• Archives of Pharmacal Research
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• v.26 no.11
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• pp.887-891
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• 2003

Novel trans-2,2-dimethylcyclopropyl nucleosides were synthesized as potential antiviral agents. The key intermediate, 3, was synthesized via five steps from ethyl chrysanthemate and condensed with purine bases using the Mitsunobu reaction to give six cyclopropyl nucleosides. These synthesized nucleosides did not show any significant antiviral activity against HSV-1, HSV-2, EMCV, Cox B3, or VSV, at concentrations up to 100 $\mu M$.

• Journal of Life Science
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• v.16 no.1
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• pp.17-21
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• 2006

The effects of Korean and Japanese radishes on inflammatory reaction that involves arachidonic acid cascades were investigated in human epithelial gastric cell. The activities of type I (porcine pancreas) and type II (Crotalus atrox) phospholipase $A_2(PLA_2$) were inhibited by radish. Cyclooxygenase-2 (COX-2) activity was significantly suppressed by radish (p<0.05, p<0.01 and p<0.005). The nitric oxide production was also inhibited by radish. The Korean radish was more effective in inhibition of $PLA_2$ and COX-2 activities and nitric oxide production than Japanease radish. These results indicate that radish has a protective effect on gastric epithelial cell inflammation by suppressing the activities of $PLA_2$ and COX-2 activities and nitric oxide production from gastric epithelial cell.

• Advances in Traditional Medicine
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• v.9 no.1
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• pp.74-82
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• 2009

Pharmacological investigations were carried out with aqueous methanolic extract (AME) of Swietenia mahagoni (L.) Jacq. (Meliaceae) leaves. Acute toxicity studies revealed that the $LD_{50}$ dose of AME was 600 mg/kg, i.p. AME was found to possess significant anti-inflammatory activity in acute, sub-chronic and chronic models of inflammation. AME selectively inhibited cyclooxygenase (COX)-2 activity, which is involved in arachidonic acid metabolism and biosynthesis of prostaglandins under inflammatory conditions. Treatment with AME significantly enhanced total peritoneal cell count and the number of macrophages in normal mice, which revealed that AME may also alter the immune response along with its anti-inflammatory effect. The saponins or the alkaloids present in AME may be responsible for the anti-inflammatory activity.

• The Korea Journal of Herbology
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• v.25 no.3
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• pp.19-25
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• 2010

Objective : The aim of this study was to investigate anti-inflammatory activity of SD-01 methanol extract in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. Methods : Cytotoxic activity of SD-01 methanol extract on RAW 264.7 cells was measured using 5-(3-caroboxymeth-oxyphenyl)-2H-tetra-zolium inner salt (MTS) assay. The nitric oxide (NO) production was measured by Griess reagent system. And proinflammatory cytokines and $PGE_2$ were measured by ELISA method. The levels of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), $I{\kappa}$-B-alpha and nuclear NF-${\kappa}$ B p65 expression were detected by western blot. Results : Our results indicated that methanol extract of SD-01 significantly inhibited the LPS-induced NO, $PGE_2$ production and iNOS, COX-2 expression accompanied by an attenuation of TNF-$\alpha$, IL-$1\beta$, IL-6 and MCP-1 production in RAW 264.7 cells. Moreover, methanol extract of SD-01 treatment also blocked LPS-induced NF-kB activation. Conclusion : These findings indicate that methanol extract of SD-01 inhibits the production of pro-inflammatory mediators and cytokines via suppression of NF-${\kappa}$ B activation. Take together, these results indicate that methanol extract of SD-01 has the potential for use as an agent of anti-chronic inflammatory diseases.

