• Biomolecules & Therapeutics
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• 제24권4호
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• pp.418-425
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• 2016

We measured anti-nociceptive activity of prim-o-glucosylcimifugin (POG), a molecule from Saposhnikovia divaricate (Turcz) Schischk. Anti-nociceptive or anti-inflammatory effects of POG on a formalin-induced tonic nociceptive response and a complete Freund's adjuvant (CFA) inoculation-induced rat arthritis pain model were studied. Single subcutaneous injections of POG produced potent anti-nociception in both models that was comparable to indomethacin analgesia. Anti-nociceptive activity of POG was dose-dependent, maximally reducing pain 56.6% with an $ED_{50}$ of 1.6 mg. Rats given POG over time did not develop tolerance. POG also time-dependently reduced serum TNF${\alpha}$, IL-$1{\beta}$ and IL-6 in arthritic rats and both POG and indomethacin reduced spinal prostaglandin E2 ($PGE_2$). Like indomethacin which inhibits cyclooxygenase-2 (COX-2) activity, POG dose-dependently decreased spinal COX-2 content in arthritic rats. Additionally, POG, and its metabolite cimifugin, downregulated COX-2 expression in vitro. Thus, POG produced potent anti-nociception by downregulating spinal COX-2 expression.

• Natural Product Sciences
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• 제15권4호
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• pp.229-233
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• 2009

The essential oil fraction was obtained from the leaves and flowers of Artemisia iwayomogi (Compositae) by steam distillation, and its main component, vulgarone B, was isolated by column chromatography. RAW 264.7 cells were used to investigate the anti-inflammatory properties of A. iwayomogi and vulgarone B. Cell viability was determined by MTT assay after treatment with various dilutions of the compounds. In addition, several assays were used to determine the effects of A. iwayomogi essential oil components on immune stimulation. Nitric oxide production in cells activated with lipopolysaccharide (LPS) was evaluated by reaction with Griess reagent. Both vulgarone B and the essential oil fraction of A. iwayomogi inhibited the production of nitric oxide. The effects on various cytokines released from the cells were also measured using ELISA. The production of prostaglandin $E_2$ was significantly decreased by treatment with A. iwayomogi oils. LPS-induced IL-$1{\beta}$ and IL-6 production were also decreased in a dose-dependent manner, but no significant effect on TNF-${\alpha}$ was observed at the concentrations tested. Finally, Western blot analysis revealed that A. iwayomogi oils reduced the levels of COX-2 and iNOS.

• Asian-Australasian Journal of Animal Sciences
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• 제10권4호
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• pp.402-407
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• 1997

This study was conducted to investigate the effects of effects of enprostil, a prostaglandin $E_2$, analogue, on liver triacylglycerol content and factors that regulate liver lipid metabolism in mice. Mice received vehicle or $10{\mu}g$ enprostil/kg body weight intraperitoneally every 6 h, and were killed at 0, 6, 12, 18 and 24 h after the first injection. Enprostil significantly lowered liver triacylglycerol content after 12 h of the first injection. However, the peroxisomal ${\beta}$-oxidation activity was inconsistent with the result of liver triacylglycerol content, because its activity was lovered by enprosil. In another experiment, the effect of enprostil on lipid metabolism in mice was investigated in a short period. Mice received $10{\mu}g$ enprostil/kg body weight intraperitoneally, and were killed after 0, 5, 10, 30 and 60 min. After 30 min, malic enzyme activity was significantly increased by the administration of enprostil compared with the activity at 5 min after. No significant changes in liver carnitine palmitoyltransferase and peroxisomal ${\beta}$-oxidation activities were observed. Plasma free fatty acid concentrations were markedly reduced from 5 through 60 min after the administration of enprostil. Consequently, enprostil suppressive effect on liver triacylglycerol concentration might result from the decreased entry of free fatty acid into liver.

