• Title/Summary/Keyword: Ligand effect

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The Effects of Cuscuta japonica Chois on Gene Expression in RANKL-induced RAW 264.7 Cell (도사자(菟絲子)가 RANKL 유도 파골세포(破骨細胞)에 미치는 영향)

  • Kim, Joon-Yeon;Hwang, Gwi-Seo
    • Journal of Society of Preventive Korean Medicine
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    • v.14 no.2
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    • pp.77-89
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    • 2010
  • Objectives : This study was performed to evaluate the effect of CJ(Cuscuta japonica Chois) on osteoclast differentiation and gene expression. Methods : The osteoclastogenesis and gene expression were determined in RANKL(receptor activator of nuclear factor kappa B ligand)-stimulated RAW 264.7. The results were summarized as followes. Results : CJ decreased the number of TRAP positive cell in RANKL-stimulated RAW264.7 cell. CJ decreased the expression of RANK(receptor activator of nuclear factor kappa B), $TNF{\alpha}$, and IL-6 in RANKL-stimulated RAW264.7 cell. CJ decreased the expression of iNOS and COX-2 in RANKL-stimulated RAW264.7 cell. CJ decreased the expression of Cathepsin K in RANKL-stimulated RAW264.7 cell. Conclusions : It is concluded that CJ might decrease the bone resorption resulted from decrease of osteoclast differentiation and it's related gene expression.

Lipopolysaccharide (LPS)-Induced Autophagy Is Responsible for Enhanced Osteoclastogenesis

  • Sul, Ok-Joo;Park, Hyun-Jung;Son, Ho-Jung;Choi, Hye-Seon
    • Molecules and Cells
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    • v.40 no.11
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    • pp.880-887
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    • 2017
  • We hypothesized that inflammation affects number and activity of osteoclasts (OCs) via enhancing autophagy. Lipopolysaccharide (LPS) induced autophagy, osteoclastogenesis, and cytoplasmic reactive oxygen species (ROS) in bone marrow-derived macrophages that were pre-stimulated with receptor activator of nuclear $factor-{\kappa}B$ ligand. An autophagy inhibitor, 3-methyladenine (3-MA) decreased LPS-induced OC formation and bone resorption, indicating that autophagy is responsible for increasing number and activity of OCs upon LPS stimulus. Knockdown of autophagy-related protein 7 attenuated the effect of LPS on OC-specific genes, supporting a role of LPS as an autophagy inducer in OC. Removal of ROS decreased LPS-induced OC formation as well as autophagy. However, 3-MA did not affect LPS-induced ROS levels, suggesting that ROS act upstream of phosphatidylinositol-4,5-bisphosphate 3-kinase in LPS-induced autophagy. Our results suggest the possible use of autophagy inhibitors targeting OCs to reduce inflammatory bone loss.

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 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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Inhibitory Effect of 4-Aryl 2-Substituted Aniline-thiazole Analogs on Growth of Human Prostate Cancer LNCap Cells

  • Baek, Seung-Hwa;Kim, Nak-Jeong;Kim, Seong-Hwan;Park, Kwang-Hwa;Jeong, Kyung-Chae;Park, Bae-Keun;Kang, Nam-Sook
    • Bulletin of the Korean Chemical Society
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    • v.33 no.1
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    • pp.111-114
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    • 2012
  • Androgen receptor (AR) is ligand-inducible nuclear hormone receptor which has been focused on key molecular target in growth and progression of prostate cancer. We synthesized a series of 4-aryl 2-substituted aniline-thiazole analogs and evaluated their anti-cancer activity in AR-dependent human prostate cancer LNCap cells. Among them, the compound 6 inhibited the tumor growth in LNCap-inoculated xenograft model.

