• The Korean Journal of Physiology and Pharmacology
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• v.13 no.5
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• pp.361-365
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• 2009

Effects of quercetin, a kind of flavonoids, on the vasodilating actions were investigated. Among the mechanisms for quercetin-induced vasodilatation in rat aorta, the involvement with the $Ca^{2+}$ activated $K^+$ ($K_{Ca}$) channel was examined. Pretreatment with NE ($5\;{\mu}M$) or KCl (60 mM) was carried out and then, the modulation by quercetin of the constriction was examined using rat aorta ring strips (3 mm) at $36.5^{\circ}C$. Quercetin (0.1 to $100\;{\mu}M$) relaxed the NE-induced vasoconstrictions in a concentrationdependent manner. NO synthesis (NOS) inhibitor, NG-monomethyl-L-arginine acetate (L-NMMA), at $100\;{\mu}M$ reduced the quercetin ($100\;{\mu}M$)-induced vasodilatation from $97.8{\pm}3.7%$ (n=10) to $78.0{\pm}11.6%$ (n=5, p<0.05). Another NOS inhibitor, L-NG-nitro arginine methyl ester (L-NAME), at $10\;{\mu}M$ also had the similar effect. In the presence of both $100\;{\mu}M$ L-NMMA and $10\;{\mu}M$ indomethacin, the quercetin-induced vasodilatation was further attenuated by $100\;{\mu}M$ tetraethylammonium (TEA, a $K_{Ca}$ channel inhibitor). Also TEA decreased the quercetin-induced vasodilatation in endothelium-denuded rat aorta. Used other $K_{Ca}$ channel inhibitors, the quercetin-induced vasodilatation was attenuated by $0.3\;{\mu}M$ apamin (a SK channel inhibitor), but not by 30 nM charybdotoxin (a BK and IK channel inhibitor). Quercetin caused a concentration-dependent vasodilatation, due to the endotheliumdependent and -independent actions. Also quercetin contributes to the vasodilatation selectively with SK channel on smooth muscle.

• Journal of the Korean Applied Science and Technology
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• v.6 no.1
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• pp.31-40
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• 1989

Five novel amphoteric surfactants of N-acyloxyethylcarboxybetaine series were synthesized via Schotten-Baumman reaction between five acid chlorides containing 10, 12, 14, 16 and 18 carbon atoms in their N-alkyl groups and dimethylaminoethanol to give the intermediate products, 2-dimethylaminoethylalkanoates(2). Quaternization of these products(2) was permitted to from 2-(acyloxyethyldimethylammonic)- acetates(3), whose structures were identified by elemental analysis, IR spectrophotometry and $^1Hnmr$ spectrometry. The yield of the final products was shown in the range of 77-80% based on the intermediate products. The surface tension of the aqueous solution of (3) was measured, and the critical micelle concentrations (cmc) were shown in the range of $2.1\;{\times}\;10^{-3}\;-\;3.3\;{\times}\;10^{-4}mol/l$, and the surface tension at cmc was 28-36 dyne/cm. Cmc was lowered gradually by the increment of the length of N-alkyl ester containing group. The isoelectric point was shown in the range of 4.44-5.20. It showed a tendency to lean toward the acidic site and its range was broadened as increase of the hydrophobic group length. A linear relationship between log cmc and the number of carbon atoms(N) in the hydrophobic alkyl chain was shown in the relative equation of log cmc=-1.75-0.1N, and the contribution rate of N on the standard free energy change in micellization, ${\bigtriangleup}({\bigtriangleup}G^{\circ}m)/{\bigtriangleup}N$, was calculated as -0.23 RT.

• Korean Chemical Engineering Research
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• v.51 no.5
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• pp.545-549
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• 2013

For the purpose of development of effective synthetic process of CHMI, a series of experiments were preformed on the preparation of CHMAIE, the intermediate of CHMI. For the first step, CHMA was synthesized by dropwise mixing of cyclohexylamine with maleic anhydride in toluene and 98.2% of theoretical CHMA was obtained by precipitation at $10^{\circ}C$ for 2 hours. The optimum reaction temperature of the esterfication, preparation reaction of CHAMIE from CHMA, was $68^{\circ}C$, and equilibrium conversion at optimum temperature was 98.5%. Equilibrium reaction time decreased with reaction temperature, and 4 hours was taken to reach equilibrium at optimum reaction temperature. Toluene in the final reaction product could be recovered by vacuum distillation. The recovery of toluene was increased with distillation temperature and 98% of toluene could be recovered at $55^{\circ}C$.

