• Title/Summary/Keyword: L-6

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Synthesis of 2',3'-Dideoxyisoguanosine from Guanosine

  • Kim, Sung-Han;Lee, Sang-Jun;Sun, Won-Suck;Oh, Sung-Wook;Kim, Jung-Han
    • Archives of Pharmacal Research
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    • v.22 no.6
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    • pp.619-623
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    • 1999
  • $2^{l},3^{l}$-dideoxyisoguanosine was synthesized from guanosine via intermediate 6-[(4-methyl-phenyl)thio]-2-oxo-9-($2^{l},3^{l},5^{l}$-tri-O-acetyl-$\beta$-D-ribofuranosyl)-2,3-dihydropurine (4). The 2-oxo, 6-amino and $5^{l}$-hydroxy triprotected isoguanosine derivative was utilized to reduce high polarity and promote poor solubility of intermediates. The protecting groups for oxo and 6-amino were easily removed in reduction of olefin in ribose without additional reaction steps.$2^{l},3^{l}$-Vicinal diol in ribose sugar moiety was transformed to olefin with Bu3SnH by radical reaction via bisxanthate. Removing $5^{l}$-O-TBDMS protecting group gave final product, $2^{l},3^{l}$-dideoxyisoguanosine (12) in a 10% overall yield.

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Synthesis of 2-(5,6-dimethoxy-l-indenyl)ethyl amine (2-(5,6-디메톡시-1-인데닐)에틸 아민의 합성)

  • 정원영;마은숙
    • YAKHAK HOEJI
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    • v.47 no.1
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    • pp.1-4
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    • 2003
  • In order to search the new serotonin bioisoster, 2-(5,6-dimethoxy-l-indenyl)ethyl amine(1) was synthesized. 3,4-Dimethoxybenzaldehyde, as starting material, was condensed with malonic acid in the presence of pyridine and piperidine to form 3,4-dimethoxycinnamic acid(2). Compound 2 was performed catalytic hydrogenation with 10% Pd-C to give propanoic acid derivative 3, which was cyclized by Friedel-Crafts acylation to afford 5,6-dimethoxyindan-l-one(4). Compound 4 was reduced with NaBH$_4$ in ethanol to obtain l-indanol 5, and it was dehydrated to give 5,6-dimethoxy-l-indene(6). This compound was lithiated with 2.5M n-butyllithium and reacted with 1,2-dibromoethane to give 2-(5,6-dimethoxy-l-indenyl)ethyl bromide(7), and which was treated with anhydrous ammonia to synthesize compound 1.

Neuroprotective Effect of l-Deprenyl Against 6-OHDA-Induced Dopamine Depletion in Rat Striatum and 6-OHDA-Induced Oxidative Stress in SH-SY5Y Cells (흰쥐 선조체에서 6-OHDA-유도 도파민 고갈 및 SH-SY5Y 세포주에서 6-OHDA-유도 산화적 스트레스에 대한 l-Deprenyl의 신경 보호효과)

  • Kim Eun-Mi;Choi Sinkyu;Lee Kyunglim;Kim Hwa-Jung
    • YAKHAK HOEJI
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    • v.49 no.4
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    • pp.355-364
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    • 2005
  • A neurotoxin, 6-hydroxydopamine (6-OHDA) has long been used to form a Parkinson's disease (PD) model by inducing the lesion in catecholaminergic pathways, particularly the nigrostriatal dopamine (DA) pathway. Whereas l-deprenyl, a selective inhibitor of monoamine oxidase (MAO) type B, is now widely used in the treatment of PD, the precise action mechanism of the drug remains elusive. In this study, we investigated whether l-deprenyl shows protective effect against the DA depletion induced by 6-OHDA in rat brain, and against 6-OHDA-induced neurotoxicity and oxidative stress in catecholaminergic neuroblastoma SH-SY5Y cells that are known to lack MAO-B activity. Pretreatment of l-deprenyl significantly enhanced the striatal DA, 3,4-dihydroxyphenylacetic acid, homovanilic acid, and 3-methoxytyramine levels compared to the untreated 6-OHDA-lesioned rat, indicating that l-deprenyl pretreatment prevents 6-OHDA-induced depletion of not only striatal dopamine but also its metabolites. Treatment of 6-OHDA for 24hrs decreased the cell viability and increase the generation of ROS in dose-dependent manners. We further investigated whether caspase activity is involved in the action of l-deprenyl. Treatment of l-deprenyl $(0.1\~100{\mu}M)$ did not produce any changes in 6-OHDA-induced cleavage of poly (ADP-ridose) polymerase in SH-SY5Y cells. Our results suggest that the neuroprotective effect of l-deprenyl against 6-OHDA is due to its increased scavenger activity, but independent of inhibition of MAO-B or caspase-3 activation.

