• The Journal of Internal Korean Medicine
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• v.23 no.1
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• pp.107-115
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• 2002

Objective : These experiments were designed to investigate the effects of Strychni Ignatii Semen on the gastrointestinal system and declining of toxicity. About experiments of acute toxicity, I investigated the quantity of Strychni $(C_{21}H_{22}N_2O_2)\;and\;LD_{50}$. In order to study the effects on gastrointestinal tract, I investigated the changes of gastric juice, discharging level of pepsin, inhibiting effects of ulceration, and transporting of intestine. Methods : Sample I : No making Strychni Ignatii Semen Sample II : Depositing for three days in water and then dry it. Sample III : Depositing for one hour in sesame oil and bum it. The results were as follows : 1. The average values of Strychnine decreased in Sample III. 2. The levels of $LD_{50}$ increased in Sample Ⅲ by about 70%. 3. In Sample III, inhibiting effects of ulceration and discharging level of pepsin were great. 4. In the level of gastric juice decreased in Sample I.II.III. 5. The transporting ability of large intestine elevated in Sample I.II.III. According to the results, making Strychni Ignatii Semen, especially Sample 3, toxicity decreased and has good effects on the gastrointestinal system.

• Toxicological Research
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• v.8 no.2
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• pp.161-170
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• 1992

The objectives of this sutdy were to investigate the effects of 8-fluorociprofloxacin(8-FCP) on the central nervous system (CNS) and to compare with those of ciprofloxacin(CP). The $LD_{50}$ values of intravenous 8-FCP were similar or slightly lower in rat (M;203.6mg/kg, F;186.1mg/kg)and markedly lower in mice (M;126.5mg/kg, F;163.1mg/kg), as compared to those of CP. However, no recognizable differences in the clinical signs and recovery were found between 8-FCP and CP in both species. In combination with fenbufen, the convulsive liability of 8-FCP was higher than that of CP. At an intravenous dose of 10mg/kg, 8-FCP provoked convulsive signs and subsequent death in mice, whereas CP produced convulsion at a dose of 40mg/kg. The hexobabital -induced sleeping time was markedly lengthened by the oral administration of 8-FCP, but slightly increased by CP. In addition, the two quinolone derivatives had analgesic effects. The analgesic activity of 8-FCP was approximately two times higher than that at CP. However, both 8-FCP and CP had little effects of pentylenetetrazole-or strychnine-induced convulsion and muscle relaxation. Our finding that 8-FCP had more remarkable CNS effects than CP strongly suggests that there should be differences in the pharmacokinetic characteristics and/or in the binding affinity for specific biologic targets, or receptors, in the CNS.

• The Korean Journal of Physiology and Pharmacology
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• v.15 no.5
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• pp.285-289
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• 2011

Shilajit, a medicine herb commonly used in Ayurveda, has been reported to contain at least 85 minerals in ionic form that act on a variety of chemical, biological, and physical stressors. The substantia gelatinosa (SG) neurons of the trigeminal subnucleus caudalis (Vc) are involved in orofacial nociceptive processing. Shilajit has been reported to be an injury and muscular pain reliever but there have been few functional studies of the effect of Shilajit on the SG neurons of the Vc. Therefore, whole cell and gramicidin-perfotrated patch clamp studies were performed to examine the action mechanism of Shilajit on the SG neurons of Vc from mouse brainstem slices. In the whole cell patch clamp mode, Shilajit induced short-lived and repeatable inward currents under the condition of a high chloride pipette solution on all the SG neurons tested. The Shilajit-induced inward currents were concentration dependent and maintained in the presence of tetrodotoxin (TTX), a voltage gated $Na^+$ channel blocker, CNQX, a non-NMDA glutamate receptor antagonist, and AP5, an NMDA receptor antagonist. The Shilajit-induced responses were partially suppressed by picrotoxin, a $GABA_A$ receptor antagonist, and totally blocked in the presence of strychnine, a glycine receptor antagonist, however not affected by mecamylamine hydrochloride (MCH), a nicotinic acetylcholine receptor antagonist. Under the potassium gluconate pipette solution at holding potential 0 mV, Shilajit induced repeatable outward current. These results show that Shilajit has inhibitory effects on the SG neurons of Vc through chloride ion channels by activation of the glycine receptor and $GABA_A$ receptor, indicating that Shilajit contains sedating ingredients for the central nervous system. These results also suggest that Shilajit may be a potential target for modulating orofacial pain processing.