• Preventive Nutrition and Food Science
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• v.22 no.1
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• pp.50-55
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• 2017

Raphanus sativus L. (RS) is a cruciferous vegetable that is widely consumed in Korea. The anticancer activity of leaves of RS (RSL) extract has been investigated; however, no studies focused on its anti-inflammatory effects. Therefore, the aim of the current study was to evaluate the anti-inflammatory effects of RSL extract. In brief, RSL powder was fractionated into n-hexane, chloroform, ethyl acetate, n-butanol, and water-soluble fractions. Lipopolysaccharide (LPS)-stimulated RAW264.7 cells were treated with each fraction for initial screening. It was found that the chloroform fraction significantly inhibited nitric oxide release in LPS-stimulated RAW264.7 cells with a half maximal inhibitory concentration value of $196{\mu}g/mL$. In addition, the mRNA and protein expression levels of inducible nitric oxide synthase, measured using reverse transcriptase-polymerase chain reaction and western blotting, respectively, were reduced in a concentration-dependent manner. Moreover, the inflammatory cyclooxygenase-2 enzyme expression decreased. Furthermore, the expression of nuclear factor-kappa B ($NF-{\kappa}B$), the key regulator of the transcriptional activation of the inflammatory cytokine genes, was reduced by the RSL chloroform fraction. Therefore, the results of our study suggest that RSL exhibits anti-inflammatory effects in LPS-stimulated macrophages via $NF-{\kappa}B$ inactivation.

• The Korea Journal of Herbology
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• v.33 no.5
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• pp.73-79
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• 2018

Objectives : Coriandrum sativum is a medicinal herb that is used to enhance organoleptic quality and food flavor and as source of natural antioxidants. This research investigated the anti-inflammatory activity of Coriandrum sativum stem methanol extract (CSSE) using RAW 264.7 cells. Methods : Production of tumor necrosis factor-${\alpha}$(TNF-${\alpha}$), interleukin (IL)-$1{\beta}$, IL-6, and nitric oxide (NO) in the culture supernatant, protein expression of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), and nuclear factor-kappa B (NF-${\kappa}B$) in the extract were assayed. Results : Treatment with CSSE ($100{\mu}g/m{\ell}$) resulted in inhibited levels of protein expression of lipopolysaccharide- (LPS-) induced iNOS, COX-2, and NF-${\kappa}B$ as well as production of TNF-${\alpha}$, IL-$1{\beta}$, IL-6, and NO induced by LPS. Conclusions : These results demonstrate that CSSE exhibits anti-inflammatory activities via decreasing production of pro-inflammatory mediators through suppression of the pathways of NF-${\kappa}B$ in LPS-induced RAW 264.7 cells. Thus, CSSE may have therapeutic potential for a variety of inflammation-mediated diseases.

• Journal of Physiology & Pathology in Korean Medicine
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• v.20 no.1
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• pp.103-114
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• 2006

Herbal mixture water extract of (Chrysanthemum morifolium, Portulaca oleracea, Sanguisorba officinalis, Sophora flavescens, Phellodendron amurense, Cnidium monnieri) which exhibit several beneficial effects including acne and skin diseases, was tested for anti-microbial activity and anti-inflammation effects. The herbal mixture extract showed antimicrobial activity against Stapylococcus epidermis, and Propionibacterium acne. The growth of Stapylococcus epidermis, and Propionibacterium acne was inhibited completely by addition of 1.0% of the extract. Also in the present study we examined the mixture extract on compound 48/80 induced allergy and LPS induced cyclooxygenase-2(COX-2) gene expression in RAW 264.7 macrophage. The results indicated the ear swelling and histamine release induced by compound 48/80 were dose-dependently reduced, ranging 28-60%, and 48-72% , respectively. Furthermore the extract inhibited the expression of LPS-induced COX-2 proteins and mRNAs without an appreciable cytotoxic effects on RAW 264.7 cells. The LPS-induced cytokine gene expression including IL-$1{\beta}$, TNF-$\alpha$, and IL-6 were dose-dependently suppressed by the mixture extract. Based on these results, it is concluded that the herbal mixture water extract can be applied to the acne and skin diseases therapy.

