• Title/Summary/Keyword: Post-synthesis

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새로운 심관관류 영상 화합물로서 $^{99m}Tc$-Ethyl-3-Isocyano-butyrate의 합성, 표지 및 체내동태에 대한 연구 (Synthesis Characterization and Biodistribution of $^{99m}Tc$-Ethyl-3-Isocyanobutyrate as a New Myocardial Perfusion Agent)

  • 이명철;조정혁;이동수;임상무;오승준;정수욱;이경한;정재민;정준기;고창순
    • 대한핵의학회지
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    • 제27권2호
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    • pp.223-232
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    • 1993
  • Technetium labeled isonitrile analogues are widely used as myocardial perfusion imaging agents. We synthesized and characterized a new isonitrile compound, ethyl 3-isocyanobutyrate(EIB). Proton and $^{13}C$ NMR spectroscopy and thin layer chromatography with a $C_{18}$ coat was performed. EIB was easily labeled with $^{99m}TcO_4^-$- with sodium dithionite. The labeling efficiency measured by RP-HPLC was over 95%. The labeled product was stable with dilution in normal saline and with prolonged incubation at room temperature. There was no formation of secondary products or free $^{99m}TcO_4^-$. In vivo kinetics study of $^{99m}Tc$ (I) labeled EIB in rabbits showed adequate myocardial uptake, good contrast against lung background, and relatively rapid liver clearance. The heart to lung ratio was over 2.5 and the heart to liver ratio was approximately from 0.4 to 5 at 60 minutes post injection. Hepatic clearance of $^{99m}Tc-MIBI$ was faster ($t_{1/2}$=6 minutes) than that of $^{99m}Tc-MIBI$. In vivo kinetics observed in dog was similar to that in rabbit but there was faster gallbladder filling, and thus lower liver background. SPECT imaging of the canine myocardium showed favorable imaging characteristics. However, biodistribution in mice demonstrated a myocardial % injected dose/organ of less than 0.1%. This was thought to be due to interspecies difference in plasma esterase activity. In human plasma, $^{99m}Tc$ ( I ) labeled EIB was stable for at least 2 hours, without production of secondary products by HPLC. We conclude that ethyl 3-isocyanobutyrate may be a potential new myocardial perfusion imaging agent and deserves further investigation as to its usefulness for clinical use.

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누에 수정란 초기발현유전자 데이터베이스 구축 (Gene expression profile of the early embryonic gene of the silkworm, Bombyx mori)

  • 최광호;구태원;김성렬;김성완;전재범;박승원;강석우
    • 한국잠사곤충학회지
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    • 제51권2호
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    • pp.191-196
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    • 2013
  • 본 연구는 누에 수정란 초기에 발현하는 유전자를 대량 선발하고, 유용 유전자의 프로모터를 개발하기 위한 연구의 일환으로 추진하였다. 산란 후 2 ~ 16시간이 경과한 누에알로부터 cDNA 유전자은행을 제작하였다. 제작된 cDNA 유전자은행으로 전체 960개 클론을 무작위 추출하여 부분 염기서열 분석을 통해 EST를 제작하였다. 분석된 652개 ESTs 중 염기서열 상동성 분석을 통해 156개의 기존 알려진 유전자와 178개의 미지의 유전자로 구성된 334개 독립유전자를 최종 선발하여 'eegEST'로 명명하였다. eegEST 분석 결과, 기존 염기서열 정보가 알려진 156개 독립유전자 중 2회 이상 출현한 유전자 수는 143개로 전체의 34%를 차지하였으며, Hsp20.8 유전자(12회)와 ubiqutin-like 유전자(11회)가 가장 높은 출현 빈도를 나타내었다. 또한 eegEST 독립유전자의 추정 기능에 따른 분류에서 곤충 수정란 발생초기에 확인할 수 있는 기관 형성과 관련한 유전자가 전체 24%를 차지하고 있었다. 본 연구에서 작성된 누에 수정란 초기 발현유전자 데이터베이스(eegEST)는 곤충 발생학 연구를 위한 정보제공 뿐 아니라 형질전환누에 제작을 위한 프로모터 개발 연구에 활용될 수 있을 것으로 기대한다.

