• Title/Summary/Keyword: B7-H4

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New inhibitors of the NF-kB activation and NO production from Artemisia sylvatica

  • Jin, Huizi;Lee, Jeong-Hyung;Lee, Dong-Ho;Kim, Young-Ho;Lee, Jung-Joon
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.67.1-67.1
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    • 2003
  • Three new guaianolide type of sesquiterpene lactones, 8${\alpha}$-angeloyloxy-1${\alpha}$-hydroxy-3${\alpha}$,4${\alpha}$-epoxy-5${\alpha}$, 7${\alpha}$H-10(14), 11(13)-guaiadien-12,6${\alpha}$-olide (1), 8${\alpha}$-methylbutyryloxy-1${\alpha}$-hydroxy-3${\alpha}$, 4${\alpha}$-epoxy-5${\alpha}$, 7${\alpha}$H-10(14),11(13)-guaiadien-12,6${\alpha}$-olide (2), and 8${\alpha}$-isovaleryloxy-1${\alpha}$-hydroxy-3${\alpha}$, 4${\alpha}$-epoxy-5${\alpha}$, 7${\alpha}$H-10(14),11 (13)- guaiadien-12,6${\alpha}$-olide (3), together with six known sesquiterpenes, artemisolide (4), 3-methoxytanapartholide (5), deacetyllaurenobiolide (6), moxartenolide (7), arteminolide B (8), and arteminolide D (9) were isolated by bioassay-guided fractionation using the NF-kB mediated reporter gene assay system. (omitted)

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Solid-phase Synthesis and Preliminary Evaluation of 1,6,8-Trisubstituted Tetrahydro-2H-pyrazino[1,2-a]pyrimidine-4,7-diones as a NF-kB Inhibitor

  • Kim, Jin-Woong;Cho, Jung-Hyuck;Han, Tae-hee;Lee, Jong-Baek;Oh, Chang-Hyun
    • Bulletin of the Korean Chemical Society
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    • v.27 no.4
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    • pp.484-488
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    • 2006
  • The solid-phase synthesis of new series of 1,6,8-trisubstituted tetrahydro-2H-pyrazino[1,2-a]pyrimidine-4,7-diones as bicyclic $\beta$-turn mimetics is described. Their NF-kB inhibition activities were tested and the effect of substituents on bicyclic ring was investigated. Among the prepared compounds, the fluorobenzyl and methoxybenzyl group substituted compounds 26 and 27 at C-1 and C-8 position showed more inhibitory activities than the others. Tested at a concentration of 10 uM, these two compounds showed a 60% inhibition against the target NF kB 549.

Refinement of the Structure of p-Dimethylaminobenzaldehyde 4-(p-Ethoxyphenyl) Thiosemicarbazone (p-Dimethylaminobenzaldehyde 4-(p-Ethoxyphenyl) Thiosemicarbazone구조의 정밀화)

  • Seo, Il-Hwan;Seo, Chu-Myeong;Park, Yeong-Ja
    • Korean Journal of Crystallography
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    • v.2 no.1
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    • pp.12-16
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    • 1991
  • C18H22N4OS, Mr=342.47, monoclinic, P2₁/c,a=11.802(2), b=31.962(2), c=9.829(2)A, β=100.12(1)˚, V=3694.8A3,F(000)=1472, Z=8, Dx=1.246 Mg m-3, Dm=1.17Mg m-3,λ=0.71073 A, μ=0.15mm-1, T=294 K. final R=0.0856 for 3718 observed reflection (Fo>3σ(Fo)) There are two molecules in an asymmetric unit and a major difference between these molecules is in the C(9)-N(1)-C(6)-C(7) torsion angles [58.8(8)˚and 1(1)˚]. Both molecules have intramolecular N(1)-H(10)'N(3) hydrogen bonds [ 2.613(7) and 2.566(7) A] and assume V-shaped conformation with N(2) atoms at the verices. The two independent molecules are linked by the two N(2)-H(11)'S' hydrogen bonds[3.367(5) A and 3.421(4)A] and the dimergen are held together by van der Waals forces.

