• Journal of Applied Biological Chemistry
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• v.60 no.3
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• pp.191-198
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• 2017

Hyaluronidase inhibitory activity as inflammatory factor of Koreinsis chinensis leaf ethanol extract was showed higher inhibitory activity than water extract. 29.5% inhibitory activity was shown at concentration of $200{\mu}g/mL$ phenolics. Lipopolysaccharide (LPS)-stimulated Raw 264.7 cells were treated with different concentrations ($5-25{\mu}g/mL$) of Koreinsis chinensis leaf extract and the amount of nitric oxide (NO) was determined; LPS-treated cells produced 3 times more NO than non-LPS treated cells. Moreover, the NO production in cells treated with Koreinsis chinensis leaf extract showed inhibitory effect in a concentration-dependent manner. Due to the stimulant-induced NO production is regulated by the inducible nitric oxide synthase (iNOS), we determined the iNOS protein level to elucidate the mechanism by which the NO production was inhibited. It was reduced by 40% with a Koreinsis chinensis leaf extract concentration of $25{\mu}g/mL$ and identified iNOS inhibition in dose-dependent manner. The prostaglandin $E_2$ production in cells treated with Koreinsis chinensis leaf extract was reduced by 26.2% at concentration of $25{\mu}g/mL$. The protein expression of cyclooxygenase-2 in LPS-treated Raw 264.7 cells was inhibited by 64% at $25{\mu}g/mL$ of Koreinsis chinensis leaf extract. Koreinsis chinensis leaf extract had a concentration-dependent inhibitory effect on the production of tumor necrosis factor-${\alpha}$ and interleukin-6 as pro-inflammatory cytokine in LPS-treated Raw 264.7 cells at $25{\mu}g/mL$ of Koreinsis chinensis leaf extract. Their levels were decreased by 61.7 and 62% respectively.

• Journal of Applied Biological Chemistry
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• v.60 no.3
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• pp.199-205
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• 2017

To investigate the anti-inflammatory activity of natural products, we determined the anti-inflammatory activity of purified epigallocatechin (EGC) from Camellia sinensis leaves. In the present study, we found that EGC inhibited the production of proinflammatory mediators (IL-6, TNF-${\alpha}$, NO, and $PGE_2$) in lipopolysaccharide (LPS)-stimulated Raw 264.7 cells. Suppression of IL-6 seems to be at least partly attributable to the inhibitory effect of EGC. TNF-${\alpha}$ is a major cytokine produced by LPS-induced macrophages, and they have a wide variety of biological functions including regulation of inflammation. The inhibition of IL-6 and TNF-${\alpha}$ production by EGC may downregulate the acute-phase response to LPS, thereby reducing LPS-induced inflammation. In addition to IL-6 and TNF-${\alpha}$, EGC effectively reduced the production of other key inflammatory mediators, including NO and $PGE_2$. The inhibitory effect of EGC on NO and $PGE_2$ production was supported by the suppression of inducible nitric oxide synthase and COX-2 at protein levels. These results support the traditional use of EGC in the alleviation of various inflammation-associated diseases and suggest that EGC might be useful in the development of new functional foods for inflammatory diseases.

• Natural Product Sciences
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• v.19 no.3
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• pp.201-205
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• 2013

Thirteen phenolic compounds, 1,4-dimethoxybenzene (1), 3,4-dihydroxybenzaldehyde (2), (2E)-3-(4-hydroxy-3,5-dimethoxyphenyl)acrylaldehyde (3), 3,7-dihydroxy-4H-chromen-4-one (4), 2,3-dihydroxy-1-(3,4-dihydroxyphenyl)propan-1-one (5), 4-hydroxy-3-methoxybenzoic acid (6), 4-hydroxy-3,5-dimethoxybenzoic acid (7), methyl 3,4-dihydroxybenzoate (8), 4-hydroxy-3,5-dimethoxybenzaldehyde (9), 3,4-dihydroxybenzoic acid (10), 3-hydroxy-1-(4-hydroxy-3-methoxyphenyl)propan-1-one (11), 2,4,6-trihydroxybenzaldehyde (12) and benzene-1,2,4-triol (13) were isolated from the heartwood of Caesalpinia sappan. Their anti-inflammatory activity was evaluated against LPS-induced NO production in macrophage RAW264.7 cells. Among them, compounds 3 and 8 showed strong inhibitory activities toward the LPS-induced NO production in macrophage RAW264.7 cells with $IC_{50}$ values of 14.5 and 21.5 ${\mu}M$, respectively.

