• Title/Summary/Keyword: LTD4

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Synthesis and Structure-Activity Relationships of Novel Compounds for the Inhibition of TNF-$\alpha$ Production

  • Park, Joon-Seok;Baik, Kyong-Up;Son, Ho-Jung;Lee, Jae-Ho;Lee, Se-Jong;Choi, Jae-Youl;Park, Ji-Soo;Yoo, Eun-Sook;Byun, Young-Seok;Park, Myung-Hwan
    • Archives of Pharmacal Research
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    • v.23 no.4
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    • pp.332-337
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    • 2000
  • This study describes the synthesis, in vitro evaluation and molecular modeling study of novel compounds for the inhibition of TNF-$\alpha$production, Among these compounds, 2-[3-(cyclopentyloxy)-4-methoxyphenyl]-1-isoindolinone (9) was selected as a lead compound and its pyridine derivative 10 was more potent in activity and safer than rolipram.

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Metabolism of Eupatilin in the Rats Using Liquid Chromatography/Electrospray Mass Spectrometry

  • Ji, Hye-Young;Lee, Hye-Won;Lee, Hong-Il;Kim, Hae-Kyoung;Shim, Hyun-Joo;Kim, Soon-Hoe;Kim, Won-Bae;Lee, Hye-Suk
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.214.2-214.2
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    • 2003
  • Eupatilin (5,7-dihydroxy-3",4",6-trimethoxyflavone) is an active ingredient of an ethanol extract of Artemisia asiatica (DA-9601) that is used in the treatment of gastritis. In vitro and in vivo metabolism of eupatilin in the rats has been studied by LC- electrospray mass spectrometry. Rat liver microsomal incubation of eupatilin in the presence of NADPH and UDPGA resulted in the formation of four metabolites (M1-M4). M1, M2, M3 and M4 were tentatively identified as 3"- or- 4"-O-demethyl-eupatilin glucuronide, eupatilin glucuronide, 6-O-demethyleupatilin and 3"-or 4"-O-demethyl- eupatilin glucuronide, eupatilin glucuronide, 6-O-demethyleupatilin and 3"-or 4"-O- demethyl-eupatilin glucuronide, eupatilin glucuronide, 6-O demethyleupatilin and 3"-or 4"-O-demethyl-eupatilin glucuronide, respectively. (omitted)

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Complete Assignment of the $^H1$ and $^{13}C$ NMR Spectra of a Sucrose Ester from Euphorbia Lathyris L.

  • Jung, Min-Hwan;Kim, Hyun-Sik;Sangdoo Ahn;Kim, Cheong-Taek;Jin, Mu-Hyun;Yim, Yong-Hyeon;Kim, Young-Kook;Jong hoa Ok
    • Journal of the Korean Magnetic Resonance Society
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    • v.4 no.2
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    • pp.125-132
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    • 2000
  • The detailed $^1$H and $^{13}$ C NMR assignments of a novel sucrose isovaleryl ester isolated from the seed of Euphorbia Lathyris L., were achieved by one-and two-dimensional techniques. The new sucrose ester was characterized as an $\alpha$-D-glucopyranoside, 3,4,6-tris-O-(3-methyl-1-oxobutyl)-$\beta$-D-fructofuranosyl, 2,6-bis(3-methylbutanoate); sucrose 4,7,8,11,12-pentaisovalerate by MS and NMR experiments.

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Development of Synthesis Process for Ammonia Borane using NaBH4 as the Hydrogen Storage Materials (NaBH4를 이용한 암모니아 보란 수소 저장 소재 합성 공정 개발)

  • Choi, Ho Yun;Park, Sung Jin;Jung, Sung Jin;Baek, Jong Min;Song, Han Dock;Kim, Jong Soo;Lee, Kun Jong;Kim, Young Lae
    • Transactions of the Korean hydrogen and new energy society
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    • v.25 no.5
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    • pp.475-481
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    • 2014
  • Ammonia borane ($NH_3BH_3$), as a source material for energy generation and hydrogen storage, has attracted growing interest due to its high hydrogen content. We have investigated the synthesis of ammonia borane from sodium borohydride ($NaBH_4$) and ammonium chloride ($NH_4Cl$) utilizing a low-temperature process. From our results, we obtained a maximum synthetic yield of 98.2% of ammonia borane complex. The diammoniate diborane (DADB) was detected in about 5~10mol% with in the solid ammonia borane by solid-state $^{11}B$-NMR analysis. The synthesized solid ammonia borane products were studied to characterize hydrogen release upon thermal dehydrogenation.

