• 대한약리학회지
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• 제18권1호
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• pp.17-22
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• 1982

Zizyphus seed(Zizyphus vulgaris Lamark var. Spinosus Bunge) has long been used as hypnotics and sedatives in oriental medicine, and it is reported that the Zizyphus seed elicited a variety of pharmacologic actions besides CNS depression. Present study was undertaken to investigate the effects of Zizyphus seed on the central nervous system and on the blood pressure. The effect of Zizyphus seed on the central nervous system was measured by the influence of thiopental sleeping time and by inhibition of chemical convulsion (strychnine and pentylenetetrazol induced). Blood pressure changes by Zizyphus extract and its mode of action were investigated. The ground Zizyphus seed was extracted with hexane and methanol, consecutively and the supernatants were discarded. The precipitate was re-extracted with distilled water and the supernatant was evaporated to a dark-brownish sticky liquid, which was used as Zizyphus seed extract in this study after dissolving in saline prior to experiment. The results are as follows. 1) Zizyphus seed extract caused marked prolongation of the thiopental sleeping time in mice. 2) The chemical convulsion by strychnine and pentylenetetrazol, and the mortality by them in chicks were not affected by pretreatment of Zizyphus seed extract. 3) Zizyphus seed extract produced transient fall of blood pressure in the cat, and this hypotentive effect was blocked partially by atropine but not affected by bilateral vagotomy and/or hexamethonium, nor propranolol and, chlorpheniramine and/or cimetidine. With the above results, it may be suggested that the water extract of Zizyphus seeds contains components producing CNS depression and hypotension. Furthermore it is felt that the cholinergic effect, but not the adrenergic or histaminergic, is partly responsible for the hypotensive effect of Zizyphus seed extract.

• Child Health Nursing Research
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• 제22권4호
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• pp.379-389
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• 2016

Purpose: A longitudinal study was conducted to explore flora colonization and oral glucose high-risk newborns during the first 7 days after birth. Methods: Oral secretions of hospitalized newborns were obtained for microbial cultures and glucose test at days 1-7 after birth. Results: Among the total 112 newborns, 40% were girls and 73% were premature. Mean gestational age was $34.4{\pm}3.2$ weeks and weight was $2,266{\pm}697.5$ grams. The most common flora included Streptococcus (28.2%), Methicillin-resistant Staphylococcus aureus (MRSA, 10.9%), Staphylococcus (6.0%) and Coagulase-Negative Staphylococcus (CNS, 4.0%). The average oral glucose level was $29.2{\pm}23.0mg/dL{\sim}58.2{\pm}39.5mg/dL$. Newborns with higher oral glucose than serum (crude odds ratio [ORc] =1.75; 95% confidence interval [CI] =1.03-2.97), phototherapy (ORc=3.30; 95% CI=2.29-4.76) and prone position (ORc= 2.04; 95% CI=1.13-3.69) were more likely to be colonized. Having oral tubes (ORc=0.42; 95% CI=0.29-0.59), parental nutrition (ORc=0.21; 95% CI=0.13-0.32) and antibiotics (ORc=0.51; 95% CI=0.36-0.73) had protective effects. For oral glucose statistical significances existed on time effect among newborns with Streptococcus (F=9.78, p=.024), MRSA (F=7.60, p=.037) or CNS (F=11.15, p=.019) and interaction between time and colonization among newborns with all of four flora (F=2.73, p=.029) or colonization with only Staphylococcus (F=2.91, p=.034). Conclusion: High-risk newborns develop flora colonization at an early period of life. Their clinical features were associated with types and time of oral flora colonization. They need close monitoring and multifaceted intervention to improve oral environment and infection control.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1998년도 Proceedings of UNESCO-internetwork Cooperative Regional Seminar and Workshop on Bioassay Guided Isolation of Bioactive Substances from Natural Products and Microbial Products
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• pp.143-143
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• 1998

Antagonists acting at the glycine site of the NMDA receptor have been gaining safer alternatives for stroke therapy because they have few adverse effect competitive and noncompetitive NMDA antagonists. Therefore, the neuroprotect novel glycine site antagonist KC0244 were evaluated in a rat model of transient comparison with GV150526A in a developmental phase. Middle cerebral artery oc was produced by insertion of a silicone-coated 4-0 nylon monofilament to the o in male Sprague-Dawley rats under isoflurane anesthesia. After 90 or 120 min retracted and the ischemic tissue reperfused. In 90-min MCAO model, GV150526A was administered 30 min before MCAO or immediately after MCAO. In 120-min MC KC0244 or GV150526A (10 mg/kg, i.p.) was administered 1 hr before MCAO or imme MCAO. Infarct volume was measured 24 hr after MCAO using the 2,3,5-triphe chloride staining method. In 90-min MCAO model, treatments with GV1505 significantly reduce infarct volume although they tended to slightly reduce cor approximately 19% compared with the nontreated group. In 120-min MCAO model with GV150526A did not either significantly reduce infarct volume although the reduce total infarct volume by approximately 16% compared with the vehicle-tre However, 1-hr preischemic and immediate treatments with KC0244 reduced total i 39 and 30% (corrected total infarct volume by 44 and 32%), respectively, co vehicle-treated control group. The results suggest that KC0244 can provid against transient focal ischemic damage with greater in vivo potency than GV150

