• Bulletin of the Korean Chemical Society
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• v.32 no.6
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• pp.2015-2020
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• 2011

A series of isoxazol-indolin-2-one was designed for GSK-3${\beta}$ inhibitors as novel anticancer agents based on their binding mode analysis in GSK-3${\beta}$ crystal structure. Total 21 compounds were synthesized and evaluated for their inhibitory activity against two tumor cell lines (DU145 and HT29). Most of the synthesized compounds were potent with above 80% inhibitory activity at 100 ${\mu}M$, and several compounds were examined for inhibitory activity against GSK-3${\beta}$. Among them, 15(Z) ($R_1$=H, $R_2$=3-Cl-phenyl) was most active with 78% inhibition of tumor cell line (HT29) at 20 ${\mu}M$ and 72% inhibition of GSK-3${\beta}$ at 20 ${\mu}M$.

• Journal of the Korean Association of Oral and Maxillofacial Surgeons
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• v.31 no.5
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• pp.363-369
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• 2005

Purpose: To determine the role of Insulin-like Growth Factor-I (IGF-I) in the regulation of Vascular Endothelial Growth Factor (VEGF) expression in MG-63 cells and then to find the mechanism b which this regulation occurs. Materials and methods: MG-63 cells were grown to confluence in 60-mm dishes. To determine the effects of IGF-I on expression of VEGF mRNA according to time and concentration, the cells were treated with 10 nM IGF-I, following isolation of total RNA and Northern blot analysis after 1, 2, 4, 8, 12, 24 hours and after 2 hours of treatment with 0.5, 2, 10, 25, 50 nM IGF-I respectively, isolation of total RNA and Northern blot analysis were followed. To determine the mechanism of action of IGF-I, inhibitors such as hydroxyurea $(76.1\;{\mu}g/ml)$, actinomycin D $(2.5\;{\mu}g/ml)$, cycloheximide $(10\;{\mu}g/ml)$ were added 1 hour after treatment of 10 nM IGF-I. Results: 1. the expression of VEGF mRNA was increased with treatment of IGF-I. 2. The expression of VEGF mRNA was increased according to time-and concentration dependent manner of IGF-I. 3. The effect of IGF-I was decreased by hydroxyuera, actinomycin D, but not by cycloheximide. Conclusion: IGF-I regulate the expression of VEGF mRNA in the level of DNA synthesis and transcription. These results could suggest that IGF-I plays an important role in angiogenesis in the process of new bone formation and remodeling.

• Korean Journal of Materials Research
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• v.24 no.4
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• pp.214-220
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• 2014

In this research, a precipitation method was used to synthesize ${\beta}-Ga_2O_3$ powders with various particle morphologies and sizes under varying precipitation conditions, such as gallium nitrate concentration, pH, and aging temperature, using ammonium hydroxide and ammonium carbonate as precipitants. The obtained powders were characterized in detail by XRD, SEM, FT-IR, and TG-DSC. From the TG-DSC result, GaOOH phase was transformed to ${\beta}-Ga_2O_3$ at around $742^{\circ}C$, and weight loss percent was about 14 % when $NH_4OH$ was used as a precipitant. Also, ${\beta}-Ga_2O_3$ formed at $749^{\circ}C$ and weight loss percent was about 15 % when $(NH)_2CO_3$ was used as a precipitant. XRD results showed that the obtained $Ga_2O_3$ had pure monoclinic phase in both cases. When $(NH)_2CO_3$ was used as a precipitant, the particle shape changed and became irregular. The range of particle size was about $500nm-4{\mu}m$ based on various concentrations of gallium nitrate solution with $NH_4OH$. The particle size was increased from $1-2{\mu}m$ to $3-4{\mu}m$ and particle shape was changed from spherical to bar type by increasing aging temperature over $80^{\circ}C$.

• Bulletin of the Korean Chemical Society
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• v.26 no.4
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• pp.634-640
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• 2005