• Polymer(Korea)
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• v.33 no.6
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• pp.569-574
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• 2009

Organic- inorganic hybrid waterborne polyurethane (PUD) is synthesized by using hybrid polyol consist of carbonate (PCD), ester (PCL), and siloxane (PDSBP) in order to enhance anti-scratch property of PUD film. The diameter of graft type PUD emulsion is bigger than that of linear type PUD due to the graft structure of hydrophobic siloxane chain. The glass transition temperature of linear type PUD increase and the decomposition temperature of linear type PUD decrease with the content of PCD polyol. While, the decomposition temperature of graft type PUD almost same with increasing PDSBP content. The anti-scratch property and pencil hardness of graft type PUD improves as adding PDSBP polyol in the hybrid polyol system. When 9 wt% of PDSBP polyol is mixed, PUD films shows excellent anti-scratch property (~3.3 N), and pencil hardness (> 9 H).

• Membrane Journal
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• v.15 no.4
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• pp.281-288
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• 2005

The hyaluronic acid (HA) with excellent biocompatibility can be combined with lactide, the ester dimer of polylactide, with good biodegradability to produce biocompatible materials applicable to drug delivery system. By freeze drying method, HA and lactide were crosslinked with crosslinking agent, 1-ethyl-3-(3-dimethyl aminopropyl) carbodiimide. Degree of lactide and EDC reaction was determined by the analysis of nuclear magnetic resonance (NMR) spectroscopy. The degree of lactide and EDC reaction increased and swelling ratio decreased as the mole ratio of lactide to HA or crosslinking agent concentration increased or reaction temperature decreased. The drug release experiment result from membranes having different degree of lactide reaction showed that drug release rate reduced in proportion to the degree of lactide reaction. The drug release experiment result from drugs having different hyrodphobicity showed that the more hydrophobic drug was released more slowly.

• Polymer(Korea)
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• v.36 no.1
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• pp.9-15
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• 2012

We prepared a series of aromatic liquid crystals (LCs) based on wholly aromatic ester units with the reactive end group methyl maleimide by means of melt condensation method, and the resulting LCs were thermally crosslinked to produce liquid crystalline thermoset (LCT) films. The synthesized LCs and LCTs were characterized with Fourier transform infrared (FTIR) spectroscopy, wide angle X-ray diffraction (WAXD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), thermomechanical analysis (TMA), and polarizing optical microscopy (POM) with a hot stage. The glass transition temperature ($T_g$) and coefficient of thermal expansion are strongly affected by the mesogen units in their main chain structures. The $p$-substituted biphenyl LC was found to have the highest thermal property value.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.5 no.1
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• pp.54-60
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• 2019

Sentinel lymph node (SLN) imaging plays an important role in surgery of patients with breast cancer and melanoma. In this study, avidin (Av), a tetrameric protein glycosylated with mannose and N-acetylglucosamine molecules, was labeled with $^{64}Cu$ and then evaluated for LN imaging. $^{64}Cu$-Labeled $NeutrAvidin^{TM}$ (NAv), a non-glycosylated form of Av, was used for comparison. 1,4,7,10-Tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid (DOTA)-conjugated Av and NAv were prepared from the corresponding proteins and DOTA-NHS ester, which were then labeled with copper-64 and purified using PD-10 columns. The numbers of DOTA molecules conjugated to Av and NAv were 4.9 and 3.3, respectively. [$^{64}Cu$]Cu-DOTA-conjugated Av and NAv were prepared in 93% and 73% radiochemical yields, respectively. In vitro serum stability study showed that copper-64 remained stable on all radiotracers for 24 h (>97%). MicroPET/CT images showed that high radioactivity was accumulated in LNs within 15 min after footpad-injection of radiotracers. Tissue distribution data of mice demonstrated significantly higher uptake in the popliteal (PO) LN than lumbar (LU) LN for $^{64}Cu$-labeled Av (relative % ID/g excluding the injection sites: 66.2% and 26.0%, respectively) compared with those of $^{64}Cu$-labeled NAv (43.0% and 49.2%, respectively). The results of this study suggest that mannose molecules on Av enabled the radiotracer to retain in the first LN after mouse footpad-injection.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.4 no.2
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• pp.57-64
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• 2018

