• 제목/요약/키워드: Imidazole

검색결과 218건 처리시간 0.031초

Mizoribine Inhibits Production of Pro-inflammatory Cytokines and $PGE_2$ in Macrophages

  • Han, Shin-Ha;Kim, Kwang-Hee;Kim, Hyun-Yul;Kwon, Jeung-Hak;Han, Nam-Joo;Lee, Chong-Kil;Kim, Kyung-Jae
    • IMMUNE NETWORK
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    • 제7권1호
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    • pp.31-38
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    • 2007
  • Background: Mizoribine (MZR) is an imidazole nucleoside isolated from Eupenicillium brefeldianum. MZR is currendy in clinical use for patients who have undergone renal transplantation. Therapeutic efficacy of MZR has also been demonstrated in rheumatoid arthritis and lupus nephritis. MZR has been shown to inhibit the proliferation or lymphocytes by interfering with inosine monophosphate dehydrogenase. Since the exact mechanism by which MZR benefits rheumatoid arthritis (RA) is not clear, we investigated the ability of MZR to direct its immunosuppressive influences on other antigen presenting cells, such as macrophages. Methods: Mouse macrophage RAW264.7 cells were stimulated with lipopolysaccharide in the presence of MZR. To elucidate the mechanism of the therapeutic efficacy in chronic inflammatory diseases, we examined the effects of MZR on the production of pro-inflammatory cytokines, nitric oxide (NO) and prostaglandin $E_2\;(PGE_2)$ in macrophages. Results: MZR dose-dependendy decreased the production of nitric oxide and pro- inflammatory cytokines such as tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$), interleukins $1{\beta}$ (IL-${\beta}$ and IL-6 $PGE_2$. Examination of gene expression levels showed that the anti-inflammatory effect correlated with the down-regulation of inducible nitiric oxide synthase expression, cycloxygenase-2 expression and TNF-${\alpha}$ gene expression. Conclusion: In this work, we resulted whether MZR $(1.25{\sim}10{\mu}g/ml)$ inhibited macrophage activation by inhibiting secretion of pro-inflammatory cytokines, NO and $PGE_2$. These findings provide an explanation for the therapeutic efficacy of MZR in chronic inflammation-associated diseases.

Synthesis, Structure and Biological Properties of a Novel Copper (II) Supramolecular Compound Based on 1,2,4-Triazoles Derivatives

  • Qiu, Guang-Mei;Wang, Cui-Juan;Zhang, Ya-Jun;Huang, Shuai;Liu, Xiao-Lei;Zhang, Bing-Jun;Zhou, Xian-Li
    • Bulletin of the Korean Chemical Society
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    • 제33권8호
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    • pp.2603-2608
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    • 2012
  • A novel mononuclear supramolecule of copper(II) has been synthesized with Ippyt ligand (Ippyt=3-(4'-imidazole phenyl)-5-(pyrid-2''-yl)-1,2,4-triazole) (1). Compound 1, namely [$Cu(Ippyt)_2(H_2O)_2$], has been characterized by single-crystal X-ray diffraction, IR spectrum, elemental analysis and thermogravimetric analysis. Structure determination reveals that the elongated-octahedral geometry is formed in the vicinity of the copper (II) atom being coordinated by four nitrogen atoms from two Ippyt ligands occupying the equatorial position and two oxygen atoms from two coordinated water molecules in the axial position, which together form the $N_4O_2$ donor set. Hydrogen bonding interactions between nitrogen and oxygen atoms result in the set up of a supramolecular network architecture. Biological properties including antibacterial activity and superoxide dismutase (SOD) mimetic activity of compound 1 have been investigated by agar diffusion method and the modified Marklund method, respectively. The results indicate that compound 1 exhibits a stronger antibacterial efficiency than the parent ligand and it also has a certain radical-scavenging activity.

