• 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.

• Journal of the Korean Society of Food Science and Nutrition
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• v.31 no.1
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• pp.92-97
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• 2002

The effects of Pueraria flos (PF) and Pueraria radix (PR) water extract on the hepatic alcohol metabolic enzyme activities were examined in rats that were orally administered ethanol (25% v/v, 5g/kg body weight/day) for 5 weeks. The PF and PR water extract were supplemented in a diet, based on 1.2 g or 2.4 g of raw PF or PR/kg body weight/body. Alcohol administration without the PF or PR supplementation significantly decreased net weight gain, feed intake and feed efficiency ratio. However. both dose of the PF of PR supplementation resulted in significant enhancement of growth and suppression of increased relative weight of liver, brain and heart by alcohol administration. Activities of hepatic alcohol dehydrogenase and microsomal ethanol oxidizing system were higher in the alcohol treated group than in the normal group, while aldehyde dehydrogenase activity was significantly lowered in the alcohol treated group. The hepatic metabolic enzyme activities altered by alcohol administration were normalized by both doses of PF or PR supplement. Hepatic monoamine oxidase activity and hydrogen peroxide, which were significantly higher in the alcohol treated group than in the normal group, were also decreased by the supplementation with either PF or PR. These results indicate that low-or high-supplementation of either water extract PF or PR may alleviate ethanol-induced hepatotoxicity by altering alcohol metabolic enzyme activities.

• Journal of the Korean Association of Oral and Maxillofacial Surgeons
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• v.36 no.5
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• pp.341-345
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• 2010

Introduction: Skeletal homeostasis is normally maintained by the stability between bone formation by osteoblasts and bone resorption by osteoclasts. However, the correlation between the inflammatory reaction and osteoblastic differentiation of cultured osteoprogenitor cells has not been fully investigated. This study examined the effects of inflammatory cytokines on the osteoblastic differentiation of cultured human periosteal-derived cells. Materials and Methods: Periosteal-derived cells were obtained from the mandibular periosteum and introduced into the cell culture. After passage 3, the periosteal-derived cells were further cultured in an osteogenic induction Dulbecco's modified Eagle's medium (DMEM) medium containing dexamethasone, ascorbic acid, and $\beta$-glycerophosphate. In this culture medium, tumor necrosis factor (TNF)-$\alpha$ with different concentrations (0.1, 1, and 10 ng/mL) or interleukin (IL)-$1{\beta}$ with different concentrations (0.01, 0.1, and 1 ng/mL) were added. Results: Both TNF-$\alpha$ and IL-$1{\beta}$ stimulated alkaline phosphatase (ALP) expression in the periosteal-derived cells. TNF-$\alpha$ and IL-$1{\beta}$ increased the level of ALP expression in a dose-dependent manner. Both TNF-$\alpha$ and IL-$1{\beta}$ also increased the level of alizarin red S staining in a dose-dependent manner during osteoblastic differentiation of cultured human periosteal-derived cells. Conclusion: These results suggest that inflammatory cytokines TNF-$\alpha$ and IL-$1{\beta}$ can stimulate the osteoblastic activity of cultured human periosteal-derived cells.

• Korean Journal of Food Science and Technology
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• v.29 no.1
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• pp.156-160
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• 1997

The monoamine oxidase (MAO, EC 1.4.3.4) plays a central role in the metabolism of many amines including the neurotransmitter monoamines. MAO is a flavoprotein found exclusively in the mitochondrial outer membrane, occuring in the MAO-A and MAO-B subtypes. MAO-A deaminates serotonin and noradrenaline much better than phenethylamine (PEA) or benzylamine (BA), and is preferentially inhibited by clorgyline, whereas MAO-B prefers PEA and BA as substrates and is preferentially inhibited by deprenyl. MAO inhibitors were among the first drugs used in the treatment of depression, and it is known to be the inhibition of MAO-A which is important for the antidepressant effect of MAO inhibitors. For the purpose of evaluating MAO inhibitory activities from natural resources, three kinds of edible mushrooms were screened by tracing the inhibitory activities against rat brain mitochondrial MAO-A, utilizing serotonin as a substrate and rat liver mitochondrial MAO-B utilizing benzylamine as a substrate. Among the tested mushrooms, Ganoderma lucidium and Lentinus edodes showed the weak inhibitory activities against MAO-B.

