• Title/Summary/Keyword: c-MES

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Synthesis and Anticonvulsant Evaluations of N-Cbz-$\alpha$-amino-N- alkoxyglutarimides

  • Kim, Min-Jeong;Byun, Ae-Sun;Choi, Jong-Won;Moon, Kyung-Ho;Lee, Chung-Kyu;Park, Min-Soo
    • Archives of Pharmacal Research
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    • v.27 no.2
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    • pp.151-155
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    • 2004
  • In our previous studies for the development of new anticonvulsant of broad spectrum, we found that N-cbz-$\alpha$-aminoglutarimides showed significant anticonvulsant activities of broad spectrum enough to be recommended for the new anticonvulsants and their anticonvulsant activities were dependent on their imide substituent groups. Based on these results, various N-cbz--$\alpha$-amino-N-alkoxyglutarimides, where the imide N-H was substituted with the hydroxy and alkoxy group, were prepared and evaluated for their anticonvulsant activities using the Maximal electroshock seizure (MES) and Pentylenetetrazole induced seizure (PTZ) tests and also the rotorod test. A series of (R) or (S)-N-cbz--$\alpha$-amino-N-alkoxyglutarimides could be prepared from the corresponding (R) or (S)-N-cbz-glutamic acid following the usual synthetic procedure. Among them, (R)-N-cbz--$\alpha$-amino-N-hydroxyglutarimide ($ED_{50}$=86.25 mg/kg) was most active in the MES test. In the case of the PTZ test, (R)-N-cbz--$\alpha$-amino-N-benzyloxyglutarimide ($ED_{50}$= 62.5 mg/kg) was most active. Among the tested compounds, 2a-c, 3a, and 3b showed anticonvulsant activities in the MES and PTZ test. All of the tested compounds, except 2f and 3f, showed significant anticonvulsant activities in the MES or PTZ test. In addition, the neurotoxicities of these compounds were comparable to other anticonvulsant drugs.

Microbiological Characteristics of Low Salt Mul-kimchi (저염 물김치의 미생물균총 특성)

  • Oh, Ji-Young;Hahn, Young-Sook;Kim, Young-Jin
    • Korean Journal of Food Science and Technology
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    • v.31 no.2
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    • pp.502-508
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    • 1999
  • Microbiological characteristics of low salt Mul-kimchi was examined. Mul-kimchi was prepared by mixing of radish (25%), green onion (2.4%), red pepper (1.9%), garlic (1.9%) and salt (0, 0.2, 0.5, 1.0, 1.5, 2.0, 2.5, 2.5, 3.0%) in water and fermented at 4, 15 and $25^{\circ}C$ for 10 days, respectively. During fermentation period, total cell, Leuconostoc sp., Lactobacillus sp., Streptococcus sp., Pediococcus sp., coliform bacteria, gram (-) bacteria and yeast cell number were counted on their selection media. The microbes in Mul-kimchi were isolated and identified. Total cell number increased as salt concentration decreased and fermentation temperature increased. Lactic acid bacteria showed the highest number in 1.0% salt concentration. Yeast cell number increased with increase of salt concentration. Lactobacillus sp. were identified Lactobacillus plantarum and L. pentosus in Mul-kimchi containing $0.2{\sim}1.0%$ salt while those of Mul-kimchi containing 3.0% salt were Lactobacillus plantarum and L. brevis. The other lactic acid bacteria were identified Leuconostoc citrum, Leu.mes.ssp.mesenteroides/dextranicum and streptococcus facium in Mul-kimchi containing $0{\sim}3.0%$ salt while Pediococcus sp. was not detected. Gram-negative Aeromonas hydrophila, Pseudomonas fluorescens, Pseu. aureofaciens and yeast Candida pelliculosa, Cryptococcus laurentii were identified in the Mul-kimchi.