The reaction of cis-[Cr([14]-decane)(OH$_2)_2]^+$ ([14]-decane = rac-5,5,7,12,12,14-hexamethyl-1,4,8,11-teraazacyclotetradecane) with auxiliary ligands {$L_a$ = citrate(cit)} leads to a new dimeric complex cis-[{Cr([14]-decane)($\mu$-cit)}$_2](ClO_4)_2$. This binuclear complex has been structurally characterized by a combination of elemental analysis, conductivity, IR and Vis spectroscopy, mass spectrometry, and X-ray crystallography. Analysis of the crystal structure of cis-[{Cr([14]-decane)($\mu$-cit)})($_2]^+$ reveals that each chromium has a distorted octahedral coordination environment and citrato ligands are monodentate to the two chromium atoms via the carboxyl groups. For dimeric complex the bridging geometry is as follows: Cr$\ldots$Cr = 7.361 $\AA$; Cr-O(average) = 1.958 (8) $\AA$; Cr-N range = 2.108 (9)-2.147(9) $\AA$; N(1)-Cr-N(3) (equatorial position) = 98.0(4)$^{\circ}$; N(2)-Cr-N(4) (axial position) = 166.4(4)$^{\circ}$; O(1)-Cr-N(2) = 98.1(4)$^{\circ}$; O(3)-Cr-N(4) = 96.6(3)$^{\circ}$; O(1)-Cr-O(3) = 90.4$^{\circ}$. The FAB mass spectrum of the dimeric complex displays peak due to the molecular ions cis-[{Cr([14]-decane)($\mu$-cit)})($_2]^+$ at m/z 1053.

• Korean Journal of Pharmacognosy
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• v.33 no.3 s.130
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• pp.245-251
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• 2002

Flavonoid seems to have various biological effects. Quercetin is a kind of natural plant flavonoids and has multiple biological effects such as antioxidant, antimutagenic and anticarcinogenec agent. Melanogenesis is a physiological process resulting in the synthesis of melanin pigments, which play a crucial protective role against skin photocarcinogenesis. This present study was designed to investigate effect of quercetin on proliferation and melanogenesis in Melan-a melanocyte cells. After 48h treatment of cells with quercetin, the cells exhibited a dose-dependent inhibition in their proliferation without apoptosis. Therefore, thε growth retardation by the extract may be due to the cell arrest or cell differentiation. We also investigated the effect of quercetin on melanogenesis of this cells. Melan-a melanocyte cells were grown for 48h in the presence of $0.01-60\;{\mu}g/ml$ quercetin and the total melanin content and activity of tyrosinase were measured. Quercetin stimulated melanization of the cells in low concentrations $(0.01-1.0\;{\mu}g/ml)$, whereas it inhibited melanization in high concentrations $(5.0-30\;{\mu}g/ml)$. It was observed that quercetin differently regulates melanogenesis of Melan-a melanocyte cells dependent on Its concentrations.

• Archives of Pharmacal Research
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• v.24 no.1
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• pp.55-63
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• 2001

Aucubin, an irdoid g1ucoside, was investigated to determine whether it has a stimulating effect on $\alpha$-amanitin excretion in $\alpha$-amanitin intoxicated rats, and whether there is binding activity to calf thymus DNA. High-performance liquid chromatography (HPLC) analysis of $\alpha$-amanitin in rat urine allowed quantitative measurement of the $\alpha$-amanitin concentration with a detection limit of 50${mu}g/ml$. In this system, a group treated with both $\alpha$-amanitin and aucubin showed that o(-amanitin was excreted about 1.4 times faster than in the $\alpha$-amanitin only treated group. Our previous results showed that the toxicity of $\alpha$-amanitin is due to specific inhibition of RNA polymerase activity and the resultant blockage of the synthesis of certain RNA species in the nucleus. However, no significant activity change on RNA polymerase from Hep G2 cells was observed when aucubin was treated with $\alpha$-amanitin at any concentration tested. Nevertheless, aucubigenin inhibited both DNA polymerase (IC50, 80.5${mu}g/ml$) and RNA polymerase (IC50, 135.0${mu}g/ml$) from the Hep G2 cells. The potential of both $\alpha$-amanitin and aucubin to interact with DNA were examined by spectrophotometric analysis. $\alpha$-Amanitin showed no significant binding capacity to calf thymus DNA, but aucubin was found to interact with DNA, and the apparent binding constant ($K_{app}$) and apparent number of binding sites per D7A phosphate ($B_{app}$) were 0.45$0.45{\times}$$10^4$ $M^{-1}$ and 1.25, respectively.

