• Korean Journal of Food Science and Technology
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• v.43 no.2
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• pp.200-205
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• 2011

In this study, antioxidant and anti-inflammatory effects of ethanol extracts from medicinal herb mixtures were investigated in vitro. Contents of total polyphenols in ethanol extracts from Houttuynia cordata Thunb. (HC), Carthamus tinctorius L. (CT), and MIX-2 (Houttuynia cordata Thunb., Acanthopanax gracilistylus Smith, Carthamus tinctorius L., Kalopanax pictus) were 58.98, 60.79 and 57.74 mg/g respectively. Radical scavenging activities of the ethanol extracts were examined using ${\alpha},{\alpha}$-diphenyl-${\beta}$-picrylhydrazyl radicals and 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) assay. Anti-inflammatory effects of ethanol extracts from medicinal herbs composites were examined using 5-lipoxygenase (5-LO), cyclooxygenase-2 (COX-2) and nitric oxide (NO) inhibition assays. The ethanol extracts from medicinal herb mixtures showed higher 5-LO and COX-2 inhibition activities than those from single medicinal herbs. The ethanol extracts from medicinal herb mixtures also showed strong anti-inflammatory activity through inhibition of NO production.

• Journal of Life Science
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• v.19 no.10
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• pp.1396-1402
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• 2009

Hizikia fusiforme is a kind of edible brown seaweed that grows mainly in the northwest Pacific including Korea, Japan and China, and has been widely used as food in Korea. Induction of cyclooxygenase-2 (COX-2) expression and prostaglandin $E_2$ ($PGE_2$) production is thought to have beneficial immunomodulatory effects in acute and chronic inflammatory disorders. In this study, we investigated the effects of extracts of H. fusiforme on the expression of COX-2 and production of $PGE_2$ in U937 human pre-monocytic cell models. In U937 cells stimulated with phorbol 12-myristate 13-acetate (PMA) to mimic inflammation, methanol extract of H. fusiforme (MEHF) and ethanol extract of H. fusiforme (EEHF), but not water extract of H. fusiforme (WEHF), inhibited PMA-induced expression of both COX-2 protein and mRNA, which was associated with inhibition of $PGE_2$ production. To investigate the mechanism by which MEHF and EEHF inhibit COX-2 gene expression and $PGE_2$ production, we examined the activation of nuclear factor-kappaB (NF-$\kappa$B) in U937 cells. Pre-treatment with MEHF and EEHF significantly attenuated the PMA-induced IkappaB degradation and prevented nuclear translocation of NF-$\kappa$B. Taken together, these findings provide important new insights into the possible molecular mechanisms of the anti-inflammatory activity of H. fusiforme.

• Food Science and Biotechnology
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• v.15 no.2
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• pp.317-320
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• 2006

Octadeca-9,12-dienyl-3,4,5-hydroxybenzoate (GA-LA) was chemically synthesized from gallic acid and linoleic acid ester, and its biological functions were tested. Radical-scavenging activity of GA-LA was comparable to those of gallic and ascorbic acids at 0.24 mM, and tyrosinase inhibition effect was higher than that of ascorbic acid. Gallic and linoleic acids did not show any tyrosinase activity. Results of cyclooxygenase (COX) inhibition effect indicate GA-LA has higher selectivity in COX-1 inhibition. GA-LA from gallic and linoleic acids could be used as functional reagent for antioxidative, skin-whitening, and anti-inflammatory effects in food, pharmaceutrical, and cosmetic industries.

