• Korean Journal of Pharmacognosy
• /
• v.29 no.3
• /
• pp.187-192
• /
• 1998

The ethyl acetate fraction of Uncariae Ramulus et Uncus, which showed anticonvulsant effects against pentylenetetrazole (PTZ) treated mice, were subjected to column chromatography to isolate ursolic acid and hyperin from active eluate. Hyperin decreased the elevated activities of GABA-T and xanthine oxidase and lipid peroxide level dose-dependently in PTZ treated mice brain tissue in vitro, but no effect on superoxide dismutase activity. The effects on such enzyme and component seemed to be related with biosynthesis or metabolism of neurotransmitters.

• YAKHAK HOEJI
• /
• v.45 no.3
• /
• pp.251-257
• /
• 2001

The study was carried out to evaluate the preliminary toxicity and general pharmacology of KML-IIU, a purified pectin from Korean Mistletoe (Viscum album coloratum). KML-IIU was administered intravenously to ICR mice and Spargue-Dawley rats to investigate the acute toxicity. LD50 values in mice and rats were above 30 $\mu$g/kg. KML-IIU had no effects on the general behaviors, acetic acid induced writhing syndrome, pentobarbial induced sleeping time, pentylenetetrazole induced convulsion and the change of body temperature. In addition, KML-IIU did not show any effects on digestive system and blood coagulation system.

• Journal of Ginseng Research
• /
• v.19 no.1
• /
• pp.22-26
• /
• 1995

The present study was undertaken to elucidate the characteristics of red ginseng total saponin in behavioral changes on ambulation, forced swim test and convulsion in mice. The ambulation and the duration of immobility on forced swim test were not affected by red ginseng total saponin. On the other hand, the duration of immobility inducted by DMI, PGL but not CIP was significantly decreased, and the onset of convulsion induced by pentylenetetrazole was significantly shortened by preadministration of red ginseng total saponin. These results suggest that red ginseng total saponin component may play an important role in modulating synergism with drugs acting on depression and convulsion, and that the characteristics of synergetic effect induced by red ginseng total saponin potentate the central norepinephrine neuron activity.

• Archives of Pharmacal Research
• /
• v.19 no.3
• /
• pp.248-250
• /
• 1996

In conclusion, a series of N-Cbz-.alpha.-amono-glutarimides (1a-f), combining common structures such as N-CO-C-N and cyclic imide in a single molecule, were prepared from the (R)- or (S)-N-Cbz-glutamic acid and evaluated for their anticonvulsant activities in MES and PTZ tests in order to develope new and broad spectrum anticonvulsant. In this study, N-Cbz-.alpha.-aminoglutarimides (1) except ac and af, showed significant anticonvulsant activity in both MES and PTZ tests enough to be recommended as promising new anticonvulsant drug candidates. Now we are continuing to investigate further anticonvulsant test (quantification)for these compounds and synthesize their analogues in order to develop more active anticonvulsant and define the structure activity relationship more precisely.

• Natural Product Sciences
• /
• v.13 no.4
• /
• pp.384-389
• /
• 2007

Treatment of mice with Korean Red Ginseng (KRG) changed glutamic acid and GABA content in the mouse brain tissue with pentylenetetrazole (PTZ)-induced convulsion. KRG were orally administered at a dose of 50, 100 mg/kg for two weeks. The electroconvulsions (MES) and PTZ-induced convulsion were reduced but those induced by strychnine, bicuculine and picrotoxin were not. PTZ-induced convulsion decreased the $\~{a}$-aminobutyric acid (GABA) content in brain compared to control group while the content was increased in KRG-treated group compared to PTZ group. In the PTZ-treated group, the GABA-transaminase (GABA-T) activity was increased by 59.6%, while no effect was observed on glutamate decarboxylase (GAD) activity. These results support that the KRG decreased the GABA contents and modulated the glutamic acid contents in the brain.

• Toxicological Research
• /
• v.12 no.2
• /
• pp.181-194
• /
• 1996

The effects of Sanjoinine-A, an alkaloid isolated from Zizyphus spinosus semens, on central nervous system and general pharmacology were studied. In summary, Sanjoinine-A depress the spontaneous locomotor activity without motor incoordination and it has slight analgesic effect. Those effects are qualitatively similar to that of diazepam but its potency is much lower than diazepam(20 times). Sanjoinine-A does not depress the electric or pentylenetetrazole induced convulsion. Those effects are dissimilar with that of diazepam. Sanjoinine-A slightly depress the spontaneous or acethylchollne induced motility of smooth muscles but degree of depressant effect was variable to tissues. Sanjoinine-A does not show any effects on digestive system, blood, kidney fuction and neural ganglion.

