• Title/Summary/Keyword: Ligand Effects

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Adsorption Characteristic of U(VI), Cu(II), Dy(III) Ions Utilizing Nitrogen-Donator Synthetic Resin (질소-주게 합성수지를 이용한 U(VI), Cu(II), Dy(III) 이온들의 흡착특성)

  • Rho, Gi-Hwan;Kim, Joon-Tae;Kim, Hee-Joung
    • Journal of environmental and Sanitary engineering
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    • v.21 no.3 s.61
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    • pp.52-60
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    • 2006
  • The ion exchange resins have been synthesized from chlormethyl styrene-1,4-divinylbenzene(DVB) with 1%, 2%, and 20%-crosslinking and macrocyclic ligand of cryptand 21 by copolymerization method and the adsorption characteristics of uranium(VI), copper(II) and dysprosium(III) metallic ions have been investigated in various experimental conditions. The synthesis of these resins was confirmed by content of chlorine, element analysis, and IR-spectrum. The effects of pH, equilibrium time, dielectric constant of solvent and crosslink on adsorption of metallic ions were investigated. The metal ion was showed fast adsorption on the resins above pH 3. The optimum equilibrium time for adsorption of metallic ions was about two hours. The adsorption selectivity determined in ethanol was in increasing order uranium$(UO^{2+}_2)\;>\;copper(Cu^{2+})\;>\;dysprosium(Dy^{3+})$ ion. The adsorption was in order of 1%, 2%, and 20% crosslink resin and adsorption of resin decreased in proportion to order of dielectric constant of solvents.

Selective Cytotoxicity Platinum (II) Complex Containing Carrier Ligand of cis-1,2-Diaminocyclohexane (Cis-Diaminocyclohexan을 배위자로 하는 배금(II)착체의 선택적 세포독성)

  • 노영수;정세영;정지창
    • Environmental Analysis Health and Toxicology
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    • v.13 no.3_4
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    • pp.87-94
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    • 1998
  • The use of cisplatin is limited by severe side effects such as renal toxicity. Our platinum-base drug discovery is aimed at developing drugs capable of diminishing toxicity and improving antitumor activity. We synthesized new Pt (II) complex analogue [Pt (cis-DACH)(DPPP)]. 2NO$_3$ (PC) containing cis-1,2-diaminocyclohexane as a carrier ligand and 1,3-bis(diphenylphosphino) propane as a leaving group. Furthermore, nitrate was added to improved the solubility. In this study, its structure was determined and its antitumor activity against SKOV-3 and NIH-OVCAR-3 human ovarian adenocarcinoma, and in vitro cytotoxicity was determined against primary cultured rabbit kidney proximal tubular and renal cortical cells of human kidney using colorimetric MTT assay. PC demonstrated acceptable antitumor activity against SKOV-3 and NIH-OVCAR-3 human ovarian adenocarcinoma and significant activity as compared with that of cisplatin. The toxicity of PC was found quite less than that of cisplatin using MTT and $^3$H-thymidine uptake tests in rabbit proximal tubular cells and human kidney cortical cells. PC was used for human cortical tissue in 7 weeks hitoculture by the glucose-consumption tests. We determined that the new platinum drug has lower nephrotoxicity than cisplatin. Based on these results, this novel platinum (II) complex compound (PC) represent a valuable lead in the development of a new anticancer chemotherapeutic agent capable of improving antitumor activity and low nephrotoxicity.

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Biopharmaceutical studies on copper(II) chelates of sulfanilamide derivatives (Sulfanilamide유도체의 동(II)착화합물에 대한 생물약제학적 연구)

