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The α-Effect in Nucleophilic Substitution Reactions of Y-Substituted-Phenyl X-Substituted-Cinnamates with Butane-2,3-dione Monoximate

  • Kim, Min-Young;Son, Yu-Jin;Um, Ik-Hwan
    • Bulletin of the Korean Chemical Society
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    • v.34 no.10
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    • pp.2877-2882
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    • 2013
  • Second-order rate constants ($k_{Ox^-}$) have been measured spectrophotometrically for nucleophilic substitution reactions of 4-nitrophenyl X-substituted-cinnamates (7a-7e) and Y-substituted-phenyl cinnamates (8a-8e) with butane-2,3-dione monoximate ($Ox^-$) in 80 mol % $H_2O$/20 mol % DMSO at $25.0{\pm}0.1^{\circ}C$. The Hammett plot for the reactions of 7a-7e consists of two intersecting straight lines while the Yukawa-Tsuno plot exhibits an excellent linearity with ${\rho}_X$=0.85 and r=0.58, indicating that the nonlinear Hammett plot is not due to a change in the rate-determining step but is caused by resonance stabilization of the ground state (GS) of the substrate possessing an electron-donating group (EDG). The Br${\o}$nsted-type plot for the reactions of Y-substituted-phenyl cinnamates (8a-8e) is linear with ${\beta}_{lg}$ = -0.64, which is typical of reactions reported previously to proceed through a concerted mechanism. The ${\alpha}$-nucleophile ($Ox^-$) is more reactive than the reference normal-nucleophile ($4-ClPhO^-$). The magnitude of the ${\alpha}$-effect (i.e., the $k_{Ox^-}/k_{4-ClPhO^-}$ ratio) is independent of the electronic nature of the substituent X in the nonleaving group but increases linearly as the substituent Y in the leaving group becomes a weaker electron-withdrawing group (EWG). It has been concluded that the difference in solvation energy between $Ox^-$ and $4-ClPhO^-$ (i.e., GS effect) is not solely responsible for the ${\alpha}$-effect but stabilization of transition state (TS) through a cyclic TS structure contributes also to the Y-dependent ${\alpha}$-effect trend (i.e., TS effect).

The clinical effects of Rabeprazole sodium (Pariet$\circledR$) in the treatment of Laryngopharyngeal Reflux (인후두역류질환 ( Laryngopharyngeal Reflux Disease. LPRD )에서 Rabeprazole Sodium (Pariet$\circledR$)의 임상효과)

  • 최홍식;김한수;최현승
    • Proceedings of the KOR-BRONCHOESO Conference
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    • 2002.12a
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    • pp.9-9
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    • 2002
  • 이비인후과 영역에 있어서 위산 역류에 의한 질환의 진단은 쉽지 않고 분명하지 않은 점이 많지만, 병변의 영향은 광범위하며, 실제로 역류에 의한 증상을 가지고 내원하는 환자도 증가하는 추세이다. 인후두역류질환의 치료는 크게 생활습관의 변경, 약물복용, 항역류수술로 나눌 수 있으며, 사용약제는 크게 두 부류로 나누는데, 제산제, H2 수용체 차단제, PPI(Proton Pump Inhibitor) 제제와 같은 산억제 약물군과 Prokinetic 약물군이다. Rabeprazole sodium(Pariet(R))은 PPI 제제에 해당하는 약제로 기존의 omeprazole, lansoprazole, pantoprazole과는 달리 대사 과정 중 CYP2C19에 대한 의존도가 낮아, 개체 간 차이가 적고 빠르고 일정하게 산분비 억제 효과를 나타내는 것으로 알려져 있은 약물이다. 2001년 5월부터 2002년 4월까지 32개 병원에서 Pariet(R) 를 복용한 2166명의 환자를 대상으로 분석하였다. 복용기간에 따라 4군(1군;1-14일, 2군;15-28일, 3군;29-56일, 4군:57일 이상)으로 나누었으며, 8가지 증상(Heart burn, Regurgitation, Chronic cough, Hoarseness, Globus sensation, Chronic throat clearing, Sore throat, Dysphagia)에 대한 호전 여부 및 후두내시경상 개선 정도, 의사에 의한 유용도 평가, 부작용 발생 여부에 대해 연구하였다. 증상개선율 50%이상을 치료 반응군으로 했을때 전체 2166명중 1627명(75.1%)에서 증상의 호전을 보았으며, 이는 복용기간이 길수록 증가하였다. 후두 내시경상 개선 정도는 현저한 개선이 32.9%, 중등도 개선이 38.7%로 대부분 환자에서 객관적인 병변의 호전을 보였으며, 유용도 평가에서는 매우 유용이 37.6%, 유용이 50.3%로 치료효과에 대한 만족도도 높은 것을 알수 있었다. PPI 제제의 부작용으로 보고되고 있는 두통, 오심, 설사, 복통. 변비, 어지럼증. 피곤 중. 소수의 환자가 두통을 호소하였으나, 그다지 심각한 정도는 아니었다. 인후두역류증 치료제로서 Pariet(R) 는 비교적 안전하고 효과가 높은 약물임이 임상 연구 결과 밝혀졌기에 보고하는 바이다.

