• 제목/요약/키워드: NMDAR

검색결과 24건 처리시간 0.034초

The Memory-Enhancing Effects of Liquiritigenin by Activation of NMDA Receptors and the CREB Signaling Pathway in Mice

  • Ko, Yong-Hyun;Kwon, Seung-Hwan;Hwang, Ji-Young;Kim, Kyung-In;Seo, Jee-Yeon;Nguyen, Thi-Lien;Lee, Seok-Yong;Kim, Hyoung-Chun;Jang, Choon-Gon
    • Biomolecules & Therapeutics
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    • 제26권2호
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    • pp.109-114
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    • 2018
  • Liquiritigenin (LQ) is a flavonoid that can be isolated from Glycyrrhiza radix. It is frequently used as a tranditional oriental medicine herbal treatment for swelling and injury and for detoxification. However, the effects of LQ on cognitive function have not been fully explored. In this study, we evaluated the memory-enhancing effects of LQ and the underlying mechanisms with a focus on the N-methyl-D-aspartic acid receptor (NMDAR) in mice. Learning and memory ability were evaluated with the Y-maze and passive avoidance tests following administration of LQ. In addition, the expression of NMDAR subunits 1, 2A, and 2B; postsynaptic density-95 (PSD-95); phosphorylation of $Ca^{2+}$/calmodulin-dependent protein kinase II (CaMKII); phosphorylation of extracellular signal-regulated kinase 1/2 (ERK 1/2); and phosphorylation of cAMP response element binding (CREB) proteins were examined by Western blot. In vivo, we found that treatment with LQ significantly improved memory performance in both behavioral tests. In vitro, LQ significantly increased NMDARs in the hippocampus. Furthermore, LQ significantly increased PSD-95 expression as well as CaMKII, ERK, and CREB phosphorylation in the hippocampus. Taken together, our results suggest that LQ has cognition enhancing activities and that these effects are mediated, in part, by activation of the NMDAR and CREB signaling pathways.

인삼 품종별 뿌리 추출물의 NMDA 수용체 길항 효과 및 진세노사이드 함량 (N-Methyl-D-Aspartate (NMDA) Receptor Antagonistic Effect and Ginsenoside Content of Panax ginseng C. A. Meyer Cultivar Root Extracts)

  • 이승은;김장욱;정현수;최재훈;지윤정;김형돈;장귀영;현동윤;김동휘
    • 한국약용작물학회지
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    • 제28권1호
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    • pp.9-20
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    • 2020
  • Background: Although a number of Panax ginseng cultivars have been developed by Korean researchers in recent years, there has been insufficient analysis of their beneficial properties. In this study, we sought to identify useful ginseng varieties as functional materials. Methods and Results: We evaluated effects of root extracts of 10 ginseng cultivars (Cheongsun; CS, Chunpoong; CP, Gopoong; GP, Gumpoong; GMP, K1, Sunhyang; SH, Sunone; SO, Sunpoong; SP, Sunun; SU and Yunpoong; YP) against the inhibitory effects of nitric oxide (NO) and reactive oxygen species (ROS) production in mouse brain microglial BV2 cells, as well as the binding of N-methyl-D-aspartate receptor (NMDAR), a marker related to memory. Ginsenosides, such as 20 (S)-protopanaxadiols (PPDs), including ginsenoside-Rb1, -Rb2, -Rb3, -Rc, -Rd, and - Rg3 and 20 (S)-protopanaxatriols (PPTs) including -Re, -Rg1, and -Rg2 were analyzed by HPLC. We observed that the cultivar GMP showed the highest inhibitory effect (60.8%) against NO production at 20 ㎍/㎖. Those cultivars showing the significantly highest inhibition effects against ROS at 20 ㎍/㎖ were K1 (57.3%), SP (54.5%), YP (53.1%), CP (51.7%), CS (50.9%) and SH (49.6%). At 50 ㎍/㎖, K1 showed the most potent inhibitory effect (51.2%) on NMDAR binding. The total phenol content of SH (1.89 mg/g) and K1 (1.73 mg/g) were higher than those of the other cultivars, whereas in terms of PD/PT ratios, the values of CP (0.98), K1 (1.05) and SO (1.05) were lower than those of the other cultivars. On the basis of correlation coefficient (0.7064) between NMDAR inhibition and ONOO- scavenging activity. Conclusions: The findings of this study indicate that the cultivars K1 and SH could be useful ginseng resources as functional materials with favorable cognition-improving and antioxidative properties.

