• Title/Summary/Keyword: $\mu$ synthesis

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Synthesis of Higenamine and its Cardiovascular Effects in Rabbit: Evidence for ${\beta}-Adrenoceptor$ agonist (Higenamine의 합성 및 가토의 심혈관계에 미치는 영향 : 베타-아드레날린성 효능 약물)

  • Chang, Ki-Churl;Lim, Jung-Kyoo;Park, Chan-Woong
    • The Korean Journal of Pharmacology
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    • v.22 no.2
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    • pp.96-104
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    • 1986
  • Higenamine, dl-1-( 4-hydroxybenzyl)-6, 7-dihydroxy-1 ,2, 3 ,4-tetrahydroisoquinoline has been synthesized and evaluated for hemodynamic actions using rabbits under pentobarbital anesthesia. Concentration-related fall of mean blood pressure was observed, where diastolic blood presure was significantly lowered at 10 ug/kg/min or above (p<.05), while the systolic blood pressure was slightly increased or unaffected, thereby, causing increment of pulse pressure. No significant change was occured in heart rate, however, carotid artery blood flow was significantly (p<.05) increased. These actions were inhibited with pretreatment of 0.3 mg/kg of propranolol, beta-adrenoceptor antagonist, 5 minutes before infusion of higenamine indicating that higenamine compete with propranolol for the so-called beta adrenergic receptor. As comparison, the same procedure was applied to isoproterenol as well, where typical antagonism of propranolol against isoproterenol was shown. From these findings the vasodilating and diastolic blood pressure lowing effects could be explained in terms of cardiac beta stimulating action, however, dopamine receptor activation could not be excluded because no significant changes observed in chronotropism.

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Effect of Various Pear Cultivars at Different Fruit Development Stages on Antioxidant and Whitening Activities (배 품종별 생육 단계에 따른 산화방지 및 미백 효과)

  • Yim, Sun-Hee;Cho, Kwang-Sik;Choi, Jin-Ho;Lee, Ju-Hyun;Kim, Myung-Su;Lee, ByulHaNa
    • Korean Journal of Food Science and Technology
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    • v.48 no.1
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    • pp.59-65
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    • 2016
  • This study was carried out to investigate the total polyphenols, antioxidant activities, and melanin synthesis inhibition of several pear cultivars (Pyruspyrifolia). The total polypenolic content of five pear cultivars was high in the unripe developmental stage. Total polyphenolic content of the Chuwhangbae cultivar extract was higher than that of other pear cultivars regardless of the developmental stage. However, the total flavonoid content did not differ between cultivars or developmental stages. The phenolic compound, arbutin has an inhibitory effect on melanogenesis. Arbutin levels in pear cultivars declined as the fruit matured. The free radical scavenging activity of the extract also decreased as the fruit ripened. In B16F10 mouse melanoma cells, most of the cultivar extracts inhibited melanin synthesis by about 50% at a $100{\mu}g{\cdot}mL^{-1}$ concentration, except in the Gamcheonbae extract until 90 days after full bloom. We have confirmed that the extract of pear cultivars have antioxidant activity and skin-whitening effects.

Screening of Lactic Acid Bacteria for Strong Folate Synthesis and Optimization of Fermentation (고엽산 생산능의 유산균 탐색 및 발효 조건 최적화)

  • Du, Kyung Min;Park, Se Jin;Park, Myung Soo;Ji, Geun Eog
    • Korean Journal of Food Science and Technology
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    • v.46 no.3
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    • pp.328-333
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    • 2014
  • Folate is a water-soluble vitamin B that is required for the synthesis of amino acids and nucleic acids. It plays an important role in cell division and cell growth in several living organisms. The purpose of this study was to screen strong folate-synthesizing bacteria and to optimize their culture conditions for folate production. Folate production was quantified by microbiological assays by using folate-dependent strain Lactobacillus rhamnosus KCTC 3237. Folate derivatives were identified by LC-MS/MS. Of the 65 strains of bifidobacteria and lactobacilli tested, L. plantarum Fol 708 demonstrated the greatest ability to produce folate. Its optimal pH for folate production was 5.5 in a pH-controlled, lab-scale fermenter. Coculturing L. plantarum Fol 708 with L. brevis GABA 100 in a milk medium enhanced the level of folate produced in comparison to culturing L. plantarum Fol 708 alone.