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The Effect of N-Substituted Alkyl Groups on the Anticonvulsant Activities of N-Cbz-${\alpha}$-amino-N-alkylsuccinimides

  • Lee, Jae-Won;Son, Ki-Chun;Jung, Kyung-Im;Choi, Jong-Won;Park, Min-Soo
    • Archives of Pharmacal Research
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    • v.20 no.1
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    • pp.53-57
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    • 1997
  • For the purpose of defining the effects of the N-substituted alkyl groups on the anticonvulsant activities of N-Cbz-.alpha.-aminosuccinimides, various (R)- and (S)-N-alkyl substituted N-Cbz-.alpha.-aminosuccinimides (1 and 2) were prepared from the corresponding (R)- and (S)-N-Cbz-aspartic acid by using known reaction and were evaluated the anticonvulsant activies in the MES and PTZ tests, including their neurotoxicities. The most active compound in the MES test was (R)N-Cbz-.alpha.-amino-N-methylsuccinimide (1b) $(ED_{50}=52.5 mg/kg, Pl=3.2)$. And in case of the PTZ test, (R)-N-Cbz-.alpha.-amino-N-ethylsuccinimide (1c) was the most active compound $(ED_{50}/=32.5mg/kg, Pl=3.1)$. The order of anticonvulsant activities of these compounds against the MES test, as judged from the ED_50values for the R series (1), was N-methyl > N-isobutyl > non-substituted > N-ethyl, N-allyl > N-benzyl compound; for the S series (2) N-methyl > N-altyl > non-substituted > N-isobutyl > N-ethyl > N-benzyl compound. The anticonvulsant activities in the PTZ tests of these compounds exhibited somewhat different pattern ; for the R series (1) Nethyl > N-methyl > N-isobutyl> non-substituted > N-allyl > N-benzyl compound in order of decreasing activity; for S series (2) N-ethyl > N-allyl, non-substituted > N-isobutyl > N-methyl > N-benzyl compound in order of decreasing activity.

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Lysophosphatidic acid increases mesangial cell proliferation in models of diabetic nephropathy via Rac1/MAPK/KLF5 signaling

  • Kim, Donghee;Li, Hui Ying;Lee, Jong Han;Oh, Yoon Sin;Jun, Hee-Sook
    • Experimental and Molecular Medicine
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    • v.51 no.2
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    • pp.9.1-9.10
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    • 2019
  • Mesangial cell proliferation has been identified as a major factor contributing to glomerulosclerosis, which is a typical symptom of diabetic nephropathy (DN). Lysophosphatidic acid (LPA) levels are increased in the glomerulus of the kidney in diabetic mice. LPA is a critical regulator that induces mesangial cell proliferation; however, its effect and molecular mechanisms remain unknown. The proportion of ${\alpha}-SMA^+/PCNA^+$ cells was increased in the kidney cortex of db/db mice compared with control mice. Treatment with LPA concomitantly increased the proliferation of mouse mesangial cells (SV40 MES13) and the expression of cyclin D1 and CDK4. On the other hand, the expression of $p27^{Kip1}$ was decreased. The expression of $Kr{\ddot{u}}ppel$-like factor 5 (KLF5) was upregulated in the kidney cortex of db/db mice and LPA-treated SV40 MES13 cells. RNAi-mediated silencing of KLF5 reversed these effects and inhibited the proliferation of LPA-treated cells. Mitogen-activated protein kinases (MAPKs) were activated, and the expression of early growth response 1 (Egr1) was subsequently increased in LPA-treated SV40 MES13 cells and the kidney cortex of db/db mice. Moreover, LPA significantly increased the activity of the Ras-related C3 botulinum toxin substrate (Rac1) GTPase in SV40 MES13 cells, and the dominant-negative form of Rac1 partially inhibited the phosphorylation of p38 and upregulation of Egr1 and KLF5 induced by LPA. LPA-induced hyperproliferation was attenuated by the inhibition of Rac1 activity. Based on these results, the Rac1/MAPK/KLF5 signaling pathway was one of the mechanisms by which LPA induced mesangial cell proliferation in DN models.

