• Title/Summary/Keyword: terminal methyl group

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Inhibitory Activitv of (1,3-Dioxolan-2-yl and Dioxan-2-yl)methylaminium Derivatives against Acetylcholinesterase (Acetylcholinesterase에 대한 (1,3-Dioxolan-2-yl 및 Dioxan-2-yl)methylaminium유도체의 저해 작용)

  • Phi, Taek-San;Kim, Yun-Bae;Kim, Jee-Cheon;Cho, Young;Sok, Dai-Eun;Cha, Seung-Hee;Seo, Won-Jun
    • YAKHAK HOEJI
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    • v.38 no.5
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    • pp.511-515
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    • 1994
  • We examined the inhibitory activity of (1,3-dioxolan-2-yl and 1,3-dioxan-2-yl)methylaminium derivatives(A; 1-8) against acetylcholinesterase. Derivatives of six-membered 1,3-dioxane exhibited more potent inhibitory effect than corresponding 5-membered 1,3-dioxolanes. The presence of methyl group at C4 position of dioxane ring was effective to increase the inhibitory potency of heterocyclic analogues. The activity of N-phenacyl-aminiums was greater than that of N,N,N-trimethyl-aminiums. In general, the terminal methyl group on 1,3-dioxane ring and the phenacyl group in ammonium compound A were assumed to be important factors to enhance the inhibitory action.

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Morphological Changes in the Mammary Organ Culture of the Rat Treated with 7,12-Dimethylbenz[$\alpha$]anthracene and N-methyl-N-nitrosourea (7,12-Dimethylbenz[$\alpha$anthracene 및 N-methyl-N-nitrosourea를 투여한 랫드 유선 조직 배양에 대한 형태학적 변화)

  • 문지영;정자영;김옥희;이형환
    • Toxicological Research
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    • v.16 no.4
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    • pp.275-284
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    • 2000
  • The organ culture model of the whole mammary gland has many advantages for the study of branching morphogenesis and biological characteristics, including tumorigenesis. Prior to whole gland organ culture, rats were treated with 7,12-dimethylbenz[a]anthracene (DMBA) or N-methyl-N-nitrosourea (MNU) for one week. The tramdorming effect and the morphological changes were assessed by the whole mount preparations and histopathological examination in terminal end buds (TEB), terminal ducts (TD), alveolar buds (AB), alveolar lobules (AL) and hyperplastic alveolar nodules (HAN) of the mammary gland. Grossfindings of the mammary glands at dissection were higher branching morphogenesis and larger volume in carcinogen-treated groups than in carcinogen-non-treated groups. Results of the whole mount method were coincided with those of the histopathological observations. Circular TEB, normally maintained AB, AL, and high cellular density were more frequently observed in carcinogen-treated groups than in carcinogen-nan-treated groups. Histopathologically, as a preneoplastic marker, HAN was maintained only in mammary organ culture of the carcinogen-treated groups. These findings suggest that in vivo trans-formation effects by carcinogens persisted during the mammary organ culture. These results were more characteristic in DMBA than in MNU-treated group. Ducts and terminal ducts appeared to have lost morphology during their growths in case of without diethylstilbestrol (DES). The fact that in vitro organ culture without DES was resulted in abnormal ductular morphogenesis confirms that DES is a physiological regulator of ductular epithelial cell growth.

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Deletion of N-terminal End Region of ErmSF Leads to an Amino Acid Having Important Role in Methyl Transfer Reaction (ErmSF에서 특이적으로 발견되는 N-terminal End Region의 점차적인 제거에 의한 활성에 중요한 아미노산의 규명)

  • Lee Hak Jin;Jin Hyung Jong
    • Korean Journal of Microbiology
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    • v.40 no.4
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    • pp.257-262
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    • 2004
  • ErmSF is one of the ERM proteins which transfer the methyl group to A2058 in 23S rRNA to confer the resis­tance to MLS (macrolide-lincosamide-streptogramin B) antibiotics on microorganism. Unlike other ERM pro­teins, ErmSF contains long N-terminal end region (NTER), of which $25\%$ is composed of arginine that is known to interact with RNA well. Gradual deletion of NTER leaded us to the point where mutant protein lost much of activity in vivo. Overexpressed and purified mutant protein showed much reduced activity in vitro: $2\%$ activity relative to that of wild type protein. This fact suggests that this amino acid interact with RNA close to meth­ylatable adenine to locate it at an active site properly.

