• Title/Summary/Keyword: C1-2

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Reactions with Heterocyclic Amidines (V). Synthesis of some new imidazo[l, 2-b] pyrazole,pyrazolo[5,1-C]-1,2,4-triazine and pyrazolo [5, 1-c]-1,2,4-triazole derivatives

  • Ali Elagamey, Abdel Ghani;Ahmed Sowellim, Salah Zaki;Mohamed Nabil, Khodeir
    • Archives of Pharmacal Research
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    • v.10 no.1
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    • pp.14-17
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    • 1987
  • Several new imidazo [1, 2-b] pyrazole, pyrazolo [5, 1-c]-1, 2, 4-triazine and pyrazolo [5, 1-c] triazole derivatives were prepared from the reaction of 3-antipyrinyl-5-aminopyrazole or its diazonium salt with .alpha.-chloroacetyl derivatives.

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The Stereospecific Analysis of the Triacylglycerols of Ginkgo Nut Oils by High-Performace Liquid Chromatography(HPLC) in the Silver Ion and Reversed Phase Modes (銀Ion 및 역상(逆相) HPLC를 이용(利用)한 입체이성체적(立體異性體的) 분석(分析)에 의한 은행종실유(銀杏種實油)의 트리글리세리드의 분자종(分子種)에 관한 연구(硏究))

  • Joh, Yong-Goe;Woo, Hyo-Kyeng;Kim, Hoon-Sook
    • Journal of the Korean Applied Science and Technology
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    • v.14 no.1
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    • pp.61-76
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    • 1997
  • Triacylglycerols of the seeds of Ginkgo biloba have been resolved by high-performace liquid chromatography(HPLC} in the silver-ion and reverse-phase modes. The fatty acids were identified by a combination of capillary gas chromatography and gas-chromatography /mass spectrometry as the methyl and /or picolinyl ester. The main components are $C_{18:2{\omega}6}$(39.0mol%), $C_{18:1{\omega}7}$(asclepic acid 21.5mol%), and $C_{18:1{\omega}9}$(oleic acid, 13.8mol%). Considerable amounts of unusual acid such as $C_{20:3{\Delta}^{5,11,14}$ (5.7mol%), $C_{18:2{\Delta}^{5,9}$(2.8mol%), and $C_{18:3}{\Delta}^{5,9,12}$(1.6mol%), were checked. In addition, an anteiso-branched fatty acid, 14-methylhexadecanoic acid, was also present as a minor component(0.9 mol%). The triacylglycerols were separated into 17 fractions by reverse-phase HPLC, and the fractionation was achieved according to the partition numnber(PN) in which a ${\Delta}^5$-non methylene interrupted double bond($^5$-NMDB) showed different behaviour from a methylene interrupted double bond in a molecule with a given cahinlength. Silver-ion HPLC exhibited excellent resolution in which fractions(23 fractions) were resolved on the basis of the number and configuration of double bonds. In this instance, the strength of interaction of a ${\Delta}^5$-NMDB system with silver ions seemed to be weaker than a methylene interrupted double bond system. The principal triacylglycerol species are as follows ; $(C_{18:2{\omega}6)2}/C_{18:1{\omega}7}$, $C_{18:1{\omega}9}/C_{18:1{\omega}7}/C_{18:2{\omega}6}$, $(C_{18:1{\omega}7)2}/C_{18:2{\omega}6}$, $C_{16:1{\omega}7}/C_{18:1{\omega}9}/C_{20:3}{\Delta}^{5,11,14}$, $C_{16:1{\omega}7}/C_{18:1{\omega}7}/C_{20:3}{\Delta}^{5,11,14}$, $C_{18:1{\omega}9}/C_{18:1{\omega}7}/C_{18:2{\omega}6}$, $C_{18:1{\omega}9}/C_{18:2}{\Delta}^{5,5}/C_{20:3}{\Delta}^{5,11,14}$, $(C_{18:1{\omega}7)2}/C_{18:2{\omega}6}$ and $(C_{18:1{\omega}9)2}/C_{18:2{\omega}6}$, while simple triacylglycerols without $C_{18:2{\omega}6})_3$ were not present. Stereospecific analysis showed that fatty acids with ${\Delta}^5$-NMDB system and saturated chains were predominantly located at the site of sn-3 carbon of glycerol backbones. It is evident that there is asymmetry in the distribution of fatty acids in the TG molecules of Ginkgo nut oils.