Facilitation of AMPA receptor-mediated steady-state current by extrasynaptic NMDA receptors in supraoptic magnocellular neurosecretory cells

  • Pai, Yoon Hyoung;Lim, Chae Seong;Park, Kyung-Ah;Cho, Hyun Sil;Lee, Gyu-Seung;Shin, Yong Sup;Kim, Hyun-Woo;Jeon, Byeong Hwa;Yoon, Seok Hwa;Park, Jin Bong
    • The Korean Journal of Physiology and Pharmacology
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    • 제20권4호
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    • pp.425-432
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    • 2016
  • In addition to classical synaptic transmission, information is transmitted between cells via the activation of extrasynaptic receptors that generate persistent tonic current in the brain. While growing evidence supports the presence of tonic NMDA current ($I_{NMDA}$) generated by extrasynaptic NMDA receptors (eNMDARs), the functional significance of tonic $I_{NMDA}$ in various brain regions remains poorly understood. Here, we demonstrate that activation of eNMDARs that generate INMDA facilitates the ${\alpha}$-amino-3-hydroxy-5-methylisoxazole-4-proprionate receptor (AMPAR)-mediated steady-state current in supraoptic nucleus (SON) magnocellular neurosecretory cells (MNCs). In $low-Mg^{2+}$ artificial cerebrospinal fluid (aCSF), glutamate induced an inward shift in $I_{holding}$ ($I_{GLU}$) at a holding potential ($V_{holding}$) of -70 mV which was partly blocked by an AMPAR antagonist, NBQX. NBQX-sensitive $I_{GLU}$ was observed even in normal aCSF at $V_{holding}$ of -40 mV or -20 mV. $I_{GLU}$ was completely abolished by pretreatment with an NMDAR blocker, AP5, under all tested conditions. AMPA induced a reproducible inward shift in $I_{holding}$ ($I_{AMPA}$) in SON MNCs. Pretreatment with AP5 attenuated $I_{AMPA}$ amplitudes to ~60% of the control levels in $low-Mg^{2+}$ aCSF, but not in normal aCSF at $V_{holding}$ of -70 mV. $I_{AMPA}$ attenuation by AP5 was also prominent in normal aCSF at depolarized holding potentials. Memantine, an eNMDAR blocker, mimicked the AP5-induced $I_{AMPA}$ attenuation in SON MNCs. Finally, chronic dehydration did not affect $I_{AMPA}$ attenuation by AP5 in the neurons. These results suggest that tonic $I_{NMDA}$, mediated by eNMDAR, facilitates AMPAR function, changing the postsynaptic response to its agonists in normal and osmotically challenged SON MNCs.

Neuronal Activity-Dependent Regulation of MicroRNAs

  • Sim, Su-Eon;Bakes, Joseph;Kaang, Bong-Kiun
    • Molecules and Cells
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    • 제37권7호
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    • pp.511-517
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    • 2014
  • MicroRNAs are non-coding short (~23 nucleotides) RNAs that mediate post-transcriptional regulation through sequence-specific gene silencing. The role of miRNAs in neuronal development, synapse formation and synaptic plasticity has been highlighted. However, the role of neuronal activity on miRNA regulation has been less focused. Neuronal activity-dependent regulation of miRNA may finetune gene expression in response to synaptic plasticity and memory formation. Here, we provide an overview of miRNA regulation by neuronal activity including high-throughput screening studies. We also discuss the possible molecular mechanisms of activity-dependent induction and turnover of miRNAs.

생후 7일, 16일된 circling mouse 청각 뇌줄기에서 N-메틸-D 아스파르트산염 수용체(NMDA receptor)에 대한 면역염색학적 분포 (Immunohistochemical Localization of NMDA Receptor in the Auditory Brain Stem of Postnatal 7, 16 Circling Mouse)

