• Archives of Pharmacal Research
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• 제7권2호
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• pp.127-132
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• 1984

Systematic pharmacological astudies on pipeline have revealed that this compound elicited diverse pharmacological activities; CNS depressant activity characterized by antagonism against electo shock seizure and by muscle relaxant activity in mice; antipyretic activity in tyyhoid vaccinated rabbits; analgesic activity as evaluated by tail-clip pressure and writhing syndrome in mice; antiinflammatory activity in carrageenin-induced edema in rats.

• 약학회지
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• 제26권4호
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• pp.189-196
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• 1982

Piperine was reported to have a potential central nervous system (CNS) depressant activity in mice. In order to search a more active and less toxic compound than piperine and to elucidate the active group of piperine, the aromatic amides (10 compeunds) and aromatic esters (10 cempounds) of 3, 4-methylenedioxycinnamic acid were synthesized and evaluated on CNS depressant activity in comparison with piperine. The pharmacological tests conducted are as follows; (1) Acute, toxicity, (2) Antagonism against strychnine induced conduced convulsion, (3) Antagonism against maximal electrobhock seizure, (4) Rotarod test, (5) Potentiation of hexobarbital sleeping time. It was observed that 3, 4-methylendioxycinanamic acid derivatives were less toxic than piperine, and showed no significant CNS depressant activities. These facts indicate that the piperoyl group might be concerned with the pharmacological activity of piperine.

• 대한약리학회지
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• 제19권1호
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• pp.77-84
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• 1983

The behavioral pattern of an animal is influenced by endogenous and endogenous stimuli such as humoral secretion, neurohumoral transmitters, drugs, light and environmental change. It has teen known that adenosine is a normal constituent of brain, and has sedative or hypnotic effects and anticonvulsant effects, inhibiting the spontaneous firing of cells in the brain via membrane adenosine receptors. Recent studies suggest that the excitatory responses to xanthines in the CNS might be related to the competitive antagonism of xanthines to adenosine. This study was undertaken to Investigate the effects of adenosine and the CNS stimulants such as picrotoxin, strychnine and caffeine on the spontaneous activity of mire, and to examine the influence of adenosine on the seizures induced by large doses of CNS stimulants. Subjects were $20{\sim}30\;g$ adult mice, and the spontaneous activity was measured using the Selective Activity Meter after intraperitoneal injection of adenosine (10 mg/kg), caffeine (100 mg/kg), strychnine(0.2 mg/kg) or picrotoxin(0.5 mg/kg) with or without adenosine pretreatment. The seizures were induced with caffeine(200, 250 and 300 mg/kg), strychnine(1.25 and 1.5 mg/kg) or picrotoxin(10 and 15 mg/kg). The results are summarized as follows : 1) The spontaneous activity in mite was significantly inhibited between 10 and 20 minutes after adenosine treatment. 2) Caffeine and picrotoxin increased the motor activity significantly while strychnine had no effect on the activity. 3) The ambulatory activity in the caffeine, strychnine and picrotoxin treated groups was significantly inhibited by adenosine pretreatment. 4) The seizures were observed with caffeine(200, 250 and 300 m9/kg), strychnine(1.25 and 1.5 mg/kg) or picrotoxin(10 and 15 mg/kg). The caffeine induced seizures were inhibited by adenosine pretreatment, but the strychnine or picrotoxin induced seizures were not affected.

• Advances in Traditional Medicine
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• 제6권3호
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• pp.221-231
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• 2006

The aim of the present study is to investigate central nervous system (CNS) activity of the methanol extracts of leaves of Caesalpinia bonducella (MECB) and stem bark of Bauhinia racemosa (MEBR) (Caesalpinaceae) in Swiss albino mice and Wistar albino rats. General behavior, exploratory behavior, muscle relaxant activity and phenobarbitone sodium-induced sleeping time were studied. The results revealed that the methanol extracts of leaves of Caesalpinia bonducella at 100 - 200 mg/kg and stem bark of Bauhinia racemosa 100 - 200 mg/kg caused a significant reduction in the spontaneous activity (general behavioral profile), remarkable decrease in exploratory behavioral pattern (Y-maze and head dip test), a reduction in muscle relaxant activity (rotarod and traction tests), and also significantly potentiated phenobarbitone sodium-induced sleeping time. The results suggest that MECB and MEBR exhibit CNS depressant activity in tested animal models.

• Advances in Traditional Medicine
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• 제6권1호
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• pp.21-26
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• 2006

The ethanolic extract of Fleurya interrupta Gaud, (Urticaceae) was tested for its possible neuropharmacological effects on experimental animals, For the primary neuropharmacological screening of this plant, the ethanolic extract of its aerial parts was subjected to preliminary evaluation for acute toxicity, antinociceptive activity and central nervous system (CNS) activities. At the doses of 125 and 250 mg/kg, the extract significantly (P < 0.01 and P < 0. 001) and dose-dependently increased the frequency of acetic acid induced writhing in mice. In the pentobarbitone induced sleeping time test, the extract at the above dose levels, significantly and dose-dependently decreased the pentobarbitone induced sleeping time (P < 0.001) and increased the time for onset of sleep (P < 0.001) in mice. In the open field and hole cross tests, test animals showed an increase in their movement in the both tests from the 2nd observation period (30 min) and persisted throughout the entire experimental period (240 min). These results of the extract may attribute a stimulating action on the CNS. On the basis of these findings, it can be assumed that the extract exerts its stimulating effect on the CNS in mice by interfering with the cortical function or increasing the effect of some CNS stimulating neurotransmitters.

