• Title/Summary/Keyword: anti-convulsant activity

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Analysis of Studies on Pyeongwi-san to Establish the Fundament for Evidence Based Medicine (EBM 기반구축을 위한 평위산 전임상 연구 문헌 분석)

  • Kim, Jung-Hoon;Lee, Jun-Kyoung;Shin, Hyeun-Kyoo
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.24 no.5
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    • pp.770-778
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    • 2010
  • To establish the fundament for EBM of Traditional Korean Medicine, the papers on Pyeongwi-san (Pingwei-san) frequently used in medical institutions of Traditional Korean Medicine were analyzed through researching domestic and international papers. The papers were classified by the registration of domestic or international journals, the year of publishment, experimental fields and the kinds of studies on biological activities. Of total 518 papers on Pyeongwi-san (Pingwei-san), 32 volumes were selected according to selection creteria. 20 volumes were published in domestic journals, 11 in Chinese journal and 1 in Japanese journal. The papers on instrumental analyses reported the quantification of standard compounds of herbal medicines in Pyeongwi-san (Pingwei-san) using HPLC, GC-MS. The papers on biological activities of Pyeongwi-san (Pingwei-san) showed improvement of gastrointestinal activity and water-electrolyte metabolism, immune regulation, anti-oxidant, anti-inflammatory, analgesic, anti-convulsant activities, hypnotic duration, blood pressure regulation, hepatic protection, congestive heart failure, anti-cancer activities. Further studies including gastrointestinal activity need to be preceeded to establish the fundament for EBM of Pyeongwi-san (Pingwei-san).

A Study on the Synthesis of Nortropinone Derivatives

  • Jung, Dai-II;Park, Chil-Sung;Choi, Hak-Ki;Kim, Dong-Hee;Lee, Do-Hun;Jung, Il-Soo;Park, Yu-Mi;Choi, Soon-Kyu
    • Journal of Life Science
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    • v.9 no.1
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    • pp.81-83
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    • 1999
  • 2,4-Disubstituted nortropinone derivatives anticipated anticonvulsant activity were respectively synthesized by the reaction of N-substituted nortropinones, ethanol, 5N-NaOH and benzaldehyde ({TEX}$R_{1}${/TEX}CHO)

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Neuroprotective Effect of Taurine against Oxidative Stress-Induced Damages in Neuronal Cells

  • Yeon, Jeong-Ah;Kim, Sung-Jin
    • Biomolecules & Therapeutics
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    • v.18 no.1
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    • pp.24-31
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    • 2010
  • Taurine, 2-aminoethanesulfonic acid, is an abundant free amino acid present in brain cells and exerts many important biological functions such as anti-convulsant, modulation of neuronal excitability, regulation of learning and memory, anti-aggressiveness and anti-alcoholic effects. In the present study, we investigated to explore whether taurine has any protective actions against oxidative stress-induced damages in neuronal cells. ERK I/II regulates signaling pathways involved in nitric oxide (NO) and reactive oxygen species (ROS) production and plays a role in the regulation of cell growth, and apoptosis. We have found that taurine significantly inhibited AMPA induced cortical depolarization in the Grease Gap assays using rat cortical slices. Taurine also inhibited AMPA-induced neuronal cell damage in MTT assays in the differentiated SH-SY5Y cells. When the neuronal cells were treated with $H_2O_2$, levels of NO were increased; however, taurine pretreatment decreased the NO production induced by $H_2O_2$ to approximately normal levels. Interestingly, taurine treatment stimulated ERK I/II activity in the presence of AMPA or $H_2O_2$, suggesting the potential role of ERK I/II in the neuroprotection of taurine. Taken together, taurine has significant neuroprotective actions against AMPA or $H_2O_2$ induced damages in neuronal cells, possibly via activation of ERK I/II.

