• Title/Summary/Keyword: FK

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Preparation of Highly Water Soluble Tacrolimus Derivatives: Poly(Ethylene Glycol) Esters as Potential Prod rugs

  • Chung, Yong-Seog;Cho, Hoon
    • Archives of Pharmacal Research
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    • v.27 no.8
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    • pp.878-883
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    • 2004
  • Tacrolimus (FK506), which is isolated from Streptomyces tsukubaensis, is a new potent immu-nosuppressant. Because of poor solubility in water, the conventional intravenous dosage forms of tacrolimus contain surfactants such as cremophor EL (BASF Wyandotte Co.) or hydroge-nated polyoxy 60 castor oil (HCO-60) which may cause adverse effects. This study relates to a polymer-tacrolimus conjugate, which can be dissolved in water, formed by chemically binding the sparingly soluble drug, tacrolimus, with the water soluble polymer, methoxypoly(ethylene glycol) (mPEG). Water soluble tacrolimus-mPEG conjugates have been synthesized and shown to be function in vitro as prodrugs. These conjugates are in the form of an ester wherein the 24-, 32- or 24,32-positions are esterified. The desired 24-, 32- or 24,32-esterified com-pounds were obtained by initially acylating of tacrolimus with iodoacetic acid at the 24-,32-, or 24,32-positions and then reacting the resulting acylated tacrolimus with a mPEG in the pres-ence of a base such as sodium bicarbonate. These conjugates were converted again into tac-rolimus by the action of enzymes in human liver homogenate, and the half-lives of the conjugates are approximately 10 min in the homogenate, indicating that the esterified tacroli-mus derivatives may be practically applicable as a prod rug for the immunosuppressant.

Scaling law in MHD turbulence small-scale dynamo

  • Park, Kiwan;Ryu, Dongsu
    • The Bulletin of The Korean Astronomical Society
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    • v.39 no.2
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    • pp.74.2-74.2
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    • 2014
  • Magnetohydrodynamics(MHD) dynamo depends on many factors such as viscosity ${\gamma}$, magnetic diffusivity ${\eta}$, magnetic Reynolds number $Re_M$, external driving source, or magnetic Prandtl number $Pr_M$. $Pr_M$, the ratio of ${\gamma}$ to ${\eta}$ (for example, galaxy ${\sim}10^{14}$), plays an important role in small scale dynamo. With the high PrM, conductivity effect becomes very important in small scale regime between the viscous scale ($k_{\gamma}{\sim}Re^{3/4}k_fk_f$:forcing scale) and resistivity scale ($k_{\eta}{\sim}PrM^{1/2}k_{\gamma}$). Since ${\eta}$ is very small, the balance of local energy transport due to the advection term and nonlocal energy transfer decides the magnetic energy spectra. Beyond the viscous scale, the stretched magnetic field (magnetic tension in Lorentz force) transfers the magnetic energy, which is originally from the kinetic energy, back to the kinetic eddies leading to the extension of the viscous scale. This repeated process eventually decides the energy spectrum of the coupled momentum and magnetic induction equation. However, the evolving profile does not follow Kolmogorov's -3/5 law. The spectra of EV (${\sim}k^{-4}$) and EM (${\sim}k^0$ or $k^{-1}$) in high $Pr_M$ have been reported, but our recent simulation results show a little different scaling law ($E_V{\sim}k^{-3}-k^{-4}$, $EM{\sim}k^{-1/2}-k^{-1}$). We show the results and explain the reason.

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The Etching Characteristics of (Ba0.6Sr0.4)TiO3 films Using Ar/CF4 Inductively Coupled Plasma (Ar/CF4 유도결합 플라즈마를 이용한 (Ba0.6Sr0.4)TiO3 박막의 식각 특성)

