• Bulletin of the Korean Chemical Society
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• v.33 no.8
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• pp.2585-2591
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• 2012

A series of heterocyclic chalcone derivatives bearing heterocycles such as thiophene or furan ring as an isostere of benzene ring were carefully prepared, and the influence of heterocycles on 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activities was systematically investigated. Structure-activity relationships (SAR) analysis showed that the activities of thiophene ring-containing chalcones were higher than those of furan ring-containing chalcones, and the presence of methyl substituent of heterocyclic ring distinctly affected the activities compared with non-substituted heterocycles in an opposite manner, with the 4'-methyl group of thiophene ring increasing activity and the 3'-methyl group of the furan ring decreasing activity. The distinct isosteric effect of heterocycles (i.e., thiophene or furan ring) on radical scavenging activities of heterocyclic chalones was distinctly demonstrated in our work.

• Korean Journal of Pharmacognosy
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• v.29 no.1
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• pp.28-34
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• 1998

It has been known that diseases related with aging or cancer result, at least in part, from free radicals, and antioxidants may reduce or prevent the abnormalities associated with free radical formation via its scavenging action. Thus, this study was carried out to investigate the antioxidative and antimicrobial activities of nut species for the purpose of developing antioxidant from natural products. Antioxidant activities of four kinds of nuts such as chestnut, groundnut, walnut and acorn were examined by measuring the radical scavenging effect on 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical. The extracts from chestnut hull and acorn barnyard millet showed strong antioxidative activities among 10 samples tested. Because of their highest antioxidative activity among 10 samples, radical scavenging effects of 4 different extract compartments (Hexane, EtOAc, BuOH and $H_2O$ extracts) from chestnut hull and acorn barnyard millet, were further examined by DPPH method. EtOAc and BuOH extracts exhibited antioxidative activities similar to those of natural, tocopherol or synthetic antioxidants, BHA. These findings demonstrates that major fraction of the antioxidative activity of chestnut hull or acorn barnyard millet was the EtOAc and BuOH extract compartments. However, antimicrobial activities against food-related bacteria and yeasts was relatively weak.

• Journal of Korean Medicine Rehabilitation
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• v.32 no.2
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• pp.1-17
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• 2022

Objectives This study was conducted to investigate the beta-glucan & ginsenoside content, antioxidant activity, anti-inflammatory effect and safety of herbal medicine mix. Methods The marker compounds contents, antioxidant activity and safety of herbal medicine mix were tested. The contents of beta-glucan and ginsenoside Rg3 were measured, the antioxidant activity was measured using 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging activity, anti-inflammatory and a safety test was conducted via single dose toxicity assessment. Results Analyzing the contents of marker compounds showed 362.3 mg/g of beta-glucan, and 0.4184 mg/g of ginsenoside Rg3. In the DPPH free radical scavenging activity, the IC50 of herbal medicine mix, was 0.146%. The scavenging activity of herbal medicine mix was 88.28% activity at 0.5% concentration, and 90.61% activity at 5% concentration. In the lipopolysaccharides (LPS) anti-inflammatory test, the herbal remix showed a significant decrease in tumor necrosis factor-alpha (TNF-𝛼) and interleukin-6 (IL-6) compared to the LPS-induced group. In the single dose toxicity test of herbal medicine mix, a dose of 2,000 mg/kg body weight (BW) was set at its highest capacity and observed after oral administration to female and male rats. No toxicological findings were recognized. It was observed that the resulting lethal dose can be set to 2,000 mg/kg BW or higher for both females and males. Conclusions The results of the experiment on herbal medicine mix showed that the marker compounds contents were beta-glucan and ginsenoside Rg3, that antioxidant activity was observed through the DPPH free radical scavenging activity, anti-inflammatory effect was observed through TNF-𝛼 and IL-6 measurement, and safety was confirmed through the single dose toxicity assessment.

• Herbal Formula Science
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• v.16 no.1
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• pp.117-130
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• 2008