  • 최인영;박기섭;김혜진;디라즈 마스키;김명주
    • Applied Microscopy
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    • 제40권2호
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    • pp.53-64
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    • 2010
  • 글루타메이트 수용체는 신경연접의 발달에서 신경연접과 정제 등에 중요한 역할을 한다. 포유류 청각뇌줄기의 가쪽위올리브 핵-안쪽마름섬유체핵 신경연접에서의 흥분성 신경전달물질의 전달은 글루타메이트와 같은 많은 흥분성 신경전달물질의 전달을 조절하므로 발생학적 연구에 매우 유용한 모델이다. 귀먹음은 흥분성 회로 또는 억제성 회로의 신경연접에서 신경전달물질들의 변화뿐 아니라 형태학적 변화도 초래하게 된다. 이런 이유로 선천적으로 태어나면서 달팽이 기관이 퇴화되는 선회생쥐는 귀먹음의 병태생리를 연구하는데 가장 좋은 동물모델이다. 그러나, 선회생쥐에서 이런 NMDA 수용체 각각의 아형들이 발달에 따라 어떻게 나타나는지에 관해서는 거의 알려진 사실이 없다. 따라서, 본 연구에서는 선천적으로 속귀에 돌연변이를 가진 선회생쥐를 이용하여 면역조직화학염색법으로 생후 7일과 16일의 쥐를 정상쥐와 비교해서 글루타메이트성의 흥분성 신호가 전달되는 청각뇌줄기의 가쪽위올리브핵(LSO)에서 N-메틸-D-아스파르 트산염(NMDA) 수용체의 아형인 NR1, NR2A, NR2B의 분포를 각각 조사하였다. 생후 7일째 선회생쥐의 NR1에 대한 면역반응성의 세기는 정상군에서 $128.67\pm8.87$로 나타났고 이형접합체에서는 $111.06\pm8.04$, 동형접합체에서는 $108.09\pm5.94$으로 나타났다. 그리고 생후 16일째 선회생쥐에서는 정상군에서 $43.83\pm10.49$, 이형접합체에서는 $40\pm13.88$, 동형접합체에서는 $55.96\pm17.35$으로 나타났다. 생후 7일째 선회생쥐의 NR2A에 대한 면역반응성의 세기는 정상군에서 $97.97\pm9.71$, 이형접합체에서 $102.87\pm9.30$, 동형접합체에서 $106.85\pm5.79$로 나타났다. 생후 16일 선회생쥐의 가쪽위올리브핵에서의 NR2A에 대한 면역반응성 세기는 정상군에서 $47.4\pm20.6$, 이형접합체에서 $43.9\pm17.5$, 동형접합체에서 $49.2\pm20.1$로 나타났다. 생후 7일의 선회생쥐의 NR2B의 면역반응성 세기는 정상군에서 $109.04\pm6.77$, 이형접합체에서 $106.43\pm10.24$, 동형접합체에서 $105.98\pm4.10$으로 나타났다. 생후 16일째 선회생쥐의 NR2B의 면역반응성의 세기는 정상군에서 $101.47\pm11.50$, 이형접합체에서 $91.47\pm14.81$, 동형접합체에서 $93.93\pm15.71$으로 나타났다. 이 결과들은 생후 7일과 16일의 선회생쥐의 가쪽위올리브핵에서 NMDA 수용체의 면역반응성의 변화를 나타낸 것으로 인간 귀먹음의 주요한 병태생리를 파악하는 데 기본적인 자료를 제시할 수 있을 것이다.

칼슘 저해제가 전침자극에 의한 척수 N-Methyl-D-Aspartate 수용체 인산화에 미치는 영향 (Effect of Intracellular Calcium Chelator on Phosphorylation of Spinal N-Methyl-D-Aspartate Receptor following Electroacupuncture Stimulation in Rats)

  • 정택근;조성우;강연경;장동호;이인선
    • 한방재활의학과학회지
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    • 제20권1호
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    • pp.27-36
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    • 2010
  • 목 적 : 본 연구는 전침 자극에 의한 척수내 N-methyl-D-aspartate(NMDA) 수용체의 NR1 및 NR2B subunit 인산화에 미치는 세포내 칼슘 저해제 bis-(2-aminophenoxy)-ethane-N,N,N',N'-tetraaceticacid(BAPTA)의 영향을 조사하였다. 방 법 : 인체의 족삼리(足三里)(ST36)와 삼음교(三陰交)(SP6)에 해당하는 혈자리에 2 Hz전침 자극을 1.0mA 세기로 30분 동안 자극하였다. 결 과 : 전침 무통각을 측정한 결과 높은 농도의 BAPTA 복강내주사 처리군에서 저하가 관찰되었다. 전침 처치 후 60분 후 분리한 $L_{4-5}$ 척수 분절에서 C-fos 발현 신경세포 수는 BAPTA 처리에 의해 감소하는데 특히 고유핵에서 저하가 현저하였다. 평균 integrated optical density로 비교한 NR1과 NR2B subunit에 대한 면역조직화학적 발현을 보면 전침 자극은 정상군에 비해 얕은 층판에서 증가하였다. NR1과 NR2B subunit의 인산화형에 대한 발현을 보면 NR1 인산화형은 척수 배각 전 부위에서, NR2B 인산화형은 얕은 층판에서 증가하였으며 BAPTA 처리에 의해 NR1 인산화형은 얕은 층판과 목 부위에서 NR2B 인산화형은 얕은 층판에서 현저한 감소를 보였다. western blot로 살펴본 BAPTA 처리에 의한 NR1 및 NR2B 인산화형 변화는 면역조직화학적 방법과 유사한 결과를 보여 주었다. 결 론 : 전침 무통각은 세포내 칼슘에 의한 척수 내 NMDA 수용체의 인산화가 중요한 요인으로 작용할 가능성이 있다.