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Biological and Physicochemical Properties of Canine Parvovirus lated from the Dogs with Diarrhea (설사증 나환견으로 부터 분리한 Canine Parvovirus의 성상에 관한 연구)

  • 최해연;정운선;전무형;박성국;민원기
    • Korean Journal of Veterinary Service
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    • v.13 no.2
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    • pp.162-183
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    • 1990
  • From 1988 to 1989, 8 strains of canine parvovirus-2 (CPV-2) were isolated from the fecal specimens from the dogs that were clinically diagnosed as canine parvoviral enteritis in the veterinary hospitals located in the regions of Taejon and Chungbuk province. Studios on biological and physicochemical properties for the isolates were carried out. The results obtained by experiments are summarized as follows. 1. Among 62 fecal samples collected from the dogs with enteric diseases, 24 (38.7%) showed the haemagglutinating activity against porcine erythrocyte, ranging from 16 to 16, 384 of HA titers. 2. When 8 fecal specimens with high HA titer over 1, 000 were inocultated into CRFX cells, intranuclear inclusion bodies were obseverd in all of eight specimens, of w)lick three specimens showed cytoplasmic inclusions concurrently with the intranuclear inclusion bodies. 3. In study on species-specificity of haemagglutinating activity of the isolates, TJ-89-1 and TJ-89-2, it was found that the isolates revealed the highest haemagglutinating activity with porcine erythrocytes, showing the relatively lower haemagglutination titers with the erythrocytes from cat and rabbit. None of erythrocytes from other animals reacted with the isolates. 4. By the cross-haemagglutination inhibition test of the Isolates with reference viruses and sera, the Isolates were evidently identified as the strains of canine parvovirus-2. 5. In Physicochemical property test, it was evident that the isolates were stable in, lipid solvent, pH and heat treatment at $56^{\circ}C$ for 30 min. and contain DNA genome. 6. When seven puppies were inoculated intraorally with the isolate at HA titer of 8, 192, all of the puppies showed the symptoms of anorexia, vomiting, diarrhea and died at the 5th to 10th days post inoculation(pi). The fecal samples from all of the puppies revealed significantly high HA titers afterward the 5th days pi. Body temperature and the number of total leucocytes were slightly increased at the early stage of infection. but extremely decreased at the stage of collapse. HI titers of the sera started to increase at the 2nd to 3rd days pi reaching 512 to 1, 024 at the 4th to 5th day pi.