  • 강필승;김경태;김동표;김창일;이수재
    • Journal of the Korean Institute of Electrical and Electronic Material Engineers
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    • v.15 no.11
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    • pp.933-938
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    • 2002
  • (Ba,Sr)TiO$_{4}$ (BST) thin films on Pt/Ti/SiO$_{2}$/Si substrates were deposited by a sol-gel method and the etch characteristics of BST thin films have been investigated as a function of gas mixing ratio. The maximum etch rate of the BST films was 440 $AA$/min under such conditions as: CF$_{4}$(CF$_{4}$+Ar) of 0.2, RF-power of 700 W, DC-bias voltage of -200 V, pressure of 15 mTorr and substrate temperature of 30 $^{circ}C$. The selectivities of BST to Pt, SiO$_{2}$ and PR were 0.38, 0.25 and 0.09, respectively. In the XPS (X-ray photoelectron spectroscopy) analysis, Barium (Ba) and Strontium (Sr) component in BST thin films formed low volatile compounds such as BaFx, SrFx, which are forms by the chemical reaction with F atoms and is removed by Ar ion bombardment. Titanium (Ti) is removed by chemical reaction such as TiF with ease. The result of secondary ion mass spectrometry (SIMS) analysis confirmed the existence of the BaFx, SrFK, TiFx.

Effect of Addition of Mushroom and Sea Tangle Extracts and Mustard Leaf on Anti-oxidant Properties of Kimchi (버섯 및 다시마 추출물과 갓의 첨가가 김치의 항산화 특성에 미치는 영향)

  • Ha, Seon-Hye;Kang, Soon Ah
    • The Korean Journal of Food And Nutrition
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    • v.31 no.4
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    • pp.471-477
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    • 2018
  • The antioxidant properties of mushroom and sea tangle extracts and mustard leaf added to Kimchi were investigated by total phenolic content, DPPH radical scavenging, ABTS anion scavenging, FRAP reducing power, and ORAC value. Total phenolic content of functional Kimchi (FK) was significantly higher than that of control Kimchi (CK). DPPH radical and ABTS anion scavenging activities of functional Kimchi were significantly higher than those of control Kimchi by 2.7 and 1.7 fold, respectively (p<0.05). Also, the FRAP reducing power and ORAC value of functional Kimchi increased compared to those of the control Kimchi by 1.6 and 1.1 fold, respectively (p<0.05). Our results suggest that functional Kimchi made by mushroom and sea tangle extracts and mustard leaf may be a potent antioxidant source and could be developed as a antioxidant functional food that may be for the effective treatment of oxidant conditions. Through continuous research and development of functional Kimchi by the use of mushroom and sea tangle extracts, it will be necessary to try to identify other functions that could be useful for preventing various diseases.

A Study of f-${\theta}$ Lens Design for Axisymmetric Spherical Surface for RGB Laser Display and its applications (RGB 레이저 가시화를 위한 축대칭 구면 f-${\theta}$ 렌즈 설계 및 프로젝션응용)

  • Lee, Y.M.;Choi, H.W.
    • Laser Solutions
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    • v.14 no.2
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    • pp.24-29
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    • 2011
  • The design of a telecentric f-${\theta}$ lens with a field of view (FOV) $30^{\circ}$ and an effective focal length of 1000mm is presented. The optical stop is placed at the front plane and the design is based on a geometric ray tracing technique, and the designed system consists of a series of convex and concave lenses. The designed f-${\theta}$ lens showed a considerable reduction in weight with a simplified structure and resulted in a good performance in the designated FOV. Detail analysis of rays is also presented. 653nm (red laser), 586nm (green laser), and 468nm (blue laser) were simulated as a light source and image illuminating source. The developed optical design requires 7 pieces of lenses made of SF1, N-FK56, N-LAK33, and BK7 glass materials. With optimal parametric design, the effective focal length was calculated to be 974.839mm which is very close to the initial design target. For the manufacturing purpose, the dimensions of lens curvature and thickness were truncated with error ranging 0.1% to 3.2%. As a result, the overall error was calculated to be 3.2% which can be still tolerable for display, laser material, and machining processing.

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Contribution of Genetic and Neuroimaging Studies towards a Better Understanding of Post-Traumatic Stress Disorder (외상 후 스트레스 장애의 이해에 있어서 유전학 및 뇌영상 연구의 기여)

  • Kim, Ji-Eun E.;Lyoo, In-Kyoon;Jun, Chan-Soo;Lee, Yu-Sang
    • Korean Journal of Biological Psychiatry
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    • v.17 no.4
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    • pp.177-193
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    • 2010
  • Significant advances have been made in understanding the biological underpinnings of post-traumatic stress disorder(PTSD), particularly in the field of genetics and neuroimaging. Association studies in candidate genes related with hypothalamic-pituitary-adrenal axis, monoamines including serotonin, dopamine and noradrenaline, and proteins including FK506-binding protein 5 and brain-derived neurotrophic factor have provided important insights with regard to the vulnerability factors in PTSD. Genome-wide association studies and epigenetic studies may provide further information for the role of genes in the pathophysiology of PTSD. Hippocampus, medial prefrontal cortex, anterior cingulated cortex and amygdala have been considered as key structures that underlie PTSD pathophysiology. Future research that combines genetic and neuroimaging information may provide an opportunity for a more comprehensive understanding of PTSD.