Development of the 4kW Photovoltaic Power Conditioning System (4kW 태양광 발전용 PCS 개발)

  • Lee, H.D.;Park, Y.H.;Jeon, S.B.;Kim, J.G.;Ryu, S.P.;Lee, S.H.
    • Proceedings of the KIPE Conference
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    • 2010.07a
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    • pp.291-292
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    • 2010
  • The main purpose of this study is to design and develop the grid connected 4kW photovoltatic PCS(Power Conditioning System) targeting for Japanese market. To make this task, the development of DC to DC converter, one phase inverter and EMI filters, and the research on connection between inverter and utility line are made. The developed 4kW PCS has fully carried out performance verifications and evaluation works and acquired the JET(Japan Electrical Safety & Environment Technology Laboratories) certification for safety and performance.

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Synthesis and Antitumor Activity of 3'-hydroxydaunorubicin and 3'-hydroxydoxorubicin Derivatives Substituted with 4'-fluorine or 4'-azide in Sugar Moiety (당부분에서 4'-플루오린 또는 4'-아자이드로 치환된 3'-히드록시다우노루비신과 3'-히드록시독소루비신 유도체의 합성과 항암활성)

  • Ok, Kwang-Dae;Park, Jeong-Bae;Kim, Moon-Sung;Jung, Dong-Yoon;Yang, Junn-Ick
    • YAKHAK HOEJI
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    • v.40 no.2
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    • pp.117-125
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    • 1996
  • 3'-Deamino-3-hydroxy-4'-fluoro- or 3'-deamino-3'-hydroxy-4'-azido-daunorubicin(6,8) and -doxorubicin(7,9) have been synthesized, respectively. Compounds 7,8 and 9 were mo re cytotoxic than daunorubicin(1) and doxorubicin(2) against L1210 murine leukemic cell in vitro. When administered intraperitoneally for 9 days starting 1 day after tumor inoculation, compounds 7(T/C 605%) and 9(T/C 488%) showed significant antitumor activity for ip-inoculuated L1210 murine leukemia at wide range of doses.

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Synthesis and de-pigmentation effect of phenolic glucoconjugates

  • Kim, Ki-Ho;Kim, Ki-Soo;Lee, Jae-Soeb;Ko, Kang-Il;Lee, Soo-Hee
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.27 no.1
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    • pp.99-109
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    • 2001
  • Novel glucoconjugates phenolic moiety, 3-(methoxycarbonyl)-4-(hydroxyphenyl)-$\beta$-D-glucopyranoside(4), 3-(methoxyacetyl)-4-(hydroxyphenyl)-$\beta$-D-glucopyranoside(7), 4-(hydroxyphenyl)-$\beta$-D-ribofuranoside(11), were synthesized. In order to investigate their depigmentation effect, inhibitory activity against mushroom tyrosinase and inhibitory activity of melanin synthesis in B16 melanoma cell were evaluated in vitro. Compound 11 showed 92.0$\mu\textrm{g}$/㎖ of tyrosinase inhibitory activity whereas compound 4 and 7 showed very low activity not less than 300$\mu\textrm{g}$/㎖. Inhibitory activities of melanin synthesis in B16 melanoma cell of compound 4, 7, and 11 were 8.7, 15.1, and 36.0%, respectively, at the concentration of 100$\mu\textrm{g}$/㎖. Inhibitory activity of compound 11 was much higher than that of arbutin at the same concentration.