Neuronal injury in AIDS dementia: Potential treatment with NMDA open-channel blockers and nitric oxide-related species

  • Lipton, Stuart A.
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1996년도 춘계학술대회
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    • pp.19-29
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    • 1996
  • The neurological manifestations of AIDS include dementia, encountered even in the absence of opportunistic superinfection or malignancy. The AIDS Dementia Complex appears to be associated with several neuropathological abnormalities, including astrogliosis and neuronal injury or loss. How can HIV-1 result in neuronal damage if neurons themselves are only rarely, if ever, infected by the vitus\ulcorner In vitro experiments from several different laboratiories have lent support to the existence of HIV- and immune-related toxins. In one recently defined pathway to neuronal injury, HIV-infected macrophages/microglia as well as macrophages activated by HIV-1 envelope protein gp120 appear to secrete excitants/neurotoxins. These substances may include arachidonic acid, platelet-activating factor, free radicals (NO - and O$_2$), glutamate, quinolinate, cysteine, cytokines (TNF-${\alpha}$, IL1-B, IL-6), and as yet unidentified factors emanating from stimulated macrophages and possibly reactive astrocytes. A final common pathway for newonal suscepubility appears to be operative, similar to that observed in stroke, trauma, epilepsy, and several neurodegenerative diseases, including Huntington's disease, Parkinson's disease, and amyotrophic lateral sclerosis. This mechanism involves excessive activation of N-methyl-D-aspartate (NMDA) receptor-operated channels, with resultant excessive influx of Ca$\^$2+/ leading to neuronal damage, and thus offers hope for future pharmacological intervention. This chapter reviews two clinically-tolerated NMDA antagonists, memantine and nitroglycerin; (ⅰ) Memantine is an open-channel blocker of the NMDA-associated ion channel and a close congener of the anti-viral and anti-parkinsonian drug amantadine. Memantine blocks the effects of escalating levels of excitotoxins to a greater degree than lower (piysiological) levels of these excitatory amino acids, thus sparing to some extent normal neuronal function. (ⅱ) Niuoglycerin acts at a redox modulatory site of the NMDA receptor/complex to downregulate its activity. The neuroprotective action of nitroglycerin at this site is mediated by n chemical species related to nitric oxide, but in a higher oxidation state, resulting in transfer of an NO group to a critical cysteine on the NMDA receptor. Because of the clinical safety of these drugs, they have the potential for trials in humans. As the structural basis for redox modulation is further elucidated, it may become possible to design even better redox reactive reagents of chinical value. To this end, redox modulatory sites of NMDA receptors have begun to be characterized at a molecular level using site-directed mutagenesis of recombinant subunits (NMDAR1, NMDAR2A-D). Two types of redox modulation can be distinguished. The first type gives rise to a persistent change in the functional activity of the receptor, and we have identified two cysteine residues on the NMDARI subunit (#744 and #798) that are responsible for this action. A second site, presumably also a cysteine(s) because <1 mM N-ethylmaleimide can block its effect in native neurons, underlies the other, more transient redox action. It appears to be at this, as yet unidentified, site on the NMDA receptor that the NO group acts, at least in recombinant receptors.

