Journal of Radiopharmaceuticals and Molecular Probes
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v.8
no.2
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pp.63-70
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2022
The development of myocardial perfusion imaging (MPI) agents has been motivated because coronary artery disease has been one of the leading causes of death worldwide since the 1960s. Several positron emission tomography (PET) MPI agents were developed, and 18F-labeled phosphonium cations were reported actively among them. In this study, we synthesized novel 18F-labeled phosphonium cations, (5-[18F]fluoropentyl)diphenyl(pyridin-2-yl)phosphonium and (2-(2-[18F]fluoroethoxy)ethyl)diphenyl(pyridin-2-yl)phosphonium, and evaluated potential as MPI agents. Two labeled compounds were synthesized via nucleophilic substitution reactions of 18F-fluoride with the appropriate tosylate precursor in the presence of Kryptofix 2.2.2 and K2CO3. MicroPET studies were performed in normal rats to evaluate in vivo distribution of radiolabeled phosphonium cations for 60 min. The radiolabeled compounds were synthesized with 5%-10% yield. The radiochemical purity of labeled compounds was > 98% by analytical HPLC, and the specific activity was > 11.8 GBq/µmol. The result of microPET studies of these labeled compounds in rats showed intense uptake in the myocardium at 30 and 60 min. The results suggest that these 18F-labeled novel phosphonium cations would have potential as promising candidates for myocardial perfusion imaging.
Hasan, Maher Abd Ali;Jasim, Kareem Ali;Miran, Hussein Ali Jan
Korean Journal of Materials Research
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v.32
no.2
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pp.66-71
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2022
In this article, Pb2Ba1.7Sr0.3Ca2Cu3O10+δ superconductor material was synthesized using conventional solid-state reaction method. X-ray diffraction (XRD) analysis demonstrated one dominant phase 2223 and some impurities in the product powder. The strongest peaks in the XRD pattern were successfully indexed assuming a pseudo-tetragonal cell with lattice constants of a = 3.732, b = 3.733 and c = 14.75 Å for a Pb-Based compound. The crystallite size and lattice strain between the layers of the studied compound were estimated using several methods, namely the Scherrer, Williamson-Hall (W.H), size-strain plot (SSP) and Halder Wagner (H.W) approach. The values of crystallite size, calculated by Scherrer, W.H, SSP and H.W methods, were 89.4540774, 86.658638, 87.7555823 and 85.470086 Å, respectively. Moreover, the lattice strain values obtained by W.H, SSP and H.W methods were 0.0063240, 0.006325 and 0.006, respectively. It was noted that all crystallite size results are consistent; however, the best method is the size-strain plot because it gave a value of R2 approaching one. Furthermore, degree of crystallites was calculated and found to be 59.003321%. Resistivity analysis suggests zero-resistance, which is typical of superconducting materials at critical temperature. Four-probe technique was utilized to measure the critical temperature at onset Tc(onset), zero resistivity Tc(off set), and transition (width ΔT), corresponding to temperatures of 128 K, 116 K, and 12 K, respectively.
Purpose $^{18}F-THK5351$ is the newly developed PET probe for tau imaging in alzheimer's disease. The purpose of study was to establish the automated production of $^{18}F-THK5351$ on a commercial module. Materials and Methods Two different approaches were evaluated for the synthesis of $^{18}F-THK5351$. The first approach (method I) included the nucleophilic $^{18}F$-fluorination of the tosylate precursor, subsequently followed by pre-HPLC purification of crude reaction mixture with SPE cartridge. In the second approach (method II), the crude reaction mixture was directly introduced to a semi-preparative HPLC without SPE purification. The radiosynthesis of $^{18}F-THK5351$ was performed on a commercial GE $TRACERlab^{TM}$$FX-_{FN}$ module. Quality control of $^{18}F-THK5351$ was carried out to meet the criteria guidelined in USP for PET radiopharmaceuticals. Results The overall radiochemical yield of method I was $23.8{\pm}1.9%$ (n=4) as the decay-corrected yield (end of synthesis, EOS) and the total synthesis time was $75{\pm}3min$. The radiochemical yield of method II was $31.9{\pm}6.7%$ (decay-corrected, n=10) and the total preparation time was $70{\pm}2min$. The radiochemical purity was>98%. Conclusion This study shows that method II provides higher radiochemical yield and shorter production time compared to the pre-SPE purification described in method I. The $^{18}F-THK5351$ synthesis by method II will be ideal for routine clinical application, considering short physical half-life of fluorine-18 ($t_{1/2}=110min$).