식물에서 shikimate 및 방향족 아미노산 생합성 경로와 이의 대사공학적 응용 (Biosynthetic pathway of shikimate and aromatic amino acid and its metabolic engineering in plants)

  • 임선형;박상규;하선화;최민지;김다혜;이종렬;김영미
    • Journal of Plant Biotechnology
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    • 제42권3호
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    • pp.135-153
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    • 2015
  • 식물의 페닐알라닌, 티로신, 그리고 트립토판과 같은 방향족 아미노산은 단백질 합성의 구성 성분 뿐만 아니라 다양한 이차 대사물질들의 전구물질들이다. 이러한 방향족 아미노산 유래의 화합물들은 식물의 색소와 세포벽 구성성분을 포함하는 다양한 페놀릭 화합물들의 구성성분이자, 옥신과 살리실산과 같은 식물 호르몬으로써 중요한 역할을 수행한다. 또한 이들은 인간의 영양과 건강을 증진하는 높은 잠재력을 지니는 알칼로이드 및 글루코시놀레이트와 같은 천연산물로써 역할을 한다. 방향족 아미노산의 생합성경로는 shikimate 경로로부터 유래되는 공통의 중간기질인 chorismate를 공유한다. 트립토판은 중간기질로 anthranilate를 통해 합성되고, 페닐알라닌 및 티로신은 중간기질인 prephenate를 통해 합성된다. 본 논문에서는 방향족 아미노산 생합성경로에 관련한 모든 단계의 효소와 전사/전사후 수준에서의 그들의 유전자 조절에 대한 최근 연구들에 대해 종합적으로 되짚어 보면서, 추가적으로 식물의 방향족 아미노산 유래의 천연물질 생산을 증진시키기 위해 그 동안 시도되어온 대사 공학적 노력들에 대해서 소개하고자 한다.

Synthesis of New 4-Oxo-2-Thioxo-1,2,3,4-Tetrahydropyrimidine Derivatives with an Incorporated Thiazolidinone Moiety and Testing Their Possible Serine Protease and Cercarial Elastase Inhibitory Effects with a Possible Prospective to Block Penetration of Schistosoma mansoni Cercariae into the Mice Skin

  • Bahgat Mahmoud Mohamed;Maghraby Amany Sayed;Heiba Mogeda Emam;Ruppel Andreas;Fathalla Omar Abd-elfattah Mohamed
    • Archives of Pharmacal Research
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    • 제28권9호
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    • pp.1002-1012
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    • 2005
  • 5-Substituted 4-oxo-2-thioxo-1,,2,3,4-tetrahydropyrimidine were synthesized by interaction of 4­oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonylhydrazide with some aldehydes to give the corresponding Schiff-bases, which after cyclization gave corresponding thiazolidinones. For some of the thiazolidinones, Mannich bases reaction was carried out. All the derivatives were tested for their possible inhibitory effect on Schistosoma mansoni cercarial elastase (CE). Only, N'-(4-methylbenzyledine)-4-oxo-2-thioxo-1,2 ,3,4-tetrahydropyrimidine-5-sulfonylhydrazide was found to have potent inhibitory effect on the CE activity with $IC_{50} = 264{\mu}M.$ Upon its use as a paint for mice tails before infection with S. mansoni cercariae, the compound formulated in jojoba oil caused a significant reduction ($93\%$; P-value = 0.0002) in the worm burden. IgG & IgM in mice sera were measured by using several S. mansoni antigens by ELISA. Sera from treated infected mice (TIM) 2, 4, and 6 weeks (W) post infection (PI) showed 1.2 folds lower, 1.2 folds higher, 1.7 folds lower IgM reactivity against soluble cercarial antigenic preparation (CAP), respectively, when compared with sera collected from infected untreated mice (IUM). Sera from TIM 2, 4, and 6WPI showed 1.3, 1.6, and 1.7 folds higher IgG reactivity, respectively against CAP than the IgG reactivity from IUM. Sera from TIM 2, 4 and 6WPI showed 1.5, 1.2 folds lower and 1.4 folds higher IgM reactivity, respectively against soluble worm antigenic preparation (SWAP) when compared with sera collected from IUM. Sera from TIM 2, 4, and 6WPI showed 1.4, 1 folds lower and 1 fold higher IgG reactivity, respectivley to SWAP when compared with sera from IUM. Sera from TIM 2, 4, and 6WPI had generaly lower IgM and IgG reactivities against soluble egg antigen (SEA) when compared with sera from IUM.