• 생약학회지
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• 제48권1호
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• pp.31-37
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• 2017

Glutamate-induced oxidative stress results in neuro-degenerative disorders in many central nervous system (CNS) such as Alzheimer's disease, ischemia, Huntington's disease, and Parkinson's disease. Our study was performed to investigate neuroprotective effects of Allium hookeri extracts (leaf, root, and whole) on glutamate-induced HT22 cells. In this study, ethanol extract of A. hookeri showed the outstanding neuroprotective effect in HT22 cells. In addition, we found that ethanol extract of A. hookeri root increased heme oxygenase (HO)-1 in HT22 cells. Moreover, ethanol extract of A. hookeri root also upregulated nuclear accumulation of nuclear factor E2-related factor 2 (Nrf2) in HT22 cells. These results demonstrate that ethanol extract of A. hookeri root contributes neuroprotective effects against glutamate-induced oxidative stress in HT22 cells, via Nrf2-mediated HO-1 expression. Our study suggests that ethanol extract of A. hookeri root could be the potential agent for the treatment of many neuro-degenerative diseases.

• 대한약리학회지
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• 제5권2호
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• pp.87-92
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• 1969

The effects of dephenylhydantoin, strychnine, coramine, d-amphetamine and chlorpromazine on $QO_2$ and non-inulin space $Na^+$, $K^+$ concentration of rat cerebral cortical slices incubated in pH 7.4 glycylglycine glucose saline was investigated. In general, there are decreased non-inulin space $Na^+$ concentration or increased non-inulin space $K^+$ concentration or both when the ratio of respiration to non-inulin space is greater than control group except in case of chlorpromazine $10^{-4}\;M$. And it is suggested that the ratio of respiration to non-inulin space is responsible more closely for the non-inulin space Na, K concentration than $QO_2$ expressed per tissue wet weight. Effects of diphenylhydantoin and several other agents on electrolytes and the electroshock seizure threshold are discussed.

• Biomolecules & Therapeutics
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• 제21권2호
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• pp.107-113
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• 2013

Plasminogen activator inhibitor-1 (PAI-1) is a member of serine protease inhibitor family, which regulates the activity of tissue plasminogen activator (tPA). In CNS, tPA/PAI-1 activity is involved in the regulation of a variety of cellular processes such as neuronal development, synaptic plasticity and cell survival. To gain a more insights into the regulatory mechanism modulating tPA/PAI-1 activity in brain, we investigated the effects of proteasome inhibitors on tPA/PAI-1 expression and activity in rat primary astrocytes, the major cell type expressing both tPA and PAI-1. We found that submicromolar concentration of MG132, a cell permeable peptide-aldehyde inhibitor of ubiquitin proteasome pathway selectively upregulates PAI-1 expression. Upregulation of PAI-1 mRNA as well as increased PAI-1 promoter reporter activity suggested that MG132 transcriptionally increased PAI-1 expression. The induction of PAI-1 downregulated tPA activity in rat primary astrocytes. Another proteasome inhibitor lactacystin similarly increased the expression of PAI-1 in rat primary astrocytes. MG132 activated MAPK pathways as well as PI3K/Akt pathways. Inhibitors of these signaling pathways reduced MG132-mediated upregulation of PAI-1 in varying degrees and most prominent effects were observed with SB203580, a p38 MAPK pathway inhibitor. The regulation of tPA/PAI-1 activity by proteasome inhibitor in rat primary astrocytes may underlie the observed CNS effects of MG132 such as neuroprotection.

• 터널과지하공간
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• 제17권3호
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• pp.203-215
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• 2007

암반의 역학적 변형거동과 안정성은 불연속면의 역학적 특성에 크게 좌우되기 때문에 터널이나 암반구조물의 안정성 해석 및 설계를 위해서는 반드시 암반 불연속면의 역학적 성질을 규명할 필요가 있다. 지하암반 절리면의 실제 거동을 실내에서 정확히 모사하기 위해 본 연구에서는 일련의 일정 수직강성 조건하 직접 전단시험을 수행하여 초기 수직응력, 전단속도 그리고 절리면의 거칠기가 거친 화강암 절리면의 전단거동특성에 미치는 영향을 살펴보았다. 일정 수직강성 조건에서 거친 암석절리에 대한 시험 결과 전단거동은 일반적으로 1차 정점 전단응력에서의 전단응력 감소 정도에 따라 크게 두 가지 형태의 전단거동을 보이는 것으로 구분되었다. 초기 수직응력이 증가함에 따라 정점 전단변위와 1차 정점 전단응력은 증가하지만 마찰각과 정점 마찰계수의 경우 감소하는 것으로 나타났으며, 전단강성과 평균마찰계수의 경우는 초기 수직응력에 영향을 받지 않는 것으로 나타났다. 거친 절리에 대한 전단속도의 영향은 초기 수직응력이 낮은 경우 일부 전단변수들에서 약간 관찰되었으나 수직응력이 증가함에 따라 대부분의 전단시험 결과변수들에서 전단속도의 영향은 미미하였다. 거칠기에 따른 전단거동의 변화를 분석하였으나 명확한 관련성이 나타나는 경우보다 시료간의 편차가 심한 경우가 많았다.