Kim, Eun-Jung;Choi, Tae-Hyun;Ahn, Soon-Hyuk;Kim, Byoung-Soo;Park, Hyun;Cheon, Gi-Jeong;Rhee, Hak-June;An, Gwang-Il
Nuclear Medicine and Molecular Imaging
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v.43
no.5
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pp.478-486
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2009
Purpose: 5-iododeoxyuridine analogues have been exclusively developed for the potential antiviral and antitumor therapeutic agents. In this study, we synthesized carbocyclic radioiododeoxyuridineanalogue (ddIVDU) and carbocyclic intermediate as efficient carbocyclic radiopharmaceuticals. Materials and Methods: The synthesis is LAH reduction, hetero Diels-Alder reaction as key reactions including Pd(0)-catalyzed coupling reaction together with organotin. MCA-RH7777 (MCA) and MCA-tk (HSV1-tk positive) cells were treated with various concentration of carbocyclic ddIVDU, and GCV. Cytotoxicity was measured by the MTS methods. For in vitro uptake study, MCA and MCA-tk cells were incubated with 1uCi of [$^{125}I$]carbocyclic ddIVDU. Accumulated radioactivity was measured after various incubation times. Results: The synthesis of ddIVDU and precursor for radioiodination were achieved from cyclopentadiene in good overall yield, respectively. The radioiododemetallation for radiolabeling gave more than 80% yield with > 95% radiochemical purity. GCV was more toxic than carbocyclic ddIVDU in MCA-tk cells. Accumulation of [$^{125}I$]carbocyclic ddIVDU was higher in MCA-tk cells than MCA cells. Conclusion: Biological data reveal that ddIVDU is stable in vitro, less toxic than ganciclovir (GCV), and selective in HSV1-tk expressed cells. Thus, this new carbocyclic nucleoside, referred to in this paper as carbocyclic 2',3'-didehydro-2',3'-dideoxy-5- iodovinyluridine (carbocyclic ddIVDU), is a potential imaging probe for HSV1-tk.
Kang M. Y.;Han M. S.;Lee S. C.;Kim J. H.;Sohn S. H.
Reproductive and Developmental Biology
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v.29
no.1
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pp.1-7
/
2005
Telomeres consisting of (TTAGGG)n tandem repeat DNA sequences and associated proteins are essential for chromosome stability and related with cell senescence, apoptosis and cancer. The telomerase is a ribonucleoprotein which act as a template for the synthesis of telomeric DNA. This study was carried out to identify the distribution of telomeres on mouse chromosomes and also to analyze the amount of telomeres and telomerase activity of mouse embryos at early embryonic stages. Germ cells and early embryos from 1 cell to blastocyst stage were analyzed. The amount of telomeres was analyzed by quantitative fluorescence in situ hybridization technique(Q-FISH) using a human telomeric DNA probe, and telomerase activity was measured by telomeric repeat amplification protocol assay(TRAP). In results, the telomeres on mouse chromosomes were distributed at the ends of all autosomes and sex chromosomes. Although the quantity of telomeres varied among chromosomes, most of chromosomes had higher amount in q-arm telomeres than in p-arm telomeres. The results of Q-FISH indicated that the relative amount of telomeres of mouse embryos in each embryonic stage was approximately the same except the higher amount in blastocysts. Using TRAP assay on mouse embryos, telomerase activity was detected in all preimplantation stages from mature oocytes to blastocysts. Especially the telomerase activity was significantly increased at the morula and blastocyst stage. In conclusion, there may be a close association between the amount of telomeres and telomerase activity in early embryonic stages, and analysis of telomere quantity and telomerase activity on early development will be helpful for the investigation of embryogenesis and embryonic cell differentiation in mice.
