• Title/Summary/Keyword: L-glutamate

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Distinct $[^3H]$MK-801 Binding Profiles with the Agonist, Partial Agonist, and Antagonist Acting at the Glycine Binding Site of the N-Methyl-D-Aspartate Receptor

  • Cho, Jung-sook;Park, No-Sang;Kong, Jae-Yang
    • Biomolecules & Therapeutics
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    • v.4 no.2
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    • pp.196-201
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    • 1996
  • The N-methyl-D-aspartate (NMDA) receptor-ion channel complex is activated by the simultaneous presence of L-glutamate and glycine, allowing the binding of MK-801 to the phencyclidine (PCP) site of the receptor. The $[^3H]$MK-801 binding assay system was established for determination of pharmacological functions of test compounds acting at the glycine site of the receptor. The binding in the presence of 0.1 $\mu$M L-glutamate was increased by an agonist (glycine) in a dose-dependent fashion, while decreased by either partial agonist (R-(+)-HA-966) or antagonist (5,7-dichlorokynurenic acid: 5,7-DCKA). To distinguish partial agonism from antagonism, various concentrations of 7-chlorokynurenic acid (7-CKA) were added in the assay to eliminate the interference of the endogenous glycine present in the membrane preparations. The bindings in the presence of L-glutamate (0.1$\muM$) and 7-CKA (1, 5, or 10$\muM$) were increased by R-(+)-HA-966. Being a weak partial agonist, the extent of potentiation was much less than that by the agonist. These binding profiles were clearly distinguishable from those by the antagonist, 5,7-DCKA, which exhibited no intrinsic activity. The binding assays established in the present study are a useful system to classify ligands acting at the glycine site of the NMDA receptor by their pharmacological functions.

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Norfloxacin Release from Polymeric Micelle of Poly($\gamma$-benzyl L-glutamate)/Poly(ethylene oxide)/Poly($\gamma$-benzyl L-glutamate)/ Block Copolymer

  • 나재운;정영일;조종수
    • Bulletin of the Korean Chemical Society
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    • v.19 no.9
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    • pp.962-967
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    • 1998
  • Block copolymers consisting of poly(rbenzyl L-glutamate) (PBLG) as the hydrophobic part and poly(ethylene oxide) (PEO) as the hydrophilic part were synthesized and characterized. Polymeric micelles of the block copolymers (abbreviated GEG) were prepared by a dialysis method. The GEG block copolymers were associated in water to form polymeric micelles, and the critical micelle concentration (CMC) values of the block copolymers decreased with increasing PBLG chain length in the block copolymers. Transmission electron microscopy (TEM) observations revealed polymeric micelles of spherical shapes. From dynamic light scattering (DLS) study, sizes of polymeric micelles of GEG-1, GEG-2, and GEG-3 copolymer were 106.5±59.2 nm, 79.4±46.0 nm, and 37.9±13.3 nm, respectively. The drug loading contents of GEG-1, GEG-2 and GEG-3 polymeric micelles were 12.6, 11.9, and 11.0 wt %, respectively. These results indicated that the drugloading contents were dependent on PBLG chain length in the copolymer; the longer the PBLG chain length, the more the drug-loading contents. Release of norfloxacin (NFX) from the nanoparticles was slower in higher loading contents of NFX than in lower loading contents due to the hydrophobic interaction between PBLG core and NFX.

A Study on Nitrogen Metabolism of Lemnaceae: Assimilation of Nitrate and Ammonia in Spirodela polyrhiza and Lemna aequinoctialis (개구리밥과 식물의 질소대사에 관한 연구: 개구리밥(Spirodela polyrhiza)과 좀개구리밥(Lemna aequinoctialis)의 NO3-와 NH4-의 동화작용)

  • 장남기
    • Journal of Plant Biology
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    • v.34 no.4
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    • pp.253-260
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    • 1991
  • Spirodela polyrhiza and Lemna aequinoctialis often occurred at the sites of high ammonium concentration and at the sites of high nitrate concentration, respectively. We investigated the different distribution between two species in relation to the type of nitrogen sources and their concentrations. Our experiments showed that L. aequinoctialis grew faster than S. polyrhiza in nitrate media with lower than 15 mM concentration. The nitrate uptake was also faster in L. aequinoctialis than in S. polyrhiza. However, neither differences in growth nor in uptake patterns between these two species were observed in ammonium media. Glutamine synthetase (GS), glutamate dehydrogenase (GDH) and glutamate synthetase (GOGAT) activities were higher in L. aequinoctialis. In particular, nitrate reductase activity (NRA) in L. aequinoctialis was 12.1 times as high as that in S. polyrhiza. These results showed that the two species responded varyingly to the types of nitrogen sources and their concentrations. Therefore, the difference in geographic distribution between the two species appeared to reflect the interspecific differences in enzyme activities and, subsequently, nitrogen absorption abilities.