Optimal concentrations of plant growth regulators and AgNO3 for the improvement of regeneration efficiency in Chrysanthemum morifolium 'Ohblang' (국화 '오블랑'의 재생 효율 증진을 위한 식물생장조절제와 AgNO3 적정 농도 선별)

  • Yeo Jin Youn;Yong Joon Yang
    • Journal of Plant Biotechnology
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    • v.50
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    • pp.169-175
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    • 2023
  • A plant regeneration system was developed through shoot organogenesis from in vitro leaf explants of Chrysanthemum morifolium 'Ohblang'. The effects of different concentrations of plant growth regulators and AgNO3 on efficient shoot regeneration and inhibition of browning were evaluated in chrysanthemum. The explants were cultured on MS shoot induction medium supplemented with 12 combination treatments of 6-benzyladenine (BA) 0.5, 1.0 and 2.0 mg/L, and α-naphthaleneacetic acid (NAA) 0.2, 0.5, 1.0 and 2.0 mg/L in darkness for 6 weeks and cultured under a 16/8 h photoperiod for 6 weeks. The highest shoot regeneration was obtained from the explants cultured on the medium with 1.0 mg/L BA and 1.0 mg/L NAA. Based on this result, AgNO3 was added to a shoot induction medium containing MS salts, vitamins, 1.0 mg/L BA, 1.0 mg/L NAA, 30 g/L sucrose, and 6 g/L agar to reduce browning of chrysanthemum leaf explants. In the control treatment without AgNO3, leaf explants turned brown at the cut edge; however, browning was not observed in AgNO3 treatments. Shoot organogenesis was higher at low concentrations of AgNO3 and decreased with an increase in AgNO3 concentration. The explants cultured on shoot induction medium (MS salts, vitamins, 1.0 mg/L BA, 1.0 mg/L NAA) with 1 mg/L of AgNO3 produced the highest shoot regeneration with 2.6 shoots per explants and a browning index of 0.7. When the regenerated shoots were detached from the explants and cultured on MS medium, the shoots were elongated and rooted successfully.

Effect of disulphide bond position on salt resistance and LPS-neutralizing activity of α-helical homo-dimeric model antimicrobial peptides

  • Nan, Yong-Hai;Shin, Song-Yub
    • BMB Reports
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    • v.44 no.11
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    • pp.747-752
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    • 2011
  • To investigate the effects of disulphide bond position on the salt resistance and lipopolysaccharide (LPS)-neutralizing activity of ${\alpha}$-helical homo-dimeric antimicrobial peptides (AMPs), we synthesized an ${\alpha}$-helical model peptide ($K_6L_4W_1$) and its homo-dimeric peptides (di-$K_6L_4W_1$-N, di-$K_6L_4W_1$-M, and di-$K_6L_4W_1$-C) with a disulphide bond at the N-terminus, the central position, and the C-terminus of the molecules, respectively. Unlike $K_6L_4W_1$ and di-$K_6L_4W_1$-M, the antimicrobial activity of di-$K_6L_4W_1$-N and di-$K_6L_4W_1$-C was unaffected by 150 mM NaCl. Both di-$K_6L_4W_1$-N and di-$K_6L_4W_1$-C caused much greater inhibitory effects on nitric oxide (NO) release in LPS-induced mouse macrophage RAW 264.7 cells, compared to di-$K_6L_4W_1$-M. Taken together, our results indicate that the presence of a disulphide bond at the N- or C-terminus of the molecule, rather than at the central position, is more effective when designing salt-resistant ${\alpha}$-helical homo-dimeric AMPs with potent antimicrobial and LPS-neutralizing activities.

The Effect of Vitamin {TEX}$B_{6}${/TEX} Deficiency on the Utilization and Recuperation of Stored Fuel in Highly Intense Exercised Rats