Journal of the Korean Crystal Growth and Crystal Technology
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v.12
no.2
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pp.68-72
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2002
The $\beta$-$FeSi_2$ and $\alpha$-$FeSi_2$ single crystals were synthesized by chemical vapour transport (CVT) using iodine as a transporting agent from the commercially available $FeSi_2$ powder. The $FeSi_2$ powder together with iodine were sealed in an evacuated quartz ampoule and the ampoule then being placed in two-zone electrical furnace for growing crystal. The CVT of $FeSi_2$ with iodine yielded $\beta$-$FeSi_2$ and $\alpha$-FeSi$_2$ single crystals at deposition temperature of 750 and $950^{\circ}C$ respectively. The source temperature was $1050^{\circ}C$ in both cases. The crystals of the $\alpha$-FeSi$_2$ phase were typically plate shaped with dimensions of about $10\times 10 \textrm{mm}^2$, whereas the crystals of orthorhombic $\beta$-$FeSi_2$ phase grew predominantly in the fonts of thin needle of about 10 mm in length. The composition of$\alpha$-FeSicrystal determined by electron probe microanalysis (EPMA) resulted in Si-rich $FeSi_{2.58}$ . 57. Furthermore, the CVT $\beta$-$FeSi_2$ crystal was found to be transformed to the high temperature $\alpha$-$FeSi_2$phase above $930^{\circ}C$.
Telomeres consist of TTAGGG tandem repeated DNA sequences with specific proteins and locate at chromosome ends. Telomeres are essential for chromosome stability and are related with cell senescence, apoptosis and cancer. Telomerase is a ribonucleoprotein which has a template for the synthesis of telomeric DNA. This study was carried out to analyze the amount of telomeric DNA and telomerase activity in cattle cells. Analysis of the quantity of telomere in lymphocytes was done at different ages, sex and among Korean cattle and Holstein breeds. The telomerase activity was also analyzed in liver, brain, heart, kidney, and testis tissues of fetal calf and of 18 month old cattle. The amount of telomeres in lymphocytes and other tissue cells was analyzed by Quantitative-Fluorescence in situ Hybridization (Q-FISH) technique using a telomeric DNA probe. Telomerase activity was analyzed by Telomeric Repeat Amplification Protocol assay (TRAP). The amount of telomeric DNA on the lymphocytes during the whole life span was decreased along with age. Quantity of telomeres in Korean cattle was significantly higher than that in Holstein breed. The amount of telomeric DNA in males was significantly higher than that in females. Telomerase activity was up-regulated in most bovine tissues during fetal stage, but was down-regulated in most tissues at mature 18 month age except the testis cells. This study indicates that the amount of telomeres and telomerase activity of cells can be used as an age marker or/and a physiological marker of cattle.
Kim, Dong-Yeon;Yu, Kook-Hyun;Bom, Hee-Seung;Min, Jung-Joon
Nuclear Medicine and Molecular Imaging
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v.41
no.6
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pp.561-565
/
2007
Purpose: Lipophilic cations including tetraphenylphosphonium (TPP) salts penetrate the hydrophobic barriers of the plasma and mitochondrial membranes, resulting in accumulation in mitochondria in response to the negative inner transmembrane potentials. The development of radiolabeled phosphonium cations as a noninvasive imaging agent may serve as a new molecular "voltage sensor" probe to investigate the role of mitochondria in the pathophysiology and diagnosis of cancer. Materials and Methods: We have synthesized a reference compound (4-fluorophenyl)triphenylphosphonium (TPP) and a labeled compound $[^{18}F]$TPP via two step nucleophilic substitution of no-carrier-added $[^{18}F]$fluoride with the precursor, 4-iodophenyltrimethylammonium iodide, in the presence of Kryptofix-2.2.2 and $K_2CO_3$. Result: The reference compound (4-fluorophenyl)triphenylphosphonium (TPP) was synthesized in 60% yield. The radiolabeled compound $[^{18}F]$TPP was synthesized in $10\sim15%$ yield. The radiochemical purity of the $[^{18}F]$TPP was $95.57{\pm}0.51%$ (n=11). Conclusion: $[^{18}F]$TPP was successfully synthesized that might have a potential to be utilized as a novel myocardial or cancer imaging agent for PET. However, it is required to improve the radiochemical yield to apply $[^{18}F]$TPP in preclinical or clinical researches.