Thermal Rearrangement of 1,1-Disubstituted 2-Vinylcyclopropanes to 4,4-Disubstituted Cyclopentenes (두 치환체를 가진 비닐시클로프로판의 시클로펜텐으로의 열적자리 옮김반응)

  • Iwhan Cho;Kwang-Duk Ahn
    • Journal of the Korean Chemical Society
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    • v.22 no.3
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    • pp.158-163
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    • 1978
  • The four 1,1-disubstituted 2-vinylcyclopropanes, 1,1-diphenyl-2-vinylcyclopropane (1a), 1,1-dicyano-2-vinylcyclopropane(1b), ethyl 1-cyano-2-vinylcyclopropanecarboxylate(1c), and diethyl 2-vinylcyclopropane-1,1-dicarboxylate(1d) rearranged below $300{\circ}C$ to the corresponding 4,4-disubstituted cyclopentenes, 4,4-diphenylcyclopentene(2a), 3-cyclopentene-1,1-dicarboxylate(2d). Diphenpyl derivative 1a rearranged almost quantitatively to 4,4-diphenylcyclopentene(2a) at the temperature of $250{\circ}C$. Although dicyano derivative 1b in solution underwent the thermal rearrangement at rather low temperature of $170{\circ}C$, the other vinylcyclopropanes, 1c and 1d, in solution rearranged thermally above $220{\circ}C$. In the thermal reaction of 1b, 1c, and 1d considerable amounts of polymers 3 were also produced. Also detected product was the ring-opened diene, ethyl 2-cyano-2,4-hexadienoate(4), in case of the pyrolysis of 1c. The observed facile rearrangement of disubstituted vinylcyclopropanes was explained by the radical stabilization effect of substituents on the diradical intermediates 5.

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GENETIC SUSCEPTIBILITIES OF CYTOCHROME P450 1A1, 2E1, AND N-ACETYLTRANSFERASE 2 TO THE RISKS FOR KOREAN HEAD AND NECK CANCER PATIENTS (한국인 두경부암종 환자에서 Cytochrome P450 1A1, 2E1 및 N-acetyltransferase 2 효소의 다형성 분석에 따른 유전적 감수성에 대한 연구)

  • Lee, Young-Soo;Kim, Te-Gyun;Woo, Soon-Seop;Shim, Kwang-Sub;Kong, Gu
    • Maxillofacial Plastic and Reconstructive Surgery
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    • v.22 no.4
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    • pp.373-382
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    • 2000
  • Individual genetic susceptibilities to cancers may result from several factors including differences in xenobiotics metabolism to chemical carcinogens, DNA repair, altered oncogenes and suppressor genes, and environmental carcinogen exposures. Among them, genetic polymorphisms of metabolizing enzymes to chemical carcinogens have been recognized as a major important host factors in human cancers. They have two main types of enzymes: the phase I cytochrome P-450 mediating enzymes (CYPs) and phase II conjugating enzymes. The purpose of this study is to determine the frequencies of genotypes of phase I (CYP1A1 and CYP2E1) and phase II (NAT2) metabolizing enzymes in healthy control and head and neck cancer patients of Korean and to identify the relative high risk genotypes of these metabolizing enzymes to head and neck cancer in Korean. The author has analyzed 132 head and neck cancer patients and 113 healthy controls using polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP). The results were as following; 1. The frequencies of genotypes of CYP1A1, CYP2E1 and NAT2 in healthy control were as following; CYP1A1 exon 7 polymorphism; Ile/Ile: Ile/Val: Val/Val = 59.3%: 36.3%: 4.4% CYP2E1 Pst I polymorphism, C1/C1: C1/C2: C2/C2 = 61.1%: 32.1%: 6.2% NAT2 polymorphism; F/F: F/S: S/S = 43.4%: 48.7%: 8.0% 2. In analysis of phase I enzyme, Val/Val genotype in CYP1A1 exon 7 polymorphism and C2/C2 genotype in CYP2E1 Pst I polymorphism were associated with relative high risks to head and neck cancers (Odds' ratio: 2.09 and 1.37, respectively). 3. Among the genotypes of NAT2 enzyme polymorphism, S/S genotype of NAT2 enzyme had 1.03 times of relative risk to head and neck cancers. 4. In combined genotyping of CYP1A1, CYP2E1, and NAT2 enzymes polymorphisms, the patients with Val/Val and C1/C1, C2/C2 and fast acetylator, and Val/Val and fast acetylator had higher relative risks than the patients with each baseline of combined genotypes (Odds' ratio: 2.82, 1.98 and 2.1, respectively). These results suggest the combined genotypes of Val/Val and C1/C1, C2/C2 and fast acetylator, and Val/Val and fast acetylator were more susceptible to head and neck cancers in Korean. And genotyping of metabolizing enzymes could be useful for predicting individual susceptibility to head and neck cancer.