  • Cho, Youn-Ok
    • Preventive Nutrition and Food Science
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    • v.1 no.1
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    • pp.75-79
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    • 1996
  • The purpose of this study was to investigate the effect of vitamin {TEX}$B_{6}${/TEX} deficiency on the utilization and recuperation of stored fuel in exercising rats. Thirty six rats were fed either a vitamin {TEX}$B_{6}${/TEX} deficient diet(-{TEX}$B_{6}${/TEX}) or a control diet(+{TEX}$B_{6}${/TEX}) for 5 weeks, then subdivided into 3 group: non-exercise group(NE), exercise group(EX), exercise and recuperation group(EX). EX group were exercised in treadmill({TEX}$10^{o}${/TEX}, 0.5~0.8km/h)for 2 hours and ER group were recuperated three days with the respective diet after exercise. Glucose(GLU), glycogen(GLY), protein(PRO), trigyceride(TG) and free fatty acid(FFA) were compared in plasma(P), liver(L) and skeletal muscle(M) of rats. Compared to +{TEX}$B_{6}${/TEX} rats, in NE group, the level of L-GLY of -{TEX}$B_{6}${/TEX} rats was higher, M-TG, L-PRO of -{TEX}$B_{6}${/TEX} rats were lower and there were no differences in P-PRO, P-FFA, P-TG, M-GLY, M-PRO and L-TG. In EX group, the levels of P-FFA, L-PRO of -{TEX}$B_{6}${/TEX} rats were higher. P-TG, L-TG of -{TEX}$B_{6}${/TEX} rats were lower and there was no difference in L-GLY. In EG group, the levels of P-GLU, P-PRO, P-RG, L-PRO of -{TEX}$B_{6}${/TEX} rats were lower and there were no differences in L-GLY, L-TG, M-TG and M-GLY. these results suggest that a lowered intake of vitamin {TEX}$B_{6}${/TEX} may impair the recuperation of aminals after exercise related to exercise fuel stores although there is a compensation among stored fuel utilization during exercise.

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A Natural L-Arginine Analog, L-Canavanine-Induced Apoptosis is Suppressed by Protein Tyrosine Kinase p56lck in Human Acute Leukemia Jurkat T Cells (인체 급성백혈병 Jurkat T 세포에 있어서 L-canavanine에 의해 유도되는 세포자살기전에 미치는 단백질 티로신 키나아제 p56lck의 저해 효과)

  • Park, Hae-Sun;Jun, Do-Youn;Woo, Hyun-Ju;Rue, Seok-Woo;Kim, Sang-Kook;Kim, Kyung-Min;Park, Wan;Moon, Byung-Jo;Kim, Young-Ho
    • Journal of Life Science
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    • v.19 no.11
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    • pp.1529-1537
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    • 2009
  • To elucidate further the antitumor effects of a natural L-arginine analogue, L-canavanine, the mechanism underlying apoptogenic activity of L-canavanine and its modulation by protein tyrosine kinase $p56^{lck}$ was investigated in human Jurkat T cells. When the cells were treated with 1.25 to 2.5 mM L-canavanine for 36 h, several apoptotic events including mitochondrial membrane potential (${\Delta\Psi}m$) loss, activation of caspase-9, -3, -8, and -7, poly (ADP-ribose) polymerase (PARP) degradation, and DNA fragmentation were induced without alteration in the levels of Fas or FasL. These apoptotic changes were more significant in $p56^{lck}$-deficient Jurkat clone JCaM1.6 than in $p56^{lck}$-positive Jurkat clone E6.1. The L-canavanine-induced apoptosis observed in $p56^{lck}$-deficient JCaM1.6 cells was significantly reduced by introducing $p56^{lck}$ gene into JCaM1.6 cells by stable transfection. Treatment of JCaM1.6/lck cells with L-canavanine caused a transient 1.6-fold increase in the kinase activity of $p56^{lck}$. Both FADD-positive wild-type Jurkat T cell clone A3 and FADD-deficient Jurkat T cell clone I2.1 exhibited a similar susceptibility to the cytotoxicity of L-canavanine, excluding involvement of Fas/FasL system in triggering L-canavanine-induced apoptosis. The L-canavanine-induced apoptotic sub-$G_1$ peak and activation of caspase-3, -8, and -7 were abrogated by pan-caspase inhibitor (z-VAD-fmk), whereas L-canavanine-induced activation of caspase-9 was not affected. These results demonstrated that L-canavanine caused apoptosis of Jurkat T cells via the loss of ${\Delta\Psi}m$, and the activation of caspase-9, -3, -8, and -7, leading to PARP degradation, and that the $p56^{lck}$ kinase attenuated the ${\Delta\Psi}m$ loss and activation of caspases, and thus contributed as a negative regulator to L-canavanine-induced apoptosis.

