• 동의신경정신과학회지
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• 제10권2호
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• pp.85-103
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• 1999

In order to prove the anticonvulsive effect of the fragrance of Magnoliae Flos in convulsion-induced mice, experiments were performed on anticonvulsive effect, GABA level, glutamic acid level, GABA-T activity and GAD activity. The results were obtained as follows: 1. As far as anticonvulsive effect was concerned, on the convulsion induced by such as maximal electric seizure, strychnine, bicuculline, or picrotoxin it was not significant, but the convulsion induced by pentylenetetrazole it was significant comparing to the control group. 2. GABA level was increased significantly in mice. 3. Glutamic acid level was decreased significantly in mice. 4. GABA-T activity was decreased by the fragrance of Magnoliae Flos. 5. The fragrance of Magnoliae Flos was not effective in GAD activity. From above result, the fragrance of Magnoliae Flos had significant effects on convulsion induced by pentylenetetrazole, so it is expected to clinical application on convulsive diseases such as epilepsy.

• 동의신경정신과학회지
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• 제18권3호
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• pp.83-95
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• 2007

This study was performed to examine the anticonvulsant effects of the extracts of JeongGan-Tang and explanation of its action mechanism. Method: 1) The inhibitory effect on convulsions induced by pentylenetetrazole, picrotoxin and strychnine was investigated in vivo 2) The inhibitory effect on GABA transaminase activity was evaluated in vivo and in vitro. 3) The brain GABA level and glutamate level in pentylenetetrazole-induced convulsion model were analyzed by HPLC, Results: 1) JeongGan-Tang showed the significant effect on the pentylenetetrazole-induced convulsion, which may mean that its anticonvulsant effect would be resulted from the activation of GABA receptor and chloride channel rather than the presynaptic- or postsynaptic inhibition. 2) JeongGan-Tang exhibited proper inhibitory activity on GABA transaminase in vitro and in vivo. 3) JeongGan-Tang increased the brain GABA level but did not affect the brain glutamate content, which may suggest that this drug supresses the convulsion by increase of GABA, an inhibitory neurotransmitter. Conclusion : JeongGan-Tang can be used as an anticonvulsant prescription by the modulation of GABAergic neurotramission.

• BMB Reports
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• 제53권9호
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• pp.484-489
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• 2020

Epilepsy is a neurological disorder characterized by unpredictable seizures, which are bursts of electrical activity that temporarily affect the brain. Cereblon (CRBN), a DCAFs (DDB1 and CUL4-associated factors), is a well-established protein associated with human mental retardation. Being a substrate receptor of the cullin-RING E3 ubiquitin ligase (CRL) 4 complex, CRBN mediates ubiquitination of several substrates and conducts multiple biological processes. In the central nervous system, the large-conductance Ca²⁺-activated K⁺ (BK_Ca) channel, which is the substrate of CRBN, is an important regulator of epilepsy. Despite the functional role and importance of CRBN in the brain, direct injection of pentylenetetrazole (PTZ) to induce seizures in CRBN knock-out mice has not been challenged. In this study, we investigated the effect of PTZ in CRBN knock-out mice. Here, we demonstrate that, compared with WT mice, CRBN knock-out mice do not show the intensification of seizures by PTZ induction. Moreover, electroencephalography recordings were also performed in the brains of both WT and CRBN knockout mice to identify the absence of significant differences in the pattern of seizure activities. Consistently, immunoblot analysis for validating the protein level of the CRL4 complex containing CRBN (CRL4^Crbn) in the mouse brain was carried out. Taken together, we found that the deficiency of CRBN does not affect PTZ-induced seizure.

• The Korean Journal of Physiology and Pharmacology
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• 제18권3호
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• pp.269-278
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• 2014

Various antiepileptic drugs (AEDs) especially enzyme-inducing AEDs might be associated with increased vascular risk, through impairment of the endogenous antioxidative ability which may trigger oxygen-dependent tissue injury. Lamotrigine (LTG) a non-enzyme-inducing AED has scarce information regarding its effects on oxidative stress. The present study aimed to study the possible modulation of vascular risk factors of epileptogenesis by LTG, in a rat model of kindling seizure induced by pentylenetetrazole (PTZ). Four groups of male Wister rats were used; vehicle control group, PTZ group (alternate day PTZ, 30 mg/kg, i.p), LTG/PTZ group (LTG 20 mg/kg/day p.o and alternate day PTZ) and LTG group. The study period was 5 weeks. Lipoproteins and total homocysteine (tHcy), malondialdehyde (MDA) and reduced glutathione (GSH) were measured. Aortic endothelial function study and histopathological examination of the rats' brains, aortas and coronaries were conducted. Serum total cholesterol (TC), triglyceride (TG) and low-density lipoprotein cholesterol (LDL-C), tHcy, MDA, GSH levels were significantly higher in epileptic rats than normal controls rats. A decrease in HDL-cholesterol with high atherosclerotic index was also demonstrated. The administration of LTG improved the PTZ-kindled seizures. It produced a significant decrease in TC, TG and LDL-cholesterol, MDA, aortic GSH and increase in HDL-cholesterol with no significant effect on serum GSH and tHcy levels. LTG improved endothelium-dependent relaxation, decreased hippocampal neurodegenerative changes and atherosclerotic changes of aortas and coronaries. LTG decreased seizures severity, hippocampal damage and improved vascular risk markers in this rat model of kindling seizures.