• Biomolecules & Therapeutics
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• v.2 no.4
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• pp.336-342
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• 1994

The general pharmacological properties of EPO were investigated in various animals administering intravenously and in vitro system. The results were as follows. 1. Central nervous system: EPO at doses of 70, 700, 7000 U/kg showed no effect In mice on general behavior, on strychnine- and pentetrazol-induced convulsion and on acetic acid-induced writhing syndrome. The hexobarbital-induced sleeping time in mice was slightly reduced by EPO at a dose of 7000 U/kg but did not change at doses of 70, 700 U/kg. The body temperature in rats was slightly decreased by EPO at doses of 700, 7,000 U/kg but the change was in normal physiological range. 2. Respiratory and cardiovascular system: EPO showed no effect on respiratory rate, blood pressure, heart rate, femoral blood flow, and electrocardiogram in anesthetized dogs at doses of 70, 700, 7000 U/kg. 3. Smooth muscle: EPO at concentrations of 70, 700 U/ml had no effect on the contractile response of isolated guinea pig ileum to histamine and acetylcholine. 4. Water and electrolytes excretion: EPO at dose above 700 U/kg increased urine volume in rats but did not affect the concentrations of $Na^{+},\;K^{+},\;Cl^{-}$ in urine. 5. Gastrointestinal system: EPO(70, 700, 7000 U/kg) had no effect on the intestinal charcoal meal propulsion 6. Blood coagulation system: The administration of EPO(70, 700, 7000 U/kg) had no effect on the plasma prothrombin time(PT) and activated partial thromboplastin time(APTT) in mice. Platelet aggregation induced by ADP and collagen was not influenced by EPO(70 U/ml, 700 U/ml). The overall results obtained indicated that EPO exerts almost no serious pharmacological effect even at a 100-fold clinical dose(7000 U/kg).

• Parasites, Hosts and Diseases
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• v.60 no.5
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• pp.339-344
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• 2022

The development of drug resistance is one of the most severe concerns of malaria control because it increases the risk of malaria morbidity and death. A new candidate drug with antiplasmodial activity is urgently needed. This study evaluated the efficacy of different dosages of aqueous extract of Strychnos ligustrina combined with dihydroartemisinin and piperaquine phosphate (DHP) against murine Plasmodium berghei infection. The BALB/c mice aged 6-8 weeks were divided into 6 groups, each consisting of 10 mice. The growth inhibition of compounds against P. berghei was monitored by calculating the percentage of parasitemia. The results showed that the mice receiving aqueous extract and combination treatment showed growth inhibition of P. berghei in 74% and 94%, respectively. S. ligustrina extract, which consisted of brucine and strychnine, effectively inhibited the multiplication of P. berghei. The treated mice showed improved hematology profiles, body weight, and temperature, as compared to control mice. Co-treatment with S. ligustrina extract and DHP revealed significant antimalarial and antipyretic effects. Our results provide prospects for further discovery of antimalarial drugs that may show more successful chemotherapeutic treatment.

• Biomolecules & Therapeutics
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• v.28 no.2
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• pp.137-144
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• 2020