• Journal of Ginseng Research
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• 제37권4호
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• pp.401-412
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• 2013

Korean Red Ginseng (KRG) is an oriental herbal preparation obtained from Panax ginseng Meyer (Araliaceae). To expand our understanding of the action of KRG on central nervous system (CNS) function, we examined the effects of KRG on tissue plasminogen activator (tPA)/plasminogen activator inhibitor-1 (PAI-1) expression in rat primary astrocytes. KRG extract was treated in cultured rat primary astrocytes and neuron in a concentration range of 0.1 to 1.0 mg/mL and the expression of functional tPA/PAI-1 was examined by casein zymography, Western blot and reverse transcription-polymerase chain reaction. KRG extracts increased PAI-1 expression in rat primary astrocytes in a concentration dependent manner (0.1 to 1.0 mg/mL) without affecting the expression of tPA itself. Treatment of 1.0 mg/mL KRG increased PAI-1 protein expression in rat primary astrocytes to $319.3{\pm}65.9%$ as compared with control. The increased PAI-1 expression mediated the overall decrease in tPA activity in rat primary astrocytes. Due to the lack of PAI-1 expression in neuron, KRG did not affect tPA activity in neuron. KRG treatment induced a concentration dependent activation of PI3K, p38, ERK1/2, and JNK in rat primary astrocytes and treatment of PI3K or MAPK inhibitors such as LY294002, U0126, SB203580, and SP600125 (10 ${\mu}M$ each), significantly inhibited 1.0 mg/mL KRG-induced expression of PAI-1 and down-regulation of tPA activity in rat primary astrocytes. Furthermore, compound K but not other ginsenosides such as Rb1 and Rg1 induced PAI-1 expression. KRG-induced up-regulation of PAI-1 in astrocytes may play important role in the regulation of overall tPA activity in brain, which might underlie some of the beneficial effects of KRG on CNS such as neuroprotection in ischemia and brain damaging condition as well as prevention or recovery from addiction.

• 생명과학회지
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• 제21권6호
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• pp.796-804
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• 2011

본 연구에서는 파의 항염증 효과를 밝히고 그 생화학적 기전 해석을 위해 LPS로 활성화된 BV2 microglia를 이용하여 iNOS, COX-2 및 염증성 cytokine의 발현 및 그 산물에 미치는 파 추출물의 영향을 조사하였다. 그 결과 파 추출물은 LPS 처리에 의한 BV2 세포의 iNOS의 발현을 전사 및 번역 수준에서 처리 농도 의존적으로 억제시켰으며, 특히 파 전체 에탄올 추출물(EEWA)의 효과가 가장 탁월하였다. LPS로 유도한 COX-2의 mRNA 및 단백질 발현 역시 파 추출물 처리에 의하여 감소되었으며 뿌리 에탄올 추출물(EERA) 처리군에서 가장 현저한 억제가 관찰되었다. 아울러 염증 반응의 또 다른 주요인자인 염증성 cytokine들(TNF-${\alpha}$, IL-$1{\beta}$ 및 IL-6)의 mRNA 변화를 조사한 결과 파 추출물이 대체적으로 이들 cytokine의 발현을 억제하는 경향을 보였으며, 최종산물인 TNF-${\alpha}$와 IL-6의 생성량 역시 유의한 수준은 아니었으나 감소하는 경향을 보였다. 본 연구의 결과는 파의 추출물은 iNOS, COX-2 및 염증성 cytokine의 발현을 조절함으로서 신경염증 반응을 효과적으로 억제하며, 향후 지속적인 연구가 필요하지만 신경 보호 작용에 탁월한 효능이 있음을 보여주는 것으로 생각된다.

• Natural Product Sciences
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• 제13권3호
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• pp.268-271
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• 2007

Glutamate-induced oxidative injury contributes to neuronal degeneration in many central nervous system (CNS) diseases, such as epilepsy and ischemia. Bioassay-guided fractionation of the MeOH extract of the seeds of Alpinia katsumadai Hayata (Zingiberaceae) furnished three phenolic compounds, alpinetin (1), pinocembrin (2), and (+)-catechin (3). Compounds 2 and 3 showed the potent neuroprotective effects on glutamate-induced neurotoxicity and reactive oxygen species (ROS) generation in the mouse hippocampal HT22 cells. In addition, Compounds 2 and 3 showed significant DPPH free radical scavenging effect. These results suggest that compounds 2 and 3 could be the effective candidates for the treatment of ROS-related neurological diseases.