• Biomolecules & Therapeutics
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• v.23 no.3
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• pp.275-282
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• 2015

In the present study, we synthesized a series of novel 7-methoxy-N-(substituted phenyl)benzofuran-2-carboxamide derivatives in moderate to good yields and evaluated their neuroprotective and antioxidant activities using primary cultured rat cortical neuronal cells and in vitro cell-free bioassays. Based on our primary screening data with eighteen synthesized derivatives, nine compounds (1a, 1c, 1f, 1i, 1j, 1l, 1p, 1q and 1r) exhibiting considerable protection against the NMDA-induced excitotoxic neuronal cell damage at the concentration of $100{\mu}M$ were selected for further evaluation. Among the selected derivatives, compound 1f (with $-CH_3$ substitution at R2 position) exhibited the most potent and efficacious neuroprotective action against the NMDA-induced excitotoxicity. Its neuroprotective effect was almost comparable to that of memantine, a well-known NMDA antagonist, at $30{\mu}M$ concentration. In addition to 1f, compound 1j (with -OH substitution at R3 position) also showed marked anti-excitotoxic effects at both 100 and $300{\mu}M$ concentrations. These findings suggest that $-CH_3$ substitution at R2 position and, to a lesser degree, -OH substitution at R3 position may be important for exhibiting neuroprotective action against excitotoxic damage. Compound 1j was also found to scavenge 1,1-diphenyl-2-picrylhydrazyl radicals and inhibit in vitro lipid peroxidation in rat brain homogenate in moderate and appreciable degrees. Taken together, our structure-activity relationship studies suggest that the compound with $-CH_3$ substitution at R2 and -OH substitution at R3 positions of the benzofuran moiety might serve as the lead exhibiting potent anti-excitotoxic, ROS scavenging, and antioxidant activities. Further synthesis and evaluation will be necessary to confirm this possibility.

• Korean Journal of Plant Resources
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• v.26 no.2
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• pp.149-158
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• 2013

The objective of this study was to investigate the antioxidative capacity of ethanol extracts from Sanguisorbae officinalis L. root (Sanguisorbae radix) in vitro. The concentration of Sanguisorbae radix extract at which DPPH radical scavenging activity was inhibited by 50% was 0.33 mg/mL, which was similar to $IC_{50}$ of ${\alpha}$-tocopherol (0.40 mg/mL), as compared to 100% by pyrogallol as a reference. Total antioxidant status was examined by total antioxidant capacity against ABTS radical reactions. Total antioxidant capacities of Sanguisorbae radix extract were significantly (p<0.05) higher than those of ${\alpha}$-tocopherol. Superoxide scavenging activities of Sanguisorbae radix extract were significantly (p<0.05) higher than those of catechin. Oxygen radical absorbance capacities of Sanguisorbae radix extract were significantly (p<0.05) higher than those of ascorbic acid. Cupric reducing antioxidant capacities of Sanguisorbae radix extract were significantly (p<0.05) higher than those of ${\alpha}$-tocopherol. Sanguisorbae radix extract prevented supercoiled DNA strand breakage induced by hydroxyl radical and peroxyl radical. Total phenolic contents of Sanguisorbae radix extract at concentrations of 0.5 and 5 mg/mL were 0.50 and 3.33 mM gallic acid equivalents, respectively. Sanguisorbae radix extract at concentration of 0.01, 0.1 and 0.5 mg/mL inhibited 0.2 mM tert-butyl hydroperoxide-induced cytotoxicity by 33.8, 79.1 and 96.9%, respectively, in HepG2 cell culture system. Thus, strong antioxidant and cytotoxicity-ihnibiting effects of Sanguisorbae radix extract seem to be due to, at least in part, the prevention from free radicals-induced oxidation as well as high levels in total phenolic contents.

• Journal of the korean academy of Pediatric Dentistry
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• v.39 no.3
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• pp.233-241
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• 2012

Photodynamic therapy (PDT) is a technique that involves the activation of photosensitizer by light in the presence of tissue oxygen, resulting in the production of reactive radicals capable of inducing cell death. The aim of this study was to evaluate the effect of PDT on Streptococcus mutans in planktonic conditions, previously treated with different photosensitive concentrations of erythrosine, using halogen and LED curing unit as a light source. And we compared the effects of PDT on six strains of S. mutans isolated from oral cavity and reference strain. As a result, S. mutans was susceptible to the combination of hand held photopolymerizer (HHP) and erythrosine. The higher concentration of erythrosine in the presence of light irradiation induced greater effects in reduction of viability of S. mutans. Isolated S. mutans showed a significant reduction in bacterial counts of the groups submitted to PDT compared to the control groups. And they appeared to be similar or slightly lower antimicrobial effect compared with reference strain. However, the difference was not significant (p < 0.05). In conclusion, PDT using erythrosine as a photosensitizing agent and HHP as a light source could be an efficient option for diseases caused by S. mutans.

