• Title/Summary/Keyword: Chain Structure

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Stereotactic Neurotomy of the Ganglion Impar through the Sacrococcygeal Junction in Cancer-Related Perianal Pain -A case report- (회음부 암성 통증환자에서 시행한 천미골 접합부를 이용한 외톨이 교감 신경절의 정위적 신경절제술 -증례 보고-)

  • Kim, Keun Sook;Ko, Hyun Hak;Hwang, Sung Mi;Lim, So Young;Hong, Soon Yong;Shin, Keun Man
    • The Korean Journal of Pain
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    • v.18 no.2
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    • pp.263-266
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    • 2005
  • The ganglion impar is a solitary retroperitoneal structure at the caudal end of the paravertebral sympathetic chain. Block of this ganglion has been advocated as a means of managing intractable perineal pain. In 1990, Plancarte et al performed a neurolytic block of the ganglion impar using 4-6 ml of 10% phenol through the intergluteal skin over the anococcygeal ligament. However, technical difficulties are encountered with the placement of the needle while performing this technique, with complications from the injection of phenol also being a possibility. In 1995, a modified approach for blocking the ganglion impar through the sacrococcygeal ligament was introduced by Wemm and Saberski. We used a radiofrequency (RF) lesion generator to create a controlled and localized lesion with a lower incidence of neural damages compared to chemical neurolysis. RF thermocoagulation of the ganglion impar through the sacrococcygeal ligament was performed on a 70-year-old male patient with constant anal pain using a curved TEW electrode. The patient has been relieved of his pain, without serious complication. Therefore, this technique may be an easier and safer approach, which is associated with fewer chances of complications.

Increased Refolding Yield of Disulfide Bond Bridged Fab-Toxin Homodimers by the Insertion of CH3 Domains

  • Song Jeong-Wha;Won Jae-Seon;Lee Yong-Chan;Choe Mu-Hyeon
    • Journal of Microbiology and Biotechnology
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    • v.16 no.7
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    • pp.1104-1110
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    • 2006
  • Recombinant antibody-toxin is a bifunctional protein that binds and kills a target cell expressing a specific antigen on the surface of the cell, and its structure is chimeric, in which a toxin is fused to an antigen-binding domain such as scFv or Fab. Divalent antibody-toxin molecules showed higher cytotoxicities against cancer cell lines than monovalent molecules. However, the yields of the divalent molecules were very low. In this study, we introduced the CH2, CH3, or CH2-CH3 (=Fc) domain of antibody in the middle of the Fab-toxin between the hinge region of human IgG1 and the toxin domain to increase the yield. The covalently bonded dimer could be formed by three disulfide bridges from cysteine residues in the hinge region. The molecule with the CH3 domain showed about 3-fold higher dimerization yield than previously constructed Fab-toxin molecules, while maintaining the cytotoxic activity comparable to that of scFv-toxin. However, the introduction of CH2 or Fc domain to the same position showed little effect on the dimerization yield. We also observed that the introduction of the CH3 region made it possible to form noncovalently associated dimer molecules.

Physiological, Pharmacological and Toxicological Implications of Heterodimeric Amino Acid Transporters