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Determination of Li generated from 10B(n·α)7Li reaction in Boric acid solution (붕산수용액에서 10B(n·α)7Li 핵반응에 의해 생성된 Li 정량)

  • Choi, Ke-Chon;Jung, Yongju;Yoon, Jei-Won;Kim, Won-Ho
    • Analytical Science and Technology
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    • v.16 no.6
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    • pp.443-449
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    • 2003
  • Thermal neutron irradiation experiment of boric acid solution was carried out using HANARO in following three conditions: (A) $^{10}B$ concentration = $203.0{\mu}g/mL$, irradiation time = 1 hr; (B) $^{10}B$ concentration = $381.4{\mu}g/mL$, irradiation time = 1 hr; (C) $^{10}B$ concentration = $381.4{\mu}g/mL$, irradiation time = 0.5 hr. The amount of lithium produced from $^{10}B(n{\cdot}{\alpha})^7Li$ reaction which was generated on neutron irradiation, was measured by flameless atomic absorption spectroscopy. The concentration of $^7Li$ measured in the three experiments was $0.18{\mu}g/mL$ (78.3% of theoretical value, $0.23{\mu}g/mL$) in (A), $0.31{\mu}g/mL$ (70.5% of theoretical value, $0.44{\mu}g/mL$) in (B) and $0.16{\mu}g/mL$ (71.6% of theoretical value, $0.22{\mu}g/mL$) in (C). The pH value of irradiated boric acid was shifted to considerably low. It is estimated that boric acid would be transformed into the polyborate fonn, by radiolysis products of water, which has high dissociation constant.

Effects of Amitriptyline and Imipramine on Superoxide Generation, Myeloperoxidase Release, Leukotriene $B_4$ in Human Neutrophils (Amitriptyline과 Imipramine이 호중구에서의 Superoxide 생성, Myeloperoxidase 유리, Leukotriene $B_4$생성과 칼슘 동원에 나타내는 영향)

  • Shin Yong-Kyoo;Lee Chung-Soo;Lee Kwang-Soo
    • The Korean Journal of Pharmacology
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    • v.31 no.1 s.57
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    • pp.123-133
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    • 1995
  • A number of tricyclic antidepressants appear to have inhibitory action on calmodulin. Although amitriptyline, imipramine and doxepine have been shown to inhibit calcium uptake, oxidative phosphorylation and ATPase activities, effects of amitriptyline, imipramine and doxepine on functional responses of human neutrophils have not been elucidated. In this study, effects amitriptyline, imipramine and doxepine on superoxide and hydrogen peroxide generation, myeloperoxidase release, leukocriene B4 formation and intracellular calcium level were investigated. Superoxide and hydrogen peroxide production in heat aggregated IgG-activated neutrophils were inhibited by amitriptyline, imipramine and doxepine. EDTA, EGTA, verapamil and bepredil inhibited heat aggregated IgG-induced superoxide production. Chlorpromazine, trifluoperazine, staurosporine and H-7 also inhibited it. PMA-induced superoxide production was inhibited by amitriptyline, imipramine, doxepine, chlorpromazine and H-7. Amitriptyline, imipramine, chlorpromazine and trifluoperazine inhibited the myeloperoxidase release by heat aggregated IgG. Productions of $LTB_4$, and 5-HETE in heat aggregated IgG-activated neutrophils were inhibited by amitriptyline, imipramine and doxepine. In neutrophils, elevation of intracellular calcium induced by heat aggregated IgG was inhibited by amitriptyline, imipramine, doxepine, chlorpromazine and EGTA, while verapamil slightly inhibited increase of intracellular calcium and H-7 did not inhibit it. These results suggest that the inhibitory effect of amitriptyline, imipramine and doxepine on respiratory burst, myeloperoxidase release and LTB4 production in heat aggregated IgG-activated neutrophils appears to be ascribed to the inhibition of calcium mobilization, calmodulin and protein kinase C.

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Synthesis of 2-Substituted 4H-Thieno[2,3-b][1]benzothiopyran-4-ones as Potential Chemotherapeutic Agents

  • El-Subbagh, H.I.;Yousif, M.Y.;El-Eman, A.A.;El-Kerdawy, M.M.
    • Archives of Pharmacal Research
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    • v.12 no.2
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    • pp.135-137
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    • 1989
  • A convenient route is reported for the synthesis of certain series of 4H-thieno[2,3-b][1]benzothiopyran-4-ones, carrying various substituents at position 2 such as arylazomethines (7,8), thiazolidin-4-ones (9-13), ${\alpha},\;{\beta}-unsaturated$ ketones (16,17), 2-pyridones (19-23), tetrahydrothiophen-4-ones (24,28), and nitroalkenes (29,30), as potential schistosomicidal or antihistaminic agents.