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Participation of NMDA and non-NMDA glutamate receptors in the formalin-induced inflammatory temporomandibular joint nociception

  • Yang, Gwi-Y.;Lee, Ju-H.;Ahn, Dong-K.
    • International Journal of Oral Biology
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    • v.32 no.2
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    • pp.59-65
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    • 2007
  • It has been well known that excitatory amino acids, primarily glutamate, are involved in the transmission of nociception in pathological and physiological conditions in the spinal and brainstem level. Recently, peripheral glutamate also play a critical role in the peripheral nociceptive transmissions. The present study investigated the role of N-methyl-D-aspartic acid (NMDA) or non-NMDA ionotropic glutamate receptors in formalin-induced TMJ pain. Experiments were carried out on male Sprague-Dawley rats weighing 220-280 g. Intra-articular injection was performed under halothane anesthesia. Under anesthesia, AP-7 (10, $100\;{\mu}M$, $1\;mM/20\;{\mu}L$), a NMDA receptor antagonist, or CNQX disodium salt (0.5, 5, 50, $500\;{\mu}M/20\;{\mu}L$), a non-NMDA receptor antagonist, were administered intra-articularly 10 min prior to the application of 5% formalin. For each animal, the number of behavioral responses, such as rubbing and/or scratching the TMJ region, was recorded for nine successive 5-min intervals. Intra-articular pretreatment with 1 mM of AP-7 or $50\;{\mu}M$ CNQX significantly decreased the formalin-induced scratching behavioral responses during the second phase. Intra-articular pretreatment with $500\;{\mu}M$ of CNQX significantly decreased the formalin-induced scratching behavior during both the first and the second phase. These results indicate that the intra-articular administration of NMDA or non-NMDA receptor antagonists inhibit formalin-induced TMJ nociception, and peripheral ionotropic glutamate receptors may play an important role in the TMJ nociception.

Neuroprotective Effects of Extracts from Diospyros kaki L. Peel (단감(Diospyros Kaki L.)껍질 추출물의 신경세포 보호 효과)

  • Lee, Mi-Ra;Moon, Seong-Hee;Choi, Ae-Ran;Lee, Seung-Cheol;Ahn, Kwnag-Hwan;Park, Hae-Ryong
    • Korean journal of food and cookery science
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    • v.27 no.4
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    • pp.67-73
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    • 2011
  • This study was performed to assess the neuroprotective effects of methanolic extracts from sweet persimmon peel (PPE) against glutamate-induced cytotoxicity in hybridoma N18-RE-105 cells. The neuroprotective effects of PPE in N18-RE-105 cells were measured using the MTT reduction assay, LDH release assay, and phase-contrast microscopy. The results of the MTT reduction assay showed that treating cells with 500 ${\mu}g/ml$ PPE resulted in cell viability of 66.9%. Additionally, the morphological changes and the results of the LDH release assay showed that glutamate-induced damage to nerve cells was strongly inhibited by PPE. GSH content of N18-RE-105 cells was 3.5 ${\mu}M$ compared to that of the control, whereas pretreatment with 500 ${\mu}g/ml$ PPE increased GSH content by 4.7 ${\mu}M$. PPE was fractionated with hexane, and that layer had the highest neuroprotective effects in glutamate-stressed N18-RE-105 cells. In conclusion, our data showed that glutamate potentiated the effects of N18-RE-105 cell death by a mechanism involving oxidative stress. Therefore, PPE may be a potential candidate for prevention and therapy of neurodegenerative diseases.

Pigment and Monacolin K Content of Beni-koji Fermented with Soybean Curd Residue (비지홍국의 색소 및 Monacolin K 함량)

  • 윤은경;김영희;김순동
    • Food Science and Preservation
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    • v.10 no.3
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    • pp.360-364
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    • 2003
  • This study was conducted to investigate the preparation possibility of Beni-koji by Monascus pilosus using dried soybean curd residue(Biji). The additional effect of water(0-50%), glucose(0-10%, w/w), monosodium glutamate(0-0.l%, w/w) and citrus peel water extracts (0-0.5%, v/w) on the pigment and monacolin K content of the Biji Beni-koji were examined. Optimal added amounts of water was 20% of dried Biji. The highest pigment content(OD at 500 nm) of Biji Beni-koji was 1.06 in 10% glucose, 2.26 in 0.01% monosodium glutamate and 2.61 in 0.4% citrus peel water extracts. The content of monacolin K in the Biji Beni-koji added with 10% glucose, 0.01% monosodium glutamate and 0.4% citrus peel water extracts showed 96.38 mg%(w/w), 118.25 mg%(w/w) and 104.50 mg%(w/w), respectively.