• 한국동물학회:학술대회논문집
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• 한국동물학회 2001년도 한국생물과학협회 학술발표대회
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• pp.207.3-208
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• 2001

No Abstract, See Full Text

• 약학회지
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• 제42권3호
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• pp.330-335
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• 1998

Gastrodia elata (GE) is a oriental medicinal herb which has been used traditionally for the treatment of various brain diseases including convulsion and epilepsy. In orde r to examine the mechanism of anticonvulsive effect, we treated the methanol extract of GE (500mg/kg, P.0) to the pentylenetetrazole (PTZ)-induced convulsive rats. Methanol extracts of GE significantly inhibited (35%) the convulsion state as well as the level of lipid peroxidation (25%) in the brain. The ether fraction of methanol extracts among the others effectively ibhibited in vitro lipid peroxidation dose dependently ($5.O{\times}10^{-6}{\sim}2.O{\times}1O^{-5}g/ml$). The scavenging effect on hydroxy radicals was found in all the fractions of ether, butanol, and dichloromethane. These results suggest that the anticonvulsive effect of GE is possibly due to the antioxidative effects of the active components in GE.

• 대한한방소아과학회지
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• 제10권1호
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• pp.245-263
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• 1996

In order to investigate the effects of Yangsymtang on the activities of central nervous system, we observed the effects on convulsions induced by pentylenetetrazole, strychnine and picrotoxin. The sedative those on spontaneous motor activity and by rota rod method, the those on sleeping time induced by barbiturate and the alleviative those on pain induced by acetic acid and hind limb pressure also were analyzed. The results were as follows: 1. The solid extracts of Yangsymtang showed no anticonvulsive effects on convulsions induced by pentylenetetrazole, strychnine and picrotoxin. 2. As to the sedative effects by rota rod method, th solid extracts of Yangsymtang were recognized as significance(P<0.01). 3. The sleeping time induced by thiopental sodium was not prolonged by the oral administration of the solid extracts of Yangsymtang. 4. The oral administration of Yangsymtang did not influenced the sleeping induced by pentobarbital sodium significantly. 5. As to the effects on spontaneous motor activity, the oral administration of Yangsymtang made spontaneous motor activity decrease significantly(P<0.05). 6. The oral administration of Yangsymtang was significant on pain induced by acetic acid(P<0.001). 7. As to alleviative effects on pain induced by hind limb pressure. The solid extracts of Yangsymtang were not significant.

• Biomolecules & Therapeutics
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• 제3권3호
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• pp.199-204
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• 1995

Gastrodia elata is a medicinal plant which has been used as anticonvulsant in Korea, Japan and China. This study was conducted to examine the action mechanism of Gastrodia elata centering around the change of GABA and glutamic acid level in brain while observing the anticonvulsive effect in PTZ-induced seizure model. Seizures were reduced effectively by pretreatment of ether soluble part of methanol extract of Gastrodia elata. The pretreatment of ether soluble part inhibited not only the decrease of brain GABA level but also the increase of brain glutamic acid level observed in PTZ model of convulsive dose. Although there was not any change in glutamic acid level, the same development was also observed in the model of subconvulsive dose. From above results, it seems that the anticonvulsive component of Gastrodia elata is lipophilic, and its action mechanism is originated from both control action of GABA level and inhibition of glutaminergic neurotransmission.

• 동의생리병리학회지
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• 제25권4호
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• pp.614-619
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• 2011

Nelumbo nucifera(NN) is a oriental medicinal herb which has been used traditionally for the treatment of antidiarrhea, sedative action and various brain diseases including convulsion and epilepsy. In order to examine the mechanism of anticonvulsive effect, we treated the methanol extract of NN(100, 200 mg/kg, P.0) to the sleeping time and pentylenetetrazole(PTZ)-induced convulsive mice. The methanol extract of NN prolonged sleep time by pentobarbital. Methanol extracts of NN were not effected the concentration of GABA and GABA-T activity in the brain of PTZ-induced mice. Methanol extracts of NN significantly inhibited the convulsion state as well as the level of lipid peroxidation in the brain. The butanol and dichloromethane fraction of methanol extracts among the others effectively inhibited in vitro lipid peroxidation dose dependently($5.0{\times}10^{-6}\sim2.0{\times}10^{-5}\;g/ml$). These results suggest that the anticonvulsive effect of NN is possibly due to the antioxidative effects of the free radical formation at brain for the PTZ-induced convulsion if it were by due to generating system.

• 약학회지
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• 제30권4호
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• pp.163-168
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• 1986

Thirteen compounds were synthesized by condensing the N-heterocyclic amines (piperidine, pyrrolidine, morpholine) and secondary aliphatic amines (dimethylamine, diethylamine) with 3,4-methylenedioxyphenylalkenoic acid chlorides for developing CNS depressants. Among them, N, N-diethyl-3,4-methylenedioxycinnamamide (IX) and N, N-dimethyl-5-(3,4-methylenedioxyphenyl)-2, 4-pentadienoic acid amicle (XII) exhibited strong activity in antagonism against pentylenetetrazole-induced convulsion, strychnine-induced convulsion and maximal electroshock seizure. N, N-Dimethyl-3, 4-methylenedioxycinnamide (VIII) showed more potent activity in antagonism against strychnine-induced convulsion and maximal electroshock seizure and in the prolongation of hexobarbital sleeping time.