• Biomolecules & Therapeutics
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• v.5 no.1
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• pp.36-42
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• 1997

To investigate effects of ginseng total saponin (GTS) on the ethylcholine aziridnium ion (AF64A) -induced glutamatergic nervous system, rats were pretreated with the infusion of AF64A (3 nmole) into lateral ventricle and were posttreated with 50 mg/kg of GTS, i.p., for 1 week. Twenty four hours after the last administration, rats were sacrificed and the levels of glutamate and taurine, [$^3$H]dizocilpine ([$^3$H]MK801) binding sites and glutamine synthetase activity were assessed in striatum, hippocampus and frontal cortex. The levels of striatal glutamate after GTS treatment in rats were decreased. And the levels of glutamate were decreased in striatum and frontal cortex and increased in hippocampus by the infusion of AF64A. However, the AF64A-induced changes of glutamate were returned to the control level by the administration of GTS in striatum, frontal cortex and hippocampus. After the infusion of AF64A, the level of taurine was decreased in striatum and increased in hippocampus. GTS administrations in the AF64A-treated rats restored to the control level of taurine in the decreased striatal level of taurine, but not in the elevated level of hippocampal taurine. The specific [$^3$H]MK801 binding sites in hippocampus was significantly decreased but not in striatum and frontal cortex after the administration of AF64A. Although GTS itself did not affect the specific [$^3$H]MK801 binding sites, GTS administrations in the AF64A-treated rats did decrease the binding sites of (\`H)Mk801 in all examined regions. The activities of striatal glutamine synthetase were decreased after GTS treatment. The activities of striatal glutamine synthetase (GS) were decreased in AF64A-treated groups. However, the decreased striatal GS activities by AF64A were returned to the control level by GTS treatment. Furthermore, GTS administrations in the AF64A-treated rats increased the hippocampal GS activities. The results indicatethat GTS may adjust the levels of glutamate and taurine constantly and may induce increase in AF64A-induced decrease of GS activity. Thus, it suggests that GTS may antagonize changes in central glutamatergic nervous system induced by AF64A. Also it suggests that the actions of GTS may differently affect in the disease state.

• Polymer(Korea)
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• v.27 no.3
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• pp.217-225
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• 2003

We fabricated the 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU, carmustine)-loaded PLGA wafers containing poly(N-vinylpyrrolidone) (PVP) or tedium chloride (NaCl) in order to control the release profile of drug in special shape (3 in diameter, 1 mm in thickness) by direct compression method. In vitro release profiles of BCNU could be controlled by additives contained in the wafers. Initial release amount, release rate and duration of BCNU could be controlled with presence of PVP or NaCl. In vitro antitumor activity accessed using 9L gliosarcoma cell line has been evaluated by assaying the viability of cells treated with BCNU released from the wafers containing additives resulting in continuous growth inhibition of 9L gliosarcoma tumor cells. Specially, the continuous growth inhibition of BCNU-loaded PLGA wafers containing additives was more effective than that of non-additive BCNU-loaded PLGA wafers. The cytotoxic effect of the drug from the wafers containing NaCl as compared to wafers containing PVP was more enhanced.

• School Mathematics
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• v.4 no.3
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• pp.375-399
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• 2002

When a curriculum change is being an issue, the editorships and the promotive directions reflect to supplement the social requests. However it is often criticized that such changes in the textbook itself are not satisfactory enough as to coherent to the editoships. And we set the following research questions; (1) One of the most important changes in the new 7th curriculum is to encourage the students' activities. We checked if it is well suited in the new textbooks. (2) Often textbook itself is not important In class, while instructor or students want something else other than the one suggested in the textbook. We asked 187 teachers how they use the textbooks in class. To answer (1), we checked up the introductory - activity - contents with 7 categories, which are ${\circled1}$ of real life sources ${\circled2}$ in use of concrete manipulative ${\circled3}$ in use of computers or calculators ${\circled4}$ in use of historical resources ${\circled5}$ stimulating to recall a relevant previous knowledges ${\circled6}$ of coherence between the activity and the exploratory contexts. ${\circled2}$ were increased, rewarding to the decrease of ${\circled5}$, in the new textbooks, while changes in ${\circled3}$ and ${\circled4}$ were not enough to talk about increments. Especially slight decrease in ${\circled6}$ were detected and it seemed to attribute to the unmatchable use of ${\circled1}$ and ${\circled2}$ with the explanation of mathematical subjects, which also implies how difficult to match ${\circled1}$ and ${\circled2}$ with ${\circled6}$. Analyzing the reponses of (2), about 70% of the teachers used the introductory activities in the textbook, which led better attention of sudents, while 30% of teachers do not use it because they felt that its inroductory activities had not been adequate for their purposes. Teachers counted inadequacy reasons for not being helpful in class, lack of time or lack of support of students, etc. Those teachers use introductory activities invented of their own for classes. As some results of the study, we suggest firstly that authors of textbooks have to get more informations to provide ways to entcourage students' interest in mathematics classes. The ways must be practical and brain storming as well as More use of computers and calculators and mathematical history are expected. Secondly, we are emphasizing the feedbacks between the textbook authors and the users(teachers and students) through internet. Which, we anticipate, will get better communications between them and be a good foundations of continuous modifications of textbooks.