Studies on the Zr-Pyrithione Complex (지르코늄-피리치온 착물에 관한 연구)

  • Kwon, Chung-Moo;Rhee, Gye-Ju
    • Journal of Pharmaceutical Investigation
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    • v.20 no.3
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    • pp.145-152
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    • 1990
  • Zirconium pyrithione complex was prepared by reaction of sodium-pyrithione solution and zirconyl chloride solution. The physico-chemical properties of the complex was examined by means of IR, XRD, DSC and NMR. And the stability of Zr-complex was investigated on the basis of accelerated stability analysis under conditions of temp. elevation, UV radiation and pH dependence. The result indicates that the ratio of the ligand to metal in Zr-pyrithione complex was determined 4:1, and its stability constant was $4.643{\times}10^4$. The rate order of decomposition of the complex was apparent first-order reaction of which rate constant and the decomposition rate was not only accelerated by effect of heat and UV radiation but was catalyzed by specific acid-base catalysis considered the pH dependence for the hydrolysis of the complex and the suspension was most stable over the range pH 4-8 indicating that solvent catalysis is the primary made of reaction in this region.

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Discovery of Novel TRPV1 Ligands through Rational Approach Based on Its Putative Endogenous Ligand, 12(S)-HPETE

  • Min, Kyung-Hoon;Lee, Seul;Kim, Hwa-Soon;Suh, Young-Ger
    • Bulletin of the Korean Chemical Society
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    • v.31 no.6
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    • pp.1501-1505
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    • 2010
  • We report design and synthesis of the novel TRPV1 ligands through a rational approach. Simplified analogues of 12(S)-HPETE showing TRPV1 agonistic effect are disclosed. Biological evaluation revealed that substitution of functional groups without any change in conformation converted agonist into antagonist. Our work provided key information with regard to TRPV1 agonist/antagonist switching.

Modulation of Phytotropin Receptors by Fluoride and ATP

  • Nam, Myung-Hee;Kang, Bin-G.
    • BMB Reports
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    • v.28 no.6
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    • pp.552-555
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    • 1995
  • Treatment of microsomal vesicles isolated from etiolated Pisum sativum L cv. Alaska epicotyl tissue with agents inhibiting protein dephosphorylation, namely NaF and/or ATP, resulted in increased binding of the phytotropin NPA to the putative auxin efflux carriers localized on the plasma membrane. The phytotropin effect was especially conspicuous if the vesicles were simultaneously treated with Triton X-100. Kinetic analysis of the binding indicated the existance of two distinct sites for NPA, each having different affinities. Increased binding of the phytotropin to the membrane where protein dephosphorylation was inhibited was attributable to the increased ligand affinity of both sites. Treatment of tissue segments with flubride was found to enhance in vivo auxin transport. Implications of covalent modification of the auxin efflux carrier complex for the regulation of membrane transport of auxin molecules are discussed.

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Sphingosine 1-phosphate mediated suppression of leptin secretion in rat adipocytes.

  • Jun, Dong-Jae;Kim, Kyong-Tai
    • Proceedings of the Korean Biophysical Society Conference
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    • 2001.06a
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    • pp.49-49
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    • 2001
  • Sphingosine 1-phosphate is a metabolite of complex sphingolipids that acts as both a second messenger and as a high-affinity ligand for cell surface receptor. Since the possible involvement of sphingosine 1-phosphate has not been investigated in adipocyte, we examined the response of intracellular calcium ([Ca$^{2+}$]$_{i}$) and intracellular cAMP ([cAMP]$_{i}$ and the effect of sphingosine 1-phosphate on adipocyte function using rat primary adipocyte.(omitted)ted)

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Influence of [VO4]3- Bridges on Magnetic Coupling in Ba2V3O9 Studied by Molecular Orbital Calculations

  • Kang, Dae-Bok
    • Bulletin of the Korean Chemical Society
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    • v.33 no.7
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    • pp.2341-2344
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    • 2012
  • A molecular orbital study is presented of the magnetic coupling in the one-dimensional vanadium oxide $Ba_2V_3O_9$ with a bridge formed by two different types of $VO_4$ tetrahedra. The concept of complementary versus counter-complementary effect has been used to explain the structural origin of the magnetic behavior of the compound. Namely, the observed antiferromagnetic coupling is dominated by the orbital complementarity of the V(1) tetrahedra sharing only one oxygen corner with two adjacent $VO_6$ octahedra. The second type of V(2) tetrahedra does not provide a noticeable contribution to the magnetic coupling due to the orbital counter-complementarity of the bridging ligand.