• Korean Journal of Pharmacognosy
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• v.50 no.1
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• pp.32-36
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• 2019

Dendropanax morbifera Leveille, an endemic species in Korea, is best known as a tree that produces a resinous sap. Although D. morbifera is used in folk medicine for various diseases, its active ingredients are largely unknown. In this study, we investigated antioxidative activities of ethanolic extracts of three parts of this plant including leaves, debarked stems, and roots. The root extracts exhibited strong 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) scavenging activity compared with leaf or stem extracts. The root extracts showed hepatoprotective activity against t-butyl hydroperoxide-induced HepG2 cells, and reduced the ROS level in the cells. The root fractions lowered the mRNA level of COX-2 on lipopolysaccharide-stimulated Raw246.7 cells. These results suggest that ethanolic root extracts of D. morbifera are a source of antioxidant and hepatoprotective compounds, which indicate a potential for a botanical drug.

• IMMUNE NETWORK
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• v.3 no.1
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• pp.69-77
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• 2003

Background: Celecoxib, a COX-2 specific inhibitor, has recently been used for the treatment of rheumatoid arthritis. However, the molecular and cellular mechanisms of celecoxib against RA inflammation remain to be defined. To elucidate the action mechanism of celecoxib on inflammatory cells, we investigated the effect of celecoxib on the production of two important mediators of inflammation, nitric oxide and PGE2 Methods: RAW 264.7 cells stimulated with LPS were preincubated with various concentrations of celecoxib (from $10^{-8}$ to $10^{-5}$ M) and $10{\mu}M$ hydrocortisone, respectively. The production of NO and PGE2, the end products of iNOS and COX-2 genes, were estimated in culture supernatants by Greiss method and EIA, respectively. The expression of iNOS gene, COX-2 gene, $NF-{\kappa}B$, and $I-{\kappa}B$ were determined by RT-PCR and western blot analysis. Results: Celecoxib and hydrocortisone inhibited the production of NO and PGE2 in dose dependent manner, when RAW 264.7 cells were stimulated with LPS. The expression of iNOS was also down-regulated by celecoxib and hydrocortisone. Interestingly, COX-2 gene differentially expressed according to the dose of celecoxib, a decrease with lower dose ($10^{-8}$ M) but an increase with higher dose ($10^{-5}$ M). $NF-{\kappa}B$ binding activity was decreased by lower dose of celecoxib, whereas was not affected by higher dose of it. The expression of $I-{\kappa}B$ was suppressed by higher dose of celecoxib. Conclusion: The celecoxib strongly suppressed the production of NO and PGE2 in LPS-stimulated RAW264.7 cells. The decrease of NO seems to be linked to the inhibition of iNOS by celecoxib. The lower and higher dose of celecoxib differentially regulated the COX-2 expression and $NF-{\kappa}B$ activity.

• Journal of the Korean Society of Food Science and Nutrition
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• v.40 no.10
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• pp.1361-1370
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• 2011

Antioxidant and anti-inflammatory activities of eugenol and its derivatives from clove (Eugenia caryophyllata Thunb.) were evaluated using in vitro assay systems by measuring 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical, cyclooxygenase-2 (COX-2), and 15-lipoxygenase (15-LOX). Among eight different crude medicinal drugs tested, volatile extracts of clove extracted by steam distillation extraction (SDE) showed potent DPPH radical scavenging activity ($IC_{50}$=8.85 ${\mu}g/mL$) as well as strong inhibitory activity against COX-2 (58.15%) and 15-LOX (86.15%) at 10 ${\mu}g/mL$ and 25 ${\mu}g/mL$, respectively. Major volatile components of clove were identified as eugenol, trans-caryophyllene, and acetyleugenol by GC-MS analysis. Out of three eugenol derivatives, eugenol, methyl eugenol, and acetyl eugenol, eugenol showed the strongest DPPH radical scavenging activity and COX-2 inhibitory activity, whereas methyl eugenol exhibited the strongest 15-LOX inhibitory activity. Finally, the contents of the three eugenol derivatives in clove were quantified by analytical HPLC. Contents of eugenol and acetyl eugenol in clove were 6.95% and 1.85% per dry weight, respectively. These results suggest that eugenol and its derivatives in steam distilled extract of clove may be useful as potential antioxidant and anti-inflammatory agents.