Proceedings of the Korean Society of Dyers and Finishers Conference
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2010.03a
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pp.40-40
/
2010
Studies on attractive color changing property of dye chromophore and fluorophore have been greatly enjoyed in the related industrial and research fields such as optoelectronics, chemosensor, biosensor and so on. The optical property based on D-$\Pi$-A intramolecular charge transfer (ICT) system of chromophore molecules can be utilized as suitable sensing probes for checking media polarity and determining colorimetric chemosensing effect, especially heavy metal detection. These finding are obtained by absorption and emission properties. In this work, donor-acceptor D-$\Pi$-A type fluorescent dyes were designed and synthesized with the corresponding donor and acceptor groups. The selected donor moieties might be provided prominent amorphous properties which are very useful in designing and synthesizing functional polymers and in fabricating devices. Another reasons to choose are commercial availabilities in high purity and low price. Donor-bridge-acceptor (D-A) type dyes can produce impressive optical-physical properties, yielding them potentially suitable for applications in the synthesis of small functional organic molecules. Small organic functional molecules have unique advantages, such as better solubility, amorphous character, and represent an area of research which needs to be explored and developed. Currently, their applications in metalorganic compounds is rapidly expanding and becoming widespread in self-assembly processes, photoluminescence applications, chiral organocatalysts, and ingrafts with nanomaterials. Colloidal nanoparticles have received great attentions in recent years. The photophysical properties of nanoparticles, particularly in terms of brightness, photostability, emission color purity and broad adsorption range, are very attractive functions in many applications. To our knowledge background, colloidal nanoparticles have been enjoyed their applications in bio-probe research fields. This research interest can be raised by the advantages of the materials such as high photoluminescence quantum yields, sharp emission band, long-term photostability and broad excitation spectra. In recent, the uses of nanoparticles being embedded in a polymer matrix and binded on polymer surface have been explored and their properties such as photo-activation and strong photoluminescence have been proposed. The prepared chromophores and nanoparticles were investigated with absorption and emission properties, solvatochromic behaviors, pH induced color switching effects, chemosensing effects and HOMO/LUMO energy potentials with computer simulation. In addition, synthesized fluorophore dyes and particles were applied onto PE/Aramid fiber fluorescing colorations. And the related details were then discussed.
Proceedings of the Korean Vacuum Society Conference
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2010.02a
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pp.59-59
/
2010
Graphene is a 2-D sheet of $sp^2$-bonded carbon arranged in a honeycomb lattice. This material has attracted major interest, and there are many ongoing efforts in developing graphene devices because of its high charge mobility and crystal quality. Therefore clear understanding of the substrate effect and mechanism of synthesis of graphene is important for potential applications and device fabrication of graphene. In a published paper in J. Phys. Chem. C (2008), the effect of substrate on the atomic/electronic structures of graphene is negligible for graphene made by mechanical cleavage. However, nobody shows the interaction between Ni substrate and graphene. Therefore, we have studied this interaction. In order to studying these effect between graphene and Ni substrate, We have observed graphene synthesized on Ni substrate and graphene transferred on $SiO_2$/Si substrate through Raman spectroscopy. Because Raman spectroscopy has historically been used to probe structural and electronic characteristics of graphite materials, providing useful information on the defects (D-band), in-plane vibration of sp2 carbon atoms (G-band), as well as the stacking orders (2D-band), we selected this as analysis tool. In our study, we could not observe the doping effect between graphene and Ni substrate or between graphene and $SiO_2$/Si substrate because the shift of G band in Raman spectrum was not occurred by charge transfer. We could noticed that the bonding force between graphene and Ni substrate is more strong than Van de Waals force which is the interaction between graphene and $SiO_2$/Si. Furthermore, the synthesized graphene on Ni substrate was in compressive strain. This phenomenon was observed by 2D band blue-shift in Raman spectrum. And, we consider that the graphene is incommensurate growth with Ni polycrystalline substrate.
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