Korean traditional medicine has been used for the treatment of the various diseases based on both oriental medicinal theory and clinical trials. Thus, the prescriptions of Korean traditional medicine would be useful for the development of new therapeutics. This research focuses on the fundamental study in Korean traditional prescriptions for the development of new hepatoprotective agents. We found two prescriptions. Injinho-Tang and Osumogwa-Tang, showed the significant DPPH free radical scavenging and hepatoprotective effect, respectively. It is well-known that free radical scavenging effect is related to the prevention of various pathological events including liver injury. This paper deals with hepatoprotective effects on tacrine-induced cytotoxicity in Hep G2 cells, free radicals scavenging on both DPPH and superoxide of above two prescriptions. Hot water extract of Injinho-Tang did not show the significant hepatoprotective effect on tacrine-induced cytotoxicity in Hep G2 cells, however, it shows the significant scavenging effects for both DPPH and superoxide radicals. On the other hand, all of the hot water extracts of constituent herbal drugs in Injinho-Tang exhibited the promising protective effect on tacrine-induced cytotoxicity in Hep G2 cells. Of these, water extract of Rhei Rhizoma showed the most prominent effect on tacrine-induced cytotoxicity in Hep G2 cells. Bioassay-guided fractionation of Rhei Rhizoma extract has furnished four compounds, and their chemical structures have been identified by comparison of their spectral data with those of literature as chrysophanol (1), emodin (2), 3,5-dihydroxy-4'- methoxystilbene (3), and rhapontigenin (4), respectively. Among the isolated compounds, compounds 2-4 revealed the significant hepatoprotective effect in vitro when their $EC_{50}$ values compare with that of silybin, as a positive control. It also exhibited that emodin possessed the most hepatoprotective effect among these active compounds. In case of Osumogwa-Tang, its hot water extract showed the moderate protective effect on tacrine-induced cytotoxicity in Hep G2 cells. Hot water extract of Chaenomelis Fructus, one of the constituent herbal drug of this prescription, exhibited the significant hepatoprotective effect with $EC_{50}$ value of $7.8{\pm}0.1\;{\mu}g/ml$, however, it showed strong cytotoxicity in Hep G2 cells above the concentration of $25\;{\mu}g/ml$. It was revealed that both hot water extract of Evodiae Fructus and its butanol soluble fraction showed the moderate hepatoprotective effect but concentration-dependent activity in Hep G2 assay system. Two quinolone alkaloids, evocarpine and dihydroevocarpine, also tested for their hepatoprotective effects on tacrine-induced cytotoxicity in Hep G2 cells, however, these two compounds derived from the Evodiae Fructus as the major constituents did not show in vitro hepatoprotective effect. From these results, it would be necessary to further isolation of its hepatoprotective compounds from the butanol soluble fraction of the hot water extract of Evodiae Fructus.

• The Journal of Korean Medicine
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• v.28 no.1 s.69
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• pp.148-158
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• 2007

Objective : The objective of this study was to investigate the antioxidant effects of Mori Folium extract. Methods Total antioxidant status was examined by total antioxidant capacity(TAC) and total antioxidant response(TAR) against potent free radical reactions. The effect of Mori Folium extract was examined by measuring total phenolic content, concentration at which 1,1-dipheny1-2-picrylhydrazyl(DPPH) radical scavenging activity was inhibited, inhibitory effect on lipid peroxidation, and the effect on reactive oxygen species(ROS) generation. Results : 1. TAC and TAR of Mori Folium extract at the concentration of 5 mg/ml were 1.61 and 1.24 mM Trolox equivalents, respectively. 2. Total phenolic content of Mori Folium extract at the concentration of 5 mg/Ml was 1.70 mM gallic acid equivalent. 3. Concentration of Mori Folium extract at which DPPH radical scavenging activity was inhibited by 50% was 2.29 m9/m4 as compared to 100% by Pyrogallol solution as a reference. 4. The inhibitory effect of the extract on lipid peroxidation was examined using rat liver mitochondria induced by FeSO$_4$/ascorbic acid. Mori Folium extract at the concentration of 10 mg/ml significantly decreased thiobarbituric acid reactive substances(TBARS) concentration. The extract prevented lipid peroxidation in a dose-dependent 5. The effect of Mori Folium extract on reactive oxygen species(ROS) generation was examined using a celt-free system induced by hydrogen peroxide FeSO$_4$. Addition of 1 mg/ml of Mori Folium extract significantly reduced dichlorofluorescein(DCf) fluorescence. The extract caused concentration-dependent attenuation of the increase in DCF fluorescence, indicating that the extract significantly prevented ROS generation in vitro. Conclusion ; The antioxidant effects of Mori Folium extract seem to be due, at least in part, to the prevention offree radical-induced oxidation, fllowed by inhibition of lipid peroxidation.

• Journal of Acupuncture Research
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• v.15 no.2
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• pp.135-145
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• 1998

Bupleury radix has been used for the treatment of fever, liver disease, inflammation in traditional medicine. The present study was carried out to evaluate the antioxidant effects of Bupleury radix aqua-acupuncture solution (BRAS) in vitro. Oxygen derived free radicals produced in the course of normal aerobic life, such as superoxide anion radical($O_2^-$ ), hydroxyl radicaI( OH), hydrogen peroxide($H_2O_2$) and singlet oxygen($^1O_2$) can attack polyunsaturated fatty acid in cell membranes, enzymes, other cell compounds, and give rise to lipid peroxidation, DNA damage, lipofuscin accumulation, structure alteration of cell membrane and cell death. In this study, antioxidant effects of BRAS on lipid peroxidation were determined according to the method of TBA. BRAS inhibited markedly peroxidation of linoleic acid during the autoxidation, and also inhibited lipid peroxidation induced by hydroxyl radical derived from $H_2O_2-Fe^{2+}$ in rat liver homogenate. And BRAS showed 30% scavenging effect on DPPH radical, also exhibited a 30% inhibitory effect on superoxide generation from xanthine-xanthine oxidase system. In addition, BRAS protected the cell death induced by tert-butyl hydroperoxide(t-BHP) and significantly increased cell viability in the normal rat liver cell(Ac2F).

