• Title/Summary/Keyword: High-level Synthesis

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Synthesis and evaluation of inhibitors for Polo-box domain of Polo-like kinase 1

  • Eun Kyoung Ryu
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.6 no.2
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    • pp.139-145
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    • 2020
  • Polo-like kinase 1 (Plk1) is a key protein in mitosis and has been validated as a target for tumor therapy. It is well known to highly overexpress in many kinds of tumor, which has been implicated as a potential biomarker for tumor treatment and diagnosis. Plk1 consists of two domains, the N-terminus kinase domain and the C-terminus polo-box domain (PBD). The inhibitors have been developed for PBD of Plk1, which were shown a high level of affinity and selectivity for Plk1 that led to mitotic arrest and apoptotic cell death. This review discusses the inhibitors for PBD of Plk1 that are suitable for in vivo tumor treatment. They can be further extended for developing in vivo imaging probes for early diagnosis of tumor.

Synthesis and Electrochemical Performance of Ni-rich NCM Cathode Materials for Lithium-Ion Batteries (리튬이온전지 양극활물질 Ni-rich NCM의 합성과 전기화학적 특성)

  • Kim, Soo Yeon;Choi, Seung-Hyun;Lee, Eun Joo;Kim, Jeom-Soo
    • Journal of the Korean Electrochemical Society
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    • v.20 no.4
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    • pp.67-74
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    • 2017
  • Layered Ni-rich NCM cathode materials $Li[Ni_xCo_{(1-x)/2}Mn_{(1-x)/2}]O_2$ ($x{\geq}0.6$) have advantages of high energy density and cost competitive over $LiCoO_2$. The discharge capacity of NCM increases proportionally to the Ni contents. However, there is a problem that it is difficult to realize the stable electrochemical performance due to cation mixing. In this study, synthesis conditions for the layered Ni-rich NCMs are investigated to achieve deliver the ones having good electrochemical performances. Synthesis parameters are atmosphere, lithium source, synthesis time, synthesis temperature and Li/M (M=transition metal) ratio. The degree of cation mixing gets worse as the Ni content is increased from $Li[Ni_{0.6}Co_{0.2}Mn_{0.2}]O_2$ (NCM6) to $Li[Ni_{0.8}Co_{0.1}Mn_{0.1}]O_2$ (NCM8). It is confirmed that higher level of cation mixing affects negatively on the electrochemical performance of NCMs. Optimum synthesis conditions are explored for NCMx (x=6, 7, 8) in order to reduce the cation mixing. Under optimized conditions for three representative NCMx, a high initial discharge capacity and a good cycle life are obtained for $180mAh{\cdot}g^{-1}$, 96.2% (50 cycle) in NCM6, $187mAh{\cdot}g^{-1}$, 94.7% (50 cycle) in NCM7, and $201mAh{\cdot}g^{-1}$, 92.7% (50 cycle) in NCM8, respectively.

The Effect of Dietary Protein and Calcium Levels on the Cadmium Detoxication on Rats (식이 단백질과 Ca 수준이 흰쥐의 Cd 해독에 미치는 영향)