  • 김재백
    • YAKHAK HOEJI
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    • v.15 no.2
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    • pp.41-52
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    • 1971
  • Cu(II) chelates of several sulfanilamide derivatives (Sulfa-Cu) were prepared and their effects on solubility, absorptivity in intestinal lumen, biding tendency with serum protein and erythrocytes, concentration in rabbit blood, and acetylation rate were studied in comparison with their free ligand forms. For solubility concerned, the partition coefficients of Sulfa-Cu are decreased as following order: Sulfadimethoxine Copper chelate (SDM-Cu), Sulfamethoxypyridazine Copper chelate (SD-Cu), Sulfamerazine Copper chelate (SM-Cu), Sulfaisoxazole Copper chelate (SIX-Cu). The partition coefficients of SDM-Cu and ST-Cu were much greater than those of ligands. this phenomenone acounts for the rapid absorption of SDM-Cu and ST-Cu in the rat small intestine (in situ). The Sulfa-Cu were absorbed at the intestinal lumen of a rat in the rate of first order and there was no difference between long acting sulfa drugs and their Cu0chelates in biological half lives. In binding experiments, sulfa-Cu binded with serum protein in lower ratio than their ligands except SIX-Cu. On other hand, acetylation rates of sulfa-Cu were higher than those of free sulfa drugs and the acetylation rate were higher than those of free sulfa drugs and powder. In a experiment on Sulfa-Cu concentration in rabbit blood, the half lives of SD-Cu, SIX-cu, ST-Cu, and SM-Cu were longer than those of their ligands. Above all, the half life of SD-Cu appeared to be approximately 3.5 times logner than that of corresponding ligand, SD. When absorption of sulfa drugs or sulfa-Cu at the small intestinal lumen of a rat and the concentration in rabbit blood after absorption were compared, it was found that there was not always conrrelated.

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Rates of Conformational Change of 3,3-Dimethylpiperidine and Solvent Effects on Its Conformation When Coordinated to the Paramagnetic Undecatungstocobalto(II)silicate Anion Studied by 1H NMR Spectroscopy

  • 현재원;소현수
    • Bulletin of the Korean Chemical Society
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    • v.18 no.9
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    • pp.961-965
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    • 1997
  • 1H NMR spectra of 3,3-dimethylpiperidine (1) at -70 to 30 ℃ exhibit gradual change from slow to rapid exchange between two alternate chair forms. The exchange rate constant was determined as a function of temperature by simulating the line shape of the signal from the two methyl groups using the modified Bloch equations. The resulting free energy of activation is ΔG* = 44.4±1.9 kJ mol-1 at 298 K. The 1H NMR spectrum of a D2O or dimethylsulfoxide-d6 (DMSO-d6) solution containing 1 and [SiW11CoⅡO39]6- exhibits separate signals for the free ligand and the complex, indicating that the ligand exchange is slow on the NMR time scale. In D2O the piperidine ring is frozen as a chair form even at room temperature with the cobalt ion bonded to the axial position of the nitrogen atom. When DMSO-d6 is added to the D2O solution, the NMR spectral change suggests that a rapid exchange occurs between the chair form and another conformer. It is proposed that the conformation of ^b1^b coordinated to [SiW11CoⅡO39]6- in DMSO-d6 is close to a twist form.

Inhibitory effects of Oxya chinensis sinuosa ethanol extract on RANKL-induced osteoclast differentiation

  • Ra-Yeong Choi;Bong Sun Kim;Sohyun Park;Minchul Seo;Joon Ha Lee;HaeYong Kweon;In-Woo Kim
    • International Journal of Industrial Entomology and Biomaterials
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    • v.48 no.1
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    • pp.13-18
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    • 2024
  • The rice field grasshopper, Oxya chinensis sinuosa (OC), has traditionally been utilized in Korea for various purposes; however, its potential benefits in the context of osteoporosis remain unclear. The results revealed that OC ethanol extract (OCE) significantly inhibited the formation and activity of tartrate-resistant acid phosphatase (TRAP)-positive cells in receptor activator of nuclear factor-κB ligand (RANKL)-stimulated RAW264.7 cells. Furthermore, OCE, at concentrations ranging from 100 to 400 ㎍/mL, demonstrated a dose-dependent reduction in the protein expression of osteoclast-specific markers, including nuclear factor of activated T cell cytoplasmic 1, c-Src, and TRAP, when compared to RANKL stimulation alone. Additionally, OCE significantly inhibited RANKL-induced activation of p38 mitogen-activated protein kinase (MAPK) and c-Jun N-terminal kinase (JNK) but not the activation of extracellular signal-regulated kinase. Collectively, these results indicate that OCE suppresses osteoclastogenesis by attenuating the phosphorylation of p38 MAPK and JNK. Consequently, these findings suggest that OCE holds promise for the prevention of osteoporosis.