• 대한치과교정학회지
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• 제42권3호
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• pp.118-128
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• 2012

Objective: The aim of this study was to investigate and compare the in vivo effects of prostaglandin E2 (PGE2) administered by different methods on orthodontic tooth movement and bone metabolism macroscopically, histopatologically, and biochemically. Methods: Forty-five young adult New Zealand rabbits were randomly divided into 3 experimental groups (n = 10/group), 1 positive control group (n = 10), and 1 negative control group (n = 5). The experimental rabbits were fitted with springs exerting 20-g reciprocal force on the maxillary incisors and PGE2 (10 ${\mu}g/mL$) was administered by the intravenous, submucosal, or intra ligamentous route aft er appliance insertion and on days 1, 3, 7, and 14 thereafter. All rabbits were sacrificed on day 21 and their premaxillae were resected for histologic evaluation. Results: Tooth movement was observed in the experimental and positive control groups, but the intraligamentous PGE2 group had the highest values of all analyzed parameters, including serum calcium and phosphorus levels and osteoclastic and osteoblastic populations (p < 0.001). Conclusions: Sub mucosal and intraligamentous PGE2 administration significantly increases orthodontic tooth movement and bone metabolism, but the intraligamentous route seems to be more effective.

• Biomolecules & Therapeutics
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• 제9권3호
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• pp.188-193
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• 2001

Free radical scavengers or quenching agents for reactive oxygen species (ROS) present in consumable fruits, vegetables, and beverages have received considerable attention as potential antioxidants, and thus uses for treatment of several human diseases. In this study, grapevine shoot extract (GSE) containing high concentration of resveratrol and viniferine was evaluated for antioxidant potential and inhibition of pro-inflam-matory mediator production. Utilizing 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenging activity and xanthine oxidase (XOD) inhibition assay the GSE showed inhibitory effects of DPPH radical scavenging and XOD activity with the $IC_{50}$/ values of 34.5 and 155 $\mu\textrm{g}$/ml, respectively. In addition, GSE also exhibited the inhibition of prostaglandin E$_2$ (PGE$_2$) and nitric oxide (NO) production in lipopolysaccharide (LPS)-induced mouse macrophage RAW264.7 cells with the $IC_{50}$/ value of 6.4 and 14.5 $\mu\textrm{g}$/ml, respectively. This result suggests that grapevine shoot extract has the potential activity as a natural antioxidant or antiinflammatory agent.

• Biomolecules & Therapeutics
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• 제3권2호
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• pp.132-135
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• 1995

Several clofibrate congeners (bezafibrate, gemfibrozil and fenofibrate) were investigated the relationship between effects on the aggregation induced by aggregating agents (thrombin, arachidonic acid, ADP and collagen) and arachidonic acid metabolism in rabbit homogenized platelet. In platelet aggregation study, all drugs produced no significant inhibition (data not shown) in arachidonic acid and thrombin. Also platelet aggregation by ADP was not changed in bezafibrate and Inhibited dose dependently in fenofibrate and gemfibrozil. Platelet aggregation by collagen was inhibited dose dependently and significantly (from p<0.5 to p<0.001) by gemfibrozil and fenofibrate at concentrations between 20 and 400 $\mu$M. In arachidonic acid metabolism study, synthesis of thromboxane $B_2$ was not changed in rabbit platelet membranes and that of prostaglandin $E_2$ and $F_{2{\alpha}}$ was slightly increased by all drugs. It was concluded that clofibrate congeners inhibited ADP and collagen induced rabbit platelet aggregation and inhibition of collagen induced aggregation was probably mediated through some mechanism (pathway) other than arachidonic acid metabolism, judging from arachidonic acid metabolites (thromboxane $B_2$, prostaglandin $E_2$and $F_{ 2{\alpha}}$) synthesis in rabbit homogenized Platelet.

• 사상체질의학회지
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• 제3권1호
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• pp.151-172
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• 1991

Comparative blood analysis was carried out to investigate the change of blood constituent in TAE-EUM-IN group and control group. RBC, WBC, hemoglobin, hematocrit, total protein, triglyceride, phospholipid, total cholesterol, LDL-cholesterol, HDL-cholesterol, BUN, creatinine, ACTH, cortisol and prostaglandin E and $F_2{\alpha}$ were measured. And the following results were obtained: 1. In the change of blood cell, the value of hematocrit showed significant difference, while that of RBC, WBC and himoglobin didn't. 2. In the change of protein, the value of total protein showed significant difference, but that of albumin didn't. 3. In the change of lipid and cholesterol in serum, the value of triglyceride, phospholipid, total cholesterol and LDL-cholesterol indicated significant difference, while that of HDL-cholesterol indicated significant difference, while that of HDL-cholesterol didn't. 4. The value of BUN in serum represented significant difference, but that of creatinine didn't. 5. The value of cortisol in plasma showed significant difference, but that of ACTH didn't. 6. The value of prostaglandin E and $F_2{\alpha}$ in plasma showed significant difference. These results suggest that investigation on hormones and blood constituents enables objectification in differentiation of four types of physical constitution.