${\omega}-[^{18}F]$-Fluorohexadecanoic acid (FHA) has been used for imaging of fatty acid metabolism of myocardium. To increase retention of radiolabeled fatty acid by blocking ${\beta}$-oxidation, methyl branched analogues have been used. In this experiment, we tried to synthesize 18F-labeled ${\alpha}-$, ${\beta}-$ and ${\omega}-FHA$ for imaging of the myocardial fatty acid metabolism. We synthesized ${\alpha}-$, ${\beta}-$ and ${\omega}$-mesylated methyl hexadecanoates and labeled with $^{18}F$ by reacting with $[^{18}F]$TBAF in acetonitrile at $80^{\circ}C$ for 10 min. Methyl ester group was removed by 1 M NaOH at $80^{\circ}C$ for 5 min. The yields of ${\alpha}-[^{18}F]$ and ${\omega}-[^{18}F]FHA$ were 25.5 and 45.5%, respectively [EOS]. However, ${\beta}-[^{18}F]FHA$ was not labeled at all due to a fast elimination reaction. The biodistribution study in ICR-mice showed that ${\omega}-[^{18}F]FHA$ has higher myocardial uptake and lower liver uptake than ${\alpha}-[^{18}F]FHA$. The electron-withdrawing effect of fluorine at ${\alpha}-$ position is believed to be the major factor affecting the biodistribution.

• Journal of Microbiology and Biotechnology
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• v.33 no.12
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• pp.1563-1575
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• 2023

Acyl-coenzyme A (CoA):diacylglycerol acyltransferase 2 (DGAT2) catalyzes the last stage of triacylglycerol (TAG) synthesis, a process that forms ester bonds with diacylglycerols (DAG) and fatty acyl-CoA substrates. The enzymatic role of Dgat2 has been studied in various biological species. Still, the full description of how Dgat2 channels fatty acids in skeletal myocytes and the consequence thereof in glucose uptake have yet to be well established. Therefore, this study explored the mediating role of Dgat2 in glucose uptake and fatty acid partitioning under short interfering ribonucleic acid (siRNA)-mediated Dgat2 knockdown conditions. Cells transfected with Dgat2 siRNA downregulated glucose transporter type 4 (Glut4) messenger RNA (mRNA) expression and decreased the cellular uptake of [1-¹⁴C]-labeled 2-deoxyglucose up to 24.3% (p < 0.05). Suppression of Dgat2 deteriorated insulin-induced Akt phosphorylation. Dgat2 siRNA reduced [1-¹⁴C]-labeled oleic acid incorporation into TAG, but increased the level of [1-¹⁴C]-labeled free fatty acids at 3 h after initial fatty acid loading. In an experiment of chasing radioisotope-labeled fatty acids, Dgat2 suppression augmented the level of cellular free fatty acids. It decreased the level of re-esterification of free fatty acids to TAG by 67.6% during the chase period, and the remaining pulses of phospholipids and cholesteryl esters were decreased by 34.5% and 61%, respectively. Incorporating labeled fatty acids into beta-oxidation products increased in Dgat2 siRNA transfected cells without gene expression involving fatty acid oxidation. These results indicate that Dgat2 has regulatory function in glucose uptake, possibly through the reaction of TAG with endogenously released or recycled fatty acids.

• Bulletin of the Korean Chemical Society
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• v.26 no.1
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• pp.91-96
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• 2005

O-(3-[$^{18}$F]Fluoropropyl)-L-tyrosine (L-[$^{18}$F]FPT) was synthesized by nucleophilic radiofluorination followed by acidic hydrolysis of protective groups and evaluated with 9 L tumor bearing rat. L-[$^{18}$F]FPT is an homologue of O-(2-[$^{18}$F]fluoroethyl)-L-tyrosine (L-[$^{18}$F]FET) which recently is studied as a tracer for tumor imaging using positron emission tomography (PET). [$^{18}$F]FPT was directly prepared from the precursor of O-(3-ptoluenesulfonyloxypropyl)- N-(tert-butoxycarbonyl)-L-tyrosine methyl ester. FPT-PET image was obtained at 60 min in 9 L tumor bearing rats. The radiochemical yield of [$^{18}$F]FPT was 0-45% (decay corrected) and the radiochemical purity was more than 95% after HPLC purification. The total time elapsed for the synthesis of [$^{18}$F]FPT was 100 min from EOB (End-of-bombardment). A comparison of uptake studies between [$^{18}$F]FPT and [$^{18}$F]FET was performed. In biodistribution, [$^{18}$F]FPT showed similar pattern with [$^{18}$F]FET in various tissues, but [$^{18}$F]FPT showed low uptake in brain. Furthermore, [$^{18}$F]FPT showed higher tumor-to-brain ratio than [$^{18}$F]FET. In conclusion, [$^{18}$F]FPT seems to be more useful amino acid tracer than [$^{18}$F]FET for brain tumors imaging with PET.