• Journal of Chest Surgery
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• v.29 no.8
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• pp.850-860
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• 1996

Oxygen free radicals and their metabolites have been implicated as possible causes of reperrusion injury In animal models. Their role in the clinical setting is still controversial. The aim of this study was to evaluate the degree of tissue damage, oxidative stress. and changes in the antioxidant enzyme system in patients undergoing cor nary artery bypass graft operations(CABG) with myocardial protection by cold blood cardioplegia. In patients undergoing CABG(n:10). the levels of lactate dehydrogenate(LDH), creatine phosphokinase MB fraction(CK-MB), and malondialdehyde(M DA) were measured In the coronary sinus effluent before aortic cross clamping and 20 minutes after reperfusion. At the same time, the myocardial tissue activities of superoxide dismutase(SOD). catalase(CAT), glutathione peroxiddse(GSHPX), glutathione reductase (GSSGRd), and glucose 6-phosphate dehydrogenate(GfPDH ) were determined in the right atrial auricle excised before aortic cross clamping and in the left atrial auricle excised 20 minutes after reperfuslon. The levels of increased significantly after reperrusion(p< U.05). There were no significant changes in CAT and CfPDH levels. Western blot analysis was performed to study the induction of antioxidant enzyme and demonstrated increased amount of Cu,Zn-SOD.

• Reproductive and Developmental Biology
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• v.33 no.2
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• pp.99-105
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• 2009

Curcumin is a major active component of the food flovour tumeric. It has been used for the treatment of many diseases such as inflammatory and infectious diseases, cancer and other disease due to its antioxidant properties. Curcumin is a powerful scavenger of many free radicals such as superoxide anion, hydroxyl radical and nitric oxide. The objective of this study was to investigate the antioxidative effects of curcumin against hydrogen peroxide on semen quality during in vitro storage of boar semen. The sperm treated with different concentration of curcumin (1, 5 and 10 ${\mu}M$) in the presence or absence of hydrogen peroxide (250 ${\mu}M\;H_2O_2$) were incubated for 3, 6 and 9 hr at $37^{\circ}C$ and analyzed sperm characteristics such as motility, membrane integrity (MI), lipid peroxidation (LPO), reactive oxygen species (ROS) and DNA fragmentation (DF). The sperm motility and MI in $H_2O_2$ treated group ($47.8%{\pm}6.8$ and $24.8%{\pm}2.2$) were significantly decreased when compare to curcumin treated group ($79.8%{\pm}2.7$ and $34.6%{\pm}1.0$, respectively) irrespective of incubation periods(p<0.05). The LPO of spermatozoal plasma membrane was measured by thiobarbituric acid (TBA) reactions for malondialdehyde (MDA), MDA level in control ($11.6{\pm}0.6\;nmol/L{\times}10^6$) and curcumin groups ($10.7{\pm}0.3\;nmol/L{\times}10^6$) were lower than those of curcumin plus $H_2O_2$ ($17.1{\pm}0.8\;nmol/L{\times}10^6$) or $H_2O_2$ group ($22.5{\pm}1.9\;nmol/L{\times}10^6$) from 3 to 9 hr incubation periods. The DF by sperm chromatin dispersion (SCD) test and ROS production measured by 2',7'-dichlorofluorescein (DCF) fluorescence intensity were no significantly difference through all experimental groups (p>0.05). Correlation among evaluation methods for sperm quality, motility vs MI and DF vs ROS was positively correlated while motility vs DF and ROS vs LPO were negatively correlated in all treatment groups. These results demonstrate that curcumin can effectively improve the sperm quality during in vitro storage of boar semen through its hydrogen peroxide scavenging mechanism as an antioxidant.

• Microbiology and Biotechnology Letters
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• v.41 no.4
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• pp.433-441
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• 2013

In this study, the anti-oxidative, anti-inflammatory, anti-melanogenic activities of Endlicheria anomala (Nees) Mez methanol extract (EAME) were evaluated by use of in vitro assays and cell culture model systems. The results revealed that EAME scavenges various radicals such as 1,1-diphenyl-2-picryl hydrazyl hydrogen peroxide induced reactive oxygen species, and lipopolysaccharide induced nitric oxide. Furthermore, EAME induced the expression of anti-oxidative enzymes such as heme oxygenase 1, thioredoxin reductase 1, NAD(P)H dehydrogenase 1, and their upstream transcription factor, nuclear factor-E2-related factor 2. Moreover, EAME inhibited in vitro DOPA oxidation and 3-isobutyl-1-methylxanthine induced melanogenesis in B16F10 cells. Its anti-melanogenic activity will have originated from the inhibition of tyrosinase enzyme activity and melanogenesis related protein expression. Taken together, these results provide the important new insight that E. anomala possesses various biological activities such as anti-oxidative, anti-inflammatory, and anti-melanogenic. Therefore, it might be utilized as a promising material in the fields of nutraceuticals and cosmetics.