Oxidative Inactivation of Peroxiredoxin Isoforms by H2O2 in Pulmonary Epithelial, Macrophage, and other Cell Lines with their Subsequent Regeneration (폐포상피세포, 대식세포를 비롯한 각종 세포주에서 H2O2에 의한 Peroxiredoxin 동위효소들의 산화에 따른 불활성화와 재생)

  • Oh, Yoon Jung;Kim, Young Sun;Choi, Young In;Shin, Seung Soo;Park, Joo Hun;Choi, Young Hwa;Park, Kwang Joo;Park, Rae Woong;Hwang, Sung Chul
    • Tuberculosis and Respiratory Diseases
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    • v.58 no.1
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    • pp.31-42
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    • 2005
  • Background : Peroxiredoxins (Prxs) are a relatively newly recognized, novel family of peroxidases that reduce $H_2O_2$ and alkylhydroperoxide into water and alcohol, respectively. There are 6 known isoforms of Prxs present in human cells. Normally, Prxs exist in a head-to-tail homodimeric state in a reduced form. However, in the presence of excess $H_2O_2$, it can be oxidized on its catalytically active cysteine site into inactive oxidized forms. This study surveyed the types of the Prx isoforms present in the pulmonary epithelial, macrophage, endothelial, and other cell lines and observed their response to oxidative stress. Methods : This study examined the effect of exogenous, excess $H_2O_2$ on the Prxs of established cell lines originating from the pulmonary epithelium, macrophages, and other cell lines, which are known to be exposed to high oxygen partial pressures or are believed to be subject to frequent oxidative stress, using non-reducing SDS polyacrylamide electrophoresis (PAGE) and 2 dimensional electrophoresis. Result : The addition of excess $H_2O_2$ to the culture media of the various cell-lines caused the immediate inactivation of Prxs, as evidenced by their inability to form dimers by a disulfide cross linkage. This was detected as a subsequent shift to its monomeric forms on the non-reducing SDS PAGE. These findings were further confirmed by 2 dimensional electrophoresis and immunoblot analysis by a shift toward a more acidic isoelectric point (pI). However, the subsequent reappearance of the dimeric Prxs with a comparable, corresponding decrease in the monomeric bands was noted on the non-reducing SDS PAGE as early as 30 minutes after the $H_2O_2$ treatment suggesting regeneration after oxidation. The regenerated dimers can again be converted to the inactivated form by a repeated $H_2O_2$ treatment, indicating that the protein is still catalytically active. The recovery of Prxs to the original dimeric state was not inhibited by a pre-treatment with cycloheximide, nor by a pretreatment with inhibitors of protein synthesis, which suggests that the reappearance of dimers occurs via a regeneration process rather than via the de novo synthesis of the active protein. Conclusion : The cells, in general, appeared to be equipped with an established system for regenerating inactivated Prxs, and this system may function as a molecular "on-off switch" in various oxidative signal transduction processes. The same mechanisms might applicable other proteins associated with signal transduction where the active catalytic site cysteines exist.

Synthesis and 3D-QSAR of p-Hydroxybenzohydrazide Derivatives With Antimicrobial Activity Against Multidrug-Resistant Staphylococcus aureus (다중의약품에 저항하는 Staphylococcus aureus 균에 항균성을 가지는 파라-히드록시벤조히드라자이드 유도체의 합성과 구조-활성관계 3차원 정량분석)

  • Bhole, Ritesh P.;Bhusari, Kishore P.
    • Journal of the Korean Chemical Society
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    • v.54 no.1
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    • pp.77-87
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    • 2010
  • Hospital-acquired methicillin-resistant Staphylococcus aureus (MRSA) has been an increasing problem worldwide since the initial reports over 40 years ago. To examine new drug leads with potential antibacterial activities, Various N'-[(-3-substituted-4-oxo-1,3-thiazolidin-2-ylidene]-4-hydroxy benzohydrazide (4a-4.i) and N'-[-(3,4-disubstituted)-1,3-thiazolidin-2ylidene)]-4-hydroxybenzohydrazide from (5.a-5.i) to (10.a-10.i) were synthesized using appropriate synthetic route. The entire test compounds (4.a-4.i) and from (5.a-5.i) to (10.a-10.i) were assayed in vitro against s. aureus strain. The minimum inhibitory concentration (MIC) was determined for test compounds and for reference standards. The test compounds showed significant antibacterial activity against the strains used, when tested in vitro. In general, p-hydroxybenzohydrazide ring and substituted thiazoline ring are essential for antimicrobial activity. Among the compounds tested, compounds 6.f, 7.g, 9.f and 10.f, 10 i were found to be most potent. The test compounds were found nontoxic upto the dose level of 2000 ${\mu}g$/mL. The intact compounds were then subjected for 3D-QSAR studies. 3D-QSAR study based on the principal of alignment of pharmacophoric features by Schrodinger PHASE module. The 3D-QSAR study allowed us to confirm the preferential binding mode of p-hydroxybenzohydrazide inside the active site.