플립칩 본딩용 비전도성 접착제의 속경화거동 평가기법 (Evaluation Method for Snap Cure Behavior of Non-conductive Paste for Flip Chip Bonding)

  • 민경은;이준식;이소정;이성;김준기
    • Journal of Welding and Joining
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    • 제33권5호
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    • pp.41-46
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    • 2015
  • The snap cure NCP(non-conducive paste) adhesive material is essentially required for the high productivity flip chip bonding process. In this study, the accessibility of DEA(dielectric analysis) method for the evaluation of snap cure behavior was investigated with comparison to the isothermal DSC(differential scanning calorimetry) method. NCP adhesive was mainly formulated with epoxy resin and imidazole curing agent. Even though there were some noise in the dielectric loss factor curve measured by DEA, the cure start and completion points could be specified clearly through the data processing of cumulation and deviation method. Degree of cure by DEA method which was measured from the variation of the dielectric loss factor of adhesive material was corresponded to about 80% of the degree of cure by DSC method which was measured from the heat of curing reaction. Because the adhesive joint cured to the degree of 80% in the view point of chemical reaction reveals the sufficient mechanical strength, DEA method is expected to be used effectively in the estimation of the high speed curing behavior of snap cure type NCP adhesive material for flip chip bonding.

Cu-Cu 접착부의 고온고습 내구성에 미치는 경화제 및 촉매제의 영향 (Effects of Hardeners and Catalysts on the Reliability of Copper to Copper Adhesive Joint)

  • 민경은;김해연;방정환;김종훈;김준기
    • 한국재료학회지
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    • 제21권5호
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    • pp.283-287
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    • 2011
  • As the performance of microelectronic devices is improved, the use of copper as a heat dissipation member is increasing due to its good thermal conductivity. The high thermal conductivity of copper, however, leads to difficulties in the joining process. Satisfactory bonding with copper is known to be difficult, especially if high shear and peel strengths are desired. The primary reason is that a copper oxide layer develops rapidly and is weakly attached to the base metal under typical conditions. Thus, when a clean copper substrate is bonded, the initial strength of the joint is high, but upon environmental exposure, an oxide layer may develop, which will reduce the durability of the joint. In this study, an epoxy adhesive formulation was investigated to improve the strength and reliability of a copper to copper joint. Epoxy hardeners such as anhydride, dihydrazide, and dicyandiamide and catalysts such as triphenylphosphine and imidazole were added to an epoxy resin mixture of DGEBA and DGEBF. Differential scanning calorimetry (DSC) analyses revealed that the curing temperatures were dependent on the type of hardener rather than on the catalyst, and higher heat of curing resulted in a higher Tg. The reliability of the copper joint against a high temperature and high humidity environment was found to be the lowest in the case of dihydrazide addition. This is attributed to its high water permeability, which led to the formation of a weak boundary layer of copper oxide. It was also found that dicyandiamide provided the highest initial joint strength and reliability while anhydride yielded intermediate performance between dicyandiamide and dihydrazide.

사과나무 부란병(腐爛病)에 대(對)한 Prochloraz와 Triadimefon의 항균성(抗菌性) (Antifungal Activity of Prochloraz and Triadimefon on Valsa ceratosperma)

  • 홍종욱;이동진;김장억
    • Current Research on Agriculture and Life Sciences
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    • 제7권
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    • pp.33-40
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    • 1989
  • Imidazole계(系) 농약(農藥)인 prochloraz와 triazole계(系)인 triadimefon의 사과나무 부란병균(腐爛病菌)(Valsa ceratosperma)에 대한 항균력(抗菌力) 및 지방산(脂肪酸)의 조성변화(組成變化)에 미치는 영향(影響)을 조사(調査)한 결과(結果)는 다음과 같다. 균(菌)이 생육(生育)하고 있는 PS액체배지(液體培地)에 두 약제(藥劑)를 각각(各各) 처리(處理)하였을 때의 $I_{50}$값은 prochloraz의 경우는 1~5ppm이었고 triadimelon은 5~10ppm이었으며 prochloraz의 저해능(沮害能)이 다소 높았다. 균사(菌絲)의 현미경(顯微鏡) 관찰결과(觀察結果) 약제(藥劑) 처리구(處理區)에서는 모두 균사(菌絲)의 이상생육현상(異常生育現象)이 관찰(觀察)되었다. 균체(菌體)에 약제(藥劑)를 처리(處理)함으로 인해서 지질(脂質)의 변화(變化)를 조사(調査)한 결과(結果) 균체중(菌體中)의 총지질(總脂質) 및 지방산(脂肪酸)의 함량변화(含量變化)는 없는 것으로 나타났다.