• Korean Journal of Pharmacognosy
• /
• v.24 no.3
• /
• pp.231-234
• /
• 1993

Neuropharmacological profile of Humulus lupulus (hop) extract was studied in mice. At doses above 100 mg/kg(i.p.), it decreased spontaneous locomotor activity and raised the nociceptive threshold in the hot-plate test. At doses above 250 mg/kg (i.p.), it increased pentobarbital-induced sleeping time and produced muscle relaxant effect. At the dose of 500 mg/kg, anticonvulsive effect against pentylenetetrazole-induced convulsion and hypothermic effect was observed.

• Journal of Life Science
• /
• v.12 no.5
• /
• pp.505-514
• /
• 2002

The aim of this study was to evaluate the anticonvulsant activity of four agents derived from tropinone (T-1: 2,4-dipyrrolylmethenylnortropinone, T-2: 2,4-diphenylmethenylnortropinone, T-3 : 2,4-difurfurylmethenylnortropinone, T-4 : 2,4-dimethoxyphenylmethenylnortropinone) in NIH Swiss mouse. Pentylenetetrazole (nZ) was injected via intraperi-toniurn in mouse and Maximal Electroshock (MES) stimulation was through both conjunctivas by electrodes. Tropinone derivatives were treated at 15 minutes before PTZ or MES procedure. PIZ of 25 mg/kg induced generalized seizure in mouse, effects of tropinone derivatives on PTZ-induced seizure were monitored. Compared with control group, T-4 decreased seizure grade most effectively. Also T-4 increased onset time of PTZ-induced seizure. This result showed that T-4 is most effective on PTZ-induced seizure. In MES-induced seizure, T-1 decreased seizure grade and recovery time. nNOS expression in hippocampus and cortex were increased in nZ- and MES-induced seizure animals compared with control. Pretreatment of tropinone derivatives in PTZ-induced seizure did not affected nNOS expression in brain tissues, but T-1 and T-4 decreased nNOS expression in cortex of MES-induced seizure animals. These findings suggest that tropinone derivatives have specific anticonvulsant activities according to PTZ- and MES-induced seizure. 2,4- dimethoxyphenylmethenylnoroopinone is most effective in PTZ-induced seizure and 2,4-di methoxyphenylmethenylnortropinone is most effective in MES-induced seizure.

• Archives of Pharmacal Research
• /
• v.19 no.4
• /
• pp.312-316
• /
• 1996

A series of N-Cbz${alpha}$-aminosucinimides (1), combining common moieties of various anticonvulsants such as N-CO-C-N and cyclic imide in a single molecule, were synthesized from the corresponding (R)- and (S)-N-Cbz-aspartic acid (2). And their in vivo anticonvulsant evaluations in MES and PTZ test were investigated. And also the rotorod test for neurotoxicity was investigated. All the tested compounds (1), except 1c and 1f, showed significant anticonvulsant activities in both MES and PTZ test. And the most active compound among them in MES test was (R)-N-Cbz-${alpha}$-amino-N-methylsuccinimide (1b) $(ED_50/=52.5 mg/kg)$ and (S)-N-Cbz-aminosuccinimide((1d) was most active in PTZ test $(ED_50/=78.1 mg/kg)$. And the $TD_50$ values of the tested compounds were above 117.5 mg/kg. These pharmacological data were comparable to those of currently available anticonvulsants. And also we found that the pharmacological effects were dependent on their N-substituted alkyl chains and their stereochemistry.

• Biomolecules & Therapeutics
• /
• v.11 no.3
• /
• pp.183-189
• /
• 2003

General phannacological properties of IH-901, a new pharmacological composition as an intestinal metabolite formed from ginseng protopanaxadiol saponins, were investigated in experimental animals administered orally and in vitro test system. IH-901 had no effects on general behavior, pentobarbital sleeping time, spontaneous motor activity, motor coordination of mice, normal body temperature, chemoshock produced by pentylenetetrazole and writhing syndromes induced by 0.8％ acetic acid at the dose of 25 and 250 mg/kg. Gastric secretion of rats and intestinal motility in mice were not also influenced by the administration of IH-901 at doses of 25 and 250 mg/kg. IH-901 (25 and 250 mg/kg) did not change the mean arterial blood pressure and heart rate in conscious rats. IH-901 had no effect on the respiratory rate at the same doses when it was given to anesthetized rats. In in vitro experiments, IH-90l at the concentration of 25$\mu\textrm{g}$/L did not show any direct effect and inhibitory or augmentative action on the histamine-or acetylcholine-induced contractions in the isolated ileum of guinea-pig. Based on these results, it was concluded that IH-901 did not induce any adverse effects in experimental animals.