Construction of Glomerular Epithelial Cells Expressing Both Immune Tolerance and GFP Genes and Application to Cell Therapy by Cell Transplantation

  • Ohga, Masahiro;Ogura, Mariko;Matsumura, Mastoshi;Wang, Pi-Chao
    • Biotechnology and Bioprocess Engineering:BBE
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    • v.7 no.5
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    • pp.303-310
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    • 2002
  • Cell therapy applied to wound healing or tissue regeneration presents a revolutionary realm to which principles of gene engineering and delivery may be applied. One promising application is the transplantation of cells into the wounded tissue to help the tissue repair. However, when cells are transplanted from in vitro to in vivo, immune rejection occurs due to the immune response triggered by the activation of T-cell, and the transplanted cells are destroyed by the attack of activated T-cell and lose their function. Immune suppressant such as FK506 is commonly used to suppress immune rejection during transplantation. However, such kind of immune suppressants not only suppresses immune rejection in the periphery of transplanted cells but also suppresses whole immune response system against pathogenic infection. In order to solve this problem, we developed a method to protect the desired cells from immune rejection without impairing whole immune system during cell transplantation. Previously, we reported the success of constructing glomerular epithelial cells for removal of immune complex, in which complement receptor of type 1 (CR1) was over-expressed on the membrane of renal glomerular epithelial cells and could bind immune complex of DNA/anti-DNA-antibody to remove immune complex through phagocy-tosis [1]. Attempting to apply the CR1-expressing cells to cell therapy and evade immune rejection during cell transplantation, we constructed three plasmids containing genes encoding a soluble fusion protein of cytolytic T lymphocyte associated antigen-4 (CTLA4Ig) and an enhanced green fluorescent protein (EGFP). The plasmids were transfected to the above-mentioned glomerular epithelial cells to express both genes simultaneously. Using the clone cells for cell transplantation showed that mice with autoimmune disease prolonged their life significantly as compared with the control mice, and two injections of the cells at the beginning of two weeks resulted in remarkable survivability, whereas it requires half a year and 50 administrations of proteins purified from the same amount of cells to achieve the same effect.

Influence of Ketamine and Midazolam on the Analgesic Effect of Epidural Bupivacaine and Fentanyl after Low Abdominal Surgery (하복부수술 후 경막외 부피바케인과 펜타닐에 첨가한 케타민과 미다졸람의 제통효과)

  • Jung, Jai Yun;Park, Sun Young;Kim, Yong Ik
    • The Korean Journal of Pain
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    • v.19 no.1
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    • pp.87-90
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    • 2006
  • Background: There are many ways to provide superior analgesia for postoperative pain after abdominal surgery of which epidural analgesics with opioids and local analgesics are the most useful. In an effort to maximize the level of analgesia and to minimize the side effects, ketamine, midazolam, clonidine, and adrenalin can be co-administrated as an adjuvant. This study examined the analgesic effect and side effects of midazolam compared with those given an epidural injection of bupivacaine, fentanyl and ketamine. Methods: In a double blind randomized controlled trial, 50 patients received either fentanyl $0.3{\mu}g/kg/h$ and ketamine 0.1 mg/kg/h (Group FK) or fentanyl $0.3{\mu}g/kg/h$, ketamine 0.1 mg/kg/h and midazolam 0.4 mg/h (Group FKM), added to 0.125% of bupivacaine at a rate of as much as 2 ml/h, for patient controlled epidural analgesia (PCEA) after low abdominal surgery. Ten minutes before surgery, the patients received either 10 ml of 0.125% bupivacaine with 0.5 mg/kg of ketamine or 10 ml of 0.125% bupivacaine with the same amount of normal saline, added to fentanyl $50{\mu}g$. The pain score and the side effects were recorded at 1, 3, 6, and 24 hours after surgery. Results: There was no difference in the pain score except for the VAS on coughing 1 hour after surgery. FKM group had fewer side effects. Conclusions: There was a better analgesic effect and fewer side effects with the addition of epidural midazolam to bupivacaine and fentanyl with ketamine formula. However, more study on the dose and route of administration will be needed.

