• Title/Summary/Keyword: Ligand effect

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Optical Resolution of DABS-Amino Acids with Mobile Chiral Chelate Addition (키랄킬레이트 이동상첨가법에 의한 답실아미노산의 광학이성질체 분리)

  • Lee, Seon Haeng;O, Dae Seop;Byeon, Seong Gu
    • Journal of the Korean Chemical Society
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    • v.34 no.4
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    • pp.345-351
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    • 1990
  • Optical isomers of DABS-amino acids have been separated in a reversed phae high performance liquid chromatography by adding Cu (Ⅱ)-L-Proline chelate to the mobile phase. The retention behaviors for the DABS-amino acids are discussed in terms of pH of the mobile phase and the concentrations of acetonitrile, Cu (Ⅱ) complex, and buffer. The selectivity of the optical isomers of DABS-amino acids increases with the pH of the mobile, and the concentration of the chelate, but decreases with concentration of the oganic modifier. The concentration of buffer does not affect the optical separation selectivity. A separation mechanism is illustrated by cis and trans formation based on the steric effect of the ligand exchange reaction between DABS-amino acids and the copper chelate.

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Shigyungbanha-tang Exhibits Anti-inflammatory Effects by Inhibiting $I{\kappa}B-{\alpha}$ Degradation in LPS-stimulated Peritoneal Macrophages (LPS로 유도한 복강대식세포에서 $I{\kappa}B-{\alpha}$ 분해억제에 의한 시경반하탕(柴梗半夏湯)의 항염증효과)

  • Shin, Jo-Young;Lee, Si-Hyeong;Lee, Seung-Eon
    • The Journal of Internal Korean Medicine
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    • v.28 no.3
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    • pp.442-452
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    • 2007
  • Objectives : The purpose of this study was to investigate the toll-like receptor (TLR)-4 mediated anti-inflammatory effects of extract from Shigyungbanha-tang (SBT) on the peritoneal macrophage. Methods : To evaluate of TLR-4 mediated inflammatory of SBT. we examined NO and cytokine production in TRL-4 ligand (LPS : lipopolysaccharide) induced macrophages. Furthermore, we examined its molecular mechanism using western blot. Results : Extract from SBT itself does not have any cytotoxic effect in the peritoneal macrophages. Extract from SBT reduced LPS-induced nitric oxide (NO). tumor necrosis factor-alpha ($TNF-{\alpha}$), interleukin (IL)-6 and IL-12 production in peritoneal macrophages. SBT inhibited degradation of inhibitor kappa B-alpha ($I{\kappa}B-{\alpha}$) in the TLR-4 mediated peritoneal macrophages. Conclusions : These results suggest that SBT inhibits NO and cytokines production through inhibiting nuclear factor-kappaB (NF-${\kappa}$B) activation in peritoneal macrophage and that SBT may be beneficial oriental medicine for inflammation.

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Condensable InP Quantum Dot Solids

  • Tung, Dao Duy;Dung, Mai Xuan;Jeong, Hyun-Dam
    • Proceedings of the Korean Vacuum Society Conference
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    • 2012.02a
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    • pp.541-541
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    • 2012
  • InP quantum dots capped by myristic acid (InP-MA QDs) were synthesized by a typical hot injection method using MA as stablizing agent. The current density across the InP-MA QDs thin film which was fabricated by spin-coating method is about $10^{-4}A/cm^2$ at the electric field of 0.1 MV/cm from I-V measurement on a metal-insulator-metal (MIM) device. The low conductivity of the InP-MA QDs thin film is interpreted as due to the long interdistances among the dots governed by the MA molecules. Therefore, replacing the MA with thioacetic acid (TAA) by biphasic ligand exchange was conducted in order to obtain TAA capped InP QDs (InP-TAA). InP-TAA QDs were designed due to: 1) the TAA is very short molecule; 2) the thiolate groups on the surface of the InP-TAA QDs are expected to undergo condensation reaction upon thermal annealing which connects the QDs within the QD thin film through a very short linker -S-; and 3) TAA provides better passivation to the QDs both in the solution and thin film states which minimizing the effect of surface trapping states.

