of tumor necrosis factor-$\alpha$, interleukin-6, cyclooxygenases-2 and nitric oxide in lipopolysaccaride-stimulated mouse peritoneal macrophages. Our study suggests an important molecular mechanism of PA, which might explain its beneficial effect in the regulation of inflammatory reactions.

• 대한약학회:학술대회논문집
• /
• 대한약학회 2000년도 NEW STRATEGY FOR DRUG DEVELOPMENT IN POST-GENOMIC ERA(대한약학회)
• /
• pp.191.2-191.2
• /
• 2000

• Biomolecules & Therapeutics
• /
• 제14권1호
• /
• pp.11-18
• /
• 2006

Certain flavonoids possess anti-inflammatory activity. Besides their antioxidative property, the cellular action mechanisms of flavonoids include an inhibition of arachidonate metabolizing enzymes such as cyclooxygenases and lipoxygenases, and a down-regulation of proinflammatory gene expression such as cyclooxygenase-2, inducible nitric oxide synthase and tumor necrosis factor-$\alpha$. In this review, the recent findings of anti-inflammatory flavonoid research since 2004 were summarized. And the cellular mechanisms on signal transduction pathways were also discussed.

• 약학회지
• /
• 제47권2호
• /
• pp.69-77
• /
• 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.

• Natural Product Sciences
• /
• 제18권4호
• /
• pp.211-214
• /
• 2012

Since 15-hydroxyprostaglandin dehydrogenase (15-PGDH) is the key metabolic enzyme of prostaglandin $E_2$ ($PGE_2$), inhibition of 15-PGDH is supposed to facilitate various physiological functions by increasing $PGE_2$. Methanol extract of Artemisia argyi (AAME) inhibited 15-PGDH ($IC_{50}$: $13.13{\mu}g/mL$) with relatively low cytotoxicity ($IC_{50}$: $415.00{\mu}g/mL$) and elevated extracellular $PGE_2$ levels in HaCaT cells. Real-time PCR analysis showed that AAME decreased significantly mRNA expression of PG transporter (PGT) in HaCaT cells. These results indicate that AAME could be applicable to functional materials as a 15-PGDH inhibitor and PGT expression inhibitor for the upregulation of extracellular $PGE_2$ level.

• 한국산학기술학회:학술대회논문집
• /
• 한국산학기술학회 2011년도 춘계학술논문집 2부
• /
• pp.1068-1071
• /
• 2011

Cyclooxygenases (COX)-2 has been highly expressed in a variety of tumor cells and involved inflammatory process, tumor-associated angiogenesis, and vascular functions but the underlying mechanism is not clearly elucidated. We here investigated the molecular mechanism by which COX-2 regulates tumor-associated angiogenesis. In vivo, we injected B16-F1 cells overexpressed with COX-2 or mock in wild type or eNOS-deficient mice. Tumor cells overexpressed with COX-2 increase tumor-associated angiogenesis and tumor growth compared with control cells and that the effect of COX-2 was lower in eNOS-deficient mice than wild type mice. These results may contribute to further understanding of the regulation of angiogenesis by COX during tumor metastasis and inflammation.

• 동의생리병리학회지
• /
• 제22권2호
• /
• pp.415-421
• /
• 2008

Pro-inflammatory mediators, such as prostaglandin $E_2$ (PGE2), nitric oxide (NO), and cyclooxygenases-2 (COX-2), play pivotal roles in normal as well as transformed cells. Previous studies have shown that Euphorbiae humifusae Wind exhibits anti-proliferative and antioxidant activities. However, the it's anti-inflammatory properties are unclear. In this study, we examine the effects of water extract of E. humifusae (WEEH) on the expression of COX-2 and the production of $PGE_2$ in human lymphatic U937 cells. Treatment of phorbol 12-myristate-13-acetate (PMA) significantly induced COX-2 expression and $PGE_2$ production in U937 cells. However, pretreatment WEEH markedly inhibited the PMA-induced COX-2 expression and $PGE_2$ production in a dose-dependent manner. Moreover, WEEH prevented the elevated early growth response gene-1 (Egr-1) expression and nuclear factor-kappaB ($NF{-\kappa}B\; p65$) nuclear translocation stimulated by PMA treatment. Taken together, the present data indicate that WEEH exhibits anti-inflammatory properties by suppressing the transcription of pro-inflammatory cytokine genes through the $NF{-\kappa}B$ and Egr-1 signaling pathway.