Production of γ-Aminobutyric Acid Using Immobilized Glutamate Decarboxylase from Lactobacillus plantarum (Lactobacillus plantarum 유래 글루탐산 탈탄산효소의 고정화를 이용한 γ-aminobutyric acid의 생산)

  • Lee, Sang-Jae;Lee, Han-Seung;Lee, Dong-Woo
    • Microbiology and Biotechnology Letters
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    • v.43 no.3
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    • pp.300-305
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    • 2015
  • The glutamate decarboxylase gene (gadB) from Lactobacillus plantarum WCFS1 was cloned and expressed as an N-terminal hexa-histidine-tagged fusion protein in Escherichia coli BL21 (DE3) as the host strain. Purified glutamate decarboxylase (GAD) was immobilized onto porous silica beads by covalent coupling. The pH dependence of activity and stability of the immobilized GAD was significantly altered, when compared to those of the free enzyme. Immobilized GAD was stable in the range of pH 3.5 to 6.0. The resulting packed-bed reactor produced 41.7 g of γ-aminobutyric acid/l·h at 45℃.

Optimization of gamma-Aminobutyric Acid Bioconversion by Recombinant Escherichia coli (재조합 Escherichia coli를 이용한 gamma-Aminobutyric Acid 전환 반응 최적화)

  • Le Vo, Tam Dinh;Hong, Soon-Ho
    • KSBB Journal
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    • v.27 no.2
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    • pp.127-130
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    • 2012
  • In this study, the effects of pH, temperature, IPTG concentration and substrate (MSG) concentration on gamma-aminobutyric acid (GABA) production in engineered Escherichia coli were investigated. Glutamate decarboxylase and glutamate/GABA antiporter were overexpressed in GABA aminotransferase knock-out strain for GABA production. The result of optimization study showed the GABA bioconversion was optimized at pH 3.5, $30^{\circ}C$, 0.5 mM IPTG, 10 g/L MSG. At this condition, 5.23 g/L of final GABA concentration of was achieved from 10 g/L of MSG, which corresponded to a GABA yield of 85.77%.

Isolation and Characterization of Lactobacillus buchneri Strains with High ${\gamma}$-Aminobutyric Acid Producing Capacity from Naturally Aged Cheese

  • Park, Ki-Bum;Oh, Suk-Heung
    • Food Science and Biotechnology
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    • v.15 no.1
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    • pp.86-90
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    • 2006
  • Two lactic acid bacteria (LAB) with high ${\gamma}$-aminobutyric acid (GABA)-producing capacity were isolated from naturally aged cheese. Examination of the biochemical features using an API kit indicated that the two strains belonged to Lactobacillus. They were gram positive, rod-type bacteria, and fermented arabinose, melezitose, melibiose and xylose, but did not utilize cellobiose or trehalose. 16S rDNA sequencing analysis confirmed that they were Lactobacillus buchneri and Lactobacillus sp. They were accordingly named as Lactobacillus buchneri OPM-1 and Lactobacillus sp. OPM-2, and could produce GABA from MRS broth supplemented with 10 g/L of monosodium glutamate (MSG) at a productivity of 91.7 and 116.7 mg/L/hr, respectively. Cell extracts of L. buchneri OPM-1 and Lactobacillus sp. OPM-2 showed glutamate decarboxylase (GAD) activity, for which the optimum pH and temperature were 5.5 and $30^{\circ}C$, respectively.

Polymeric Micelle Formation of Multiblock Copolymer Composed of Poly( $\gamma$-benzyl L-glutamate) and Poly(ethylene oxide)

  • Na, Jae Un;Jeong, Yeong Il;Jo, Jong Su
    • Bulletin of the Korean Chemical Society
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    • v.21 no.4
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    • pp.383-388
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    • 2000
  • Multiblock copolymers consisting of poly( g-benzyl L-glutamate) (PBLG) as the hydrophobic part and poly(ethylene oxide) (PEO) as the hydrophilic part (GEG) were synthesized and characterized. GEG polymeric micelles were prepared by the dialysis technique. Particle size distributions based on intensity,volume, and number-average were 22.6 $\pm$ 11.9 nm, 23.5 $\pm$ 4.6 nm, and 23.7 $\pm$ 37 nm, respectively. It was observed that par-ticle size and size distribution of GEG polymeric micelles changed significantly with the choice of initial sol-vent. Transmission electron micrographs (TEM) showed the polymeric micelles to be spherically shaped, with sizes ranging from 20 nm to 40 nm in diameter. Fluorescence spectroscopy measurements suggested that GEG block copolymers wereassociated in water to form polymeric micelles, and the critical micelle concentrations (CMC) value of the block copolymers was 0.0094 g/L. Further evidenceof micelle formation of GEG block copolymers and limited mobility of the PBLG chain in the core ohe micelle was obtained with 1 H NMR in D2O.