• Bulletin of the Korean Chemical Society
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• 제32권6호
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• pp.2015-2020
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• 2011

A series of isoxazol-indolin-2-one was designed for GSK-3${\beta}$ inhibitors as novel anticancer agents based on their binding mode analysis in GSK-3${\beta}$ crystal structure. Total 21 compounds were synthesized and evaluated for their inhibitory activity against two tumor cell lines (DU145 and HT29). Most of the synthesized compounds were potent with above 80% inhibitory activity at 100 ${\mu}M$, and several compounds were examined for inhibitory activity against GSK-3${\beta}$. Among them, 15(Z) ($R_1$=H, $R_2$=3-Cl-phenyl) was most active with 78% inhibition of tumor cell line (HT29) at 20 ${\mu}M$ and 72% inhibition of GSK-3${\beta}$ at 20 ${\mu}M$.

• Biomolecules & Therapeutics
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• 제21권5호
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• pp.371-380
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• 2013

Doxorubicin is still main drug in chemotherapy with limitation of use due to adverse drug reaction. Increased oxidative stress and alteration of nitric oxide control have been involved in cardiotoxicity of doxorubicin (DOX). A Disintegrin And Metalloproteinase (ADAMs) are transmembrane ectoproteases to regulate cell-cell and cell-matrix interactions, but role in cardiac disease is unclear. The aim of this study was to determine whether DOX activates peroxynitrite and ADAM 10 and thus ADAM and matrix metalloproteinase (MMP) induce cardiac remodeling in DOX-induced cardiomyopathy. Adult male Sprague-Dawley rats were subjected to cardiomyopathy by DOX (6 times of 2.5 mg/kg DOX over 2-weeks), and were randomized as four groups. Then followed by 3, 5, 7, and 14 days after cessation of DOX injection. DOX-injected animals significantly decreased left ventricular fractional shortening compared with control by M-mode echocardiography. The expressions of cardiac nitrotyrosine by immunohistochemistry were significant increased, and persisted for 2 weeks following the last injection. The expression of eNOS was increased by 1.9 times (p<0.05), and iNOS was marked increased in DOX-heart compared with control (p<0.001). Compared to control rats, cardiac ADAM10- and MMP 9- protein expressions increased by 20 times, and active/total MMP 9 proteolytic activity showed increase tendency at day 14 after cessation of DOX injection (n=10, each group). DOX-treated $H_9C_2$ cell showed increased ADAM10 protein expression with dose-dependency (p<0.01) and morphometric changes showed the increase of ventricular interstitial, nonvascular collagen deposition. These data suggest that activation of cardiac peroxynitrite with increased iNOS expression and ADAM 10-dependent MMP 9 expression may be a molecular mechanism that contributes to left ventricular remodeling in DOXinduced cardiomyopathy.

• 한국콘텐츠학회:학술대회논문집
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• 한국콘텐츠학회 2007년도 추계 종합학술대회 논문집
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• pp.698-702
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• 2007

최근 영화 및 드라마, CF 등 각종 영상물에서는 하나의 화면이 서로 다른 영상들로 분할되어 구성된 장면들을 흔히 접할 수 있다. 2001년 미국에서 제작되어 2008년 시즌7 방영을 앞두고 있는 드라마 '24'에는 이런 화면분할 장면이 빈번히 등장하고 있다. '24'는 하루 동안에 발생한 일들을 한 시간짜리 24개 에피소드로 나눠 리얼타임 형식으로 보여주는 드라마로써 화면분할 장면을 통해 여러 곳에서 동시에 벌어지고 있는 사건들을 효과적으로 전달하고 있다. 특히 감각적으로 분할된 프레임들은 서로 충돌과 어울림 등의 관계를 맺으며 시청자들의 시선을 사로잡는다. 본 논문은 드라마 '24'에 등장하는 화면분할 장면을 구성하는 프레임들 간의 상호관계를 화면구성 원리를 통하여 분석하여, 시청자들의 시선을 사로잡는 원인을 영화 몽타주 이론을 통하여 살펴보고자 한다.

• Bulletin of the Korean Chemical Society
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• 제26권9호
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• pp.1359-1365
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• 2005