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FORTRAN Program "PHYLS" for the Geometrical Prediction of the Structures of 1M and $2M_1$ 2:1 Phyllosilicates Having Space Groups C2/m, C2, and C2/c (공간군 C2/m, C2, 및 C2/c를 갖는 1M 및 $2M_1$ 2:1 층상 규산염 광물 구조의 기하학적 예측을 위한 포트란 프로그램 "PHYLS")

  • ;M. Slaughter
    • Journal of the Mineralogical Society of Korea
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    • v.11 no.1
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    • pp.45-67
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    • 1998
  • FORTRAN program PHYLS was developed to model the structures of 2:1 1M and 2M1 phyllosilicates on the basis of geometrical analyses. Input to PHYLS requires the chemical composition and d(001) spacing of the mineral. The output from PHYLS consists of the coordinates of the crystallographically independent sites in the unit cell, and such structural parameters as the cell dimensions, interaxial angle, cell volume, interatomic distances, and deformation angles of the polyhedra. PHYLS can generate these structural details according to the user's choice of space group and cation configuration. User can choose one of such space groups as C2/m, C2,and C2/c and such cation configurations as random and ordered tetrachedral/octahedral cation configurations. PHYLS simulated the structures of dioctahedral and trioctahedral phyllosilicates having random tetrahedral cation configuration fairly close to the reported experimentally determined structures. In contrast, the simulated structures for ordered tetrahedral cation configurations showed greater deviation from the experimentally determined structures than those for random configurations. However, if the cations were partially ordered and the sizes of the tetrahedra became similar, the simulated PHYLS may be helpful in various investigations on the relationships between structures and physicochemical properties of the phyllosilicates.

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Two Possible Space Groups of Ttis(tekaethylammonium) [bis(trimetaphosphate $\kappa^3O, O^', O^{"}$)] Vanadate(3-),$[V(P_3O_9)_2](NC_8H_{20})3$ (Tris(tetraethylammnnium) [bis(trimetaphosphate $\kappa^3O, O^', O^{"}$)] Vamdate(3-),$[V(P_3O_9)_2](NC_8H_{20})_3$,의 두가지 가능한 공간군)

  • 서일환;이진호
    • Korean Journal of Crystallography
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    • v.5 no.1
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    • pp.1-6
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    • 1994
  • Two possible space groups of the comfound, VP6N3018C24H:60, are: P 1, a=14.022(1), b=12.644(2), c= 12.640(1)A, a=8038(1), B=102.12(1), r=102.16(1), V=2124.1A3, Z=2, μ=0.47cm-1, d=1.46g/cm3, R=0.083 for 3350 independent reflections with Fo>4o IFI, and C2/c, a=19.32(2), b=16.32(2), c=14.02(1)A, B=105.98(5), β=105.98(5), V=4248.2A3, Z=4 R=0.083 for 1590 independent reflections with Fo>4c IFoI . In the space group P T, there are two monlecules in a unit cell. Vanadium atoms in the two monlecules occupy the two different special positions such that the complete monlecules are accomplished by the two independent center of symmetry. Therefore two different half molecules of bis(trimetaphosphate)vanadate and three molecules of tetraethylammonium are the asymmetric unit in a unit cell. In the space group C2/c, however, the vanadium atom is located at a special position with centrosymmetry, and a two-fold symmetry axis passes through C2/c, N2 and C25 atoms. Therefore the asymmrtic unit in a unit cell consists of a half molecule of bis(trimetaphosphate)vanadate and one and a half molecules of tetraethylammonium. All the molecular conformations in both space groups are very similar: six oxygen atoms coordinated to a vanadium atom in the bi s(trimetaphosphate)vanadate molecule form an octahedron and the four carbon atoms bonded to a nitrogen atom in the tetraethylammonium molecule are disordered so that the eight carbon atoms around nitrogen atom exhibit an irregular dodecahedral form.