• Archives of Pharmacal Research
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• 제27권3호
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• pp.314-318
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• 2004

Microglia are the major inflammatory cells in the central nervous system and become activated in response to brain injuries such as ischemia, trauma, and neurodegenerative diseases including Alzheimer's disease (AD). Moreover, activated microglia are known to release a variety of proinflammatory cytokines and oxidants such as nitric oxide (NO). Minocycline is a semi-synthetic second-generation tetracycline that exerts anti-inflammatory effects that are completely distinct form its antimicrobial action. In this study, the inhibitory effects of minocycline on NO and prostaglandin E$_2$ (PGE$_2$) release was examined in lipopolysaccharides (LPS)-challenged BV2 murine microglial cells. Further, effects of minocycline on inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) expression levels were also determined. The results showed that minocycline significantly inhibited NO and PGE$_2$ production and iNOS and COX-2 expression in BV2 microglial cells. These findings suggest that minocycline should be evaluated as potential therapeutic agent for various pathological conditions due to the excessive activation of microglia.

• 한방안이비인후피부과학회지
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• 제29권4호
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• pp.24-33
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• 2016

Objectives : This study is to investigate the anti-inflammatory and anti-oxidant effects of Tongbi-san extract (TS) on RAW264.7 macrophages using by cell cytotoxicity, Nitric Oxide (NO) and Prostaglandin $E_2$ ($PGE_2$) production and 1,1-diphenyl-2-picryl ghdrazyl (DPPH) free radical scavenging capability. Methods : Cell cytotoxicity was measured by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The production of NO was measured by Griess assay. The production of $PGE_2$ was measured by immunoassay. And the anti-oxidant activity was measured by the DPPH method. Results : TS did not increased significantly compared to the TS untreated group in the cell cytotoxicity. TS inhibited NO and $PGE_2$ production in lipopolysaccharide-stimulated RAW 264.7 cells. TS had the DPPH free radical scavenging capability. Conclusion : The anti-inflammtory and anti-oxidant effects of TS may be use for a treatment of anti-inflammatory diseases.

• IMMUNE NETWORK
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• 제6권3호
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• pp.123-127
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• 2006

Background: Caveolin-1 is a principal component of caveolae membranes in vivo. Although expression of caveolae structure and expression of caveolin family, caveolin-1, -2 and -3, was known in chondrocytes, the functional role of caveolae and caveolins in chondrocytes remains unknown. In this study, we investigated the role of caveolin-1 in articular chondrocytes. Methods: Rabbit articular chondrocytes were prepared from cartilage slices of 2-week-old New Zealand white rabbits by enzymatic digestion. Caveolin-1 cDNA was transfected to articular chondrocytes using LipofectaminePLUS. The cyclooxygenase-2 (COX-2) expression levels were determined by immunoblot analysis, immunostaining, immunohistochemistry, and prostaglandin $E_2\;(PGE_2)$ assay was used to measure the COX-2 activity. Results: Ectopic expression of caveolin-1 induced COX-2 expression and activity, as indicated by immunoblot analysis and $PGE_2$ assay. And also, overexpression of caveolin-1 stimulated activation of p38 kinase and ERK-1/-2. Inhibition of p38 kinase and ERK-1/-2 with SB203580 and PD98059, respectively, led to a dose-dependent decrease COX-2 expression and $PGE_2$ production in caveolin-1-transfected cells. Conclusion: Taken together, our data suggest that ectopic expression of caveolin-1 contributes to the expression and activity of COX-2 in articular chondrocytes through MAP kinase pathway.