• The Journal of Korean Medicine
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• v.26 no.1 s.61
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• pp.37-45
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• 2005

In the present study, we examined the effect of crude methanolic extract (CME) from Euonymus alatus (Thunb.) Sieb on arachidonic acid (AA) cascade in SKBR3 human breast cancer cell line. CME had a potent inhibitory activity of prostaglandin E2 (PGE2) release induced by A23187, a $Ca^{2+}$ ionophore. The inhibition was concentration-dependent, with the 50 value of about 5 M. CME had no inhibitory effect on A23187-induced phosphorylation of p42/p44 extracellular signal regulated kinase/mitogen-activated protein kinase or on the liberation of [14C]-AA from the cells labeled with [14C]-AA. However, CME concentration-dependently inhibited the conversion of AA to $PGE_2$ in microsomal preparations, showing its possible inhibition of cyclooxygenase (COX). In enzyme assay in vitro, CME inhibited the activities of both constitutive COX (COX­I) and inducible COX (COX-2) in a concentration-dependent manner, with the 50 values of about 0.8 and 2M, respectively. Lineweaver-Burk plot analysis indicated that CME competitively inhibited the activities of both COX-l and -2. This study is a first demonstration that CME directly inhibits COX activity.

• Archives of Pharmacal Research
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• v.28 no.2
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• pp.203-208
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• 2005

Scoparone is a major component of the shoot of Artemisia capillaris (Compositae), which has been used for the treatment of hepatitis and biliary tract infection in oriental countries. In the present study we observed that, scorparone exhibited no cytotoxic effect in unstimulated macrophages, but reduced the release of nitric oxide (NO) and prostaglandin $E_2\;(PGE_2)$ upon stimulation by IFN-${\gamma}$/LPS or LPS. The inhibitory effects were found to be in conjuction with the suppression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in IFN-${\gamma}$/LPS stimulated RAW 264.7 cells. Moreover, scoparone also attenuated the production of tumor necrosis factor (TNF)-${\alpha}$, interleukin (IL)-$1{\beta}$ and IL-6 in LPS-stimulated RAW264.7 cells. These results suggest that scoparone decreases the production of the inflammatory mediators such as NO and $PGE_2$ in macrophages by inhibiting iNOS and COX-2 expression.

• Journal of Nutrition and Health
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• v.35 no.10
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• pp.1038-1044
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• 2002

The study was designed to observe the effect of conjugated linoleic acid (CLA) on tumor incidence, eicosanoid formation and antioxidant enzyme activities in colonic mucosa and the fecal excretion of deoxycholic acid and lithocholic acid in 1,2-dimethylhydrazine (DMH)-treated rats. One hundred twenty male Sprague Dawley rats were divided into 2 groups, BT (beef tallow diet) group and FO (fish oil diet) group, and each group was again subdivided into 2 groups depending on CLA supplementation, i.e.4 groups of BT, BTC, FO, FOC. All rats were fed experimental diet for 30 weeks, which contained 12% (wt/wt) total dietary fat including 1% (wt/wt) CLA, and were intramuscularly injected with DMH for 6 weeks to give total dose of 180 mg/kg body. CLA-supplemented to BT and FO diet reduced tumor incidence, eicosanoid (PGE$_2$ and TXA$_2$) level in colonic mucosa. N-3 fatty acids (mainly DHA) of fish oil diet (FO, FOC group) also reduced tumor incidence and significantly reduced eicosanoid (PGE$_2$ and TXA$_2$) level in colonic mucosa. CLA supplementation and n-3 fatty acid significantly increased colonic mucosal level of superoxide dismutase and glutathione peroxidase activities but reduced secondary bile acids (deoxycholic acid and lithocholic acid) excretion in the feces. In conclusion, CLA supplementation and n-3 fatty acid could reduce tumor incidence by reducing eicosanoids and increasing antioxidant enzyme activities in colon and decreasing the excretion of deoxycholic acid and lithocholic acid in the feces. The data might suggest that CLA supplementation and n-3 DHA rich fish oil may modulate colon carcinogenesis.termediate level of endurance exercise training for 6 weeks did not influence concentrations of most of free amino acid in soleus muscle of rats collected at an overnight fasted and rested state. In contrast, isolucine and leucine concentrations in extensor digitorum longus muscle of exercise-trained rats were significantly lower than those for control animals. These results indicate that aerobic energy metabolism had not been efficiently conducted, and thereby the utilization of BCAA for energy substrate was enhanced in fast twitch oxidative glycolytic fibers of extensor digitorum longus muscle of rats followed exercise-training protocol for 6 weeks.