The Crystal and Molecular Structure of Z-3-P-Tolylthio-4-Nitro-3-Hexene (Z-3-파라-톨릴치오-4-니트로-3-헥센의 결정 및 분자구조)

  • An, Jung Tae;Gene B. Carpenter
    • Journal of the Korean Chemical Society
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    • v.34 no.2
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    • pp.130-135
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    • 1990
  • The title compound (C13H17NO2S) is monoclinic, space group P21/a, with a = 13.756 (3), b = 9.310(4), c = 21.305(3) $\AA$, $\beta$ = 95.0。, Z = 8, V = 2718.11 $\AA$3, Dc = 1.23$g·{\cdot}cm-3$, (Mo k$\alpha$) = 0.71069$\AA$,$\mu$ = 2.18 cm-1, F(000) = 1071.86, T = 298, R = 0.085 for 2935 unique observed reflections with I >2.0$\sigma$(I). The structure was solved by direct methods. The C-H bond lengths and the methyl groups are fixed and refined as their ideal geometry by allowing to ride on the parent atoms. Both molecules A and B have almost same structures except for two terminal ethyl groups. The ethylene-like skeleton including the nitro group in one molecule is nearly perpendicular to the plane of the methylbenzene group and two ethyl groups form a cis-type structure which has the dfferent orientations between two molecules; in the molecule A, two terminal methyl groups being the opposite directional arrangement against the plane of its skeleton, while in the B, with the same directional structure from its plane. The molecules in the crystal are packed together by non-bonded van der Waals forces.

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The Synthetic Approaches to Modify Methyl (Pyro)pheophorbide a

  • Wang, Jin-Jun;Han, Guang-Fan;Lee, Jong-Cheol;Shim, Young-Key
    • Journal of Photoscience
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    • v.9 no.2
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    • pp.178-181
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    • 2002
  • Pyropheophorbide and pheophorbide-photosensitizers as chlorin analogues are promising new compounds for PDT because the chlorin analogues are activated with much longer red light at > 670nm and produce less long-term normal tissue phototoxicity than Photofrin. The various chlorin derivatives can be obtained by moditying peripheral substituted group among which meso-H, vinyl group and exocyclic ring are the most active positions. These characteristics prompted us to introduce various groups for constructing modified pyropheophorbide and pheophorbide a compounds. A stereospecific introduction of various double bonds at 3-position was performed to methylpheophorbide a to give a long hydrophobic moiety and cyclic derivatives. Chlorin-C$_{60}$ dyad and chlorin- $C_{60}$-porphyrin triad also were easily prepared by the reaction of terminal aldehyde of methyl pyropheophorbide a. For the reaction on meso $\delta$-position bromination and Vismeier formylation can occur. N,N-dimethylaminoacrolein also reacted on $\delta$-position and was cyclized to isobacteriochlorin, but other modification has not been succeeded. Exocyclic keto function was also modified to give purpurin derivatives, bicyclic and spiro compounds. In this presentation we report a series of modified pyropheophorbide and pheophorbide a derivatives.s.

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Isolation and Structural Analysis of MB4-03, an $\alpha$-Amylase Inhibitor Produced by Streptomyces sp. DMCJ-49 (Streptomyces sp. DMCJ-49 균주가 생산하는 Alpha-Amylase 저해제 MB4-03의 분리와 구조분석)

  • 염대현;최응철;김병각;김진웅
    • Microbiology and Biotechnology Letters
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    • v.18 no.4
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    • pp.338-343
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    • 1990
  • MB4-03, an $\alpha$-amylase inhibitor was isolated from the culture broth of Streptomyces sp. DMCJ-49 and purified through ion-exchange chromatography, adsorption, and gel filtration. The results of various instrumental analyses showed that the inhibitor was one of oligosaccharides that had glucoses as its major component and that its molecular weight was about 2000. And one methyl group which seemed to be related with the inhibitory activity of this compound was identified. From the CMR spectrum, it was elucidated that this compound was composed of $\alpha$ -D-glucopyranoses which were linked together by $\alpha$ (I -, 4) bond configuration. As the inhibitory effect of this compound was reduced after incubation with $\beta$-amylase, the maltose units was seemed to exist at non-reducing terminal side of it.

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CRYSTAL STRUCTURE OF tRNA ($m^1$ G37) METHYLTRANSFERASE