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The Synthesis and Characterization of Some Novel Thioethers: Thio-Subsituted [3]Cumulenes, -1-Buten-3-ynes and Buta-1,3-dienes

  • Ibis, Cemil;Sahin, Aysecik
    • Bulletin of the Korean Chemical Society
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    • v.31 no.8
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    • pp.2255-2260
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    • 2010
  • In this study, some novel thiosubstituted butenyne (3a-d, 7b, 15b), butadiene (4a-b, 4d, 5a, 5c, 6b, 8e, 9c, 10b, 16b, 18e) and [3]cumulene (11a-b with isomer 3a-b, 12a with isomer 13a, 14b, 17e) compounds were synthesized from the reaction of 2H-pentachloro-1,3-butadiene with thiols. The new compounds were characterized by elemental analysis, mass spectrometry, UV-vis, IR, 1H NMR, NMR ($^{13}C$ or APT) spectroscopy.

Effect of pH on Rheological Properties of Dysphagia-Oriented Thickened Water

  • Yoon, Seung-No;Yoo, Byoungseung
    • Preventive Nutrition and Food Science
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    • v.21 no.1
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    • pp.73-77
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    • 2016
  • Flow and dynamic rheological properties of thickened waters prepared with commercial food thickeners were investigated at different pH levels (3, 4, 5, 6, and 7). The commercial xanthan gum (XG)-based thickener (thickener A) and starch-based thickener (thickener B), which have been commonly used in a domestic hospital and nursing home for patients with swallowing difficulty (dysphagia) in Korea, were selected in this study. Thickened samples with both thickeners at different pH levels showed high shear-thinning flow behaviors (n=0.08~0.22). Thickened samples at pH 3 showed higher n values and lower consistency index (K) values when compared to those at other pH levels. The K values of thickener A increased with an increase in pH level, while the n values decreased, showing that the flow properties greatly depended on pH. There were no noticeable changes in the K values of thickener B between pH 4 and 7. At pH 3, the thickened water with thickener A showed a higher storage modulus (G') value, while that with thickener B showed a lower G'. These rheological parameters exhibited differences in rheological behaviors between XG-based and starch-based thickeners, indicating that the rheological properties of thickened waters appear to be greatly influenced by the acidic condition and the type of food thickener. Appropriately selecting a commercial food thickener seems to be greatly important for the preparation of thickened acidic fluids with desirable rheological properties for safe swallowing.

MTF Evaluation and Clinical Application according to the Characteristic Kernels in the Computed Tomogrsphy (Kernel 특성에 따른 MTF 평가 및 임상적 적용에 관한 연구)

  • Yoo, Beong-Gyu;Lee, Jong-Seok;Kweon, Dae-Cheol
    • Progress in Medical Physics
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    • v.18 no.2
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    • pp.55-64
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    • 2007
  • Our objective was to evaluate the clinical feasibility of spatial domain filtering as an alternative to additional image reconstruction using different kernels in CT. Kernels were grouped as H30 (head medium smooth), B30 (body medium smooth), S80 (special) and U95 (ultra sharp). Derived from thin coilimated source images, four sets of images were generated using phantom kernels. MTF (50%, 10%, 2%) measured with H30 (3.25, 5.68, 7.45 Ip/cm) B30 (3.84, 6.25, 7.72 Ip/cm), S80 (4.69, 9.49, 12.34 Ip/cm), and U95 (14.19, 20.31, 24.67 Ip/cm). Spatial resolution for the U95 kernel (0.6 mm) was 33.3% greater than that of the H30 and B30 (0.8 mm) kernels. Initially scanned kernels images were rated for subjective image qualify, using a five-point scale. Image scanned with a convolution kernel led to an increase in noise (U95), whereas the results for CT attenuation coefficient were comparable. CT images increase the diagnostic accuracy in head (H30), abdomen (B30), temporal bone and lung (U95) kernels may be controlled by adjusting CT various algorithms, which should be adjusted to take into account the kernels of the CT undergoing the examination.

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