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감초 육성품종 뿌리 추출물의 In vitro 활성 평가 (Evaluation of the In vitro Activity of Glycyrrhiza Cultivar Roots)

  • 이승은;이정훈;박춘근;김형돈;이윤지;서경혜;정현수;장재기;김동휘
    • 한국약용작물학회지
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    • 제27권2호
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    • pp.115-125
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    • 2019
  • Background: Glycyrrhiza radix (licorice root) have been used as an oriental medicine material for long time, and its protective effects on oxidative stress, inflammation and cognition deficit have been recently reported. However, the cultivation of Glycyrrhiza species as medicinal crops is associated with some problems such as low productivity and early leaf fall, etc. To resolve this problems, Glycyrrhiza cultivars have been developed by direct hybridization of each Glycyrrhiza species by Korean researchers. The present study was conducted to compare the Glycyrrhiza cultivar radix (Dagam, Sinwongam and Wongam) for their anti-oxidation, anti-inflammation, and cognition improvement effects and levels of liquiritin, isoliquiritigenin and licochalcone in order to select an excellent cultivar as a material resource. Methods and Results: For evaluating the inhibitory efficacies of the Glycyrrhiza cultivar extracts on oxidative stress and inflammation in BV2 cells, we measured their reactive oxygen species (ROS) production and nitric oxide (NO) release after treating them with lipopolysccharide. The scavenging activities on 2,2-diphenyl-1-picrylhydrazyl (DPPH) and peroxynitrite ($NOO^-$) radicals were evaluated. Cell proliferation and N-methyl-D-aspartate receptor (NMDAR) inhibition were analyzed. The total phenol, liquiritin, isoliquiritigenin and licochalcone A content in the extracts of the three culivars were quantified. Furthermore, the correlation coefficient between the activities and contents of total phenol, liquiritin, isoliquiritigenin and licochalcone A were also calculated. The results indicated that Sinwongam exhibited potent anti-oxidant, anti-inflammatory and NMDAR inhibititory activities. Sinwongam also showed higher total phenol and licochalcone A contents than the other cultivars. Among the three cultivars, Dagam exhibited a positive effects on NO release inhibition, cell proliferation and contents of liquiritin and isoliquiritigenin. Conclusions: Sinwongam is expected to be the most useful resource as a functional material for anti-oxidation/anti-inflammation and cognition improvement among the three studied licorice cultivars.

트레드밀 운동이 노화 흰쥐 소뇌의 성상세포 활성과 퍼킨제 세포 및 운동기능 변화에 미치는 영향 (Effects of Treadmill Exercise on Cerebellar Astrocyte Activation and Purkinje Cell, and Motor Function in Aged Rats)

  • 이효철;김형준
    • 한국체육학회지인문사회과학편
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    • 제58권4호
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    • pp.481-492
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    • 2019
  • 본 연구는 12주간의 트레드밀 운동이 노화 흰쥐 소뇌의 성상세포 활성과 퍼킨제 세포 발현 및 운동기능 변화에 미치는 영향에 대해 알아보았다. Sprague-Dawley(SD) 흰쥐를 실험처치에 따라 (1)젊은 통제집단 (Young Control Group; YCG; 3months aged; n=10), (2) 노화 통제집단 (Old Control Group; OCG; 24months aged; n=10), (3) 노화 운동집단 (Old Exercise Group; OEG; 24months aged; n=10)으로 구분한 후 OEG는 트레드밀 운동을 시간과 강도를 점증적으로 증가하여 12주간, 주 5회 실시하였다. 실험결과 rota-rod 검사에서 운동기능이 OCG에 비해 OEG에서 증가하는 것으로 나타났으며(p<.05) 그 수준은 YCG와 유사한 것으로 나타났다. calbindin-양성 퍼킨제 세포의 발현도 OCG에 비해 OEG의 소뇌 충부에서 증가하였으며(p<.05), 그 수준은 YCG와 유사하였다. GFAP-, NMDAR-양성세포의 발현도 OEG에서 증가하였다(각각 p<.001). GFAP, GLAST 단백질 수준은 OCG에 비해 OEG에서 증가하였으며(p<.05, p<.001) 그 수준은 YCG와 유사하였다. BDNF, NGF 수준은 YCG에서 가장 높았으며 OCG에 비해 OEG에서 증가하는 것으로 나타났다(p<.001, p<.05). 이상의 결과를 종합하면 규칙적인 운동은 성상세포의 활성을 향상시킬 뿐만 아니라 신경영양인자의 증가를 통하여 소뇌의 퍼킨제 세포 발현과 운동기능을 개선시키는 것으로 판단된다.