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A Synthesis and Characterization of Pt(II) Complexes with Bipyrimidin-based Back-bone System (비피리미딘계 배위자를 골격으로 하는 Pt(II)착체의 합성 및 특성)

  • Son, Seokhwan;Ahn, Hogeun;Chung, Minchul
    • Korean Chemical Engineering Research
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    • 제54권4호
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    • pp.555-559
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    • 2016
  • In this study, new platinum complexes were synthesized utilizing the ligand of a 2,2'-bispyrimidine (bpim), 2,2'-bipyridine (bpy), 5,5'-dimethyl-2,2'-bipyridine (5,5-mebpy), 5'-bromo-2,2'-bipyridine (5-brbpy), 5,5'-dibromo-2,2'-bipyridine (5,5-brbpy), 4,4'-dimethyl-2,2'-bipyridine (4,4-mebpy), 4,4'-dihexyl-2,2'-Bipyridine (4,4-hebpy), 1,10'-Phenanthroline (phen), 3,4,7,8'-tetramethyl-1,10'-Phenanthroline (3,4,7,8-phen). In order to determine chemical structure of Synthesized platinum complexes, $^1H(^{13}C)$-NMR, UV-vis and FT-IR were used and optical physics and chemical properties were measured PL. In the case of platinum complexes, wavelength has been identified 356~421 nm. Quantum efficiency in DMSO solution was appeared 0.05~0.46.

Tensile Properties of Powder Metallurgy Processed PM Cu-7.5Ni-5Sn Alloy with Different Heat Treatment Conditions (분말야금법으로 제조된 Cu-7.5Ni-5Sn 합금의 열처리 조건에 따른 기계적 특성의 변화)

  • Ryu, Jae-Cheol;Kim, Sang-Sik;Han, Seung-Jeon;Kim, Chang-Ju
    • Korean Journal of Materials Research
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    • 제9권9호
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    • pp.905-912
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    • 1999
  • Tensile properties of powder metallurgy (PM) processed Cu-7.5Ni-5Sn alloys, either as-received or additionally solution heat treated, were examined as a function of aging time. It was found that the as-received Cu-7.5Ni-5Sn alloys showed an abrupt increase in tensile strength after aging at $350^{\circ}C$ for 20 minutes, due to the metastable ${\gamma}$\\` precipitation and a marginal Spinodal decomposition. The resolutionized PM Cu-7.5Ni-5Sn alloys, on the other hand, showed a gradual increase in tensile strength from the very early stage of aging. The overall tensile strength of resolutionized PM Cu-7.5Ni-5Sn alloys, however, was lower than that of the as-received and aged counterparts, due to the grain growth during resolutionization. Afterprolonged aging for the as-received PM Cu-7.5Ni-5Sn alloys, a considerable amount of discontinuous precipitates formed along the grain boundaries. The formation and growth kinetics of such discontinuous precipitates appeared to be dependent on the heat treatment conditions, and affect the mechanical properties greatly.

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Characteristics of Rice Mutants Resistant to 5- Methyltryptophan (벼 5-methyltryptophan 저항성 돌연변이체의 특성)

  • 이효연;강권규;노일섭;이춘환;권혜경;박현숙
    • KOREAN JOURNAL OF CROP SCIENCE
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    • 제40권5호
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    • pp.637-643
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    • 1995
  • TR75, a rice (Oryza sativa L. var. Sasanishikj) mutant resistant to 5-methyltryptophan (5MT) was segregated from the progenies of its initial mutant line, TR1. The 5MT resistance of TR75 was inherited in the M$_{8}$ generations as a single dominant nuclear gene, and was also expressed in callus derived from seeds, roots, and anthers as well as in the seedlings. The callus induced from these organs could grow at 50 mg/1 of 5MT, whereas the growth of wild-type callus was completely inhibited even at 25 mg/1. The seedlings of TR75 did not show resistance to L-azetidine-2-carboxylic acid, S-2-aminoethyl-L-cysteine, p-fluoro-DL-phenylalanine. The content of free amino acids in the TR75 homozygous seeds increased approximately 1.5 to 2.0 fold compared to wild-type seeds. Especially, the contents of tryptophan, phenylalanine and aspartic acid were 5.0, 5.3 and 2.7 times higher than those of wild-type seeds, respectively.y.