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Research on ultra-precision fine-pattern machining through single crystal diamond tool fabrication technology (단결정 다이아몬드공구 제작 기술을 통한 초정밀 미세패턴 가공 연구)

  • Jung, Sung-Taek;Song, Ki-Hyeong;Choi, Young-Jae;Baek, Seung-Yub
    • Design & Manufacturing
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    • v.14 no.3
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    • pp.63-70
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    • 2020
  • As the consumer market in the VR(virtual reality) and the head-up display industry grows, the demand for 5-axis machines and grooving machines using on a ultra-precision machining increasing. In this paper, ultra-precision diamond tools satisfying the cutting edge width of 500 nm were developed through the process research of a focused ion beam. The material used in the experiment was a single-crystal diamond tool (SCD), and the equipment for machining the SCD used a focused ion beam. In order to reduce the influence of the Gaussian beam emitted from the focused ion beam, the lift-off process technology used in the semiconductor process was used. 2.9 ㎛ of Pt was coated on the surface of the diamond tool. The sub-micron tool with a cutting edge of 492.19 nm was manufactured through focused ion beam machining technology. Toshiba ULG-100C(H3) equipment was used to process fine-pattern using the manufactured ultra-precision diamond tool. The ultra-precision machining experiment was conducted according to the machining direction, and fine burrs were generated in the pattern in the forward direction. However, no burr occurred during reverse machining. The width of the processed pattern was 480 nm and the price of the pitch was confirmed to be 1 ㎛ As a result of machining.

In Vitro Effects of Cooking Methods on Digestibility of Lipids and Formation of Cholesterol Oxidation Products in Pork

  • Hur, Sun Jin;Lee, Seung Yuan;Moon, Sung Sil;Lee, Seung Jae
    • Food Science of Animal Resources
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    • v.34 no.3
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    • pp.280-286
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    • 2014
  • This study investigated the effects of cooking methods on the digestibility of lipids and formation of cholesterol oxidation products (COPs) in pork, during in vitro human digestion. Pork patties were cooked using four different methods (oven cooking, pan frying, boiling, and microwaving), to an internal temperature of approximately $85^{\circ}C$. The digestibility of pork patties were then evaluated, using the in vitro human digestion model that simulated the composition (pH, minerals, surfaceactive components, and enzymes) of digestive juices in the human mouth, stomach, and small intestine. The total lipid digestibility was higher after microwave cooking, whereas pan-frying resulted in lower in vitro digestibility, compared to the other cooking methods. The microwaving method followed by in vitro digestion also showed significantly higher content of free fatty acids and thiobarbituric acid reactive substances (TBARS), compared to the other cooking methods; whereas, the pan frying and boiling methods showed the lowest. Cholesterol content was not significantly different among the cooked samples before, and after in vitro human digestion. The formation of COPs was significantly higher in the microwave-treated pork samples, compared to those cooked by the other methods, which was consistent with the trend for lipid peroxidation (TBARS). We propose that from the point of view of COPs formation and lipid oxidation, the pan-frying or boiling methods would be useful.

Pattern Development of Tight-fitting Pants for Men Using Measurements of Size Korea 2004 (Size Korea 2004의 한국인 인체치수를 이용한 남성용 밀착 팬츠 패턴 개발)

  • Jeong, Yeon-Hee
    • Korean Journal of Human Ecology
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    • v.15 no.5
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    • pp.791-802
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    • 2006
  • The construction of athlete's tight-fitting garments by reducing the elastic knit pattern is an interesting subject, which directly influences the performance of the wearer. Therefore, relationships between the reduction rates of the men's pants pattern obtained using measurements of Size Korea 2004 and clothing fitting were explored to improve clothing comfort. Two pattern making methods were developed and the reduction rates were applied to those pants depending on the parts of human body. The four male subjects were university students in the ages of 20 to 24. Subjective wear sensations of the experimental garments were rated using seven Likert scales during 4 consecutive days. While wearing the garments, subjects were kept four various postures including waist flexion and sitting etc by requests of the researchers. Likert type scale was used for the evaluation and 7 point indicates that it gave the best fit as tight-fitting pants. As results, differences in the length and girth between two piece pants pattern(style 1) and one piece pants pattern(style 2) were 0.0$\sim$0.3cm. Between two pattern making methods, one piece pants pattern(the style 2) was superior to two piece pants pattern in terms of subjective sensation and fit. Among eight tight-fitting pants, C, D, G, H pants were superior in terms of fitting and stability of waist and hip part to the others. ill case of tight-fitting pants, the reduction rate of the pattern in the course direction, the reduction rate of T2/3(66%) was better than that of T/2(50%), but the reduction rate of the pattern in the wale direction, that of the part of crotch, which was very sensitive part, should be kept the same as suggested earlier by Ziegert(1988).