Effects of 5-Aminolevulinic Acid on Growth and Inhibition of Various Plant Species

  • Kuk, Yong-In;Lim, Gyeong-Seob;Chon, Sang-Uk;Hwang, Tay-Eak;Guh, Ja-Ock
    • 한국작물학회지
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    • 제48권2호
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    • pp.127-133
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    • 2003
  • The purpose of this study is to investigate the positive or negative effects of 5-aminolevulinic acid(ALA) on the growth of several crops and weeds, by applying a seed soaking treatment, foliar treatment, and application timing, while comparing biological activity between ALA produced by chemical synthesis (Synthetic-ALA) and extracellularly-accumulated ALA by overexpressing the hemeA gene isolated from Bradyrhizobium japonicum(Bio-ALA). Seed soaking treatment of ALA in barley (five cultivars) and wheat (five cultivars) had not shown positive effects at lower concentrations, 0.05 to 0.5 mM as well as negative effects at higher concentrations, 1 to 30 mM. In rice, there also was no positive effect by seed soaking treatment of ALA at lower concentrations, although the rice became damaged by an application of 5 and 10 mM ALA. Growth in barley cultivars, Ganghossalbori, Naehanssalbori, Songhakbori, Saessalbori, and Daehossalbori were increased up to 14%, 19-51 %, 17-64%, 18-23%, and 22-38% by ALA foliar application at lower concentrations, 0.05 to 0.5 mM, respectively. On the other hand, the growth in barley cultivars was inhibited by ALA foliar application at higher concentrations. Barley responded more positively to ALA foliar application than wheat and rice. The growth stimulation caused by ALA seed soaking treatment was less than by ALA foliar treatment. ALA treatment at the 1.5-leaf stage increased growth of barley by 19-58%, while pretreatment to seeds, post-emergence treatment at 3 days after seeding, 3-leaf stages, and 5-leaf stages had not shown positive effects. Thus, the positive effects of ALA on barley were dependent greatly upon the timing of application and its concentration. Monocots weeds were more sensitive to ALA foliar treatment than dicotyledonous weeds. A monocot weed, Setaria viridis L. was the most susceptible plant to ALA while a dicotyledonous weed, Plantago asiatica L. was the most tolerant. No significant difference in biological activity between bio-ALA and synthetic ALA on barley, wheat, rice, and weed, Ixeris dentate tested was observed. Thus, ALA produced by microorganisms would be a potent substance to be used effectively in agricultural production.

Anti-Proliferative Activity of OD78 Is Mediated through Cell Cycle Progression by Upregulation p27kip1 in Rat Aortic Vascular Smooth Muscle Cells

  • Tudev, Munkhtsetseg;Lim, Yong;Park, Eun-Seok;Kim, Won-Sik;Lim, Il-Ho;Kwak, Jae-Hwan;Jung, Jae-Kyung;Hong, Jin-Tae;Yoo, Hwan-Soo;Lee, Mi-Yea;Pyo, Myoung-Yun;Yun, Yeo-Pyo
    • Biomolecules & Therapeutics
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    • 제19권2호
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    • pp.187-194
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    • 2011
  • Atherosclerosis and post-angiography restenosis are associated with intimal thickening and concomitant vascular smooth muscle cell (VSMC) proliferation. Obovatol, a major biphenolic component isolated from the Magnolia obovata leaf, is known to have anti-inflammatory and anti-tumor activities. The goal of the present study was to enhance the inhibitory effects of obovatol to improve its potential as a preventive or therapeutic agent in atherosclerosis and restenosis. Platelet-derived growth factor (PDGF)-BB-induced proliferation of rat aortic smooth muscle cells (RASMCs) was examined in the presence or absence of a newly synthesized obovatol derivative, OD78. The observed anti-proliferative effect of OD78 was further investigated by cell counting and [$^3H$]-thymidine incorporation assays. Treatment with 1-4 ${\mu}M$ OD78 dose-dependently inhibited the proliferation and DNA synthesis of 25 ng/ml PDGF-BB-stimulated RASMCs. Accordingly, OD78 blocked PDGF-BB-induced progression from the $G_0/G_1$ to S phase of the cell cycle in synchronized cells. OD78 decreased the expression levels of CDK4, cyclin E, and cyclin D1 proteins, as well as the phosphorylation of retinoblastoma protein and proliferating cell nuclear antigen; however, it did not change the CDK2 expression level. In addition, OD78 inhibited downregulation of the cyclin-dependent kinase inhibitor (CKI) $p27^{kip1}$. However, OD78 did not affect the CKI $p21^{cip1}$ or phosphorylation of early PDGF signaling pathway. These results suggest that OD78 may inhibit PDGF-BB-induced RASMC proliferation by perturbing cell cycle progression, potentially through $p27^{kip1}$ pathway activation. Consequently, OD78 may be developed as a potential anti-proliferative agent for the treatment of atherosclerosis and angioplasty restenosis.