  • Kanai, Yoshikatsu;Endou, Hitoshi
    • The Korean Journal of Physiology and Pharmacology
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    • v.8 no.3
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    • pp.117-127
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    • 2004
  • The heterodimeric amino acid transporter family is a subfamily of SLC7 solute transporter family which includes 14-transmembrane cationic amino acid transporters and 12-transmembrane heterodimeric amino acid transporters. The members of heterodimeric amino acid transporter family are linked via a disulfide bond to single membrane spanning glycoproteins such as 4F2hc (4F2 heavy chain) and rBAT $(related\;to\;b^0,\;^+-amino\;acid\;transporter)$. Six members are associated with 4F2hc and one is linked to rBAT. Two additional members were identified as ones associated with unknown heavy chains. The members of heterodimeric amino acid transporter family exhibit diverse substrate selectivity and are expressed in variety of tissues. They play variety of physiological roles including epithelial transport of amino acids as well as the roles to provide cells in general with amino acids for cellular nutrition. The dysfunction or hyperfunction of the members of the heterodimeric amino acid transporter family are involved in some diseases and pathologic conditions. The genetic defects of the renal and intestinal transporters $b^{0,+}AT/BAT1\;(b^{0,+}-type\;amino\;acid\;transporter/b^{0,+}-type\;amino\;acid\;transporter\;1)$ and $y^+LAT1\;(y^+L-type\;amino\;acid\;transporter\;1)$ result in the amino aciduria with sever clinical symptoms such as cystinuria and lysin uric protein intolerance, respectively. LAT1 is proposed to be involved in the progression of malignant tumor. xCT (x-C-type transporter) functions to protect cells against oxidative stress, while its over-function may be damaging neurons leading to the exacerbation of brain damage after brain ischemia. Because of broad substrate selectivity, system L transporters such as LAT1 transport amino acid-related compounds including L-Dopa and function as a drug transporter. System L also interacts with some environmental toxins with amino acid-related structure such as cysteine-conjugated methylmercury. Therefore, these transporter would be candidates for drug targets based on new therapeutic strategies.

Differential Effects of Tautomycetin and Its Derivatives on Protein Phosphatase Inhibition, Immunosuppressive Function and Antitumor Activity

  • Niu, Mingshan;Sun, Yan;Liu, Bo;Tang, Li;Qiu, Rongguo
    • The Korean Journal of Physiology and Pharmacology
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    • v.16 no.2
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    • pp.145-151
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    • 2012
  • In the present work, we studied the structure-activity relationship (SAR) of tautomycetin (TMC) and its derivatives. Further, we demonstrated the correlation between the immunosuppressive fuction, anticancer activity and protein phosphatase type 1 (PP1) inhibition of TMC and its derivatives. We have prepared some TMC derivatives via combinatorial biosynthesis, isolation from fermentation broth or chemical degradation of TMC. We found that the immunosuppressive activity was correlated with anticancer activity for TMC and its analog compounds, indicating that TMC may home at the same targets for its immunosuppressive and anticancer activities. Interestingly, TMC-F1, TMC-D1 and TMC-D2 all retained significant, albeit reduced PP1 inhibitory activity compared to TMC. However, only TMC-D2 showed immunosuppressive and anticancer activities in studies carried out in cell lines. Moreover, TMC-Chain did not show any significant inhibitory activity towards PP1 but showed strong growth inhibitory effect. This observation implicates that the maleic anhydride moiety of TMC is critical for its phosphatase inhibitory activity whereas the C1-C18 moiety of TMC is essential for the inhibition of tumor cell proliferation. Furthermore, we measured $in$ $vivo$ phosphatase activities of PP1 in MCF-7 cell extracts treated with TMC and its related compounds, and the results indicate that the cytotoxicity of TMC doesn't correlate with its $in$ $vivo$ PP1 inhibition activity. Taken together, our study suggests that the immunosuppressive and anticancer activities of TMC are not due to the inhibition of PP1. Our results provide a novel insight for the elucidation of the underlying molecular mechanisms of TMC's important biological functions.

Chemical Degradation of e-PTFE Support Used in PEMFC after Fenton Reaction (고분자연료전지에 사용되는 e-PTFE 지지체의 펜톤반응 후 화학적 열화)

  • Oh, Sohyeong;Lim, Daehyun;Lee, Mooseok;Lee, Donghoon;Park, Kwonpil
    • Korean Chemical Engineering Research
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    • v.58 no.4
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    • pp.536-540
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    • 2020
  • The support of the PEMFC membrane plays a key role in improving mechanical durability. The e-PTFE used as a support is chemically stable, so electro-chemical degradation in the PEMFC driving process has been rarely studied. In this study, we investigated whether e-PTFE is chemically stable to radicals and hydrogen peroxide during Fenton reaction. After the Fenton reaction, the main chain of e-PTFE broke, resulting in a change in the chemical structure and morphology of the support, resulting in a decrease in tensile strength. The results of this study showed that electrochemical degradation of the membrane ionomer in the PEMFC process occurs inside the membrane by radicals and hydrogen peroxide, so that electrochemical degradation may also occur at the e-PTFE support in the cell.