• Journal of the Korean Society of Food Science and Nutrition
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• v.38 no.2
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• pp.142-145
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• 2009

The cytotoxic activity against human cancer cells and anti-tumor effect in Balb/c mice of a 70% ethanol extract from masou salmon (MSE) was investigated. The cancer cell lines including human breast adenocarcinoma (MCF-7), human lung carcinoma (A549), human hepatoblastoma (HepG2), human gastric carcinoma (AGS), human cervical adenocarcinoma (HeLa) and transformed primary human embryonal kidney (293) exposed to MSE decreased cell viability as indicated by the MTT assay. The MSE shows significant cytotoxicity on MCF-7, A549, HepG2, AGS and HeLa cells, and are more active than 293 cells. The treatment with 1 mg/mL MSE resulted in 9.2%, 12.7%, 16.6%, and 16.9% cell survival against A549, MCF-7, HepG2, and AGS cells, respectively. Moreover, anticancer effect in vivo of MSE was tested in the animal system using Balb/c mice transplanted sarcoma-180 cells. MSE showed inhibition of tumor growth and the rate of inhibition was 44.7% and 55.7% at the 25 mg/kg body weight and 250 mg/kg body weight, respectively. Thus, we suggest that MSE could be a beneficial material for human cancer prevention.

• Clinical and Experimental Pediatrics
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• v.48 no.6
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• pp.649-654
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• 2005

Purpose : The present study examined how changes in cerebral hemodynamics in newborn piglets with bilirubin infusion can be evaluated by near infrared sepctroscopy(NIRS). Methods : Seventeen newborn piglets were randomly divided into the following three experimental groups : six in the control group(CG); seven in the bilirubin infusion group(BG), and four in the bilirubin infusion with 7-nitroindazole group(NG). To achieve the concentration of bilirubin above 20 mg/dL, we injected a bolus of 40 mg/kg of bilirubin intravenously, followed by 30 mg/kg/hr of bilirubin continuous intravenous infusion. All groups were monitored with cerebral hemodynamics using near infrared spectroscopy(NIRS) and their brain cortexes were harvested and the activities of $Na^+$, $K^+$-ATPase, level of conjugated dienes, ATP and phosphocreatine(PCr) were determined biochemically. Results : No changes took place in CG. In BG and NG, base excess, pH, and MABP decreased, and lactate level in blood increased. Cerebral $Na^+$, $K^+$-ATPase activity and ATP, PCr level in BG significantly decreased and conjugated dienes increased compared to CG. These abnormalities observed in the BG were significantly improved in the NG. In continuous NIRS monitoring, [$HbO_2$], [HbT], and [HbD] in BG were significantlly decreased compared to CG. However these abnormalities between NG and CG were not significantly different. There were no significant differences in $ScO_2$ between the study groups. Conclusion : Our study suggests cerebral hemodynamic changes could be monitored by non-invasive NIRS in newborn piglets with bilirubin infusion.

• The Journal of the Korea Contents Association
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• v.15 no.9
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• pp.418-424
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• 2015

In this study, we proceed if there are any changes in binding ability of receptor-ligand in some degree of SA and in radioactive uptake from the corpus striatum based on small animal experiment in vivo based on the S.A values. By dividing 18F-Fallypride into 3 S.A values(high S.A : 43.29~74 GBq/umol, ordinary S.A : 20.72~29.23 GBq/umol, low S.A : 6.29~8.51 GBq/umol), we injected directly into the veins and performed 90 minutes of dynamic scan using Micro PET. After scanning, we compared and analyzed with Binding Potential (Binding Potential) from the bilateral striatum. high SA and low SA, ordinary SA and low SA showed significant differences. Also, in the image comparison using 18F-Fallypride show high radioactive uptake in the striatum at high SA and ordinary SA, but the radioactive uptake at low SA is lower than other two SA. Since 18F-Fallypride has affinity to dopamine D2/3 pharmacokinetic, the difference of Binding Potentials at decreased level of SA values was not that significant. However, further PET research of the corpus striatum using 18F-Fallypride is necessary because the differences in images and Binding Potentials at 6.5 times smaller SA values compared to high SA value showed were significant.