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Heterogeneous Porous WO3@SnO2 Nanofibers as Gas Sensing Layers for Chemiresistive Sensory Devices

  • Bulemo, Peresi Majura;Lee, Jiyoung;Kim, Il-Doo
    • 센서학회지
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    • 제27권5호
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    • pp.345-351
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    • 2018
  • We employed an unprecedented technique to synthesize porous $WO_3@SnO_2$ nanofibers exhibiting core-shell and fiber-in-tube configurations. Firstly, 2-methylimidazole was uniformly incorporated in as-spun nanofibers containing ammonium metatungstate hydrate and the sacrificial polymer (polyacrylonitrile). Secondly, the 2-methylimidazole on the surfaces of nanofibers was complexed with tin(II) chloride ($SnCl_2$) via simple impregnation of the as-spun nanofibers in ethanol containing tin(II) chloride dihydrate ($SnCl_2{\cdot}2H_2O$). The presence of vacant p-orbitals in tin (Sn) and the nucleophilic nitrogen on the imidazole ring allowed for the reaction between $SnCl_2$ and 2-methylimidazole, forming adducts on the surfaces of the as-spun nanofibers. The calcination of these nanofibers resulted in porous $WO_3@SnO_2$ nanofibers with a higher surface area ($55.3m^2{\cdot}g^{-1}$) and a better response to 1-5 ppm of acetone than pristine $SnO_2$ NFs synthesized using a similar method. An improved response to acetone was achieved upon functionalization of the $WO_3@SnO_2$ nanofibers with catalytic palladium nanoparticles. This work demonstrates the potential application of $WO_3@SnO_2$ nanofibers as sensing layers for chemiresistive sensory devices for the detection of acetone in exhaled breath.

Pilocarpus jaborandi로부터 필로카르핀의 효소반응추출 (Enzymatic Extraction of Pilocarpine from Pilocarpus jaborandi)

  • 조전호;사우라브 바타라이;오태진;장종화
    • 한국미생물·생명공학회지
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    • 제41권2호
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    • pp.236-241
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    • 2013
  • 필로카르핀은 Pilocarpus 속으로부터 유일하게 분리되는 이미다졸계 알칼로이드로서 상당히 제약적으로 중요하다. Pilocarpus jaborandi로부터 필로카르핀을 추출하기 위하여 환경친화적인 효소를 이용한 추출법을 이용하였다. 본 연구에서는 상업적으로 이용할 수 있는 효소칵테일인 Viscozyme$^{(R)}$L을 사용하였다. 추출 조건은 기질, 효소, 온도 및 pH 등에 기초하여 최적화되었다. 가장 높은 수율을 위한 최적화 조건은 pH4인 50 mM 아세트산 40 ml 하에서 $45^{\circ}C$, 100 mg 기질, 30시간 반응이였다. 최적의 추출 효소농도는 10%이였다. Viscozyme$^{(R)}$L 처리로부터 얻어진 전체 필로카르핀 함유량($1.14{\mu}g/mg$) 수준은 기존 처리방법에서 얻어지는 양($0.37{\mu}g/mg$)보다 3.08배 높은 것을 확인하였다.

모르핀내성시 뇌실내 NO 합성억제제 투여가 모르핀의 진통효과에 미치는 형향 (Supraspinal Nitric Oxide Synthesis Inhibition Enhanced Antinociception of Morphine in Morphine Tolerant Rats)

  • 송호경;장연
    • The Korean Journal of Pain
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    • 제14권2호
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    • pp.225-230
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    • 2001
  • Background: Opioids such as morphine are widely used in the treatment for pain, but chronic treatment with morphine can be complicated by the development of tolerance. The mechnisms of tolerance were still not completely understood, but recently it has been reported that NOS inhibitors can prevent development of morphine tolerance in animals. The present study accessed the possible role of supraspinal NO on antinociceptive effect of morphine in morphine tolerance using a highly specific inhibitor of the neuronal isoform of NOS, 1-(2-trifluoromethylphenyl) imidazole (TRIM). Methods: Thirty two male SD rats (300 g) were prepared with intracerebroventricular (icv) and IV cannulae. We administrated IV morphine, 3 mg/kg, daily for 4 days, resulting in tolerance. On the fifth day, a challenge dose of morphine, 3 mg/kg, was administered following pretreatment with icv TRIM, $10{\mu}g$. We also evaluated the antinociceptive effect of icv TRIM alone and the effect on a single dose of morphine (3 mg/kg) in morphine nave rats. Antinociception from morphine was determined by response to intraplantar injection of 5% formalin $100{\mu}l$ was qualified as the number of flinches in the first 0-10 min (first phase), 10-40 min Phase IIa, and 40-60 min (Phase IIb). Results: Pretreatment with icv TRIM significantly enhanced the antinociceptive effects of systemically administered morphine in morphine tolerant rats. The antinociceptive effect of morphine in opioid nave rats was also significantly increased by pretreatment with icv TRIM. Conclusions: Our results further support the hypothesis that supraspinal NO modulates morphine-sensitive nociceptive process in morphine tolerance due to chronic intravenous administration.