A series of new chiral [iminophosphoranyl]ferrocenes, {${\eta}^5-C_5H_4-(PPh_2=N-2,6-R_2-C_6H_3)$}Fe{${\eta}^5-C_5H_3-1-PPh^2-2-CH(Me)NMe_2$} (1: R = Me, $^iPr$), {${\eta}^5{-C_5H_4-(PPh_2=N-2,6-R_2}^1-C_6H_3)$}Fe{${\eta}^5-C_5H_3-1-(PPh_2=N-2,6-R_2-C_6H_3)-2-CH(Me)R_2$} (2: $R^1\;=\;Me,\;^iPr;\;R^2\;=\;NMe_2$, OMe), and $({\eta}^5-C_5H_5)Fe${${\eta}^5-C_5H_4-1-PR_2-2-CH(Me)N=PPh_3$} (3:R = Ph, $C_6H_{11}$) have been prepared from the reaction of [1,1'-diphenylphosphino-2-(N,N-dimethylamino) ethyl]ferrocene with arylazides (1 & 2) and the reaction of phosphine dichlorides ($R_3PCl_{2}$) with [1,1'-diphenylphosphino-2-aminoethyl]ferrocene (3), respectively. They form palladium complexes of the type $[Pd(C_3H_5)(L)]BF_4$ (4-6: L = 1-3), where the ligand (L) adopts an ${\eta}^2-N,N\;(2)\;or\;{\eta}^2$-P,N (3) as expected. In the case of 1, a potential terdentate, an ${\eta}^2$-P,N mode is realized with the exclusion of the –=NAr group from the coordination sphere. Complexes 4-6 were employed as catalysts for allylic alkylation of 1,3-diphenylallyl acetate leading to an almost stoichiometric product yield with modest enantiomeric excess (up to 74% ee). Rh(I)-complexes incorporating 1-3 were also prepared in situ for allylic alkylation of cinnamyl acetate as a probe for both regio- and enantioselectivities of the reaction. The reaction exhibited high regiocontrol in favor of a linear achiral isomer regardless of the ligand employed.

• 대한전자공학회논문지SD
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• 제49권3호
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• pp.21-29
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• 2012

본 논문에서는 H.264/AVC 부호화기의 성능 향상을 위해 고성능 CAVLC 부호화기의 하드웨어 구조를 제안한다. 기존의 CAVLC 부호화기는 변환계수의 재정렬 과정이 포함되어 변환계수를 저장해야 할 버퍼와 버퍼제어를 위한 추가적인 사이클이 필요하므로 하드웨어 면적이 증가하고 불필요한 사이클이 수행된다. 제안한 CAVLC는 CAVLC의 파라미터 중에 Runbefore를 순방향 탐색기법으로 계산하고 그 외 파라미터들은 역방향 탐색기법으로 계산하여 변환계수의 재정렬 과정을 수행하지 않는다. 또한, 제안한 CAVLC 부호화기에 조기 종료 모드를 적용하고 2단 파이프라인 구조를 사용하여 CAVLC의 수행 사이클 수를 감소시켰다. 제안한 CAVLC 부호화기의 하드웨어 구조를 매그나칩 공정 $0.18{\mu}m$ 셀 라이브러리로 합성한 결과, 최대동작 주파수는 125MHz이며 게이트 수는 17k이다. 제안한 CAVLC 부호화기의 하드웨어 구조를 H.264/AVC 표준 참조 소프트웨어 JM13.2에서 추출한 데이터를 이용하여 테스트한 결과, $16{\times}16$ 매크로블록을 처리하는데 평균적으로 36.0사이클이 소요되어 기존의 CAVLC 부호화기보다 성능이 57.8% 향상됨을 확인하였다.

• The Plant Pathology Journal
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• 제32권3호
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• pp.216-227
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• 2016

Biological control agents (BCAs) from different microbial taxa are increasingly used to control bacterial wilt caused by Ralstonia solanacearum. However, a quantitative research synthesis has not been conducted on the role of BCAs in disease suppression. Therefore, the present study aimed to meta-analyze the impacts of BCAs on both Ralstonia wilt disease suppression and plant (host) growth promotion. The analysis showed that the extent of disease suppression by BCAs varied widely among studies, with effect size (log response ratio) ranging from -2.84 to 2.13. The disease incidence and severity were significantly decreased on average by 53.7% and 49.3%, respectively. BCAs inoculation also significantly increased fresh and dry weight by 34.4% and 36.1%, respectively on average. Also, BCAs inoculation significantly increased plant yield by 66%. Mean effect sizes for genus Pseudomonas sp. as BCAs were higher than for genus Bacillus spp. Among antagonists tested, P. fluorescens, P. putida, B. cereus, B. subtilis and B. amyloliquefaciens were found to be more effective in general for disease reduction. Across studies, highest disease control was found for P. fluorescens, annual plants, co-inoculation with more than one BCA, soil drench and greenhouse condition were found to be essential in understanding plant responses to R. solanacearum. Our results suggest that more efforts should be devoted to harnessing the potential beneficial effects of these antagonists, not just for plant growth promoting traits but also in mode of applications, BCAs formulations and their field studies should be considered in the future for R. solanacearum wilt disease suppression.