• The Korea Journal of Herbology
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• v.37 no.6
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• pp.19-28
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• 2022

Objectives : To develop natural ingredients that help prevent or treat anti-inflammatory-related diseases and use themas basic data, we investigated anti-inflammatory activity of Cynanchi Atrati Radix Et Rhizoma water extracts(CWE) in lipopolysaccharide(LPS)-induced murine macrophage cell line, RAW 264.7 cells. Methods : The cell viabilities were evaluated with RAW 264.7 cells. The production of nitric oxide(NO), prostaglandin E2(PGE2), pro-inflammatory cytokines such tumor necrotic factor(TNF)-α and interleukin(IL)-6 were assessed in LPS-induced RAW 264.7 cell treated with CWE. Furthermore, the protein expression of inducible nitric oxide synthase (iNOS), cyclooxygenase-2(COX-2), and mitogen-activated protein kinase(MAPK) were assessed by western blotting. Results : In RAW 264.7 cell, the cell viability by CWE treatment was more than 98.4% at a concentration of 100-400 ㎍/mL. At a concentration of 800 ug/ml of CWE, the cell viability was as low as 86%. At doses of 100, 200 and 400 ㎍/mL, CWE inhibited the production of NO, PGE2, TNF-𝛼 and IL-6 in a dose-dependent manner and also decreased the expression of iNOS and COX-2 from LPS-induced RAW 264.7 cells. In addition, CWE significantly inhibited the MAPK pathway including decreased the phosphorylation of the p38, c-Jun N-terminal kinase(JNK) and extracellular signal-regulated kinase(ERK1/2). Conclusions : Our study provides evidence that CWE inhibits the production of main pro-inflammatory molecules in LPS-induced RAW 264.7 cells via expression of p38, JNK, and ERK1/2 MAPK signaling pathways. Therefore, CWE is expected to be widely used as a natural ingredient for anti-inflammatory functional foods or pharmaceuticals in the future.

• The Korea Journal of Herbology
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• v.24 no.2
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• pp.49-56
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• 2009

Objectives : Inflammation is important event in the development of vascular diseases including hypertension, atherosclerosis, and restenosis. Bodusan (BDS) was a traditional Korean herbal medicine and widely used in treatment of gastrointestinal complaint and stomach ulcer. The aim of this study was to determine whether BDS and its components inhibit production of nitrite, PGE2 and proinflammatory cytokines in lipopolysaccharide (LPS)-treated RAW 264.7 macrophages. Methods : Cytotoxic activity of BDS and its components on RAW 264.7 cells was using 5-(3caroboxymcrophages. eth-oxyphenyj)-2H-tetra-zolium inner salt (MTS) assay. The nitric oxide (NO) production was measured by Griess reagent system. And proinflammatory cytokines were measured by ELISA kit. The levels of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) expression were detected by western blot. Results : Our results indicated that BDS and its components significantly inhibited the LPS-induced NO and PGE2 production. Moreover. BDS and its components inhibited iNOS and COX-2 expression accompanied by an attenuation of TNF-${\alpha}$, IL-11${\beta}$, IL-6 and MCP-1 formation in macrophages. Conclusions: These results indicate that BDS and its components have potential as an anti-inflammatory agent.

• Proceedings of the Korean Magnestics Society Conference
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• 2007.05a
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• pp.284.2-284.2
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• 2007

• Biomolecules & Therapeutics
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• v.9 no.3
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• pp.176-182
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• 2001

Some pharmacological activities of acanthoic acid, isolated from Acanthopanax koreanum root was investigated in animals. It is revealed that the compound had analgesic and anti-inflammatory activities without actions on central nervous system and showed inhibition of lipid peroxidation. The anti-inflammatory activity might be related to inhibition of prostaglandin E$_2$ synthesis in exudates of inflammation.

• Proceedings of the PSK Conference
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• 2000.04a
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• pp.150.2-151
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• 2000

• Bulletin of the Korean Chemical Society
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• v.32 no.1
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• pp.299-302
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• 2011

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.245.1-245.1
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• 2003

As part of our research to discover novel synthetic flavonoids which can be applied to chronic inflammation diseases, many structurally modified flavone analogs have been synthesized to obtain information concerning the relationships between structures and the anti-inflammatory activities. We previously reported that 7-methoxyflavone analogs generally exhibited strong inhibitory activities against cyclooxygenase-2 catalyzed prostaglandin production. (omitted)