Influence of Ketamine on the Analgesic Effect of Epidural Bupivacaine and Fentanyl after a Transabdominal Hysterectomy (전자궁적출술 후 경막외 Bupivacaine과 Fentanyl에 첨가된 Ketamine이 술 후 통증에 미치는 영향)

  • Jung, Jai Yun;Bang, Kyung Ho;Kim, Sang Hyon;Kim, Yong Ik
    • The Korean Journal of Pain
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    • v.18 no.2
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    • pp.138-141
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    • 2005
  • Background: There have been many attempts to alleviate pain after surgery, but there is no common approach to the control of postoperative pain. The use of epidural opioids, with local anesthetics, has been a widely employed formula to date. Ketamine, an N-methyl-d-aspartate receptor antagonist, has an excellent analgesic effect. Although there have been many reports on the dose and route of administrating analgesics, there have been few concerning the continuous epidural infusion of ketamine with fentanyl. We designed this study to find the effects of ketamine compared to those of epidurally injected bupivacaine and fentanyl, and used this trial to study any potential side effects. Methods: In a double blind trial, 55 patients received either fentanyl, $0.3{\mu}g/kg/h$ (Group F), or fentanyl, $0.3{\mu}g/kg/h$, and ketamine, 0.1 mg/kg/h (Group FK), added to 0.125% bupivacaine, at rates as high as 2 ml/h, for patient controlled epidural analgesia (PCEA) following a transabdominal hysterectomy. Ten minutes before the operation, patients received 10 ml of 0.125% bupivacaine, with either 0.5 mg/kg ketamine or the same amount of normal saline with $50{\mu}g$ fentanyl added. The pain scores and the side effects were recorded at 1, 3, 6 and 24 hour post operation. Results: There were no differences in the pain scores or side effects between the two groups. Conclusions: We failed to find any effect of the addition of epidural ketamine compared to the that of the bupivacaine and fentanyl formula. However, it is suggested that further investigations will be required on the dose and route of administration.

Cyclosporin A Binding Protein Type-19 kDa Peptidyl-Prolyl Cis/Trans Isomerase from Euglena gracilis

  • SONG HYUK-HWAN;PARK SUNG-YONG;LEE CHAN
    • Journal of Microbiology and Biotechnology
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    • v.15 no.5
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    • pp.1047-1053
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    • 2005
  • Cyclosporin A binding protein type-19 kDa peptidyl-prolyl cis/trans isomerase (PPIases, EC 5.2.1.8) of Euglena gracilis was purified and some of its biochemical characters were elucidated. Purification of the PPIase was achieved by employing a series of steps involving ammonium sulfate precipitation, Superdex G-75 gel filtration chromatography, Mono­Q anion and Mono-S cation exchange chromatographies, and Superdex S-200 gel filtration chromatography on FPLC. Purified PPIase had a specific activity of 8,250 units/mg, showing a 27-fold increase compared with that of cell-free extract of Euglena gracilis. The enzyme consisted of a single polypeptide chain with a molecular mass of 19 kDa. It showed high substrate specificity to succinyl-Ala-Ala-Pro-Phe-p-nitroanilide, and $k_{car}/K_{m}$, for this substrate was found to be $61.19{\times}10^5/sec$. The isomer distributions were investigated at an equilibrium of seven different peptide substrates, varying Xaa in Suc-Ala-Xaa-Pro-Phe-p-nitroanilide in dimethylsulfoxide. The cis/trans equilibrium constants were estimated to be from 0.14 (Ile) to 0.63 (Gly), which correspond to $12.00\%\;to\;38.52\%$ of the cis population, respectively, under experimental condition. The enzyme was highly sensitive to the immunosuppressive ligand cyclosporin A, but not to other immunosuppressants such as FK506 and rapamycin. Thus, it appears to belong to the class of cyclophilin.