Synthesis of PLLA-block-PMMA Copolymer and Characteristics of Biaxially Oriented PLA Film Including the Same (PLLA-block-PMMA 공중합수지의 합성 및 이를 포함하는 PLA 이축연신 필름의 특성)

  • Kim, Moon-Sun;Lee, Sangeun
    • Applied Chemistry for Engineering
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    • v.26 no.3
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    • pp.251-258
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    • 2015
  • In the study, PLLA with 12,000 g/mol ($M_n$) and 14,000 g/mol ($M_w$) was synthesized from L-lactide, and used to synthesize PLLA-Br intermediate. PLLA-block-PMMA with 84,000 g/mol ($M_n$) and 126,000 g/mol ($M_w$) was finally synthesized from PLLA-Br intermediate. The glass transition temperature ($T_g$) and initial pyrolysis temperature of PLLA-block-PMMA are $95.5^{\circ}C$ and $289^{\circ}C$, respectively. The PLA film of $50{\pm}3{\mu}m$ thickness was prepared by blending PLA with 9 phr PLLA-block-PMMA followed by stretching biaxially at 3 times under $95^{\circ}C$, and annealing at $120^{\circ}C$ for 2 min. The light transmittance at 550 nm and tensile strength of the film are 88.5% and 44.5 MPa, respectively. To enhance the tensile strength of PLA film, it was required to keep the film more than 2 min at $120^{\circ}C$ during the annealing step after a biaxially orientation.

Addition Polymerization of 5-Norbornene-2-carboxylic Acid Esters Using Palladium Catalyst System: Synthesis of Monomers, Effect of Their Stereochemistry on Polymerization Behavior (Palladium 촉매를 이용한 5-Norbornene-2-carboxylic Acid Esters의 부가 중합: 단량체의 합성, 단량체의 Stereochemistry(Endo-, Exo-이성질체)가 고분자의 중합 거동에 미치는 영향)

  • Chung, Hae-Kang;Shim, Hyoug-Sub;Jeon, Seung-Ho;Kim, Ji-Heung;Nam, Sung Woo;Jeon, Boong Soo;Kim, Young Jun
    • Polymer(Korea)
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    • v.39 no.3
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    • pp.487-492
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    • 2015
  • The effects of chemical structure of alkyl groups of norbornene carboxylic alkyl esters(methyl, octyl, 4-chlorobenzyl) and endo/exo ratios of norbornene monomers on activity of palladium catalyst and polymerization behavior were investigated. Norbornene ester monomers were synthesized from the reaction of 5-norborene-2-carboxylic acid and various alcohols. Polymerization catalyst, di-${\mu}$-chloro-bis(-methoxybicyclo[2,2,1]-hept-2-ene)palladium(II) (DCBMP), was synthesized according to the literature procedure and silver hexafluoroantimonate ($AgSbF_6$) was used as a conjugate anion source. Gel permeation chromatography (GPC), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC) were the principal techniques for polymer characterization and $^1H$ NMR spectroscopy was used for chemical structures determination of monomers and polymers. For all of the norbonene alkyl esters GPC data showed that when the amounts of endo isomers exceeded those of exo isomers decreased molecular weight polymers were obtained probably due to the decreased catalyst activity. Polymerizations were conducted by varying the monomer/catalyst mole ratios (100:1, 200:1, 300:1). When 300:1 monomer/catalyst ratio was employed it was possible to synthesize high molecular weight ($M_n=27500g/mol$), film forming polymer from exo-norbornene carboxylic acid octyl ester.