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Emission Characteristics of VOC due to Major Industrial Activities in the Ban Wall Industrial Complex (안산시 반월공단을 중심으로 한 주요 배출시설의 업종 및 배출시설별 VOC의 배출특성)

  • Im, M.S.;Kim, K.H.;Choi, Y.J.;Jeon, E.C.
    • Journal of Korean Society for Atmospheric Environment
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    • v.22 no.3
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    • pp.325-336
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    • 2006
  • The presence of volatile organic compounds (VOC), produced and released from both anthropogenic and natural sources, can accelerate the degradation of air quality in the surrounding area. In this study, we investigated the emission concentrations of VOC based on a total of 115 sample analysis made from 47 companies (representing 17 types of industry) at the Ban Wall industrial complex (Jun. 2004 to Jan. 2005). Through a statistical analysis of these measurement data, we inspected the emission characteristics of VOC in relation with industrial type and processing unit. When these data were compared each other, toluene was found to record the highest value of 423 ppb followed by ethylbenzene (68.3 ppb), m, p-xylene (43.6 ppb), o-xylene (27.2 ppb), styrene (23.9 ppb), and benzene (16.4 pub). In addition, by converting these VOC concentration data into malodor intensity, we attempted to account for their distribution patterns in terms of relative contribution to the malodor formation. The results of odor intensity conversion generally indicated that the odor intensities of individual VOC do not exceed the degree of 1. When our VOC results were compared against other odorous compounds measured concurrently, the results were highly contrasting each other. Despite relative insignificance as odorous compounds, these VOCs are generally found ubiquitously and in abundant quantities in this strong source area.

Role of Phospholipase $A_2$ in Hypoxia-Induced Renal Cell Injury

  • Choi, Won-Rak;Ko, Sun-Hee;Cho, Su-In;Woo, Jae-Suk;Jung, Jin-Sup;Lee, Sang-Ho;Kim, Yong-Keun
    • The Korean Journal of Physiology and Pharmacology
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    • v.3 no.1
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    • pp.93-100
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    • 1999
  • The present study was designed to assess the roles of $PLA_2$ activation and arachidonic acid (AA) metabolites in hypoxia-induced renal cell injury. Hypoxia increased LDH release in a dose-dependent manner in rabbit renal cortical slices, and this increase was significant after 20-min hypoxia. The hypoxia-induced LDH release was prevented by amino acids, glycine and alanine, and extracellular acidosis (pH 6.0). Buffering intracellular $Ca^{2+}$ by a chelator, but not omission of $Ca^{2+}$ in the medium produced a significant reduction in hypoxia-induced LDH release. The effect of hypoxia was blocked by $PLA_2$ inhibitors, mepacrine, butacaine, and dibucaine. A similar effect was observed by a 85-kD $cPLA_2$ inhibitor $AACOCF_3.$ AA increased hypoxia-induced LDH release, and albumin, a fatty acid absorbent, prevented the LDH release, suggesting that free fatty acids are involved in hypoxia-induced cell injury. These results suggest that $PLA_2$ activation and its metabolic products play important roles in pathogenesis of hypoxia-induced cell injury in rabbit renal cortical slices.