Application of Principle in Metal-Ligand Complexation to Remove Heavy Metals : Effects of Metal Concentration, pH and Temperature (금속(金屬)-Ligand 착염형성(錯鹽形成)에 의한 중금속(重金屬) 제거방법(除去方法)에 관(關)한 연구(硏究) : 중금속(重金屬) 농도(濃度), pH 및 온도(溫度)의 효과(效果))

  • Yang, Jae-E;Shin, Yong-Keon;Kim, Jeong-Je
    • Korean Journal of Soil Science and Fertilizer
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    • v.26 no.1
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    • pp.37-42
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    • 1993
  • Influences of metal concentration, pH and temperature on metal-ligand precipitate formation were investigated, as a part of projects for removing heavy metals from aqueous solution employing the principles in metal-ligand complexation. Aqueous solutions of HA or FA were reacted with those of heavy metals with 1:1 ratio. Efficiency of humic (HA) or fulvic acid (FA) on removing metals was evaluated by separating the precipitates from soltuions with the filtering method. When HA was a counter ligand, there existed three ranges of metal concentrations affecting precipitation : precipitate fromation was not available, was reached to the maximum, and afterwards was decreased again. The concentration ratios of metal to HA for initiating complexation were dependent upon kinds of metal and concentrations of ligand. Amount of Pb to form maximum precipitates per unit mg of HA was 1.3 times higher than that of Cu. When FA was a counter ligand, concentrations of metal-FA precipitates were increased proportionally with the treated metal concentrations. Efficiency of FA fro removing Pb was nearly 100%, but it was ranged from 12 to 19% for Cu, depending on FA concentration. pH exerted a considerable effect on complexation between Pb and FA, showing precipitates were increased six times at most per unit increase of pH. Ranges of pH increasing significantly the mounts of precipitates were coincied with pH jump ranges of the titration curve of organic ligands. As increasing temperature from 15 to $55^{\circ}C$, increases of FA-Cu precipitates were doubled, but those of FA-Pb were accounted for only 6%, However, HA-metal complexation was not affected by temperature.

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Theoretical Study of the N-(2,5-Methylphenyl)salicylaldimine Schiff Base Ligand: Atomic Charges, Molecular Electrostatic Potential, Nonlinear Optical (NLO) Effects and Thermodynamic Properties

  • Zeyrek, Tugrul C.
    • Journal of the Korean Chemical Society
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    • v.57 no.4
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    • pp.461-471
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    • 2013
  • Optimized geometrical structure, atomic charges, molecular electrostatic potential, nonlinear optical (NLO) effects and thermodynamic properties of the title compound N-(2,5-methylphenyl)salicylaldimine (I) have been investigated by using ab initio quantum chemical computational studies. Calculated results showed that the enol form of (I) is more stable than keto form. The solvent effect was investigated for obtained molecular energies, hardneses and the atomic charge distributions of (I). Natural bond orbital and frontier molecular orbital analysis of the title compound were also performed. The total molecular dipole moment (${\mu}$), linear polarizability (${\alpha}$), and first-order hyperpolarizability (${\beta}$) were calculated by B3LYP method with 6-31G(d), 6-31+G(d,p), 6-31++G(d,p), 6-311+G(d) and 6-311++G(d,p) basis sets to investigate the NLO properties of the compound (I). The standard thermodynamic functions were obtained for the title compound with the temperature ranging from 200 to 450 K.