A Hardware Design of Ultra-Lightweight Block Cipher Algorithm PRESENT for IoT Applications (IoT 응용을 위한 초경량 블록 암호 알고리듬 PRESENT의 하드웨어 설계)

  • Cho, Wook-Lae;Kim, Ki-Bbeum;Shin, Kyung-Wook
    • Journal of the Korea Institute of Information and Communication Engineering
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    • v.20 no.7
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    • pp.1296-1302
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    • 2016
  • A hardware implementation of ultra-lightweight block cipher algorithm PRESENT that was specified as a block cipher standard for lightweight cryptography ISO/IEC 29192-2 is described in this paper. Two types of crypto-core that support master key size of 80-bit are designed, one is for encryption-only function, and the other is for encryption and decryption functions. The designed PR80 crypto-cores implement the basic cipher mode of operation ECB (electronic code book), and it can process consecutive blocks of plaintext/ciphertext without reloading master key. The PR80 crypto-cores were designed in soft IP with Verilog HDL, and they were verified using Virtex5 FPGA device. The synthesis results using $0.18{\mu}m$ CMOS cell library show that the encryption-only core has 2,990 GE and the encryption/decryption core has 3,687 GE, so they are very suitable for IoT security applications requiring small gate count. The estimated maximum clock frequency is 500 MHz for the encryption-only core and 444 MHz for the encryption/decryption core.

Effect of $SO_2$ on Leaf Tip Blight of Ginkgo biloba caused by Coniothyrium sp. (은행나무의 잎끝마름병에 미치는 $SO_2$ 의 영향)

  • Kang, Yun-Jie;Park, So-Hong;Lee, Du-Hyung;Bae, Gong-Young
    • Korean Journal of Environmental Agriculture
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    • v.18 no.2
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    • pp.179-184
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    • 1999
  • To examine the relationship between air pollution and occurrence of disease in plants, we investigated the alteration of physiology and biochemistry of Ginkgo biloba by inoculating with Coniothyrium sp. and fumigating with 0.1 ${\mu}l/l\;SO_{2-}$ Visual damage did not appear but photosynthesis, $CO_2$ use efficiency(CUE) and water use efficiency(WUE) were reduced when G. biloba was exposed to $SO_{2-}$for 7days (8 hours a day). When inoculated with Coniothyrium sp., the seventies of damage in G. biloba showed a threefold difference between $SO_{2-}$ treatment (SI) and $SO_{2-}$ free treatment (SFI) at day 42 from initial inoculation. Little difference was observed in sugar contents that may be used pathogens feed, among control, SFI and SI. In spite of the reduction in photosynthetic rate, sugar contents and CUE were maintained. WUE was enhanced 13% more at SI than SFI. The $CO_2$fixation boosted because of enhanced WUE, and thus sugar synthesis was not affected. In addition, sugar transport seems to be retarded for some internal alteration. Consequently, the severity of SI was more serious than that of SFI because Coniothyrium sp. easily invades into the physical texture of G. biloba weakened by $SO_2$ fumigation and because sugar was accumulated in leaves of G. biloba.

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Synthesis of Pb(Mg1/3Nb2/3)O3 by Coprecipitation (공침법에 의한 Pb(Mg1/3Nb2/3)O3 합성)

  • Hwang, Jai Suk;Lee, Chul Tae
    • Applied Chemistry for Engineering
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    • v.5 no.5
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    • pp.862-870
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    • 1994
  • $Pb(NO_3)_2$, $Mg(NO_3)_2$ and $NbCl_5$ were used as starting materials and made into solutions. For $Pb(Mg_{1/3}Nb_{2/3})O_3$ composition, each solution measured was mixed and heated to $70^{\circ}C$ to resolved $PbCl_2$ precipitated at lower temperature coprecipitates were formed by adding oxine and ammonia gas under pH ranging 8 to 10, and the prepared coprecipitates were filtered and washed by distilled water. The $Pb(Mg_{1/3}Nb_{2/3})O_3$ powders were synthesized by calcination of coprecipitates at the temperature range of $700^{\circ}C$ to $1000^{\circ}C$, for 5hr. The average particle size of the synthesized powders showing spherical shape was $0.3{{\mu}m}$. The powders were formed to make pellets under pressure of $2000Kg/cm^2$, and the formed pellets were sintered at the temperature range of 1100 to $1200^{\circ}C$, for 5hr. The speciman sintered at $1200^{\circ}C$ showed theoretical density of 97.4%, dielectric constatnt of 17000 at 1kHz, and dielectric loss of 0.02% at 1kHz

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