• Bulletin of the Korean Chemical Society
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• v.34 no.8
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• pp.2317-2320
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• 2013

Thiourea and vinyl sulfoxide derivatives were designed based on the structures of sulforaphane and gallic acid, prepared and tested for HO-1 inducing activity as a measure of Nrf2 activation, and inhibitory effect on NO production as a measure of anti-inflammatory activity. Both series of compounds showed moderate activity on HO-1 induction, and no inhibitory effect on NO production. Interestingly the thiourea compound 6d showed better HO-1 induction (71% SFN) than the corresponding isothiocyanate compound 6a (55% SFN). Overall, it seemed that more efficient electrophile is needed to get more effective Nrf2 activator.

• Korean Journal of Pharmacognosy
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• v.36 no.3 s.142
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• pp.245-251
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• 2005

Phytochemical examination of the barks of Actinidia arguta led to the isolation of five flavonoids. Structures of compounds were elucidated as catechin (1), (-)-epicatechin (2), quercetin (3), $quercetin-3-O-{\beta}-D-glucopyranoside$ (4), $quercetin-3-O-{\beta}-D-galactopyranoside$ (5) by comparison with previously reported spectral evidences. To investigate the anti-oxidative effect and nitric oxide (NO) production inhibitory activity of these compounds, DPPH radical scavenging activity and nitric oxide production inhibitory activity in $IFN-{\gamma}$, LPS stimulated RAW 264.7 cell were examined. The $IC_{50}s$ were determinied as follows : $1\;$IC_{50}=26.61\;{\mu}g/ml$, $2\;IC_{50}=25.30\;{\mu}g/ml$, $3\;IC_{50}=20.41\;{\mu}g/ml$, $4\;IC_{50}=18.23\;{\mu}g/ml$ , $5\;IC_{50}=30.46\;{\mu}g/ml$, $6\;IC_{50}=28.0;{\mu}g/ml$, $7\;IC_{50}=27.24\;{\mu}/ml$. These NO production inhibitory effects were significantly different compared with the positive control, L-NMMA $(IC_{50}=20.77\;{\mu}g/ml)$, respectively. Compound $1\;(IC_{50}=6.19\;{\mu}g/ml)$, $2\;(IC_{50}=8.98\;{\mu}g/ml)$, $3\;(IC_{50}=7.30\;{\mu}g/ml)$ and $4\;(IC_{50}=7.64\;{\mu}g/ml)$ also showed potent antioxidative activities similar level to ascorbic acid $(IC_{50}=9.22\;{\mu}g/ml)$. These results suggest that barks of A. arguta have a potent anti-oxidative and anti-inflammatory activity.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.374.1-374.1
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• 2002

The barks o.f Pinus densiflara representative Pinus species graws in Korea, have been used for oriental traditional medicine as the remedies for rheumatitis. hemorrhage and cancer. Water soluble fraction of 80% acetone extracts from the barks af Pinus densiflera (PDB) showed nitrogen monoxide(NO) production inhibitory activity in IFN-${\gamma}$. LPS stimulated RAW 264.7 cell. (omitted)

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.194.2-194.2
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• 2003

The inhibitors of prostaglandin biosynthesis and nitric oxide production by corresponding inducible isozyme have been considered as potential anti-inflammatory and cancer chemopreventive agents. In our continuous search for cancer chemopreventive agents from natural products, we have evaluated the inhibitory potential of PGE$_2$ and NO production in lipopolysaccharide (LPS)-induced mouse macrophage RAW 264.7 cells. As a result, pinosylvin (3,5-dihydroxy-trans-stilbene), a stilbenoid, mainly found from the heartwood and leaves of the Pinus sylvestris, showed potential inhibitory activity of LPS-induced PGE$_2$ and NO production in a dose-dependent manner. (omitted)

• Archives of Pharmacal Research
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• v.27 no.12
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• pp.1220-1225
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• 2004