Epilepsy is a brain disorder that affects millions of people worldwide and is usually managed using currently available antiepileptic drugs, which result in adverse effects and are ineffective in approximately 20-25% of patients. Thus, there is growing interest in the development of new antiepileptic drugs with fewer side effects. In a previous study, we showed that a Rehmannia glutinosa (RG) water extract has protective effects against electroshock- and pentylenetetrazol (PTZ)-induced seizures, with fewer side effects. In this study, the objective was to identify the RG components that are responsible for its anticonvulsant effects. Initially, a number of RG components (aucubin, acteoside, catalpol, and mannitol) were screened, and the anticonvulsant effects of different doses of catalpol, mannitol, and their combination on electroshock- and chemically (PTZ or strychnine)-induced seizures in mice, were further assessed. Gamma-aminobutyric acid (GABA) receptor binding assay and electroencephalography (EEG) analysis were conducted to identify the potential underlying drug mechanism. Additionally, treated mice were tested using open-field and rotarod tests. Catalpol, mannitol, and their combination increased threshold against electroshock-induced seizures, and decreased the percentage of seizure responses induced by PTZ, a GABA antagonist. GABA receptor binding assay results revealed that catalpol and mannitol are associated with GABA receptor activity, and EEG analysis provided evidence that catalpol and mannitol have anticonvulsant effects against PTZ-induced seizures. In summary, our results indicate that catalpol and mannitol have anticonvulsant properties, and may mediate the protective effects of RG against seizures.

• The Journal of Internal Korean Medicine
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• v.19 no.1
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• pp.57-72
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• 1998

This study has been carried out to investigate the effects of Ukgansan(UGS) extract on anti-convulsive, antipyretic, analgesic, sedative and GABAergic system of experimental animals. The results of this study were as follows : 1. UGS extract prolonged significantly the beginning time to convulsion and death induced by strychnine. 2. UGS extract prolonged significantly the time to death induced by electrical shock of ECT unit.(3 sec, 200 F, 25 mA) 3. On the experiment of hypothermic effects of UGS extract on the rectal temperature of mouse, UGS extract decreased significantly the rectal temperature of mouse 4. On the experiment of antipyretic effects of UGS extract on the febrile induced by the subcutaneous injection of $150\;{\mu}g/kg$ endotoxin in mouse, UGS extract decreased significantly the rectal temperature of mouse. 5. On the experiment of analgesic effects of UGS extract on the writhing syndrome induced by intraperitoneal injection 0.7% acetic acid 1 ml/100g in mouse, the writhing syndrome induced by acetic acid was reduced significantly by administration of UGS extract. 6. On the experiment of effects of UGS extract on spontaneous motor activity measured by wheel cage method in mice, the spontaneous motor activity was reduced significantly by administration of UGS extract. 7. On the experiment of effects of UGS extract on the activity of GABA-transaminase(GABA-T) in mouse brains after 21 days of oral administration of UGS extract. the activity of GABA-T was reduced significantly by administration of UGS extract. 8. On the experiment of effects of UGS extract on the activity concentration of GABA in mouse brain after 21 days of oral administration of UGS extract, the activity concentration of GABA was reduced significantly by administration of UGS extract. 9 On the experiment of effect of UGS water extract on the activity of GAD in mouse brain after 21 days of oral administration of UGS extract, the activity of GAD was reduced significantly by administration of UGS extract. According to the these results, Ukgansan extracts reveal the effects on the anti-convulsive, antipyretic, analgesic, sedative and GABAergic system.

• Korean Journal of Oriental Medicine
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• v.2 no.1
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• pp.205-225
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• 1996

This study has been carried out to investigate the effects of Youngyanggaksan (YGS) extract on the anticonvulsive, antipyretic, anlgesic, sedative and GABAergic system of experimental animals. The results of this study were as follows : 1. YGS extract prolonged significantly the beginning time to convulsion and time to death induced by strychnine. 2. YGS extract prolonged significantly the time to death induced by electrical shock of ECT unit (3sec, 200F, 25mA). 3. On the experiment of hypothermic effects of YGS extract on the rectal temperature of rats, YGS extract decreased significantly the rectal temperature of rats. 4. On the experiment of antipyretic effects of YGS extract on the febrile induced by the subcutaneous injection of $150{\mu}g/kg$ endotoxin in rats, YGS extract decreased significantly the rectal temperature of rats. 5. On the experiment of analgesic effects of YGS extract on the writhing syndrome induced by intraperitoneal injection 0.7% acetic acid 1ml/100g in rats, the writhing syndrome was reduced significantly by administration of YGS extract. 6. On the experiment of sedative effects of YGS extract on spontaneous motor activity measured by wheel cage method in mice, the spontaneous motor activity was reduced significantly by administration of YGS extract. 7. On the experiment of effects of YGS extract on the activity of GABA-transaminase(GABA-T) in rat brains after 21 days of oral administration of YGS extract, the activity of GABA-T was reduced significantly by administration of YGS extract. 8. On the experiment of effects of YGS extract on the activity concentration of GABA in rat brains after 21 days of oral administration of YGS extract the activity concentration of GABA was reduced significantly by administration of YGS extract. 9. On the experiment of effects of YGS extract on the activity of GAD in rat brains after 21 days of oral adminstration of YGS extract, the activity of GAD was reduced significantly by administration of YGS extract. According to the those results, Youngyanggaksan extract reveals the effects on the anticonvulsive, antipyretic, anlgesic, sedative and GABAergic system.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1995.04a
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• pp.106-106
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• 1995