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Tetanus-induced LTD of Developing MNTB-LSO Synapses in Rat is Dependent on Postsynaptic $Ca^{2+}$

  • Ahn, Seung-Cheol
    • The Korean Journal of Physiology and Pharmacology
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    • v.11 no.3
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    • pp.79-84
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    • 2007
  • Because synaptic refinement of medial nucleus of trapezoid body (MNTB) - lateral superior olive (LSO) synapses is most active during the first postnatal week and the long term depression (LTD) has been suggested as one of its mechanisms, LTD of MNTB-LSO synapses was investigated in neonatal rat brain stem slices with the whole cell voltage clamp technique. In $Mg^{2+}$ free condition, tetanus (10 stimuli at 10 Hz for 2 min) in the current clamp mode induced a robust LTD of isolated D, L-APV-sensitive postsynaptic currents (PSCs) for more than 30 min ($n=6,\;2.4{\pm}0.4%$ of the control), while isolated CNQX-sensitive PSCs were not suppressed ($n=6,\;95.3{\pm}1.6%$). Tetanus also elicited similar LTD in the isolated GABAergic/glycinergic PSCs ($n=6,\;3.6{\pm}0.5%$) and mixed PSCs (GABAergic/glycinergic/glutamatergic) ($n=4,\;2.2{\pm}0.7%$). However, such a strong LTD was not observed in the mixed PSCs when 10 mM EGTA was added in the internal solution (n=10), indicating that postsynaptic $Ca^{2+}$ rise is needed for the strong LTD. This robust LTD might contribute to the active synaptic refinement occurring during the first postnatal week.

Condition for Mass Production of Antagonistic Bacterium Burkholderia pyrrocinia CAB08106-4 to Control Garlic White Rot (마늘 흑색썩음균핵병 방제 길항세균 Burkholderia pyrrocinia CAB08106-4의 대량배양 조건)

  • Lee, Dong Guk;Lee, Eun Sook;Kim, Jeong Seok;Baek, Cheol Ki;Park, Mae Sol;Park, Eun Hee;Lee, Suk Hee;Chung, Chang Kook
    • The Korean Journal of Mycology
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    • v.41 no.1
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    • pp.42-46
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    • 2013
  • Burkholderia pyrrocinia CAB08106-4 was parceled out from the Chungnam Agricultural Research and Extension Center, Korea to evaluate the antagonistic activity against garlic white rot caused by Sclerotium cepivorum. The optimum cultural conditions including temperature, pH, enzyme activity, carbon and nitrogen sources were determined. The optimum culture conditions of B. pyrrocinia CAB08106-4 were $286^{\circ}C$, 150 rpm and pH 7. Chitinase only showed activity among several tested enzymes. The highest cell growth was obtained with 1% glucose and 0.1% $(NH_4)_2SO_4$, respectively.

The synthesis and the structural analysis of advanced PVC plasticizer, 2,2,4-trimethyl-1,3-pentanediol-1-butyrate-3-isobutyrate

  • Cho Myo-Kyung;Ko Dong-Hyun;Lim Young-Hee;Jung Min-Hwan;Cho Hye-Sung;Ok Jong-Hoa
    • Journal of the Korean Magnetic Resonance Society
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    • v.9 no.2
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    • pp.103-109
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    • 2005
  • New PVC plasticizer, 2,2,4-trimethyl-1,3-pentanediol-1-butyrate-3-isobutyrate was synthesized via simple esterification with butyric acid and Texanol(a trademark of Eastman Chemicals), the mixture of 2,2,4-trimethyl-1,3-pentanediol-3-isobutyrate and 2,2,4-trimethyl-1,3-pentanediol-1-isobutyrate. The analysis of $^1H-1D,\;^{13}C-1D$ NMR and HMBC spectra identified internal-ester-transfer of 2,2,4-trimethyl-1,3-pentanediol-1-isobutyrate during the reaction. 2,2,4-trimethyl-1,3-pentanediol-1-butyrate-3-isobutyrate gave better properties in PVC than 2,2,4-trimethyl-1,3-pentanediol diisobutyrate(TXIB, a trademark of Eastman Chemicals) such as lower viscosity, higher tensile strength and better elongation. In particular, remarkably reduced migration compared with TXIB suggested a reduced emission of VOC(volatile organic compound) from PVC.

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