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Effect of Prostaglandin $E_2$ and Indomethacin on Electrical Activity of Isolated Cat Stomach (적출한 고양이 위(胃)의 전기활동에 미치는 prostaglandin $E_2$ 및 indomethacin의 영향)

  • Kim, Myung-Suk;Lee, Yoon-Lyur
    • The Korean Journal of Physiology
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    • v.17 no.1
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    • pp.63-69
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    • 1983
  • This study was conducted to investigate the effect of prostaglandin $E_2(PGE_2)$ and indomethacin upon the electrical activity of the isolated cat stomach muscle strips$(1.5{\times}7.0\;cm)$. Fifty-seven muscle strips, obtained from 57 cat stomachs(including corpus and antrum) were studied in a muscle chamber filled with Krebs solution(pH 7.4, temperature $36{\pm}0.5^{\circ}C$) aerated with 5% $CO_2$ in $O_2$. The electrical activity was recorded by five capillary electrodes (Ag-AgCl), of which two were placed on the corpus and three on the antrum. After recording of the electrical activity in normal Krebs solution, $PGE_2$ in concentrations of 0.25(N=7), 0.5(=7), 1(N=7) and $2{\times}10^{-7}\;M(N=6)$ were administered to 27 muscle strips, while indomethacin was applied in concentretions of 0.25(N=9), 0.5(N=10), 1(N=6) and $2{\times}10^{-3}\;M(N=5)$ to the remaining 30 strips. The mean frequency were minutely measured from each electrogastrogram. 1) By adding $PGE_2$ in all doses, gastric slow wave frequency increased significantly compared with that in resting state. 2) Following $PGE_2$ administration, peak slow wave frequency increased dose-dependently. 3) After indomethacin addition in all doses, the slow wave frequency decreased significantly compared with that in resting state. 4) Following indomethacin administration, incidence of complete abolition of slow wave increased dose-dependently, and its latent period decreased also in a dose-dependent manner. It is inferred from the above results that prostaglandin $E_2$ has a facilitatory role in the development of gastric slow wave in cat.

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Molecular Cloning of a Gene Encoding $\alpha$-L-Arabinofuranosidase from Hyperthermophile Thermotoga maritima and Characterization of Its Biochemical Properties

  • Keum, In-Kyung;Lee, Eun-Joo;Kim, Tae-Jip;Kim, Chung-Ho;Han, Nam-Soo
    • Proceedings of the Korean Society for Applied Microbiology Conference
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    • 2004.06a
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    • pp.273-277
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    • 2004
  • $\alpha$-L-Arabinofuranosidase ($\alpha$-L-AFase, EC 3.2.1.55) was isolated from hyperthermophilic microorganism, Thermotoga maritima. The open reading frame (ORF) of $\alpha$-L-AFase gene is 1,455 bp long and encodes 484 amino acid residues with a molecular weight of 55,265 Da. The ORF of $\alpha$-L-AFase gene was introduced into the E. coli expression vector, $_p/RSET-B, and overexpressed in E. coli BL21. The purified recombinant $\alpha$-L-AFase showed the highest activity at 10$0^{\circ}C$ and pH 5.5. The purified enzyme appeared to have no metal cofactor requirement. The Km and specific activity values of the recombinant enzyme were 0.99 mM and 1,200 U/mg on p-nitrophenyl-$\alpha$-L-arabinofuranoside. It released only L-arabinose from sugar beet arabinan, sugar beet debranched arabinan and oat spelts arabinoxylan but had no activity onarabinogalactan and gum arabic. This result suggests that L-arabinose could be produced from natural polysaccharides using this enzyme. Mutant enzymes which Glu26, Glu172 and Glu281 residues were replaced to alanine, aspartic acid or glutamine caused Kcat to decrease by a factor of between 10$^3$ and 10$^4$. Glu172 and Glu281 residues of $\alpha$-L-AFase are seemed to be the acid/base and nucleophile in catalytic reaction, respectively, and Glu26 is supposed to playa key role in substrate binding.ng.

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