Synthesis and Anticonvulsant Evaluation of $N-Cbz-\alpha-amino-N-alkoxysuccinimides$

  • Byun, Aseun;Kim, Min-Jeong;Park, Jong-Won;Moon, Kyung-Ho;Lee, Chung-Kyu;Park, Min-Soo
    • Archives of Pharmacal Research
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    • v.27 no.3
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    • pp.273-277
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    • 2004
  • In previous studies for the development of new anticonvulsants, we found that N-Cbz-$\alpha$-amino-N-alkylsuccinimides exhibited significant anticonvulsant activities in the Maximal electroshock seizure (MES) and Pentylenetetrazole induced seizure (PTZ) tests, and also their anticonvulsant activities were dependent on the N-alkyl substituents existent in their structures. Based on these estimations, N-Cbz-$\alpha$-amino-N-hydroxysuccinimide and various N-Cbz-$\alpha$-amino-N-alkoxysuccinimides were prepared in order to develop more active anticonvulsants and to examine the effects of N-hydoxy or N-alkoxy groups on their anticonvulsant activities. The (R)-or (S)-N-Cbz-$\alpha$-amino-N-hydroxysuccinimide and N-Cbz-$\alpha$-amino-N-alkoxysuccinimides were prepared from the corresponding (R)-or (S)-N-Cbz-aspartic acid through the known synthetic procedures. Their anticonvulsant activities in the MES and PTZ test were evaluated. All of these compounds except 3a showed significant anticonvulsant activities against the PTZ test, but these compounds were not active in the MES test. The most active compound in the PTZ test was (R)-N-Cbz-$\alpha$-amino-N-benzyloxysuccinimide (ED$_{50}$=62.5 mg/kg). In addition, the anti-convulsant activities of these compounds were dependent on their N-substited groups. The order of anticonvulsant activity against the PTZ test, as judged from the ED50 values for (R) series was N-benzyloxy > N-hydroxy > N-isopropoxy > N-methoxy > N-ethoxy; for the (S) series N-ethoxy > N-benzyloxy > N-methoxy > N-isopropoxy.y.

Modulation of the Expression of the GABAA Receptor β1 and β3 Subunits by Pretreatment with Quercetin in the KA Model of Epilepsy in Mice -The Effect of Quercetin on GABAA Receptor Beta Subunits-

  • Moghbelinejad, Sahar;Rashvand, Zahra;Khodabandehloo, Fatemeh;Mohammadi, Ghazaleh;Nassiri-Asl, Marjan
    • Journal of Pharmacopuncture
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    • v.19 no.2
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    • pp.163-166
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    • 2016
  • Objectives: Quercetin is a flavonoid and an important dietary constituent of fruits and vegetables. In recent years, several pharmacological activities of quercetin, such as its neuroprotective activity and, more specifically, its anti-convulsant effects in animal models of epilepsy, have been reported. This study evaluated the role of quercetin pretreatment on gene expression of ${\gamma}$-amino butyric acid type A ($GABA_A$) receptor beta subunits in kainic acid (KA)-induced seizures in mice. Methods: The animals were divided into four groups: one saline group, one group in which seizures were induced by using KA (10 mg/kg) without quercetin pretreatment and two groups pretreated with quercetin (50 and 100 mg/kg) prior to seizures being induced by using KA. Next, the messenger ribonucleic acid (mRNA) levels of the $GABA_A$ receptor ${\beta}$ subunits in the hippocampus of each animal were assessed at 2 hours and 7 days after KA administration. Quantitative real-time polymerase chain reaction (RT-PCR) assay was used to detect mRNA content in hippocampal tissues. Results: Pretreatments with quercetin at doses of 50 and 100 mg/kg prevented significant increases in the mRNA levels of the ${\beta}_1$ and the ${\beta}_3$ subunits of the $GABA_A$ receptor at 2 hours after KA injection. Pretreatment with quercetin (100 mg/kg) significantly inhibited ${\beta}_1$ and ${\beta}_3$ gene expression in the hippocampus at 7 days after KA injection. But, this inhibitory effect of quercetin at 50 mg/kg on the mRNA levels of the ${\beta}_3$ subunit of the $GABA_A$ receptor was not observed at 7 days after KA administration. Conclusion: These results suggest that quercetin (100 mg/kg) modulates the expression of the $GABA_A$ receptor ${\beta}_1$ and ${\beta}_3$ subunits in the KA model of epilepsy, most likely to prevent compensatory responses. This may be related to the narrow therapeutic dose range for the anticonvulsant activities of quercetin.