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Biotin-Conjugated Block Copolymeric Nanoparticles as Tumor-Targeted Drug Delivery Systems

  • Kim, So-Yeon;Cho, Seung-Hea;Lee, Young-Moo
    • Macromolecular Research
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    • v.15 no.7
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    • pp.646-655
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    • 2007
  • To achieve targeted drug delivery for chemotherapy, a ligand-mediated nanoparticulate drug carrier was designed, which could identity a specific receptor on the surfaces of tumor cells. Biodegradable poly(ethylene oxide)/poly$({\varepsilon}-caprolactone)$ (PEG/PCL) amphiphilic block copolymers coupled to biotin ligands were synthesized with a variety of PEG/PCL compositions. Block copolymeric nanoparticles harboring the anticancer drug paclitaxel were prepared via micelle formation in aqueous solution. The size of the biotin-conjugated PEG/PCL nanoparticles was determined by light scattering measurements to be 88-118 nm, depending on the molecular weight of the block copolymer, and remained less than 120 nm even after paclitaxel loading. From an in vitro release study, biotin-conjugated PEG/PCL nanoparticles containing paclitaxel evidenced sustained release profiles of the drug with no initial burst effect. The biotin-conjugated PEG/PCL block copolymer itself evidenced no significant adverse effects on cell viability at $0.005-1.0{\mu}g/mL$ of nanoparticle suspension regardless of cell type (normal human fibroblasts and HeLa cells). However, biotin-conjugated PEG/PCL harboring paclitaxel evidenced a much higher cytotoxicity for cancer cells than was observed in the PEG/PCL nanoparticles without the biotin group. These results showed that the biotin-conjugated nanoparticles could improve the selective delivery of paclitaxel into cancer cells via interactions with over-expressed biotin receptors on the surfaces of cancer cells.

Enhancement of TRAIL-Induced Apoptosis in Human Hepatocellular Carcinoma Cells by Apigenin (인체 간암세포에서 Apigenin에 의한 TRAIL 유도 Apoptosis의 증진 효과)

  • Kim, Eun-Young;Kim, An-Keun
    • YAKHAK HOEJI
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    • v.55 no.1
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    • pp.49-55
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    • 2011
  • Tumor necrosis factor-related apoptosis inducing ligand (TRAIL) is one of the promising anti-cancer agent because of its ability to selectively induce apoptosis in tumor cell lines but not in normal cells. However, TRAIL resistance has been reported in some cancer cells including hepatocarcinoma cells. Therefore, studies of agents that sensitize TRAIL-resistant cancer cells could be a effective therapeutic approach in cancer management. In our study, we examined the effect of combination of TRAIL with apigenin in human hepatocellular carcinoma cells. As a result, the combined use of TRAIL and apigenin significantly enhanced the cytotoxicity in PLC-PRF5 cells. Flow cytometry analysis after annexin V-FITC/PI dual staining showed that this increase of cell cytotoxicity was related to enhanced apoptosis in combined treatment of TRAIL with apigenin. Furthermore, synergistic induction of apoptosis was also confirmed by observation of morphological changes and annexin V-FITC/PI fluorescence. Our findings suggests that apigenin has the potential to improve the efficiency of TRAIL-based therapies in human hepatocellular carcinoma cells. Further study is needed to reveal the molecular mechanisms of this combined therapy.

Inhibitory Effect of Snake Venom Toxin on Colorectal Cancer HCT116 Cells Growth through Induction of Intrinsic or Extrinsic Apoptosis

  • Kim, Kyung Tae;Song, Ho Sueb
    • Journal of Acupuncture Research
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    • v.30 no.1
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    • pp.43-55
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    • 2013
  • I investigated whether snake venom toxin(SVT) from Vipera lebetina turanica enhances the apoptosis ability of tumor necrosis factor(TNF)-related apoptosis-inducing ligand(TRAIL) in cancer cells. TRAIL inhibited HCT116 cell growth in a dose-dependent manner. Consistent with cell growth inhibition, the expression of TRAIL receptors; DR4 and DR5 was significantly increased as well as apoptosis related proteins such as cleaved caspase-3, 8, 9 and Bax. However, the expression of survival proteins(eg, cFLIP, survivin, XIAP and Bcl2) was suppressed by the combination treatment of SVT and TRAIL. Pretreatment with the reactive oxygen species(ROS) scavenger N-acetylcysteine reduced the SVT and TRAIL-induced upregulation of DR4 and DR5 expression and expression of the apoptosis related protein such as caspase-3 and-9 as well as cell growth inhibitory effects. The collective results suggest that SVT facilitates TRAIL-induced apoptosis in human colorectal cancer HCT116 cells through up-regulation of the TRAIL receptors; DR4 and DR5 via ROS pathway signals.