  • 권오란
    • Journal of the Korean Home Economics Association
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    • v.30 no.1
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    • pp.99-113
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    • 1992
  • This study was performed to investigate the effect of dietary protein and calcium levels on cadmium detoxication in rats. Seventy male Sprague-Dawley rats weighing 208 $\pm$ 19 g were blocked into 10 groups of 7 animals according to body weight. Five groups were fed 15% protein-0.6% calcium diet with 100ppm cadmium in drinking water for first 15days and the other 5groups fed same diet without cadmium in drinking water for same period and served as controls. After this 15-day intoxication period, each one of cadmium intoxication and control groups were fed each of 4 kinds of detoxifying diets different with protein(40%, 15%) and calcium(1.3%, 0.6%) levels without cadmimum in drinking water for following 15 days of detoxifying period. Results were summarized as follows: 1) Food intake, body weight gain, F.E.R. and weights of liver, kidney and femur were increased by detoxifying diets and high protein diet was most effective in weight gains of liver and kidney. 2) When cadmium and metallothionein contents of initial intoxication group and those of all detoxication groups were compared, cadmium and metallothionein contents in the liver were not changed, but those in kidney increased, and those in intestine decreased markedly. 3) Only dietary protein level affected cadmium and metallothionein distribution among organs, and cadmium contents of whole blood, liver, kidney and femur were lower in high protein diet, but metallothionein contents in liver and kidney were higher in high protein diet. 4) Gel filtration chromatogram showed that most of cadmium in the cytosol was bound to metallothionein fractions in high protein-high calcium group. Results obtained indicated that high protein diet was effective in cadmium detoxication by increasing the induction of metallothionein synthesis. But high calcium diet did not play a role in cadmium detoxication.

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N-Nitrosodimethylamine in the Kashmiri Diet and Possible Roles in the High Incidence of Gastrointestinal Cancers

  • Chikan, Naveed A.;Shabir, Nadeem;Shaffi, Sheikh;Mir, Manzoor R.;Patel, Trupti N.
    • Asian Pacific Journal of Cancer Prevention
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    • v.13 no.3
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    • pp.1077-1079
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    • 2012
  • The Kashmiri population is culturally distinct with special dietary features owing to the temperate climatic conditions of Kashmir valley. This has habituated the population to preserve food in smoked, pickled and sundried forms which include considerable amounts of $N$-nitroso compounds (NOCs). These are known to cause cytotoxicity, DNA damage, mutation, unscheduled DNA synthesis and DNA methylation. All of these changes at molecular level are known to contribute to the pathogenesis of cancer. One of the prominent NOCs found in Kashmiri food is $N$-Nitrosodimethylamine (NDMA). Here we review the occurrence of NDMA in sundried foods, dried fish, kehwa, traditional pickle, $Brassica$ $oleracia$ and $tobbaco$. We also discuss its possible role in the high prevalence of gastrointestinal cancers in Kashmir.

Synthesis and Antibiotic activity of Dextran-Phthalysulfathiazole (Dextran-Phthalylsulfathiazole의 합성과 항균성)

  • 김판기;이기창;황성규;오세영
    • Journal of Food Hygiene and Safety
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    • v.12 no.3
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    • pp.228-233
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    • 1997
  • Drug Dclivcry system (DDS) purpose to getting better remedial result by improving medication from ordinary methods. Applied for DDS, to improve selectivity and comtinuity during absorbing and delivery step, polmer drug (prodrug) was prepared by the esterification with dextran in such of biodegradable polymer and phthalylsulfathiazole with is efficient for entilitis. The polymer durg was prepared with dextran and phthalylsulfathiazole by the esterification. The synthetic procedures of polymer drug was performed by acid chloride and DCC methods. Polymer drug was synthesized in high yield by acid chloride method than DCC method. The antibiotic activities of polymer drug exhibited growth-inhibitory activity against Staphylococcus aureus, Staphylococcus epidermidis, E. coli, Salmonella typhimurium, Klebsiella pneumoniae at the concentration of 500 *g/m* in general through in vitro. As a result of test, polymer drug has 1/2 MIC than phthalylsulfathiazole. Also, it has high level MIC as much as phthalylsulfathiazole with Proteus, Pseudomonas. We conducted possibility of DDS as an applied for medicine with synthesized polymer drug by using natrural polymer. We consider that clinical research must be followed to verify safety and efficacy for controlled release, activity and toxicity.