• The Korean Journal of Physiology and Pharmacology
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• v.2 no.5
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• pp.617-628
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• 1998

In order to understand the pathogenetic mechanism of adult respiratory distress syndrome (ARDS), the role of phospholipase A2 (PLA2) in association with oxidative stress was investigated in rats. $Interleukin-1{\alpha}\;(IL-1,\;50\;{\mu}g/rat)$ was used to induce acute lung injury by neutrophilic respiratory burst. Five hours after IL-1 insufflation into trachea, microvascular integrity was disrupted, and protein leakage into the alveolar lumen was followed. An infiltration of neutrophils was clearly observed after IL-1 treatment. It was the origin of the generation of oxygen radicals causing oxidative stress in the lung. IL-1 increased tumor necrosis factor (TNF) and cytokine-induced neutrophil chemoattractant (CINC) in the bronchoalveolar lavage fluid, but mepacrine, a PLA2 inhibitor, did not change the levels of these cytokines. Although IL-1 increased PLA2 activity time-dependently, mepacrine inhibited the activity almost completely. Activation of PLA2 elevated leukotriene C4 and B4 (LTC4 and LTB4), and 6-keto-prostaglandin $F2{\alpha}\;(6-keto-PGF2{\alpha})$ was consumed completely by respiratory burst induced by IL-1. Mepacrine did not alter these changes in the contents of lipid mediators. To estimate the functional changes of alveolar barrier during the oxidative stress, quantitative changes of pulmonary surfactant, activity of gamma glutamyltransferase (GGT), and ultrastructural changes were examined. IL-1 increased the level of phospholipid in the bronchoalveolar lavage (BAL) fluid, which seemed to be caused by abnormal, pathological release of lamellar bodies into the alveolar lumen. Mepacrine recovered the amount of surfactant up to control level. IL-1 decreased GGT activity, while mepacrine restored it. In ultrastructural study, when treated with IL-1, marked necroses of endothelial cells and type II pneumocytes were observed, while mepacrine inhibited these pathological changes. In histochemical electron microscopy, increased generation of oxidants was identified around neutrophils and in the cytoplasm of type II pneumocytes. Mepacrine reduced the generation of oxidants in the tissue produced by neutrophilic respiratory burst. In immunoelectron microscopic study, PLA2 was identified in the cytoplasm of the type II pneumocytes after IL-1 treatment, but mepacrine diminished PLA2 particles in the cytoplasm of the type II pneumocyte. Based on these experimental results, it is suggested that PLA2 plays a pivotal role in inducing acute lung injury mediated by IL-1 through the oxidative stress by neutrophils. By causing endothelial damage, functional changes of pulmonary surfactant and alveolar type I pneumocyte, oxidative stress disrupts microvascular integrity and alveolar barrier.

• Journal of Korean Society on Water Environment
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• v.20 no.1
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• pp.78-85
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• 2004

As an ozone contactor, we newly adopted HJLR (High-performance Jet Loop Reactor) for the decolorization of Reactive black 5 and the mineralization of oxalic acid, which has been applied exclusively in biological wastewater treatments and well-known for high oxygen transfer characteristics. The ozonation efficiency for organic removals and ozone utilization depending on the mass transfer rate were compared to those of Stirred bubble column reactor, which was controlled by varing energy input in the HJLR and Stirred bubble column reactor. The results were as follows; first, the decolorization rate of Reactive black 5 in the HJLR reactor was nearly proportional to the increasing $k_La$. When the $k_La$ was increased by 25 % from $13.0hr^{-1}$ to $16.4hr^{-1}$, 30 % of the k' (apparent reaction rate constant) was increased from 0.1966 to $0.2665min^{-1}$ (Stirred bubble column; from 0.1790 to $0.2564min^{-1}$). Ozone transfer was found to be a rate-determining step in decolorizing Reactive black 5, which was supported by that no residual ozone was detected in all of the experiments. Second, the mineralization of oxalic acid was not always proportional to the increasing $k_La$ in the RJLR reactor. The rate-determining step for this reaction was OH(OH radical) production with ozone transfer, because residual ozone was always detected during the ozonation of oxalic acid in contrast with Reactive black 5. This result indicates that the increase of $k_La$ in the HJLR reactor is beneficial only when there are in ozone transfer limited regions. In addition, regardless of $k_La$, the mineralization of oxalic acid was nearly accomplished within 60 minutes. It was interpreted as that the longer staying of residual ozone by whirling liquid in the HJLR reactor contributed to an high ozone utilization(83-94%), producing more OR radicals.