• Bulletin of the Korean Chemical Society
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• 제26권2호
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• pp.285-291
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• 2005

The nonstructural protein 5B (NS5B) of hepatitis C virus (HCV) is the viral RNA-dependent RNA polymerase (RdRp), which is the essential catalytic enzyme for the viral replication and is an appealing target for the development of new therapeutic agents against HCV infection. A small amount of serum from a single patient with hepatitis C was used to get the genome of a Korean HCV isolate. Sequence analysis of NS5B 1701 nucleotides showed the genotype of a Korean isolate to be subtype 1b. The soluble recombinant HCV NS5B polymerase lacking the C-terminal 24 amino acids was expressed and purified to homogeneity. With the highly purified NS5B protein, we established in vitro systems for RdRp activity to identify potential polymerase inhibitors. The rhodanine family compounds were found to be potent and specific inhibitors of NS5B from high throughput screening (HTS) assay utilizing the scintillation proximity assay (SPA) system. The binding mode of an inhibitor was analyzed by measuring various kinetic parameters. Lineweaver-Burk plots of the inhibitor suggested it binds not to the active site of NS5B polymerase, but to an allosteric site of the enzyme. The activity of NS5B in in vitro polymerase reactions with homopolymeric RNA requires interaction with multiple substrates that include a template/primer and ribonucleotide triphosphate. Steady-state kinetic parameter, such as Km, was determined for the ribonucleotide triphosphate. One of compounds found interacts directly with the viral polymerase and inhibits RNA synthesis in a manner noncompetitively with respect to UTP. Furthermore, we also investigated the ability of the compound to inhibit NS5B-directed viral RNA replication using the Huh7 cell-based HCV replicon system. The investigation is potentially very useful for the utility of such compounds as anti-hepatitic agents.

• Archives of Pharmacal Research
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• 제26권4호
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• pp.306-311
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• 2003

Soy, high dietary intake for the oriental population, is a main source of isoflavonoids. Sophoricoside (SOP) an isoflavone glycoside was isolated from immature fruits of Sophora japonica (Leguminosae family) and its inhibitory effect on chemical mediators involved in inflammatory response was investigated in this study. SOP inhibited the interleukin (IL)-6 bioactivity with an $IC_{50}$ value of 6.1 $\mu$M whereas it had no effects on IL-1$\beta$ and TNF-a bioactivities. SOP was identified as a selective inhibitor of cyclooxygenase (COX)-2 activity with an $IC_{50}$ value of 4.4 $\mu$ M, but did not show inhibitory effect on the synthesis of COX-2. However, SOP had no effect on the production of reactive oxygen species including superoxide anions and nitric oxide. These results revealed that in vitro anti-inflammatory action of SOP is significantly different from that of genistein known as a phytoestrogen of soy products. This experimental study has documented an importance of dietary soy isoflavonoids as multifunctional agents beneficial to human health, and will help to clarify protective mechanisms of SOP against inflammatory conditions.

• 한국진공학회:학술대회논문집
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• 한국진공학회 2014년도 제46회 동계 정기학술대회 초록집
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• pp.259.1-259.1
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• 2014

Recently non-thermal plasma has been frequently applied to various research fields. The liquid plasma have received much attention lately because of interests in surgical and nanomaterial synthesis applications. Especially, intensive researches have been carried out for non-thermal plasma in liquid by using various electrode configurations and power supplies. We have developed a bioplasma source which could be used in a liquid, in which outer insulator has been covered onto the outer electrode. Also we have also put an insulator between the inner and outer electrode. Based on the surface discharge mode, the nonthermal bioplasma has been generated inside a liquid by using an alternating current voltage generator with peak voltage of 12 kV under driving frequency of 22 KHz. Here the discharge voltage and current have been measured for electrical characteristics. Especially, We have measured discharge and optical characteristics under various liquids of deionized (DI) water, tap water, and saline by using monochromator. We have also observed nitric oxide (NO), hydrogen peroxide (H2O2), and hydroxyl (OH) radical species by optical emission spectroscopy during the operation of bioplasma discharge inside various kinds of DI water, tap water, and saline. Here the temperature has been kept to be $40^{\circ}C$ or less when discharge in liquid has been operated in this experiment. Also we have measured plasma temperature by high speed camera image and density by using either H-alpha or H-beta Stark broadening method.

• Bulletin of the Korean Chemical Society
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• 제30권10호
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• pp.2227-2232
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• 2009

Novel polythiol materials of urethane lens series for plastic optical lens were synthesized from polyol materials via thioisouronium of thiourea with c-HCl in refluxing aqueous solution, in which polythiol material was carried out from hydrolysis of thioisouronium by ammonia water. Their structure properties were identified by EA, EI-MS, FT-IR, $^1H\;and\;^{13}C$ NMR spectroscopies and TGA. Their ophthalmic lenses as polythiourethane material were prepared by thermal curing to an injected glass mold using the evenly solutions of diisocyanates series (TDI, XDI, HDI or IPDI) with polythiols. Polythiourethane shows that the strong stretching mode for SH group of polythiol disappeared in FT-IR spectra after thermosetting polymerization. Thermal deformation starting temperature of ophthalmic lenses was determined by TMA. Ophthalmic lenses made from characteristic polythiol and diisocyanate series have transparency, colorless and good impact strength, in which thermal resistance and impact strength of ophthalmic lenses were influenced by diisocyanate series. Physical properties of ophthalmic lens have contrast thermal resistance with impact strength. The property of thermal resistance and impact strength for respective ophthalmic lenses was examined by TMA and drop ball test.