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Synthesis, Physicochemical Properties and Antitumor Activity of 5-Fluorouracil Prodrugs (5-플로우로우라실 프로드럭의 제조, 물리화학적 성질 및 항암효과)

  • Jee, Ung-Kil;Lee, Gye-Won
    • YAKHAK HOEJI
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    • 제40권3호
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    • pp.279-292
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    • 1996
  • To assess their stability as a prodrug of 5-fluorouracil (5-FU), four N-acyloxycarbonyl derivatives (1-(N-tert-butyloxycarbonyl)glycyloxymethyl-5-FU :BGFU, 1-(N-tert-butyloxycar bonyl)-leucyloxymethyl-5-FU:BLFU, 1-(N-tert-carbobenzyloxymethyl) glycyloxymethyl-5-FU:CGFU and 1-(N-tert-carbobenzlyoxymethyl)leucyloxymethyl-5-FU:CLFU) possessing differently protected amino acids, and two acetic acid derivatives (5FU-1-acetylpentane:FUAP and 5-FU-1-acetylhexane:FUAH) were synthesized and their physicochemical properties, hydrolysis kinetics, acute toxicity and antitumor activity were evaluated. The lipid-water partition coefficients of six 5-FU prodrugs were higher than that of 5-FU and their aqueous solubilities were in the following rank order; BGFU>FUAP>CGFU>BLFU>CLFU${\simeq}$FUAH. The hydrolysis of N-acyloxycarboyl derivatives, greater at higher pH, was enhanced in presence of liver homogenate or human plasma. Meanwhile, acetic acid ester derivatives, very stable, were hydrolyzed by liver homogenate. Absorption rate constants were 0.181, 0.121, 0.111, 0.168, 0.168, 0.116 and 0.125 $hr^{-1}$ for 5-FU, BGFU, BLFU, CGFU, CLFU, FUAP and FUAH, respectively. The cytotoxicity of N-acyloxycarbonyl derivatives was 4 to 5 times lower than that of 5-FU, but that of acetic acid ester derivatives was negligeble. The $LD_{50}$ values were 204, 325.97 (133.59, amount as 5-FU), 708.16 (262.13), 663.50 (211.77), 382.33 (192.54) and 272.33 (130.09) mg/kg for 5-FU, BGFU, CGFU, CLFU, FUAP and FUAH, respectively. While N-acyloxycarbonyl derivatives showed enhanced antitumor activity and therapeutic ratio (3.30, 3.06, 4.19, 3.11 and 1.81 for BGFU, BLFU, CGFU, CLFU and 5-FU, respectively), FUAH and FUAP showed a smaller therapeutic ratio (0.79 and 0.83).

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The Solidification Microstructure of X%C-5%Cr-5%V-5%Mo-5%W-5%Co Multi-Component White Cast Iron (X%C-5%Cr-5%V -5%Mo-5%W-5%Co 다합금계백주철의 응고조직에 관한 연구)

  • Yu, Sung-Kon;Yasuhiro Matsubara
    • Korean Journal of Materials Research
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    • 제11권6호
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    • pp.472-476
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    • 2001
  • Type and three-dimensional morphology of carbides precipitated in the X(X= 1.70, 1.92, 2.21, 2.50, 2.86)%C-5%Cr-5%V-5%Mo-5%W-5%Co multi-component white cast iron were investigated using an optical microscope and SEM. The types of carbides precipitated were MC, M$_2$C and M$_{7}$C$_{3}$. Morphology of the MC carbide took three forms, that it petal-like, nodular and coral-like. MC carbide seemed to change its morphology from petal-like through nodular, and finally to coral-like with an increase in carbon content. M7C carbide was classified into lamellar and plate-like type. The lamellar M$_2$C arbide precipitated in the iron with low molybdenum and tungsten contents, and higher contents of both elements in the iron were needed to form the plate-like M$_2$C carbide. The morphology of M$_{7}$C$_{3}$ was rod-like similar to that observed in high chromium white cast iron. However, cobalt does not affect the type and morphology of precipitated carbides.des.

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Investigation of low temperature sintering property and fabrication in $Bi_2(Zn_{1/3}Nb_{2/3})_2O_7\;and\;(Bi_{1.5}Zn_{0.5})(Zn_{0.5}Nb_{1.5})O_7$ pyrochlore ($Bi_2(Zn_{1/3}Nb_{2/3})_2O_7\;and\;(Bi_{1.5}Zn_{0.5})(Zn_{0.5}Nb_{1.5})O_7$ pyrochlore의 제조 및 저온 소결 특성 고찰)