• Biomolecules & Therapeutics
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• v.5 no.1
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• pp.87-93
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• 1997

DA-5018, a new capsaicin derivative, showed potent analgesic effect comparable to that of morphine in various experimental acute pain models. in this study, whether the analgesic mechanism of DA-5018 is related to opiate receptors or prostanoids was investigated. The affinity of DA-5018 for opiate receptor was determined by receptor binding assay. The Ki values of DA-5018 for nonspecific and specific $\mu$, $textsc{k}$, $\delta$-opiate receptor was 299$\pm$8.88, 735$\pm$215, 2930$\pm$ 163, 1550$\pm$813 nM, respectively and DA-5018 exhibited lower affinity than morphine. DA-5018 (10-"~3$\times$10-′M) inhibited electrically-evoked contractions of the guinea ply ileum and rat vas deferens, and these inhibition was not antagonized by naloxone(10 nM), an opiate receptor antagonist. Antagonism of analgesic effect of 7A-5018 by naloxone was examined by tail pinch test. Analgesic action of DA-5018(0.1 ~2 mg/kg, 5.c.) was not antagonized by naloxone(1 mg/rg, i.p.). These results indicate that pharmacological action of DA-5018 is not related with opiate receptor. Cyclooxygenase and 5-lipoxygenase activities in rat peritoneal neutrophil treated with A23187 and arachidonic acid were measured by radioimmunoassay. DA-5018 stimulated the cyclooxygenase activity and the concentration show-ing the two fold increase of activity was 124$\mu$M. DA-5018 slightly inhibited 5-lipoxygenase activity and these results together indicate that analgesic action of 3A-5018 is not mediated through inhibition of cyclooxy genase or lipoxygenase. These results suggest that the analgesic effect of DA-5018 is not due to blocking opiate receptor or to inhibiting the synthesis of prostanoids in the arachidonic acid metabolism pathway.

• Journal of Life Science
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• v.18 no.4
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• pp.509-514
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• 2008

Tremendous natural product extracts were used as a herb medicine remedy or therapy for centuries. Because these extracts have various biological activities, we examined the effects of Gryllotalpa orientalis extract for anti-oxidant and anti-inflammation activity by 1,1-diphenyl-2-picrylhydrazyl (DPPH), ferric reducing ability of plasma (FRAP), hydroxy radical scarvenging and cyclooxygenase-2 promoter assays. Gryllotalpa orientalis extracts were prepared from solvents such as distilled water (DW), dimethyl sulfoxide (DMSO), ethanol and methanol. The results showed that Gryllotalpa orientalis extracts have potent DPPH (methanol extract), FRAP (DW extract) and hydroxy radical scavenging (DW and methanol extracts) activity than any other extracts used. A significant inhibition of cyclooxygenase-2 (Cox-2) promoter activity was detected in the presence of DMSO extract or ethanol extract. Collectively, the present results suggested that Gryllotalpa orientalis extract could be used for anti-oxidant and/or anti-inflammation agent for human or agricultural purposes.

• Journal of Applied Biological Chemistry
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• v.65 no.1
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• pp.23-31
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• 2022

Oxidative stress and neuroinflammation play important roles in the pathogenesis of Alzheimer's disease (AD). This study investigated the protective effects of paeoniflorin (PF) against neuronal oxidative stress and neuroinflammation in lipopolysaccharide (LPS)-induced mice. The brains of LPS-injected control group showed significantly increased neuroinflammation by activating the nuclear factor kappa B (NF-κB) pathway and increasing inflammatory mediators. However, administration of PF significantly attenuated oxidative stress by inhibiting lipid peroxidation, nitric oxide levels, and reactive oxygen species production in the brain; PF at doses of 5 and 10 mg/kg/day downregulated the expression of NF-κB pathway-related proteins and significantly decreased inflammatory mediators including inducible nitric oxide synthase and cyclooxygenase-2. Moreover, the levels of brain-derived neurotrophic factor and its receptor, tropomycin receptor kinase B, were significantly increased in PF-treated mice. Furthermore, acetylcholinesterase activity and the ration of B-cell lymphoma 2 (Bcl-2)/Bcl-2 associated X were significantly reduced by PF in the brains of LPS-induced mice, resulting in the inhibition of cholinergic dysfunction and neuronal apoptosis. Thus, we can conclude that administration of PF to mice prevents the development of LPS-induced AD pathology through the inhibition of neuronal oxidative stress and neuroinflammation, suggesting that PF has a therapeutic potential for AD.