Effects of Baicalin on the differentiation and activity of preosteoclasts

  • Ko, Seon-Yle
    • International Journal of Oral Biology
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    • v.34 no.2
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    • pp.81-86
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    • 2009
  • Baicalin is a flavonoid purified from the medicinal plant Scutellaria baicalensis. It has been reported that baicalin exhibits antibacterial, anti-inflammatory and analgesic effects. The present study was undertaken to determine the underlying cellular mechanisms of baicalin action in preosteoclasts. The effects of this flavonoid on preosteoclasts were determined by measuring osteoclast generation and osteoclast activity in macrophage-colony stimulating factor (M-CSF)-dependent bone marrow cells (MDBMCs) and in co-cultures of MDBMCs and osteoblasts. Osteoclast generation was assayed by measuring the number of tartrateresistant acid phosphatase (TRAP) (+) multinucleated cells after culture. Osteoclast activity was assayed by measuring the area of the resorption pit after culture. We found that osteoclast generation was induced by M-CSF and receptor activator of NF-kB ligand (RANKL), and by the 1.25-dihydroxycholecalciferol in our cultures. Baicalin decreased both osteoclast generation and activity in MDBM cultures and co-cultures indicating that it may inhibit bone resorption.

Effects of Stabilizing Additives on Electroless Copper Deposition (무전해 동 도금용액 속에서 안정제의 역할)

  • 최순돈;박범동
    • Journal of the Korean institute of surface engineering
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    • v.25 no.4
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    • pp.173-180
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    • 1992
  • The effects of the stabilizing additives such as NaCN, 2-MBT and Thiourea on bath decom-position, plating rate and surface morphology have been studied. Bath stability was increased in the order of an additive-free bath, and NaCN-, 2-MBT-, and Thiourea-stabilized baths. The sta-bilizing effects may be attributed to the stability of Cu(II) -complexes. The plating rate is the re-verse order of the bath stability. Accelerative effect of 2-MBT in proper quantity(0.3mg/$\ell$) may be explained by visualizing it absorbed through benzene ring or sulfur atom on portions of the sub-strates. The strong bond of the complexing part of the molecule to nearby chelated copper ions would tend to accelerate plating by making it easier for the Cu2+ -ligand bond to be broken. Sur-face morphologies of copper deposits depend on the bath additives. Electroless copper deposits from the 2-MBT stabilized baths are finer than the deposits from the NaCN- and Thiourea- stabi-lized baths due to the strong adsorption on the substrates.

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STUDY ON THE REGULATION OF OSTEOCLAST AND T CELL ACTIVATION VIA CELL MEMBRANE PROTEINS OF TNF FAMILY, CD137 LIGAND AND RANK LIGAND (TNF계 CD137L 및 RANKL의 파골세포와 T 세포에 대한 활성조절)

  • Hong, Sung-Joon;Park, Jae-Hong;Lee, Hyeon-Woo;Lee, Keung-Ho
    • Journal of the korean academy of Pediatric Dentistry
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    • v.35 no.4
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    • pp.597-606
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    • 2008
  • Resorption of alveolar bone in periodontitis is due to excessive differentiation and activation of osteoclasts. Bacterial antigens causing periodontitis activates CD4 T cells, which leads to expressing RANK ligand (RANKL) on CD4 T cells. RANKL binds RANK on preosteoclasts or osteoclasts, and enhances the differentiation preosteoclasts into osteoclasts and the activation of mature osteoclasts. CD137, one of TNF receptor (TNFR) family, expressed on activated T cells binds with CD137 ligand (CD137L) on antigen presenting cells. Cross-linking of CD137 by CD137L acts as T cell co-stimulatory signals and, therefore, enhances the activation of T cell. In this study, I elucidated the biological responses of CD137L on (pre)osteoclasts and RANKL on T cells in the context of in vivo interaction between T cells and osteoclasts. RAW264.7, murine monocytic cells, constitutively express CD137L. Ligation of CD137L with anti-CD137L mAb inhibited RANKL-induced osteoclast formation in a dosedependent manner. Bone marrow cells are expressed CD137L by the treatment with M-CSF. Cross-linking of CD137L abolished M-CSF/ RANKL-evoked the formation of multi-nucleated osteoclasts. Both mouse CD4 and CD8 T cells are expressed RANKL following their activation. Ligation of RANKL with OPG, the decoy receptor for RANKL, inhibited both CD4 and CD8 T cell proliferation. These effects were attributed to RANKL-induced apoptosis. These data indicate that CD137L and RANKL on osteoclasts and T cells, respectively provide them with inhibitory signal.

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