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Studies on the Kinetics of the Heat Sterilization (가열멸균의 동력학적연구)

  • 우종학
    • YAKHAK HOEJI
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    • v.7 no.2_3
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    • pp.42-50
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    • 1963
  • The destruction rate of microorganisms by heat follows the first order reaction. In this experiments, the calculated sterilization velocity constants of Escherichia Coli are 1.97 * $10^{-2}min^{-1}.(45{\deg}$ C), 9.53 * $10^{-2}min^{-1}.(55{\deg}$ C) and $1.858min^{-1}.(70{\deg}$ C), 2.89 * $10^{-2}min^{-1}.(80{\deg}$ C), 1.32 * $10^{-1}min^{-1}.(90{\deg}$ C), 2.87 * $10^{-1}min^{-1}.(95{\deg}$ C), 7.91 * $10^{-1}min^{-1}.(100{\deg}$ C) and $1.777min^{-1}.(105{\deg}$ C). In the results, the activation energy of E. Coli is 62.0 Cal $mole^{-1}.(45{\deg}-60-{\deg})$, that of B. Subtilis are 17.8 Cal $mole^{-1}(60{\deg}-80{\deg}$ C) and 47.1 Cal $mole^{-1}(90{\deg}-105{\deg}$ C).

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Unilateral C1 Lateral Mass and C2 Pedicle Screw Fixation for Atlantoaxial Instability in Rheumatoid Arthritis Patients : Comparison with the Bilateral Method

  • Paik, Seung-Chull;Chun, Hyoung-Joon;Bak, Koang Hum;Ryu, Jeil;Choi, Kyu-Sun
    • Journal of Korean Neurosurgical Society
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    • v.57 no.6
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    • pp.460-464
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    • 2015
  • Objective : Bilateral C1 lateral mass and C2 pedicle screw fixation (C1LM-C2P) is an ideal technique for correcting atlantoaxial instability (AAI). However, the inevitable situation of vertebral artery injury or unfavorable bone structure may necessitate the use of unilateral C1LM-C2P. This study compares the fusion rates of the C1 lateral mass and C2 pedicle screw in the unilateral and bilateral methods. Methods : Over five years, C1LM-C2P was performed in 25 patients with AAI in our institute. Preoperative studies including cervical X-ray, three-dimensional computed tomography (CT), CT angiogram, and magnetic resonance imaging were performed. To evaluate bony fusion, measurements of the atlanto-dental interval (ADI) and CT scans were performed in the preoperative period, immediate postoperative period, and postoperatively at 1, 3, 6, and 12 months. Results : Unilateral C1LM-C2P was performed in 11 patients (44%). The need to perform unilateral C1LM-C2P was due to anomalous course of the vertebral artery in eight patients (73%) and severe degenerative arthritis in three patients (27%). The mean ADI in the bilateral group was 2.09 mm in the immediate postoperative period and 1.75 mm in 12-months postoperatively. The mean ADI in the unilateral group was 1.82 mm in the immediate postoperative period and 1.91 mm in 12-months postoperatively. Comparison of ADI measurements showed no significant differences in either group (p=0.893), and the fusion rate was 100% in both groups. Conclusion : Although bilateral C1LM-C2P is effective for AAI from a biomechanical perspective, unilateral screw fixation is a useful alternative in patients with anatomical variations.