A Carbazole-Attached NO2S2-Macrocycle Exhibiting Hg2+ and Cu2+ Selectivity

  • Lee, Seul-Gi;Kang, Eun-Ju;Lee, Shim Sung
    • Bulletin of the Korean Chemical Society
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    • v.34 no.5
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    • pp.1429-1434
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    • 2013
  • A synthesis and cation-induced fluorescent behavior of the carbazole-attached $NO_2S_2$-macrocycle (L) is described and structurally characterized by single crystal X-ray analysis. The photoluminescence spectrum of L in 80% $CH_3CN/CH_2Cl_2$ displays a peak maximum at 431 nm (blue emission). In the metal-induced fluorometric experiment, L showed a drastic chelation-enhanced fluorescence quenching (CHEQ) effect only with $Hg^{2+}$ and $Cu^{2+}$. In ESI-mass study, a 1:1 stoichiometry for complexation of L with $Hg^{2+}$ was confirmed, suggesting the unique sensing behavior of the proposed ligand L due to the selective complexation affinity for $Hg^{2+}$. The observed results indicate that L is a promising turn-off type fluoroionophore for $Hg^{2+}$ and $Cu^{2+}$ detections. Additionally, the $Ag^+$ complex of the precursor macrocycle was prepared and its solid structure was crystallographically characterized.

Synthesis, Structures and Properties of Two Metal-organic Frameworks Derived from 3-Nitro-1,2-benzenedicarboxylic Acid

  • Xu, Wen-Jia;Zhang, Ling-Yu;Tang, Jin-Niu;Wang, Dai-Yin;Pan, Gang-Hong;Feng, Yu
    • Bulletin of the Korean Chemical Society
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    • v.34 no.8
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    • pp.2375-2380
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    • 2013
  • Two metal-organic frameworks based on the connectivity co-effect between rigid benzenedicarboxylic acid and bridging ligand have been synthesized $[Zn_2(3-NO_2-bdc)_2(4,4'-bpy)_2H_2O]_n$ (1), $[Co(3-NO_2-bdc)(4,4'-bpy)H_2O]_n$ (2) (where $3-NO_2-bdcH_2$ = 3-nitro-1,2-benzenedicarboxylic acid, 4,4'-bpy = 4,4'-bipyridine). The two novel complexes were characterized by IR spectrum, elemental analysis, fluorescent properties, thermogravimetric analysis, single-crystal X-ray diffraction and powder X-ray diffraction (PXRD). X-ray structure analysis reveals that 1 and 2 are two-dimensional (2D) network structures. Complex 1 and complex 2 belong to triclinic crystal with P-1 space group. The luminescence measurements reveal that two complexes exhibit good fluorescent emissions in the solid state at room temperature. Also, thermal decomposition process and powder X-ray diffraction of complexes were investigated.

An NMR Study of Solvent Interactions in a Paramagnetic System

  • Golding, R.M.;Pascual, R.O.;Suvanprakorn, C.;Dance, I.G.
    • Bulletin of the Korean Chemical Society
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    • v.27 no.11
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    • pp.1752-1756
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    • 2006
  • This study explores and interprets in a new way the complex solvent and the temperature dependence of the NMR shifts for the N-$CH_2$ protons in tris(N,N-diethyldithiocarbamato) iron(III) in acetone, benzene, carbon disulfide, chloroform, dimethylformamide and pyridine. The NMR shifts are interpreted in terms of the Fermi contact interaction and the dipolar term from the multipole expansion of the interaction of the electron orbital angular momentum and the electron spin dipolar-nuclear spin angular momentum. This analysis yields a direct measure of the effect of the solvent system on the environment of the transition metal ion. The results are analysed in terms of the crystal field environment of the transition metal ion with contributions from (a) the dithiocarbamate ligand (b) the solvent molecules and (c) the interaction of the effective dipole moment of the polar solvent molecule with the transition metal ion complex.

A Study on the Reduction of Particulate Emission Using Oil Soluble Organometallic Compounds as Combustion Improver for Heavy Fuel Oil (중질유 연소시 유용성 유기금속화합물 연소촉진제의 Dust 저감특성)

  • Kim, Dong-Chan;Nho, Nam-Sun;Woo, Je-Kyung;Kim, Jin-Hoon;Lee, Young-Sea
    • Journal of Korean Society for Atmospheric Environment
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    • v.24 no.1
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    • pp.55-62
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    • 2008
  • This study is aimed at substantially reducing the particulate matter (dust) emission during the combustion of heavy fuel in boilers by addition of combustion improver. The combustion improver used were the oil-soluble organometallic compounds that were found to be more effective than the dispersing agents that are generally used for reducing the particulate emission. The dust reduction effect was found to depend on the active materials (metals) as well as on the organic ligand part of organometallic compounds. Acetylacetonoate and naphthenate of Fe and Ca were found to be most effective for dust reduction. Addition of Fe and Ca organometallic compounds as combustion improver in concentration of 30 ppm (metal basis) to heavy fuel oil, caused dust reduction by 50 wt% to 80 wt%.