Treatment Characteristics Using Full-Scale SBR System (Full-Scale SBR 공법을 이용한 처리특성)

  • Choo, Tai-Ho;Lee, Yong-Doo;Cho, Yong-Hyun
    • The Journal of the Korea Contents Association
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    • v.6 no.10
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    • pp.34-40
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    • 2006
  • In this study, the treatment of organic matters and nutrients like Nitrogen and Phosphorus with sequencing batch reactors (SBR) was conducted. The following conclusions can be summarized from the study. The influent BOD concentration was varied 19.6 to 40.0mg/L and the effluent was 3.0 to 14.8mg/L. The variations of BOD removal efficiency during the experimental period was $47.9{\sim}88.4%$ and the average was 80.8%. The average removal efficiency was stabilized with the passage of time. Also the COD concentration was flowed into as $12.2{\sim}32.0mg/L$ and the effluent concentration was varied 3.3 to 18.6 mg/L, and then the average COD removal efficiency was 57.3%(minimun 19.2% and maximum 78.6%). But fortunately, the COD removal efficiency was also stabilized as 70.2% after 79days. In the case of T-N, the influent concentration range was $7.53{\sim}14.99mg/L$ and the effluent concentration was 6.59mg/L(the average removal efficiency was 40.3%) until the first experiment time 79days. But after normalizing the system, it was 4.44mg/L (the average removal efficiency was 56.4%). Also the influent T-P concentration was varied from 0.77 to 1.91mg/L and the effluent concentration was $0.26{\sim}1.53mg/L$. The removal efficiency was varied from 5.3 to 71.7%. considerably, therefore the average removal efficiency was 42.6%. The reason was concluded that the sludge wasn't discharged for increasing MLSS concentration.

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Numerical Analysis of Optical Soliton Transmission in Fibers with Periodically Compensated Loss (손실이 주기적으로 보상되는 광섬유에서의 솔리톤 전송에 대한 수치적 분석)

  • 이명우;김란숙;서동선
    • The Journal of Korean Institute of Communications and Information Sciences
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    • v.19 no.7
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    • pp.1191-1202
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    • 1994
  • We numerically investigate a stable propagation regime of soliton pulse trains in fibers with periodically copensated loss by lumped optical amplifiers. When amplification solition pulses is 1.2~1.5 and the minimum soliton separation normalized by the soliton width becomes about 6. In cases of L=50[km], the allowable range of A is 1.5~1.7 under =6. The maximum allowable variation of the loss compensation in each lumped amplifier becomes +-2% of the fiber loss when L=50[km], A=1.6, and =6. Generally, the allowable rages of the soliton amplitude A and amplifier gain are inversely proportional to the amplification period L.

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한강하류의 환경학적 연구 VII. 가을철 식물플랑크톤의 대발생

  • 이진환;정승원;김상훈
    • Proceedings of the Korea Society of Environmental Biology Conference
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    • 2002.05a
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    • pp.73-73
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    • 2002
  • 본 연구는 2001년 9, 10, 11월에 2주 간격으로 6개 정점에서 한강 하류 수욕6개 정점(팔당대교-행주대교)에서 식물플랑크톤 군집과 수지로한경(수온, 염분도, pH, DO, BOD, SS, TN, TP, $NO_{3}-N$, $NH_{4}-N$, $PO_{4}-P$)을 조사하였다. 수온은 7,8월에 $24~27^{\circ}C$ 로 높았으며, BOD의 평균 농도는 정점 1과 2에서 각각 1.26mg/l, i.39mg/l이었고, 정점 3~6에서 3.52~4.01mg/l이었다. $NO_{3}-N$은 정점 1에서 6까지 평균 1.36~1.98mg/l의 범위였고, $PO_{4}-P$의 평균 농도는 BOD, $NO_{3}-N$와 마찬가지로 하류오 향할수록 높아져 정점 6에서 정점 1의 39배였다. TN은 평균 1.74~6.89mg/l, TP는 0.03~0.42mg/l의 범위였다. 한강하류의 수질은 강우에 영향이 크며, 탄천의 영향을 받는 정점 3(영동대교)에서 급격히 나빠져 성산대교까지 유지되다가 안양천의 영향을 받는 행주대교에서 최고조로 악화되는 거으로 파악되었다. 식물플랑크톤 현존량은 6월 4일 평균 $5.81\times10^{6}cells/l$로 감소하였다가 7월 13일 $28.53\times10^{6}cells/l$로 증가하였다. 7월 28일과 8월 11일에 각각 $3.07~8.34\times10^{6}cells/l$로 감소하였다가 8월25일 $24.47\times10^{6}cells/l$로 다시 증가하여 조사기간 중 항시 대발생이 유지되고 있었다. 본 수역에서 우점종은, 6월에 전 조사정점에서 Aulacoseria granulata와 Aulacoseria granulata var. angustussima, 7월에는 Aulacoseria granulata var. angustussima와 Stephanodiscus hantzschii f. tenuis와 남조류인 Anabaena sp., Oscillatoria sp.가 우점을 하였다. 8월에는 남조류인 Anabaena sp. Microcystic sp. Osillatoria sp.가 높은 비율로 우점하였다. 여름철 식물플랑크톤 대발생에 영향은 수온과 직산염이 중요하였으나, 부유물질 크게 기여하지 못하였다.

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