New metabolites from the biotransformation of ginsenoside Rb1 by Paecilomyces bainier sp.229 and activities in inducing osteogenic differentiation by Wnt/β-catenin signaling activation

  • Zhou, Wei;Huang, Hai;Zhu, Haiyan;Zhou, Pei;Shi, Xunlong
    • Journal of Ginseng Research
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    • v.42 no.2
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    • pp.199-207
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    • 2018
  • Background: Ginseng is a well-known traditional Chinese medicine that has been widely used in a range of therapeutic and healthcare applications in East Asian countries. Microbial transformation is regarded as an effective and useful technology in modification of nature products for finding new chemical derivatives with potent bioactivities. In this study, three minor derivatives of ginsenoside compound K were isolated and the inducing effects in the Wingless-type MMTV integration site (Wnt) signaling pathway were also investigated. Methods: New compounds were purified from scale-up fermentation of ginsenoside Rb1 by Paecilomyces bainier sp. 229 through repeated silica gel column chromatography and high pressure liquid chromatography. Their structures were determined based on spectral data and X-ray diffraction. The inductive activities of these compounds on the Wnt signaling pathway were conducted on MC3T3-E1 cells by quantitative real-time polymerase chain reaction analysis. Results: The structures of a known 3-keto derivative and two new dehydrogenated metabolites were elucidated. The crystal structure of the 3-keto derivative was reported for the first time and its conformation was compared with that of ginsenoside compound K. The inductive effects of these compounds on osteogenic differentiation by activating the Wnt/b-catenin signaling pathway were explained for the first time. Conclusion: This study may provide a new insight into the metabolic pathway of ginsenoside by microbial transformation. In addition, the results might provide a reasonable explanation for the activity of ginseng in treating osteoporosis and supply good monomer ginsenoside resources for nutraceutical or pharmaceutical development.

Synthesis and Characterization of Poly(ethylene oxide) Derivatives Containing Carbonate Linkages (고분자 주사슬에 카보네이트 관능기가 도입된 새로운 폴리에틸렌 옥사이드 유도체의 합성 및 분석)

  • 최유선;차국찬;서정인;정동준;안정호
    • Polymer(Korea)
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    • v.25 no.6
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    • pp.759-764
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    • 2001
  • In order to obtain PEO with reduced crystallinity, novel PEO derivatives containing carbonate linkages in the main chain have been synthesized by the reaction of various molecular weight poly (ethylene glycol)s (PEGs) with dimethyl carbonate (DMC) in the presence of $H_2SO_4$ to yield methyl carbonate terminated PEGs, followed by condensation reaction under vacuum in the presence of titanium isopropoxide (TiP) catalyst. The number average molecular weight of PEGs used was in the range of 200 and 600 g/mol. The structure and compositions of the resulting polymers were characterized by $^1$H-NMR and $^{13}C-NMR$. Their thermal behavior and molecular weight were characterized by DSC/TGA and GPC, respectively.

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Zirconocene-catalyzed Copolymerizations of Ethylene with 5-Methyl-1,4-hexadiene as Non-conjugated Diene

  • Jin, Yong-Hyun;Im, Seung-Soon;Kim, Sang-Seob;Soonjong Kwak;Kim, Kwang-Ung;Kim, Keon-Hyeong;Kim, Jungahn
    • Macromolecular Research
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    • v.10 no.2
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    • pp.97-102
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    • 2002
  • The mixtures of non-conjugated dienes, 4-methyl-1,4-hexadiene and 5-methyl-1,4-hexadiene (MHD), were successfully synthesized by the reaction of isoprene with ethylene using Fe(III)-based catalyst in toluene. The conversion was over 96 mol% on the basis of the initial amount of isoprene used. The production yield for MHD was nearly 50 mol%, the other was polyisoprene. The mixtures were successfully copolymerized with ethylene by using zirconium-based metallocenes. The products were characterized by the combinations of gas chromatography, high temperature gel permeation chromatography, $^1$H NMR, $^{13}$ C NMR, high temperature $^1$H NMR, UV/visible spectroscopy, and differential scanning calorimetry. It was found that 5-methyl-1,4-hexadiene was active enough to be incorporated into the copolymer chain but the corresponding isomeric material,4-methyl-1,4-hexadiene, was inactive in metallocene-catalyzed copolymerizations. Specifically, in the zirconocene-catalyzed copolymerizations of ethylene with MHD, ansa-structure catalysts seem to be more efficient than non-bridged type zirconocene. The degree of incorporation of MHD in the resulting copolymers was able to be controlled by the amount of non-conjugated dienes used initially.