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SoC Implementation of Deblocking Filter for Block-based Compressed Images and Videos (블록 기반 압축 이미지 및 비디오를 위한 디블로킹 필터의 SoC 구현)

  • Seo, Gwang-Seok;Lee, Joo-Heung
    • Journal of IKEEE
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    • v.23 no.3
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    • pp.925-933
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    • 2019
  • In this paper, we implement ZYNQ SoC-based post-processing system that utilizes partial reconfiguration to remove blocking artifacts generated by compression algorithm. Hardware implementation of the deblocking filter in a Field Programmable Gate Array (FPGA) provides high computational capability and can be partially reconfigured to process 1080p images in real time. Partially reconfigurable areas in FPGA can be utilized to use hardware more efficiently in highly resource-constrained embedded systems. Experimental results of the proposed system show improvement of visual quality both objectively and subjectively with 0.6dB higher PSNR after deblocking filtering process. The measured power consumption of the deblocking filter during run-time is 68.33mW.

Preparation of High GABA-Enriched Yeast Extract by Non-Saccharomyces Yeasts Isolated from Korean Traditional Fermented Soybean Product

  • Song, Nho-Eul;Lee, Da-Bin;Lee, Seon-Hye;Baik, Sang-Ho
    • Microbiology and Biotechnology Letters
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    • v.49 no.3
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    • pp.320-328
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    • 2021
  • High GABA-enriched yeast extract, for various nutritionally and pharmaceutically important functional foods, was prepared using a novel isolate of Debaryomyces hansenii JBCC541. Under optimized conditions, GABA conversion rates are significantly enhanced up to 7.55 g/l by D. hansenii JBCC541, increasing their synthesis yield 40 times. The total amino acid content of the prepared yeast extract was 10733.86 mg/l (257.36 mg/g), consisting of alanine, lysine, glutamine, leucine, and valine as the primary amino acids. The GABA content was significantly enhanced up to 6790 mg/l (162.80 mg/g) in the presence of glutamic acid, with approximately 10-fold higher GABA production. Flavor amino acids were also highly enhanced, indicating that the prepared yeast extract might be useful for preparing various functional and sensuous foods. Our results were promising as a GABA-enriched yeast extract preparation tool ensuring a suitable food material level with the potential for functionally enhanced food industrial applications.

A Study on the Adsorption Kinetics of 133Cs by Different Impregnations of Prussian Blue (프러시안 블루 고정화에 따른 133Cs의 흡착거동 모델링)

  • Choi, S.S.;Lee, Y.J.;Yun, K.J.;Cho, Y.J.;Lee, J.H.;Lee, S.H.
    • Journal of the Korean Society of Safety
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    • v.36 no.1
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    • pp.80-85
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    • 2021
  • Radionuclides, particularly radioactive cesium (Cs), are a concern of human health in some nuclear power accidents. It could lead to a high level of intracellular accumulation due to its high radioactivity and long half-life. Therefore, it is imperative to develop a method to remove Cs from wastewater. Herein, we synthesized activated carbon fibers (ACFs) doped with Prussian blue (PB) via in situ methods. We classified samples by their preparation method as either physical (PB-ACF-A) or physicochemical (PB-ACF-B) syntheses for comparison. The PB-ACF-B sample showed a significant surface loss compared to PB-ACF-A but a better 133Cs adsorption capacity. All samples fit well to Langmuir isotherms and the values of qmax were directly correlated to the amount of PB on the surface of the ACFs. Adsorption characteristics were further confirmed by the calculated free energy, enthalpy, and entropy.

Expression of Genes Affecting Skin Coloration and Sugar Accumulation in 'Hongro' Apple Fruits at Ripening Stages in High Temperatures (고온에 의한 변색단계별 '홍로' 사과의 착색 및 당 축적 관련 유전자 발현 분석)