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인삼이 토끼 적혈구막의 $Na^{+}-K^{+}-ATPase$의 활성도에 미치는 영향 (Effect of Ginseng on Sodium-Potassium activated ATPase in Rabbit Red Cell Membrane)

  • 강병남;고일섭
    • The Korean Journal of Physiology
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    • 제8권1호
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    • pp.55-65
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    • 1974
  • The effect of ginseng on the ATPase activity of rabbit ref cell membrane has been investigated. The experiments were also designed to determine whether the components of ginseng could be attributed to the effect on ATPase activity which dependent upon sodium plus potassium and is sensitive to ouabain. The following results were observed. 1. The activity of the $Na^{+}-K^{+}-ATPase$ from red cell membrane is stimulated by ginseng, and the concentration of ginseng for half-maximal activity is about 15 mg%. The pH optimum for the ginseng sensitive component is 7.6. 2. The portion of the enzyme activity stimulated by ginseng is completely abolished by ouabain. 3. The activating effect of ginseng on the ATPase, with a given concentration of sodium in the medium, is increased by raising the potassium concentration but activity ratio is decreased. 4. The activating effect of ginseng on the ATPase, with a given concentration of potassium in the medium, is increased by raising the sodium concentration but the activity ratio is decreased. 5. The ATPase activity is increased by small amounts of calcium but inhibited by larger amounts and the rate of activity by ginseng is constant. 6. The action of ginseng on the ATPase activity was not related to the sulfhydryl group of cysteine, the amino group of lysine, the imidazole group of histidine, the quanidinium group of arginine, the carboxyl group of aspartic acid, or the hydroxyl group of threonine. 7. The activating effect of ginseng on the ATPase activity may be not due to a saponin which is contained in ginseng.

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Bioaccumulation of Chromium Ions by Immobilized Cells of a Filamentous Cyanobacterium, Anabaena variabilis

  • Khattar, Jasvir I.S.;Sarma, Tangirala-A.;Singh, Davinder-P.;Sharma, Anuradha
    • Journal of Microbiology and Biotechnology
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    • 제12권1호
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    • pp.137-141
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    • 2002
  • Anabaena variabilis ATCC 29413 grew in chromium (Cr) containing Chu-10 (basal) and nitrate-supplemented media, and the growth of the organism in $100{\mu}M$ chromium was found to be 50% of that in control medium. The growth in nitrate $({NO_3}^-)$ supplemented cultures was better as compared to cultures grown in basal medium. Free cells from basal and nitrate-supplemented media removed 5.2 and 7.4 nmol of chromium $mg^{-1}$protein in 8 h, respectively, from the medium containing $30{\mu}M$ chromium. The efficiency of chromium removal increased 7-fold in imidazole buffer (0.2 M, pH 7.0). A cell density equivalent to $100{\mu}g$ protein $ml^{-1}$ was found to be optimum for maximum Cr removal. Entrapment of cells in calcium-alginate beads did not affect the rate of Cr uptake by the cells. The efficiency of the laboratory-scale continuous flow bioreactor $(12.5{\times}2cm)$ loaded with alginate-immobilized cells (10 mg protein) and fed with $30{\mu}M$ chromium solution was compared at different flow rates. The efficiency of the bioreactor varied with flow rates. In terms of percent removal of Cr from influent, a flow rate of 0.1 ml $min^{-1}$ was found to be optimum for 6 h (54% Cr removal efficiency). Maximum amount of Cr (883 nmol) was removed by the cells in 3 h at a flow rate of 0.5 ml $min^{-1}$. The potential use of A. variabilis in removing Cr from industrial effluents is discussed.