  • Kim, Kwan-Soo;Yoon, Sang-Ok;Kim, Shin;Kim, Yun-Han;Kwan, Oh-Young;Park, Jong-Guk;Shim, Sang-Heung
    • Proceedings of the Korean Institute of Electrical and Electronic Material Engineers Conference
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    • 한국전기전자재료학회 2007년도 추계학술대회 논문집
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    • pp.245-245
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    • 2007
  • 본 연구는 $Bi_2O_3$, ZnO 및 $Nb_2O_5$로 이루어진 두 가지의 $Bi_2(Zn_{1/3}Nb_{2/3})_2O_7$$(Bi_{1.5}Zn_{0.5})(Zn_{0.5}Nb_{1.5})O_7$ pyrochlore를 제조한 후, ZBS 및 BZBS 유리를 각각 첨가하여 저온 소결 및 마이크로파 유전 특성을 고찰하였다. 두 가지의 pyrochlore에 대하여 하소 온도에 따른 상 합성 유무를 고찰한 결과 $900^{\circ}C$에서 단일 상을 갖는 pyrochlore를 제조할 수 있었다. 두 가지의 pyrochlore에 ZnO-rich ZBS 유리와 $Bi_2O_3$-rich BZBS 유리를 3, 5 wt%로 첨가한 후 $800{\sim}950^{\circ}C$에서 소결한 결과 ZBS 및 BZBS 유리를 5wt%를 첨가하였을 때 $900^{\circ}C$에서 소결이 가능하였다. 또한 마이크로파 유전 특성을 고찰한 결과, $(Bi_{1.5}Zn_{0.5})(Zn_{0.5}Nb_{1.5})O_7$의 pyrochlore는 고주파에서 유전 특성 측정이 되지 않았다. $Bi_2(Zn_{1/3}Nb_{2/3})_2O_7$의 pyrochlore의 경우 5 wt% ZBS 및 BZBS 유리를 첨가하여 $900^{\circ}C$에서 소결한 시편의 마이크로파 유전 특성은 ${\varepsilon}_r$= 62.8~68.3, $Q{\times}f$ value= 3,500~2,700 GHz을 나타내었다.

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Gastroprokinetic agent, mosapride inhibits 5-HT3 receptor currents in NCB-20 cells

  • Park, Yong Soo;Sung, Ki-Wug
    • The Korean Journal of Physiology and Pharmacology
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    • 제23권5호
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    • pp.419-426
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    • 2019
  • Mosapride accelerates gastric emptying by acting on 5-hydroxytryptamine type 4 ($5-HT_4$) receptor and is frequently used in the treatment of gastrointestinal (GI) disorders requiring gastroprokinetic efficacy. We tested the effect of mosapride on 5-hydroxytryptamine type 3 ($5-HT_3$) receptor currents because the $5-HT_3$ receptors are also known to be expressed in the GI system and have an important role in the regulation of GI functions. Using the whole-cell voltage clamp method, we compared the currents of the $5-HT_3$ receptors when 5-HT was applied alone or was co-applied with mosapride in cultured NCB-20 cells known to express $5-HT_3$ receptors. The $5-HT_3$ receptor current amplitudes were inhibited by mosapride in a concentration-dependent manner. Mosapride blocked the peak currents evoked by the application of 5-HT in a competitive manner because the $EC_{50}$ shifted to the right without changing the maximal effect. The rise slopes of $5-HT_3$ receptor currents were decreased by mosapride. Pre-application of mosapride before co-application, augmented the inhibitory effect of mosapride, which suggests a closed channel blocking mechanism. Mosapride also blocked the opened $5-HT_3$ receptor because it inhibited the $5-HT_3$ receptor current in the middle of the application of 5-HT. It accelerated desensitization of the $5-HT_3$ receptor but did not change the recovery process from the receptor desensitization. There were no voltage-, or use-dependency in its blocking effects. These results suggest that mosapride inhibited the $5-HT_3$ receptor through a competitive blocking mechanism probably by binding to the receptor in closed state, which could be involved in the pharmacological effects of mosapride to treat GI disorders.

Engineering of Biosynthesis Pathway and NADPH Supply for Improved L-5-Methyltetrahydrofolate Production by Lactococcus lactis