  • Ahn, Hyung-Jun;Lee, Byung-Ill;Yoon, Hye-Jin;Yang, Jin-Kuk;Suh, Se-Won
    • Proceedings of the Korea Crystallographic Association Conference
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    • 2003.05a
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    • pp.17-17
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    • 2003
  • tRNA (m¹ G37) methyltransferase (TrmD) catalyze s the trans for of a methyl group from S-adenosyl-L-methionine (AdoMet) to G/sup 37/ within a subset of bacterial tRNA species, which have a residue G at 36th position. The modified guanosine is adjacent to and 3' of the anticodon and is essential for the maintenance of the correct reading frame during translation. We have determined the first crystal structure of TrmD from Haemophilus influenzae, as a binary complex with either AdoMet or S-adenosyl-L-homocysteine (AdoHcy), as a ternary complex with AdoHcy/phosphate, and as an apo form. The structure indicates that TrmD functions as a dimer (Figure 1). It also suggests the binding mode of G/sup 36/G/sup 37/ in the active site of TrmD and catalytic mechanism. The N-terminal domain has a trefoil knot, in which AdoMet or AdoHcy is bound in a novel, bent conformation. The C-terminal domain shows a structural similarity to DNA binding domain of trp or tot repressor. We propose a plausible model for the TrmD₂-tRNA₂ complex, which provides insights into recognition of the general tRNA structure by TrmD (Figure 2).

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Investigation on Chain Transfer Reaction of Benzene Sulfonyl Chloride in Styrene Radical Polymerization

  • Li, Cuiping;Fu, Zhifeng;Shi, Yan
    • Macromolecular Research
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    • v.17 no.8
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    • pp.557-562
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    • 2009
  • The free radical polymerization of styrene was initiated with azobis(isobutyronitrile) in the presence of benzene sulfonyl chloride. Analysis of the terminal structures of the obtained polystyrene with $^1H$ NMR spectroscopy revealed the presence of a phenyl sulfonyl group at the ${\alpha}$-end and a chlorine atom at the ${\omega}$-end of each polystyrene chain. The terminal chlorine atom in the polystyrene chains was further confirmed through atom transfer radical polymerization (ATRP) of styrene and methyl acrylate using the obtained polystyrenes as macroinitiators and CuCl/2,2'-bipyridine as the catalyst system. GPC traces of the products obtained in ATRP at different reaction times were clearly shifted to higher molecular weight direction, indicating that nearly all the macroinitiator chains initiated ATRP of the second monomers. In addition, the number-average molecular weights of the polystyrenes increased directly proportional to the monomer conversions, and agreed well with the theoretical ones.

Effect of Chronic Inhibition of Nitric Oxide on Blood Pressure and Apoptosis in the Blood Pressure-Associated with Organs

  • Bae, Hyung-Joon
    • Biomedical Science Letters
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    • v.16 no.1
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    • pp.25-32
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    • 2010
  • Sprague-Dawley(SD) rats were orally administered with $N^G$-nitro-L-arginine methyl ester(L-NAME) which inhibits or blocks the production of nitric oxide from L-arginine in vascular endothelial cells and vessel tissue to statistically examine the effects of nitric oxide on some physiological changes such as blood pressure and heart rate, and to confirm the apoptosis induced by the suppressed nitric oxide activity in some related organs under light microscope. Systolic blood pressure significantly increased 28.5% by the chronic treatment of L-NAME for 8 weeks (P<0.001), no significant difference, however, was observed in heart rate between the control group and the L-NAME-treated group regardless of their age. Hematoxylin-eosin staining showed some histological alterations only in kidney among the examined organs; heart, liver, pancreas, and adrenal gland from the L-NAME-treated group. TUNEL (terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling) test showed a strong positive reaction, representing that the chronic treatment of L-NAME facilitates apoptosis, in the cortex and medulla of kidney, but not any significance detectable in the other organs. These results conclude that chronic treatment of L-NAME significantly increases blood pressure, and that the followed inhibition of nitric oxide synthesis occurs a typical inducement of apoptosis in kidney.

An Investigation of the Environment of Some Aromatic Alcohol Solubilized Aqueous Ionic Micellar Solutions by Proton Magnetic Resonance Spectroscopy

  • Chung, Jong-Jae;Kang, Jung-Bu;Lee, Kyung-Hee;Seo, Byung-Il
    • Bulletin of the Korean Chemical Society
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    • v.15 no.3
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    • pp.198-204
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    • 1994
  • Chemical shifts in aqueous sodium dodecylsulfate(SDS) micellar solution solublizing phenol, catechol, resorcinol, hydroquinone have been measured to investigate solubilization properties. Proton nuclear magnetic resonance frequencies of solubilizates as well as those of the ${\alpha}$-methylene, middle methylene and terminal methyl of SDS shift linearly as a function of solubilizate concentration. From the plots of observed chemical shift (v) vs solubilizate concentration, slope (a) and solubilizate free chemical shift ($v_0$) are obtained. They are very informative to solubilization site of the systems. Catechol and phenol solubilized SDS and catechol solubilized dodecylpyridinium chloride(DPC), dodecyltrimethylammonium bromide(DTAB) systems are studied using the same method to compare head group effect and middle methylene proton signal splitting. It is proposed that phenol and catechol are inserted into micellar interior and the number of methylenes assigned to the higher field peaks is 5.0${\pm}$0.5.