The overproduction of nitric oxide (NO) by inducible nitric oxide synthase (iNOS) is known to be responsible for vasodilation and hypotension observed in septic shock and inflammation. Inhibitors of iNOS, thus, may be useful candidates for the treatment of inflammatory diseases accompanied by overproduction of NO. In the course of screening oriental anti-inflammatory herbs for the inhibitory activity of NO synthesis, a crude methanolic extract of Curcuma zedoaria exhibited significant activity. The activity-guided fractionation and repetitive chromatographic procedures with the EtOAc soluble fraction allowed us to isolate three active compounds. They were identified as 1,7-bis (4-hydroxyphenyl)-1,4,6-heptatrien-3-one (1), procurcumenol (2) and epiprocurcumenol (3) by spectral data analyses. Their concentrations for the 50% inhibition of NO production $(IC_{50})$ in lipopolysaccharide (LPS)-activated macrophages were 8, 75, 77 ${\mu}M$, respectively. Compound 1 showed the most potent inhibitory activity for NO production in LPS-activated macrophages, while the epimeric isomers, compound 2 and 3 showed weak and similar potency. Inhibition of NO synthesis by compound 1 was very weak when activated macrophages were treated with 1 after iNOS induction. In the immunoblot analysis, compound 1 suppressed the expression of iNOS in a dose-dependent manner. In summary, 1,7-bis (4-hydroxyphenyl)-1,4,6-heptatrien-3-one from Curcuma zedoaria inhibited NO production in LPS-activated macrophages through suppression of iNOS expression. These results imply that the traditional use of C. zedoaria rhizome as anti-inflammatory drug may be explained at least in part, by inhibition of NO production.

• Journal of Applied Biological Chemistry
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• v.66
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• pp.227-235
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• 2023

The current study evaluated the presence and concentration of health-promoting phenolic antioxidants in sorghum seed accessions from seven regions in three different countries (Uzbekistan, Myanmar, and the United States). The free radical scavenging activity using the 2,2-diphenyl-1-picrylhydrazyl assay was 13.10±2.37 ㎍/mL in the Uzbekistan sorghum seed extracts, demonstrating the highest antioxidant activity. Additionally, the total phenol content was the highest in the Uzbekistan sorghum seed extracts [157.87±4.04 mg GAE/g (gallic acid equivalents per gram)]. The total flavonoid content was 12.69±0.72 mg QE/g (quercetin equivalents per gram) and represents the highest value in the Myanmar collection. The Uzbekistan collection demonstrated the greatest potential for whitening activity, with the tyrosinase inhibition rate of 79.20±4.15%. The wrinkle improvement function using elastase also showed the highest anti-aging activity of 55.85±4.78% in the same seed extract. The Uzbekistan seed extract had the highest NO production inhibitory activity of 144.35±4.55%. We conclude from these results that the Uzbekistan sorghum seed has excellent antioxidant activity, content of various functional ingredients, and anti-inflammatory activity.

• Korean Journal of Medicinal Crop Science
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• v.26 no.2
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• pp.119-126
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• 2018

Background: The flowering plant Hippophae rhamnoides L. has been used for many studies on fruit or leaf extracts. This study was conducted to investigate the development of a new cosmetic material from H. rhamnoides fruits and leaves that have by antioxidant, anti-inflammatory and wrinkle improvement activities. Methods and Results: The antioxidant abilities of H. rhamnoides extracts, including of a water-soluble fruit powder (FW), a fatsoluble fruit powder (FF), a supercritical extract of fruit by-product (BS), and a mixture of leaf and fruit (MIX), were investigated in vitro. A DPPH radical assay for antioxidant activity was performed for these fractions alongside assay to evaluate the total phenolic and flavonoid content (TPC and TFC). As expected, the MIX had the highest DPPH radical scavenging activity ($RC_{50}=10.27{\mu}g/m{\ell}$), and the TPC and TFC also were highest in MIX ($225.7mg{\cdot}GAE/g$, and $25.18mg{\cdot}QE/g$, respectively). Nitric oxide (NO) production in LPS-induced RAW264.7 cells was estimated and the results indicated an over 75% decrease of NO production in FF and MIX. In other assays, the highest elastase inhibitory activity was found in FW. Conclusions: These results revealed that H. rhamnoides extracts have a high potential for antioxidant, anti-inflammatory and antiwrinkle activities. H. rhamnoides products are suggested to be applied as the functional materials of cosmetic ingredients.