  • Lu, Chuanchuan;Liu, Yanfeng;Li, Jianghua;Liu, Long;Du, Guocheng
    • Journal of Microbiology and Biotechnology
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    • 제31권1호
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    • pp.154-162
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    • 2021
  • L-5-methyltetrahydrofolate (5-MTHF) is one of the biological active forms of folate, which is widely used as a nutraceutical. However, low yield and serious pollution associated with the chemical synthesis of 5-MTHF hampers its sustainable supply. In this study, 5-MTHF production was improved by engineering the 5-MTHF biosynthesis pathway and NADPH supply in Lactococcus lactis for developing a green and sustainable biosynthesis approach. Specifically, overexpressing the key rate-limiting enzyme methylenetetrahydrofolate reductase led to intracellular 5-MTHF accumulation, reaching 18 ㎍/l. Next, 5-MTHF synthesis was further enhanced by combinatorial overexpression of 5-MTHF synthesis pathway enzymes with methylenetetrahydrofolate reductase, resulting in 1.7-fold enhancement. The folate supply pathway was strengthened by expressing folE encoding GTP cyclohydrolase I, which increased 5-MTHF production 2.4-fold to 72 ㎍/l. Furthermore, glucose-6-phosphate dehydrogenase was overexpressed to improve the redox cofactor NADPH supply for 5-MTHF biosynthesis, which led to a 60% increase in intracellular NADPH and a 35% increase in 5-MTHF production (97 ㎍/l). To reduce formation of the by-product 5-formyltetrahydrofolate, overexpression of 5-formyltetrahydrofolate cyclo-ligase converted 5-formyltetrahydrofolate to 5,10-methyltetrahydrofolate, which enhanced the 5-MTHF titer to 132 ㎍/l. Finally, combinatorial addition of folate precursors to the fermentation medium boosted 5-MTHF production, reaching 300 ㎍/l. To the best of our knowledge, this titer is the highest achieved by L. lactis. This study lays the foundation for further engineering of L. lactis for efficient 5-MTHF biosynthesis.

Microstructure and Mechanical Properties of Ag-27.5%Cu-20.5%Zn-2.5%Mn-0.5%Ni Brazing Alloy Manufactured by Twin Roll Strip Casting (쌍롤 박판 주조법으로 제조한 Ag-27.5%Cu-20.5%Zn-2.5%Mn-0.5%Ni 브레이징 합금의 미세조직 및 기계적 특성)

  • Kim, Sung-Jun;Kang, Won-Guk;Kim, Mun-Chul;Kim, Yong-Chan;Lee, Kee-Ahn
    • Korean Journal of Metals and Materials
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    • 제47권10호
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    • pp.605-612
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    • 2009
  • The suitability of twin roll strip casting for Ag-27.5%Cu-20.5%Zn-2.5%Mn-0.5%Ni brazing alloy (known as HS-49D) was examined in the present work and the mechanical properties and microstructure of the strip were also investigated. The effect of annealing heat treatment on the properties was also studied. The new manufacturing process has applications in the production of the brazing alloy. XRD and microstructural analyses of the Ag-27.5%Cu-20.5%Zn-2.5%Mn-0.5%Ni strip revealed a eutectic microstructure of an Ag-rich matrix (FCC) and a Cu-rich phase (FCC) regardless of heat treatment. The results of mechanical tests showed tensile strength of 434 MPa and 80% elongation for the twin roll casted strip. Tensile results showed decreasing strengths and increasing elongation with annealing heat treatment. Microstructural evolution and fractography were also investigated and related to the mechanical properties.

Studies on Biological Activity of Wood Extractives (X) - Antifungal Compounds of Hovenia dulcis - (수목추출물의 생리활성에 관한 연구(X) - 헛개나무 목부의 항균활성 물질 -)

  • Choi, Yun-Jeong;Lee, Hak-Ju;Lee, Sung-Suk;Choi, Don-Ha
    • Journal of the Korean Wood Science and Technology
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    • 제31권1호
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    • pp.1-9
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    • 2003
  • Antimicrobial activities of plant extractives were investigated to develop a natural fungicide. Two stilbenoids and five flavonoids were isolated from wood extractives of Hovenia dulcis (Rhamnaceae) which had been selected due to its high antifungal activity among the tested species. The chemical structures of isolated compounds were determinded as : 5-hydroxy-7-methoxyflavone, 5,7-dihydroxyflavone (chrysin), 5,7-dihydroxyflavanone (pinocembrin), 3,5,7-trihydroxyflavanone (pinobanksin), 3,4',5,7-tetrahydroxyflavanone (aromadendrin), 3-hydroxy-5-methoxystilbene and 3,5-dihydroxystilbene (pinosylvin) on the basis of Mass and NMR spectroscopic data. According to the results of antifungal test, 3-hydroxy-5-methoxystilbene was evaluated as the strongest antifungal compound among the tested compounds and next were pinocembrin and pinosylvin, but those also had high hyphal growth inhibition activities against C. parasitica, T. versicolor, T. palustris and T. viride. However, pinobanksin, 5-hydroxy-7-methoxyflavone, chrysin and aromadendrin showed very low antifungal activity. In this regard, it could inferred that high antifungal activity of wood extractives of H. dulcis were derived from 3-hydroxy-5-methoxystilbene, pinocembrin and pinosylvin, respectively.