Protein Profile in Corpus Luteum during Pregnancy in Korean Native Cows

  • Chung, H.J.;Kim, K.W.;Han, D.W.;Lee, H.C.;Yang, B.C.;Chung, H.K.;Shim, M.R.;Choi, M.S.;Jo, E.B.;Jo, Y.M.;Oh, M.Y.;Jo, S.J.;Hong, S.K.;Park, J.K.;Chang, W.K.
    • Asian-Australasian Journal of Animal Sciences
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    • 제25권11호
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    • pp.1540-1545
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    • 2012
  • Steroidogenesis requires coordination of the anabolic and catabolic pathways of lipid metabolism, but the profile of proteins associated with progesterone synthesis in cyclic and pregnant corpus luteum (CL) is not well-known in cattle. In Experiment 1, plasma progesterone level was monitored in cyclic cows (n = 5) and pregnant cows (n = 6; until d-90). A significant decline in the plasma progesterone level occurred at d-19 of cyclic cows. Progesterone level in abbatoir-derived luteal tissues was also determined at d 1 to 5, 6 to 13 and 14 to 20 of cyclic cows, and d-60 and -90 of pregnant cows (n = 5 each). Progesterone level in d-60 CL was not different from those in d 6 to 13 CL and d-90 CL, although the difference between d 6 to 13 and d-90 was significant. In Experiment 2, protein expression pattern in CL at d-90 (n = 4) was compared with that in CL of cyclic cows at d 6 to 13 (n = 5). Significant changes in the level of protein expression were detected in 32 protein spots by two-dimensional polyacrylamide gel electrophoresis (2-DE), and 23 of them were identified by matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF-MS). Six proteins were found only in pregnant CL, while the other 17 proteins were found only in cyclic CL. Among the above 6 proteins, vimentin which is involved in the regulation of post-implantation development was included. Thus, the protein expression pattern in CL was disorientated from cyclic luteal phase to mid pregnancy, and alterations in specific CL protein expression may contribute to the maintenance of pregnancy in Korean native cows.

분무열분해법(Spray Pyrolysis)에 의한 주석산화물이 도핑된 $In_2O_3$(ITO: Indium Tin Oxide)의 분말 제조에 대한 연구 (The Studies on synthesis of $SnO_2$ doped $In_2O_3$ (ITO: Indium Tin Oxide) powder by spray pyrolysis)

  • 김상헌
    • 한국응용과학기술학회지
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    • 제31권4호
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    • pp.694-702
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    • 2014
  • 마이크론 크기를 가지는 ITO(indium tin oxide) 입자들은 인듐과 틴의 수용성 전구체들과 유기 첨가제를 분무 열분해하여 얻었다. 유기 첨가제로서는 에틸렌글리콜과 시트르산을 이용하였다. 분무 열분해 시 에틸렌글리콜과 시트르산과 같은 유기첨가제를 첨가하지 않고 얻어진 ITO 입자들은 구형이며 속이 꽉찬 형태를 가지는데 비해 유기 첨가제를 첨가하여 분무 열분해를 하면 얻어지는 ITO 입자들은 유기 첨가제의 양이 증가 할수록 껍질이 얇고 다공성이 증대된 중공 입자가 얻어진다. 유기첨가제를 첨가하지 않고 분무 열분해를 통해 얻어지는 마이크론 크기를 가지는 ITO는 $700^{\circ}C$에서 두 시간 동안의 후소성과 24 시간동안의 습식 볼밀링에 의해 나노 크기의 ITO로 전환되지 않으나, 유기첨가제를 첨가하고 분무 열분해를 통해 얻어지는 마이크론 크기를 가지는 ITO는 $700^{\circ}C$에서 두 시간 동안의 후소성과 24 시간 동안의 습식 볼밀링에 의해 나노 크기의 ITO로 쉽게 전환되었다. 응집된 나노 크기의 ITO의 일차 입자의 크기를 Debye-Scherrer 식에 의해 계산하였고 ITO 입자를 압축하여 만든 펠렛의 표면저항을 측정하였다.