• Natural Product Sciences
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• 제10권5호
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• pp.237-239
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• 2004

Mallotus nepalensis (Euphorbiaceae) is a small tree found in central and eastern Himalayas, Nepal, Wallich and Sikkim. The 90% ethanolic extract of Mallotus nepalensis exhibited mild CNS depressant activity. Four compounds, lupeol (1), ${\beta}-sitosterol$ (2), ursolic acid (3) and ${\beta}-sitosterol-\;{\beta}-D-glucoside$ (4) were isolated from the 90% ethanolic extract of this plant of which 1, 3 and 4 are being reported for the first time from this species.

• Molecules and Cells
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• 제39권12호
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• pp.888-897
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• 2016

Stable expression of Foxp3 is ensured by demethylation of CpG motifs in the Foxp3 intronic element, the conserved non-coding sequence 2 (CNS2), which persists throughout the lifespan of regulatory T cells (Tregs). However, little is known about the mechanisms on how CNS2 demethylation is sustained. In this study, we found that Ten-Eleven-Translocation (Tet) DNA dioxygenase protects the CpG motifs of CNS2 from re-methylation by DNA methyltransferases (Dnmts) and prevents Tregs from losing Foxp3 expression under inflammatory conditions. Upon stimulation of Tregs by interleukin-6 (IL6), Dnmt1 was recruited to CNS2 and induced methylation, which was inhibited by Tet2 recruited by IL2. Tet2 prevented CNS2 re-methylation by not only the occupancy of the CNS2 locus but also by its enzymatic activity. These results show that the CNS2 methylation status is dynamically regulated by a balance between Tets and Dnmts which influences the expression of Foxp3 in Tregs.

• Parasites, Hosts and Diseases
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• 제61권4호
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• pp.449-454
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• 2023

Free-living amoebae (FLA) rarely cause human infections but can invoke fatal infections in the central nervous system (CNS). No consensus treatment has been established for FLA infections of the CNS, emphasizing the urgent need to discover or develop safe and effective drugs. Flavonoids, natural compounds from plants and plant-derived products, are known to have antiprotozoan activities against several pathogenic protozoa parasites. The anti-FLA activity of flavonoids has also been proposed, while their antiamoebic activity for FLA needs to be emperically determined. We herein evaluated the antiamoebic activities of 18 flavonoids against Naegleria fowleri and Acanthamoeba species which included A. castellanii and A. polyphaga. These flavonoids showed different profiles of antiamoebic activity against N. fowleri and Acanthamoeba species. Demethoxycurcumin, kaempferol, resveratrol, and silybin (A+B) showed in vitro antiamoebic activity against both N. fowleri and Acanthamoeba species. Apigenin, costunolide, (-)-epicatechin, (-)-epigallocatechin, rosmarinic acid, and (-)-trans-caryophyllene showed selective antiamoebic activity for Acanthamoeba species. Luteolin was more effective for N. fowleri. However, afzelin, berberine, (±)-catechin, chelerythrine, genistein, (+)-pinostrobin, and quercetin did not exhibit antiamoebic activity against the amoeba species. They neither showed selective antiamoebic activity with significant cytotoxicity to C6 glial cells. Our results provide a basis for the anti-FLA activity of flavonoids, which can be applied to develope alternative or supplemental therapeutic agents for FLA infections of the CNS.

• Advances in Traditional Medicine
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• 제8권4호
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• pp.323-328
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• 2008

The MeOH extract of seeds of Cerbera odollam Gaertn. (Apocynaceae) was screened for its antibacterial, cytotoxic and neuropharmacological activities. The extract showed moderate anti-bacterial activity against Salmonella typhi, Streptococcus saprophyticus, and Streptococcus pyogenes. It exhibited high level cytotoxicity against brine shrimp ($LC_{50}$: $3\;{\mu}g/ml$). The extract potentiated pentobarbital induced sleeping time in mice which was further supported by the exploratory behavior test at dose of 25 mg/kg. The overall results tend to suggest the antibacterial, cytotoxic and CNS depressant activities of the extract.

• Journal of Pharmaceutical Investigation
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• 제9권4호
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• pp.13-22
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• 1979

Panax Ginseng C. A. Meyer which has been known for more than 2000 years, occupies a particular place in folk medicine as so called tonic remedy. The brief pharmacological action of Ginseng complied from the numerous reports can be summarized as adaptogenic effect to be increased nonspecific resistance. Among the various components of Ginseng, the effective components has been known Ginseng butanol fraction as so called Ginseng saponin. In order to study on the effect of the Ginseng butanol fraction which influences spontaneous activity by CNS drugs in mice. Experiment of response was measured the change of spontaneous activity by CNS drugs in which mice were treated Ginseng butanol fraction. A method of measuring spontaneous activity in mice used by counting the number of times which were interrupted a beam of light. Results of experiment can be summarized as follows: 1. In case of administrating Ginseng butanol fraction for 1 day, stimulating effect of Ginseng was observed in spontaneous activity by caffeine in comparison with the control. at the first, but after 45 minutes no significant change was observed. 2. In case of administrating Ginseng butanol, fraction for 5days, decreasing tendency was observed in spontaneous activity by caffeine. 3. In case of administrating Ginseng butanol fraction for 10days, marked decrease was observed in spontaneous activity by caffeine in comparison with the control. From the experiment on the increased dose of caffeine, nonsignificant change was observed in comparison with caffeine and sodium benzoate 25mg/kg group. 4. A state of increased resistance was lasted until 5 days, and after 10 days it was disappeared. 5. Otherwise, nonsignificant change was observed for chlorpromazin HCl in comparison with the control. 6. From this result, 10 days administrating of ginseng butanol fraction appeared to have increased resistance in mice against caffeine.