Chemoenzymatic Synthesis of H-shaped Amphiphilic Pentablock Copolymer and Its Self-assembly Behavior (H-형태 양친매성 펜타블록 공중합체의 화학효소적 합성과 자기회합거동 평가)

  • Chen, Peng;Li, Ya-Peng;Li, Cai-Jin;Meng, Xin-Lei;Zhang, Bao;Zhu, Ming;Liu, Yan-Jing;Wang, Jing-Yuan
    • Polymer(Korea)
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    • v.37 no.3
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    • pp.332-341
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    • 2013
  • H-shaped amphiphilic pentablock copolymers $(PSt)_2-b-PCL-b-PEO-b-PCL-b-(PSt)_2$ was synthesized via chemoenzymatic method by combining enzyme-catalyzed ring-opening polymerization (eROP) of ${\varepsilon}$-caprolactone (${\varepsilon}$-CL) and atom transfer radical polymerization (ATRP) of styrene. By this process, we obtained copolymers with controlled molecular weight and low polydispersity. The structure and composition of the obtained copolymers were characterized by nuclear magnetic resonance (NMR), gel permeation chromatography (GPC) and infrared spectroscopy analysis (IR). The crystallization behavior of the copolymers was analyzed by differential scanning calorimetry (DSC) and X-ray diffraction (XRD). The crystallization behavior of the H-shaped block copolymers demonstrated a PCL dominate crystallization. The self-assembly behavior of the copolymers was investigated in aqueous media. The hydrodynamic diameters of the copolymer micelles in aqueous solution were measured by dynamic light scattering (DLS). The morphology of the copolymer micelles was observed by atomic force microscopy (AFM) and transmission electron microscopy (TEM). The hydrodynamic diameters of spherical micelles declined gradually with the increase of the hydrophobic chain lengths of the copolymers. The critical micelle concentration (CMC) values were determined from fluorescence emission, and it was found that the CMCs decreased with an increase of PSt hydrophobic block lengths.

Liquid Crystal Polymers (X). Synthesis and Properties of New Thermotropic Main Chain Copolyesters with Either Mixed Polymethylene Spacers or Mixed Mesogenic Units (액정 중합체 (제10보). 혼합폴리에틸렌 격자나 메소젠 단위를 갖고 있는 새로운 주사슬 혼성폴리에스테르의 합성 및 성질)

  • Jung-Il Jin;Robert W. Lenz;S. Antoun
    • Journal of the Korean Chemical Society
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    • v.26 no.3
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    • pp.188-193
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    • 1982
  • Four new thermotropic copolyesters were prepared and their liquid crystal properties were investigated by differential scanning calorimetry and on a hot-stage of a polarizing microscope. Three copolyesters had same mesogenic unit, triad aromatic ester structure, interconnected through a random combination of either odd-even, or odd-odd, or even-even number of methylene groups in the polymethylene flexible spacers. Another random copolyester consisted of mesogenic units of 1 : 1 mixture of central methyl-and bromohydroquinone moieties with two flanking p-oxybenzoate units connected by decamethylene spacer. All of the polyesters formed nematic liquid crystal phase upon melting. The transitions for melting and nematic ${\to}$ isotropic transformations could be reversibly observed by DSC as well as by microscopic study. The thermodynamic properties for their liquid crystal ${\to}$ isotropic phase transitions were discussed in relation to their chemical structures.

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