Analysis of Transcriptional Activity and Estrogen Responsiveness of Regulatory Elements in Chicken Ovalbumin Promoter (닭 오브알부민 프로모터의 길이에 따른 유전자 발현 활성 및 에스트로겐 반응성 분석)

  • Yang, Hyeon;Kim, Kyung-Woon;Kim, Jeom Sun;Woo, Jae-Seok;Lee, Hwi-Cheul;Choi, Hoonsung;Jung, Sun Keun;Sureshkumar, Shanmugam;Lee, Haesun;Oh, Keon Bong;Byun, Sung June
    • Korean Journal of Poultry Science
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    • v.46 no.1
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    • pp.17-24
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    • 2019
  • Chickens have been considered as well-defined animal bioreactor. The optimized ovalbumin promoter is essential for recombinant protein production in transgenic chicken. Here we try to compare the activity and identify the effect of estrogen on ovalbumin promoter according to each promoter length with estrogen response element (ERE) existence. We cloned two (2.8 and 5.5 kb) ovalbumin promoters that the 5.5 kb contained the ERE but the 2.8 kb did not, and these two promoters were cloned to pGL4.11 vector. Additionally, we constructed another pGL4.11 vector containing of the 4.4 kb (with ERE) ovalbumin promoter deleted with 1 kb between ERE region and the 2.8 kb promoter. For reporter assay, HeLa, MES-SA, LMH/2A, and cEF cells were transfected with all the pGL4.11 vectors. The comparative analysis showed that the mutated 4.4 kb promoter has more potent activity than the 2.8 and 5.5 kb promoters in HeLa, MES-SA, and LMH/2A cells. However, there is no significant difference in cEFs. Also, these cells transfected with the mutated 4.4 kb promoter were treated with the $17{\beta}$-estradiol (0~3,000 nM) and HeLa, MES-SA, and LMH/2A cells showed estrogen responsibilities, but cEFs did not. Besides, the mutated 4.4 kb promoter has still higher activity than the 2.8 and 5.5 kb promoter, and there is no transcriptional induction effect in 2.8 kb promoter at 500 nM estrogen that is blood concentration of laying hens. Hence our study strongly suggested that the mutated 4.4 kb promoter is considered as one of the most efficient length for generating transgenic chicken.

Synthesis of 6-Alkyloxyl-3,4-dihydro-2(1H)-quinoliones and Their Anticonvulsant Activities

  • Quan, Zhe Shan;Wang, Jun-Min;Rho, Jung-Rae;Kwak, Kyung-Chell;Kang, Hee-Cheol;Jun, Chang-Soo;Chai, Kyu-Yun
    • Bulletin of the Korean Chemical Society
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    • v.26 no.11
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    • pp.1757-1760
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    • 2005
  • A series of 6-alkyloxyl-3,4-dihydro-2(1H)-quinoliones (5a-5n) were synthesized through nitration, reduction, diazotization, hydrolysis and alkylation from 3,4-dihydro-2(1H)-quinolione. Their structures were characterized by IR, $^1H$-NMR and MS. The anticonvulsant activity was evaluated by the Maximal electroshock test (MES) and the subcutaneous pentylenetetrazole (Metrazole) test (sc-Met). The neurotoxicity was measured by the Rotarod test (Tox). The result showed that 6-hexyloxy-3,4-dihydro-2 (1H)-quinolinone (5c) was potent in anti-MES and anti-scMet test with $ED_{50}$ of 24.0 mg/kg and 21.2 mg/kg, respectively, albeit its $TD_{50}$ (67.6 mg/kg) revealed the high neurotoxicity. 6-Benzyloxy-3,4-dihydro-2(1H)-quinolinone (5f) was less effective against MES induced seizure with $ED_{50}$ of 29.6 mg/kg, but no neurotoxicity was observed even under 300 mg/kg. Its Protective index (PI) was greater than 10 preferable to Phenytoin, Carbamazepin, Phenobarbital and Valproate.