• 한국독성학회:학술대회논문집
• /
• 한국독성학회 2002년도 Current Trends in Toxicological Sciences
• /
• pp.95-95
• /
• 2002

Cyclooxygenases (COXs) are key enzymes in the conversion of arachidonic acid into prostanoids, which are involved in cell proliferation and inflammation. Two distinct COXS have been identified: COX-l which is constitutively expressed and COX-2 which is induced by different products such as tumor promoters or growth factors.(omitted)

• 대한화장품학회지
• /
• 제32권3호
• /
• pp.173-180
• /
• 2006

참깨(Sesamum indicum L.)는 1년생 초본식물로서 볶은 참깨나 참기름은 우리나라 식단에서 아주 중요한 조미용 양념 및 식용유지로서 이용되고 있다. 약효로는 동맥경화, 고혈압 및 노화 예방 등으로 알려져 왔으나, 참깨에 함유되어 있는 어떤 성분이, 이들 약효에 관여하고 있는지의 과학적인 규명이 미흡한 실정이다. 본 연구에서는 천연물 유래의 새로운 노화방지제를 개발하기 위해 참깨의 리그난 화합물(sesamin, sesamol, sesaminol, sesaminol diglucosides (SDG), sesaminol triglucosides (STG))의 항염증 활성을 검색하고, 그 중에서 항염증 효과가 가장 높게 나타난 sesamin을 전처치 방법과 동시처치 방법으로 NO 생성억제효과, 세포독성, inducible nitric oxide synthase (iNOS) 및 cyclooxygenases-2 (COX-2) 발현에 미치는 영향을 탐색하고 작용기작을 규명하고자 하였다. 리그난 화합물의 NO 생성억제효과를 탐색한 결과, sesamol, sesaminol, sesamin에서 NO 생성에 미치는 억제율이 높았으나, sesamol, sesaminol은 세포독성이 나타났다. 하지만 sesamin ($IC_{50}: 64{\mu}M$)은 세포독성은 없으면서 농도의존적으로 NO 생성을 억제시켰으며, iNOS 발현에서도 억제 효과를 보여주었다. 결론적으로 sesamin은 피부노화에 원인 중 하나이며 체내 염증반응의 중요 매개인자인 NO의 생성을 억제하는 항염증 물질로서 이와 같은 연구 결과는 향후 임상에서 항염증과 관련된 새로운 항노화 전략으로 개발하기 위해 기초자료로 응응될 수 있음을 시사한다.

• Biomolecules & Therapeutics
• /
• 제20권6호
• /
• pp.520-525
• /
• 2012

Prostaglandin (PG) $E_2$, the most abundant prostaglandin in the human body, is synthesized from arachidonic acid via the actions of cyclooxygenase (COX) enzymes. $PGE_2$ exerts homeostatic, cytoprotective, inflammatory, and in some cases anti-inflammatory effects. Also, it has been reported that $PGE_2$ is involved in hair growth. Diphlorethohydroxycarmalol (DPHC) is a phlorotannin compound isolated from the brown algae Ishige okamurae, with various biological activities in vitro and in vivo. In this study, the biological effect and mechanism of action of DPHC on prostaglandin synthesis in HaCaT human keratinocytes was examined. The results showed that, in these cells, DPHC significantly and dose-dependently induced $PGE_2$ synthesis by increasing the protein and mRNA levels of COX-1 and COX-2. Interestingly, DPHC-induced COX-1 expression preceded that of COX-2. Also, while both rofecoxib and indomethacin inhibited $PGE_2$ production, the latter was seems to be the more potent. From above results, we can expect that DPHC has some beneficial effects via increasing of $PGE_2$ production.