A polysaccharide, G009, isolated from Ganoderma lucidum IY009 subjected to investigating on general pharmacology. This material at the large oral doses of 1000 and 2000mg/kg in mice did neither exhibit any abnormal behaviors nor effects on central nervous system. It also had no influences on hexobarbital-induced sleeping time, rotarod test and spontaneous activity test at each oral dose of 1000mg/kg in mice. No effects on the body temperature and on acetic acid induced writhing syndrome in mice were observed with its oral administration at 1000mg/kg, and the convulsions induced by strychnine and pentetrazole were not inhibited at its oral doses of 1000mg/kg in mice. The solution of G009 as given intravenously at the doses of 30 and 60mg/kg in rabbit had no influences on blood pressure and respiration rates and depth. In isolated organs of rat uterus and fundus muscles and guinea-pig ileum and trachea, it did not show any contraction or relaxation at the concentration of 2$\times$10$^{-3}$g/ml, and the contractive actions produced by oxytocin, acetylcholine, serotonin and histamine did not inhibited by the same doses. This material showed no effect on intestinal propulsion test in mice and gastric secretion in rats at the oral doses of 1000mg/kg. However, it is interesting that the material exhibited potent inhibition of acidified aspirin induced gastric damage at the doses of 500 and 1000mg/kg in rats.

• The Journal of Internal Korean Medicine
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• v.18 no.2
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• pp.65-82
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• 1997

This study has been carried out to investigate the effects of Cheonmagudeungyeum(CGY) extract on anti-convulsive, antipyretic, analgesic, sedative and GABAergic system of experimental animals. The results of this study were as follows : 1. CGY extract prolonged significantly the beginning time to convulsion and death induced by strychnine. 2. CGY extract prolonged significantly the time to death induced by electrical shock of ECT unit(3 sec, 200 F, 25 mA) 3. On the experiment of hypothermic effects of CGY extract on the rectal temperature of mice, CGY extract decreased the rectal temperature of mice. 4. On the experiment of antipyretic effects of CGY extract on the febrile induced by the subcutaneous injection of $150\;{\mu}g/kg$ endotoxin in mice, CGY extract decreased significantly the rectal temperature of mice. 5. On the experiment of analgesic effects of CGY extract on the writhing syndrome induced by intraperitoneal injection 0.7% acetic acid 1 ml/100g in mice, the writhing syndrome induced by acetic acid was reduced significantly by administration of CGY extract. 6. On the experiment of effects of CGY extract on spontaneous motor activity measured by wheel cage method in mice, the spontaneous motor activity was reduced significantly by administration of CGY extract 7. On the experiment of effects of CGY extract on the activity of GABA - transaminase (GABA-T) in mouse brains after 21 days of oral administration of CGY extract, the activity of GABA-T was reduced significantly by administration of CGY extract. 8. On the experiment of effects of CGY extract on the activity concentration of GABA in mouse brain after 21 days of oral administration of CGY extract, the activity concentration of GABA was reduced significantly by administration of CGY extract. 9. On the experiment of effect of CGY water extract on the activity of GAD in mouse brain after 21 days of oral administration of CGY extract, the activity of GAD was reduced significantly by administration of CGY extract. According to the these results, Cheonmagudeungyeum extracts reveal the effects on the anti-convulsive, antipyretic, analgesic, sedative and GABAergic system.