• Archives of design research
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• v.3 no.1
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• pp.17-33
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• 1990

Evaluation plays an essential role in design activity. Many theorist have agreed that designing involves problem solving or decision making. In evaluation, designers attempt to determine the value of a particular proposal arrived at by synthesis. And the results of designing, the product, is evaluated twice, objectively and subjectively.Alternatives in $$\mu$ti-objective decision problems generally possess numerous attributes by which they can be described and compared. The evaluation factors include all attributes that have levels specified by quantitative and qualitative objectives. However since qualitiative factors are difficult to quantify as $$\mu$eral estmates, these factors have tended to be ignored without regard for their importance to human content. Therefore we need some study that convert qualitative attributes into quantitative scale values. Following to Thurstone' s Psychological scaling methods (The method of successive intervals), attribute values of TV set are assigned by rating scale methods. The method of successive intervals, like the method of equal-appearing intervals, requires but a single judgement from each subject for each statement to be scaled. It is, therefore, a convinient method to use when the number of to be scaled is large. We make the assumtion that those cu$$\mu$ative proportion distributions are normal for each statement when they are projected on the unknown psychological continuum. In this study, we have determined the scale values of 42 statements of TV set by the method of successive intervals. Then we can apply a test of internal consistency similar to that used with the method of paired comparisons. We have as our absolute average deviation, -1.748/252= -0.0069. We have reason to believe that our scale values are consistent with the empirical data, because these discrepanicies are very small.

• Archives of Pharmacal Research
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• v.27 no.5
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• pp.502-506
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• 2004

Two series of 2-(5-nitro-2-furyl)- and 2-(1-methyl-5-nitro-1H-imidazol-2-yl)-5-propyl, allyl and propargyl)thio-1,3,4-thiadiazoles (6a-f) and 2-(5-nitro-2-furyl)- and 2-(1-methyl-5-nitro-1 H-imidazol-2-yl)-5-(nitrobenzyl)thio-1,3,4-thiadiazole derivatives (8a-f) have been synthesized and evaluated against Mycobacterium tuberculosis, as part of the TAACF TB screening program under direction of the US National Institute of Health, the NIAID division. Primary screening was conducted at a single concentration, 6.25 $\mu\textrm{g}$mL$^{-1}$ , against M. tuberculosis H$_{37}$ Rv in BACTEC 12B medium, using the Microplate Alamar Blue Assay (MABA). The minimum inhibitory concentration (MIC) was determined for the compounds that demonstrated $\geq$90% growth inhibition in the primary screening. A varying degree of antituberculosis activity (from 0-97% of growth inhibition) was observed with the alkylthio series (6a-f), and the nitroimidazole derivative with a propylthio group (6b) and the nitrofuran derivative with a propargylthio group (6e), were the most active compounds (MIC=3.13 and 1.56 /$\mu\textrm{g}$mL$^{-1}$ , respectively). Among the nitrobenzylthio derivatives (8a-f), all the ortho, meta and para nitrobenzyl isomers in the nitrofuran series exhibited good antituberculosis activity (MIC=3.13 $\mu\textrm{g}$mL$^{-1}$ ), while the corresponding nitroimidazole analogues were completely inactive (Inhibition=0%).

• Food Science and Preservation
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• v.21 no.5
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• pp.735-739
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• 2014

Ephedra sinica Stapf, known as a medicinal plant, inhibited not only syncytium formation, but also trafficking of viral glycoprotein, hemagglutinin-neuramidase (HN) to the cell-surface. Trafficking of viral glycoprotein to the surface of infected-cells results in syncytium formation in Newcastle disease virus (NDV)-infected baby hamster kidney (BHK) cells. Viral glycoprotein in the infected-cell is processed within the endoplasmic reticulum during routing into surface. The processing of viral glycoprotein like a N-linked oligosaccharide trimming by ${\alpha}$-glucosidase in cell is necessary for virus infection. Methanol extracts showed inhibitory activities ($IC_{50}$ $15{\mu}g/mL$) against ${\alpha}$-glucosidase. This suggested that E. sinica extracts inhibited the cell-surface expression of NDV-HN glycoprotein without significantly affecting HN glycoprotein synthesis in NDV-infected BHK cells.

• Korean Chemical Engineering Research
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• v.45 no.6
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• pp.560-565
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• 2007

Copper fine particles, ranging from $0.11{\mu}m$ to $0.64{\mu}m$ in average size, were prepared by a chemical reduction method using hydrazine ($N_2H_4$) as a reduction agent in waste copper solutions. The effect of the amount of hydrazine addition was investigated on the properties of the obtained powders. Also, the effect of the addition of dispersing agents [Polyvinyl alcohol (PVA), polyvinyl pyrrolidone (PVP)] during particle synthesis was studied. The powders, obtained from 1 M waste copper solutions, showed the mixtures of Cu and $Cu_2O$ crystals at low hydrazine addition amounts of 0.8 mol and 1.0 mol, while those exhibited pure Cu crystals at adequate hydrazine addition amount of 0.12 mol. The average size of the Cu powders decreased with increasing the concentrations of hydrazine and dispersing agents. The addition of PVA to the solutions as a dispersing agent was more effective than that of PVP in preventing the aggregation of particles.