대두 철분결합단백질 유전자 발현 형질전환 감자의 감자무름병 방어 증진효과 (Tolerance to Potato Soft Rot Disease in Transgenic Potato Expressing Soybean Ferritin Gene)

  • 배신철;여윤수;허성기;황덕주;변명옥;고승주
    • Journal of Plant Biotechnology
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    • 제29권4호
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    • pp.229-233
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    • 2002
  • 식물의 항산화력을 증진하여 식물병원균 저항성 작물을 개발하고자, 철분 결합 단백질인 대두의 ferritin 유전자를 CaMV 35S와 hsr203J promoter에 연결하여 감자에 형질전환하였다. PCR및 Northern분석에 의한 형질전환 감자에 ferritin 유전자가 존재하는 것과 이들 유전자 식물체내에서 발현되는 것을 확인하였다. ferritin 유전자를 담배 유래 병원균 특이 발현promoter인 hsr203J와 연결하여 획득된 형질전환 감자 식물체는 감자역병균 접종 후 24시간대에서 전사체 발현량이 가장 많았으며 그 후 줄어드는 경향을 나타내었다. 유전자 도입이 확인된 형질전환체 감자괴경의 철분 함량은 CaMV 35S와 ferritin 유전자 도입 형질전환체가 2.5배, hsr203J promoter와 ferritin 유전자 도입 형질전환체가 1.5배 각각 증가하는 것으로 나타냈다. 또한 이들 형질전환체는 감자 무름병균에 대한 저항성 증진효과를 관찰할 수 있었다.

이성분계 금속합금($MoRu_3$, $MoRh_3$)의 합성 및 구조분석 (Synthesis and Structural Analysis of Binary Alloy ($MoRu_3$, $MoRh_3$))

  • 박용준;이종규;김종구;김정석;지광용
    • 분석과학
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    • 제11권3호
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    • pp.189-193
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    • 1998
  • 조사후 핵연료의 용해실험 다음에 잔류된 불용성 잔유물을 구성하는 Mo, Ru, Rh 등의 원소로 이루어진 이성분계 합금인 $MoRu_3$$MoRh_3$을 아르곤 아아크로를 이용하여 $1700^{\circ}C$ 이상의 고온에서 합성하였다. 이들 합금의 정확한 구조와 결정격자상수는 ICDD(International Centre for Diffraction Data)에서 제작되는 분말회절수집철(JCPDS files) 등에 수록된 바가 없다. X선 회절분석결과 이들 두 합금은 육방밀집구조와 $P6_3/mmc$의 공간군을 갖는 $WRh_3$의 구조와 매우 유사한 것으로 나타났다. 이 화합물들의 격자상수, a와 c는 최소자승법을 이용하여 구하였다. 또한 XPS로 분석을 통하여 이들의 표면을 조사한 결과 금속 표면이 실온에서 공기와 접촉하였을 때 여러 구성성분 중에서 Mo(0)가 Mo(6+)로 산화되는 것을 확인하였는데, 아르곤이온으로 표면을 15분 정도 sputtering 하여 Mo(6+)층을 제거할 수 있었다. 합금의 구성성분 중, Mo, Ru, Rh 원소에서 내부 전자들의 결합에너지에는 커다란 변화가 없는 것으로 나타났다. 이들 화합물들의 자화율을 측정해 본 결과 2~300 K 범위에서 전형적인 Pauli-paramagnetic 행동을 보여주었다.

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