Association of CYP2E1 and NAT2 Polymorphisms with Lung Cancer Susceptibility among Mongolian and Han Populations in the Inner Mongolian Region

  • Zhang, Jing-Wen;Yu, Wan-Jia;Sheng, Xiao-Min;Chang, Fu-Hou;Bai, Tu-Ya;Lv, Xiao-Li;Wang, Guang;Liu, Su-Zhen
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.21
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    • pp.9203-9210
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    • 2014
  • Purpose: To explore associations of CYP2E1 and NAT2 polymorphisms with lung cancer susceptibility among Mongolian and Han populations in the Inner Mongolian region. Materials and Methods: CYP2E1 and NAT2 polymorphisms were detected by PCR-RFLP in 930 lung cancer patients and 1000 controls. Results: (1) Disequilibrium of the distribution of NAT2 polymorphism was found in lung cancer patients among Han and Mongolian populations (p=0.031). (2) Lung cancer risk was higher in individuals with c1, D allele of CYP2E1 RsaI/PstI, DraI polymorphisms and slow acetylation of NAT2 (c1 compared with c2, OR=1.382, 95%CI: 1.178-1.587, p=0.003; D compared with C, OR=1.241, 95%CI: 1.053-1.419, P<0.001; slow acetylation compared with rapid acetylation, OR=1.359, 95%CI:1.042-1.768, p=0.056) (3) Compared with c2/c2 and rapid acetylation, c1/c1 together with slow acetylation synergetically increased risk of lung cancer 2.83 fold. (4) Smokers with CYP2E1 c1/c1, DD, and NAT2 slow acetylation have 2.365, 1.916, 1.841 fold lung cancer risk than others with c2/c2, CC and NAT2 rapid acetylation, respectively. (5) Han smokers with NAT2 slow acetylation have 1.974 fold lung cancer risk than others with rapid acetylation. Conclusions: Disequilibrium distribution of NAT2 polymorphism was found in lung cancer patients among Han and Mongolian populations. Besides, Han smokers with NAT2 slow acetylation may have higher lung cancer risk compared with rapid acetylation couterparts. CYP2E1 c1/c1, DD and NAT2 slow acetylation, especially combined with smoking, contributes to the development of lung cancer. CYP2E1 c1/c1 or DD genotype and NAT2 slow acetylation have strong synergistic action in increasing lung cancer risk.

Effects of Benzyl Isothiocyanate and Its N-Acetylcysteine Conjugate on Induction of Detoxification Enzymes in Hepa1c1c7 Mouse Hepatoma Cells

  • Hwang, Eun-Sun
    • Preventive Nutrition and Food Science
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    • v.19 no.4
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    • pp.268-273
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    • 2014
  • The induction of detoxification enzymes by benzyl isothiocyanate (BITC) and its synthetic N-acetyl-L-cysteine (NAC) conjugate (NAC-BITC) was examined in Hepa1c1c7 murine hepatoma cells. BITC and NAC-BITC inhibited Hepa1c1c7 cell growth in a dose-dependent manner. Cell growth was 4.5~57.2% lower in Hepa1c1c7 cells treated with $0.1{\sim}1.0{\mu}M$ BITC than in control-treated Hepa1c1c7 cells. The NAC-BITC treatment had a similar inhibitory pattern on Hepa1c1c7 cell growth; $0.5{\mu}M$ and $10{\mu}M$ NAC-BITC decreased cell growth by 13.6% and 47.4%, respectively. Treatment of Hepa1c1c7 cells with $0.1{\sim}2.0{\mu}M$ BITC also elicited a dose-response effect on the induction of quinone reductase quinone reductase (QR) activity and QR mRNA expression. Treatment with $1{\mu}M$ and $2{\mu}M$ BITC caused 1.8- and 2.8-fold inductions of QR mRNA, respectively. By comparison, treatment with $1{\mu}M$ and $2{\mu}M$ NAC-BITC caused 1.6-and 1.9-fold inductions of QR mRNA, respectively. Cytochrome P450 (CYP) 1A1 and CYP2E1 induction were lower in $0.1{\sim}2{\mu}M$ BITC-treated cells than in control-treated cells. CYP2E1 activity was 1.2-fold greater in $0.1{\mu}M$ NAC-BITC-treated cells than in control-treated cells. However, the CYP2E1 activity of cells treated with higher concentrations (i.e., $1{\sim}2{\mu}M$) of NAC-BITC was similar to the activity of control-treated cells. Considering the potential of isothiocyanatesto prevent cancer, these results provide support for the use of BITC and NAC-BITC conjugates as chemopreventive agents.