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.202.4-203
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• 2003

The present study was carried out to clarify whether isoflavonoids isolated from Belamcandae Rhizoma (Iridaceae) inhibit inflammation and angiogenesis by the experimental methods in vitro and in vivo. Among the isolated isoflavonoids, such as irigenin, irisflorentine, and iristectorene B inhibited nitric oxide (NO) production, as measured by nitrite formation at 3-30 ${\mu}M$. Also these compounds reduced cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) enzyme expression in a concentration dependent manner, when measured by western blotting, at 3-30 ${\mu}M$. Irigenin, irisflorentine and iristectoren B decreased angiogenesis of chick embryos in the chorioallantoic membrane assay. These compounds also reduced the proliferation of calf pulmonary arterial endothelial (CPAE) cells and found to possess relatively weak gelatinase/collagenase inhibitory activity in vitro. These compounds, when administered subcataneously at the dose of 30mg/kg for 20 days to mice implanted with murine Lewis lung carcinoma (LLC), caused a significant inhibition of tumor volume. Therefore, antiangiogenic activities of isoflavonoids from Belamcandae Rhizoma might be due to antiproliferative activities under inhibition the induction of COX-2 and iNOS enzyme.

• Biomolecules & Therapeutics
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• v.27 no.4
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• pp.381-385
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• 2019

We attempted to examine anti-inflammatory and anti-oxidant effects of 4'-O-${\beta}$-D-glucosyl-5-O-methylvisamminol (GOMV), the first epigenetic inhibitor of histone phosphorylation at Ser10. While GOMV did not affect the viability of murine macrophage RAW 264.7 cells, it significantly suppressed lipopolysaccharide (LPS)-induced generation of prostaglandin $E_2$ ($PGE_2$) and nitric oxide (NO) through transcriptional inhibition of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS). GOMV also scavenged free radicals in vitro, increased NF-E2-related factor 2 (NRF2), and activated antioxidant response element (ARE), thereby resulting in the induction of phase II cytoprotective enzymes in human keratinocyte HaCaT cells. Finally, GOMV significantly protected HaCaT cells against 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced oxidative intracellular damages. Together, our results illustrate that GOMV possesses anti-inflammatory and anti-oxidant activity.

• Journal of Physiology & Pathology in Korean Medicine
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• v.24 no.2
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• pp.242-248
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• 2010

The present study was designed in order to determine whether Lonicerae flos (LF) could mitigate rheumatoid arthritis through inhibition of cyclooxygenase (COX)-2 and matrix metalloproteinase (MMP)-9 by regulation of macrophage migration inhibitory factor (MIF). We found that MIF mRNA expression in synoviocytes stimulated with phorbol-12-myristate-13-acetate dose-dependantly decreased by LF extract treatment (0.4 - 1.0 mg/$m{\ell}$). The distribution of MIF, COX-2 and MMP-9 positive reacted cells in LPS induced arthritis of mice were decreased by LF (45 mg/kg/day) treatment for 28 days. These data likely indicate that LF may act as MIF inhibitor and may be possible to develop useful agent for rheumatoid arthritis.

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.235.2-235.2
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• 2003

To decipher the structure-activity relationships of flavones for the inhibition of cyclooxygenase-2 catalyzed prostaglandin production, we synthesized 7-methxoyflavones, 7-hydroxyflavones, 5-methxoyflavones, 5-hydroxyflavones and flavones without any phenol group on A ring. Methoxyflavones were prepared from 2.6- and 2,4-dihydroxyacetophenones in 3 steps. Most of the methxoyflavones were converted to the corresponding hydroxyflavones by the reaction with BBr3 in good yields. (omitted)