  • Kim, Seon Ae;Ahn, Soon Young;Yun, Hae Keun
    • Journal of Bio-Environment Control
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    • v.25 no.1
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    • pp.9-15
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    • 2016
  • High temperature is one of the important environmental factors limiting cultivation of apple (Malus domestica Borkh). The expression of genes related with anthocyanin synthesis and sugar accumulation in response to high temperature was studied in the 'Hongro' apple fruits at different developmental stages in different temperature conditions through real-time PCR. Expression of ${\hat{a}}$-amylase (BMY) and polygalacturonase (PG) genes related with sugar synthesis was higher in late ripening stages than in initial ripening stages. Expression of four genes such as phenylalanine ammonia-lyase (PAL), chalcone synthase (CHS), flavanone 3-hydroxylase (F3H), and malate dehydrogenase (MDH), which were related with fruit skin coloration, increased gradually in apple fruits of the middle and late ripening stages. Interestingly, the expressions of all genes were highly inhibited expressed at $30-35^{\circ}C$ compared to $25^{\circ}C$ in all ripening stages. In the further work, investigation of expression levels of various genes could be conducted in the level of transcriptomics in fruits at the middle ripening stages to get meaningful information of ripening metabolism in apple in high temperatures.

Kisspeptin-10 Enhanced Egg Production in Quails Associated with the Increase of Triglyceride Synthesis in Liver

  • Wu, J.;Fu, W.;Huang, Y.;Ni, Y.;Zhao, R.
    • Asian-Australasian Journal of Animal Sciences
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    • v.26 no.8
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    • pp.1080-1088
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    • 2013
  • Our previous results showed that kisspeptin-10 (Kp-10) injections via intraperitoneal (i.p.) once daily for three weeks notably promoted the egg laying rate in quails. In order to investigate the mechanism behind the effects of Kp-10 on enhancing the egg laying rate in birds, this study focused on the alternations of lipids synthesis in liver after Kp-10 injections. 75 female quails (22 d of age) were allocated to three groups randomly, and subjected to 0 (control, Con), 10 nmol (low dosage, L) and 100 nmol (high dosage, H) Kp-10 injections via i.p. once daily for three weeks, respectively. At d 52, quails were sacrificed and sampled for further analyses. Serum $E_2$ concentration was increased by Kp-10 injections, and reached statistical significance in H group. Serum triglyceride (TG) concentrations were increased by 46.7% in L group and 36.8% in H group, respectively, but did not reach statistical significance, and TG contents in liver were significantly elevated by Kp-10 injections in a dose-dependent manner. Serum total cholesterol (Tch) concentrations significantly decreased in H group, while in H group the hepatic Tch content was markedly increased. The level of non-esterified fatty acid (NEFA), apolipoprotein A1 and B (apoA1 and apoB) were not altered by Kp-10 injections. The genes expression of sterol regulatory element binding protein-1 (SREBP-1), fatty acid synthetase (FAS), apolipoprotein VLDL-II (apoVLDL-II), cholesterol $7{\alpha}$-hydroxylase (CYP7A1) and vitellogenin II (VTG-II) were significantly up-regulated by high but not low dosage of Kp-10 injection compared to the control group. However, the expression of SREBP-2, acetyl-CoA carboxylase ($ACC_{\alpha}$), malic enzyme (ME), stearoyl-CoA (${\Delta}9$) desaturase 1 (SCD1), apolipoprotein A1 (apoA1), fatty acid binding protein 2 (FABP2), 3-hydroxyl-3-methyl glutaryl-coenzyme A reductases (HMGCR), estrogen receptor ${\alpha}$, ${\beta}$($ER{\alpha}$ and ${\beta}$) mRNA were not affected by Kp-10 treatment. In line with hepatic mRNA abundance, hepatic SREBP1 protein content was significantly higher in H group. Although the mRNA expression was not altered, the content of $ER{\alpha}$ protein in liver was also significantly increased in H group. However, SREBP-2 protein content in liver was not changed by Kp-10 treatment. In conclusion, exogenous Kp-10 consecutive injections during juvenile stage significantly advanced the tempo of egg laying in quails, which was associated with the significant elevation in hepatic lipids synthesis and transport.