• Korean Journal of Plant Resources
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• v.23 no.5
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• pp.445-450
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• 2010

This study was carried out to investigate the antioxidative capacity of Ampelopsis brevipedunculata 95% ethanol extracts. The concentration of A. brevipedunculata extract at which DPPH radical scavenging activity was inhibited by 50% was 0.42 mg/mL as compared to 100% by pyrogallol as a reference. Total antioxidant status was examined by total antioxidant capacity against ABTS radical reactions. Total antioxidant capacities of A. brevipedunculata extract at the concentrations of 0.1 and 1 mg/mL were 0.65 and 3.71 mM Trolox equivalents, respectively. Oxygen radical absorbance capacities of A. brevipedunculata extract at the concentrations of 5 and $100\;{\mu}g/mL$ were 22.75 and $131.25\;{\mu}M$ gallic acid equivalents, respectively. Superoxide scavenging activities of A. brevipedunculata extract at the concentrations of 0.1 and 1 mg/mL were 27.7 and 56.0%, respectively. Total phenolic contents of A. brevipedunculata extract at the concentrations of 0.5 and 2.0 mg/mL were 0.55 and 2.06 mM gallic acid equivalents, respectively. A. brevipedunculata extract at the concentration of 0.1 mg/mL inhibited 0.2 mM and 0.5 mM tert-butyl hydroperoxide induced cyototoxicity by 36.2 and 23.3%, respectively, in HepG2 cell culture system. Thus strong antioxidant and cytotoxicity-inhibiting effects of A. brevipedunculata extract seem to be due to, at least in part, the prevention from free radicals-induced oxidation as well as high levels in total phenolic contents.

• Journal of Periodontal and Implant Science
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• v.25 no.3
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• pp.529-538
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• 1995

It has been believed that the increased release of free oxygen radicals ($O_2^-,H_2O_2$, and $OH^-$) might be a factor in the pathogenesis of periodontal diseases. Antioxidant enzymes such as glutathione peroxidase(GSH-PX) and catalase can protect the tissue damage from the $H_2O_2$. In order to investigate the GSH-PX and catalase activity in the blood plasma and red blood cells(RBCs) of the patients with periodontitis, 19 patients who had good general health, attachment loss more than 6 mm and bone loss were selected as periodontitis group, 7 patients who had severely inflamed gingiva were selected as gingivitis group, and 15 volunteers with good general and periodontal health were selected as normal group. 17 of 26 patients were performed scaling and root planing to reduce the gingival inflammation for gingivitis and periodontitis groups, and were selected as posttreatment group. After blood plasma and RBCs were collected and separated 1 ml of peripheral blood from each subject, GSH-PX activity in blood plasma and RBCs was measured by the same method that Stefan et al. did, and catalase activity in RBCs was measured by the same method that Beers et al. did. The difference of GSH-PX and catalase activity between normal, gingivitis, and periodontitis groups was statistically analyzed by ANOVA with SPSS/PC+ program, and the difference between pretreatment and posttreatment groups was analyzed by Student t-test. The results were as follows : 1. GSH-PX activity in blood plasma was significantly lower in the gingivitis group($0.8683{\pm}0.0658$), periodontitis group($0.7130{\pm}0.1333$) than in the normal group($1.0241{\pm}0.0801$)(p<0.05), and GSH-PX activity in RBCs was significantly lower in the gingivitis groupt. $0.8156{\pm}0.1167$), periodontitis group($0.7533{\pm}0.1185$) than in the normal group($l.1963{\pm}0.2044$)(P<0.05), but there was no statistical significance in the difference of GSH-PX activity in RBCs between the gingivitis group and periodontitis group(p>0.05). 2. Catalase activity in RBCs was siginficantly lower in the periodontitis group($117.34{\pm}35.01$) than in the normal group($l52.38{\pm}32.09$)(p<0.05). 3. GSH-PX activity in blood plasma was significantly increased in the posttreatment groupe $1.0376{\pm}0.2820$) compared to the pretreatment group(0.7608 0.1600) (p<0.05), and GSH-PX activity in RBC was significantly increased in the posttreatment group($1.0421{\pm}0.2330$) compared to the pretreatment group($0.7728{\pm}0.1210$)(p<0.05). 4. There was no statistical significance in the difference of catalase activity in RBCs between the pretreatment group($112.04{\pm}43.65$) and posttreatment group($l33.41{\pm}39.16$)(p>0.05).The results, within the limits of the present experiment, suggest that the lowered activity of GSH-PX and catalase in blood plasma and RBCs may be related with periodontopathogenesis.