A study on the establishment of an MES system that converges design, processing, and measurement during cutting (절삭가공 시 설계, 가공, 측정을 융합한 MES 시스템 구축에 관한 연구)

  • Park, Hae-Woong;Lee, Seung-Wook;Han, Heui-Bong;Yun, Jae-Woong;Choi, Kye-Kwang;Han, Seong-Ryeol;Kim, Kyung-A;Lee, Chun-Kyu
    • Design & Manufacturing
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    • v.15 no.2
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    • pp.42-48
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    • 2021
  • In this paper, when manufacturing large/multi-mold parts (more than 30 core parts),A mold manufacturing (tolerance) management system was established through design-processing linkage.The mold manufacturing (tolerance) management system is a design-based measurement shape/measurement position determination system, M/C processing-linked measurement drive system,It is composed of four parts: CAD-linked measurement result analysis system and manager mold part quality management system.In addition, the constructed system was applied to the field and the effect of system construction was evaluated by comparing it with the existing process.As a result of the evaluation, the measurement precision is within 0.02mm, and the time it takes to measure after the end of processing is shorter than that of the existing process.(12 hours → 2 hours) It was shortened to 16.7%.In addition, it was confirmed that the time required for reprocessing after measurement was reduced by 25% (4 hours → 1 hour) compared to the existing process.

Microfabricated Disposable Microchip with a Capillary Electrophoresis and Integrated Amperometric Detection (모세관 전기영동 및 전기화학적 검출 시스템을 위한 일회용 마이크로칩)

  • Kim, Ju-Ho;Kang, C.J.;Kim, Yong-Sang
    • Proceedings of the KIEE Conference
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    • 2004.07c
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    • pp.2131-2133
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    • 2004
  • 모세관 전기영동 및 전기화학적 검출 시스템을 마이크로 시스템에 적용하여 ITO 유리기판과 polydimethylsiloxane (PDMS)로 제작하였다. 제작된 모세관 전기영동 및 전기화학적 검출 시스템은 일회용으로 사용가능하며 전기화학적 검출에 아주 적합한 특성을 보인다. 모세관 전기영동 및 전기화학적 검출 시스템은 주입과 분리 채널 (80 ${\mu}m$${\sim}$ 40 ${\mu}m$ 깊이)을 가진 PDMS 층과 유리기판 위에 검출 전극으로 사용되는 ITO가 형성된 층으로 구성된다. PDMS 층과 ITO 유리 기판은 UV-$O_3$ cleaner를 사용하여 접합하였다. 완충용액은 10 mM 2-(N-morpholino)ethanesulfonic acid (MES)를 사용하였고 분석물질은 1 mM 농도의 dopamine과 1 mM 농도의 catechol을 사용하였다. 60 V/cm 전계로 주입 및 분리를 하였으며 작업전극과 기준전극 간의 전위는 +600 mV로 유지하며 분석물질의 농도에 비례하는 전류량법으로 측정하였다. 전기화학적 검출 회로는 천기영동 전계의 간섭으로부터 분리하였다. 10 mM MES 완충용액에서 바탕 전류의 크기가 ${\sim}$10 pA 일 때 측정전류 값은 10 nA이다. 측정된 피크 값은 기존의 Au 전극과 비교하여 선택성, 감도, 분해능이 유사한 특성을 보여준다.

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Screening of high Antibacterial Lactic Acid bacteria for the Preparation of Dongchimi-Juice for Naengmyon (냉면용 동치미액 제조를 위한 항균 활성이 높은 젖산균의 선발)

  • 조신호
    • The Korean Journal of Food And Nutrition
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    • v.12 no.1
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    • pp.69-76
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    • 1999
  • In order to screen lactic acid bacterial starter having high antibacterial activity and giving good flavor in Dongchmi for Naengmyon antibacterial activity and acid producing ability of 24 strains of Kimchi lactic acid bacteria were tested. Among 24 strains tested Leuconostoc mesenteroides subsp. mesenteroides C16, Leu. paramesenteroides C18 Lactobacillus bavaricus B01, B06, C19, C32 Lac. homohiochii B21 and B22 showed high antibacterial activity and their antibacterial activities were more active against Listeria monocytogenes and Staphylococcus aureus than against Escherichia coli and Salmonella typhimurium. The odors of Dongchimi-juices fermented with Leu. mesenteroides or Leu. paramesenteroides were more favorable than those with Lac. bavaricus or Lac. homohiochii. But the odors of Naengmyon-broths which were made with each Dongchimi-juice were not significantly different each other. In consideration of antibacterial ac-tivity and flavor of Dongchimi-juice two strains of lactic acid bacteria Lac. homohiochii B21 and Leu. mes-enteroides subsp. mesenteroides C16 were finally screened out as Dongchimi starters.

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