• Proceedings of the Korean Society of Applied Pharmacology
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• 2003.11a
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• pp.61-61
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• 2003

The ethanol extract of peony root (Paeonia Lactiflora Pall, Paeoniaceae) and its major active components including gallic acid and methyl gallate were evaluated for their protective effects against free radical generation and lipid peroxidation. And protective effects against hydrogen peroxide-induced oxidative DNA damage in a mammalian cell line were performed. The ethanol extract of peony root (PRE), gallic acid and methyl gallate were shown to possess the significant free radical scavenging effect against 1,1-diphenyl-2-picryl hydrazine (DPPH) radical generation and were revealed the inhibitory effect of lipid peroxidation as expressed by malondialdehyde (MDA) formation. They were also found to strongly inhibit hydrogen peroxide-induced DNA damage from NIH/3T3 fibroblasts, assessed by single cell gel electrophoresis. Furthermore, oral administration of 50% PRE (50% ethanol extract), gallic acid and methyl gallate potently inhibited micronucleated reticulocyte (MNRET) formation of mouse peripheral blood induced by KBrO3 treatment in vivo. Therefore, PRE containing gallic acid and methyl gallate may be a useful natural antioxidant by scavenging free radicals, inhibition of lipid peroxidation and protecting oxidative DNA damage.

• YAKHAK HOEJI
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• v.45 no.3
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• pp.258-268
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• 2001

Garlic has been known to be effective against the gastrointestinal diseases which can be induced by production of oxygen-derived free radical. It has been shown that bamboo salt is effective on the treatment and prevention of various gastrointestinal disorders. Bamboo salt is a processed salt invented by a Korean, ll-Hoon Kim. It has been reported that garlic and bamboo-salt are useful to the treatment of gastric disorders in Korea. To clarify the protective mechanism of the garlic-bamboo salt mixture, the gas-tropathy was induced in rats with alcohol-salicylate and the activities of the free radical scavenging enzymes were examined. In this study, we found that the garlic-bamboo salt mixture reduced the severity of hemorrhagic lesion in gastric mucosa in the rats. In addition, the activities of superoxide dismutase (SOD), glutathione peroxidase (GPx), glutathione reductase (GR) were significnatly increased and the total content of GSH was recovered. From those results, we concluded that the protective effect of the garlic-bamboo salt mixture on gastropathy in rats is its ability to recover the level of GSH and to increase the activities of the free radical scavenging enzymes (SOD, GPx, GR).

• Journal of Pharmacopuncture
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• v.10 no.3
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• pp.53-62
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• 2007

Objective The objective of this study was to investigate the antioxidative effects of Puerariae Radix extract. Method Total antioxidant capacity (TAC), Total antioxidant response (TAR), Total phenolic content, Reactive oxygen species (ROS), 1,1-Diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activities, lipid peroxidation were examined. Result Total antioxidant status was examined by total antioxidant capacity(TAC) and total antioxidant response(TAR) against potent free radical reactions. TAC and TAR of Puerariae Radix extract at the concentration of 5 mg/ml were 2.02 and 1.50 mM Trolox equivalents, respectively. Total phenolic content of Puerariae Radix extract at the concentration of 5 mg/ml was 2.29 mM gallic acid equivalent. Concentration of Puerariae Radix extract at which DPPH radical scavenging activity was inhibited by 50% was 5.91 mg/ml as compared to 100% by pyrogallol solution as a reference. The inhibitory effect of the extract on lipid peroxidation was examined using rat liver mitochondria induced by FeSO4/ascorbic acid. Puerariae Radix extract at the concentration of 1 mg/ml slightly but significantly decreased TBARS concentration. The extract further prevented lipid peroxidation in a dose-dependent manner. The effect of Puerariae Radix extract on reactive oxygen species (ROS) generation was examined using cell-free system induced by hydrogen peroxide/FeSO4. Addition of 1 mg/ml of Puerariae Radix extract significantly reduced dichloroflurescein (DCF) fluorescence. The extract caused concentration-dependent attenuation of the increase in DCF fluorescence, indicating that the extract significantly prevented ROS generation in vitro. Thus antioxidant effects of Puerariae Radix extract seem to be due to, at least in part, the prevention from free radicals-induced oxidation, followed by inhibition of lipid peroxidation. Conclusion As a result, Puerariae Radix seems to have antioxitative effect and antioxidant compount.

• Journal of the Korean Society of Food Science and Nutrition
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• v.44 no.2
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• pp.281-286
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• 2015

In this study, free radical scavenging activities (ABTS, DPPH, NBT, TBARS, and ORAC) and anti-obesity potential were evaluated using 50% ethanol extract from fermented Curcuma longa L. (FCE50). FCE50 showed free radical scavenging activities and anti-oxidant potential. Lipid accumulation and intracellular TG content were significantly reduced by 25.8% and 28.6%, respectively, by $250{\mu}g/mL$ of FCE50 compared to adipocytes. Glucose uptake was significantly reduced by 12.0%. FCE50 significantly reduced mRNA expression of acetyl-CoA carboxylase in 3T3-L1 cells. These results indicate that the anti-adipogenic effect of FCE50 might be due to its radical scavenging activity and anti-oxidant potential.