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1.
The methanolic extract of rhizomes of Cyperus articulatus, a plant used in traditional medicine in Africa and Latin America for many diseases, possesses anticonvulsant activity in mice. This extract protected mice against maximal electroshock (MES)- and pentylenetetrazol (PTZ)-induced seizures. It also delayed the onset of seizures induced by isonicotinic acid hydrazide and strongly antagonized N-methyl-D-aspartate-induced turning behavior. The ED(50) for protection against seizures was 306 (154-541) mg/kg intraperitoneally (i.p.) for the PTZ test and 1005 (797-1200) mg/kg i.p. for the MES test. The ED(50) of methanolic extract against N-methyl-D-aspartate-induced turning behavior was 875 (623-1123) mg/kg i.p. C. articulatus L. methanolic extract protected 54% of mice from seizures induced by strychnine at the dose of 1000 mg/kg i.p. but had no or a moderate effect only against picrotoxin- or bicuculline-induced seizures. With these effects, the rhizome of C. articulatus L. possesses anticonvulsant properties in animals that might explain its use as a traditional medicine for epilepsy in Africa.  相似文献   

2.
AIM OF THE STUDY: To investigate the anticonvulsant activity of root bark extract of Carissa edulis. MATERIALS AND METHODS: The median lethal dose (LD(50)) of Carissa edulis extract was determined using Lork's method (1983). The anticonvulsant activity of the extract was assessed in pentylenetetrazole (PTZ)-induced convulsion in mice and maximal electroshock test (MEST) in chicks, with benzodiazepine and phenytoin as standard drugs, respectively. While mechanistic studies were conducted using both flumazenil, a GABA(A)-benzodiazepine receptor complex site antagonist and naloxone a non-specific opioid receptor antagonist. RESULTS: The median lethal dose (LD(50)) of Carissa edulis was 282.8mg/kg and over 5000mg/kg following intraperitoneal and oral administration, respectively. Carissa edulis produced 40% and 20% protection against convulsion at 5 and 20mg/kg, respectively, compared with 100% protection with benzodiazepine. The mean onset and percentage protection against convulsion in Carissa edulis extract-treated mice were reduced by flumazenil and naloxone. Carissa edulis exhibited dose-dependent inhibition of the convulsion induced by MEST with 20mg/kg providing 90% protection while phenytoin (20mg/kg) produced 100% protection. CONCLUSION: These results suggest that Carissa edulis possesses biologically active constituent(s) that have anticonvulsant activity which supports the ethnomedicinal claims of the use of the plant in the management of epilepsy.  相似文献   

3.

Aim of the study

To systematically investigate the anticonvulsant activity of methanol extract of Benkara malabarica roots and to provide a biochemical basis elucidating its mode of action.

Methods

The median lethal dose (LD50) of Benkara malabarica extract was determined. The anticonvulsant activity of the extract was assessed in strychnine-induced and isoniazide-induced convulsion models; phenytoin (20 mg/kg) and diazepam (1 mg/kg) were used as standards, respectively. Percentage protection provided by the drug was accounted as decrease in the number of convulsions within 8 h of observation. Mechanism of action was studied by performing GABA transaminase (GABA-T) assay, isolated from rat brain. Active constituent was isolated and characterized from the plant extract.

Results

The median lethal dose (LD50) of Benkara malabarica was found to be more than 500 mg/kg. It demonstrated 30% and 35% protection against strychnine-induced convulsions and 60% and 80% protection against isoniazide-induced convulsions, at doses of 25 mg/kg and 50 mg/kg, respectively. Enzyme assay results revealed that Benkara malabarica extract possesses GABA-T inhibitory activity (IC50 = 0.721 mg/ml). Scopoletin which was identified as the major constituent of the extract was found to be an inhibitor of GABA-T (IC50 = 10.57 μM).

Conclusions

The anticonvulsant activity of the plant extract is predominantly GABA mediated and may be due to the action of scopoletin alone or is a result of synergy of different compounds in the extract in which scopoletin is the major constituent.  相似文献   

4.
Anticonvulsant and neurotoxicity profile of Nardostachys jatamansi in rats   总被引:1,自引:0,他引:1  
Ethanol extract of the roots of Nardostachys jatamansi DC. (Valerianaceae) was studied for its anticonvulsant activity and neurotoxicity, alone and in combination with phenytoin in rats. The results demonstrated a significant increase in the seizure threshold by Nardostachys jatamansi root extract against maximal electroshock seizure (MES) model as indicated by a decrease in the extension/flexion (E/F) ratio. However, the extract was ineffective against pentylenetetrazole (PTZ)-induced seizures. Nardostachys jatamansi root extract also showed minimal neurotoxicity against rotarod test at doses that increased the seizure threshold. Further, pretreatment of rats with phenytoin at a dose of 12.5, 25, 50 and 75 mg/kg in combination with 50mg/kg of Nardostachys jatamansi root extract resulted in a significant increase in the protective index (PI) of phenytoin from 3.63 to 13.18. The dose response studies of phenytoin alone and in combination with Nardostachys jatamansi extract on the serum levels of phenytoin clearly demonstrated the synergistic action of both the drugs.  相似文献   

5.
Preliminary pharmacological studies were performed on the methanol extract of Bixa orellana L. (Bixaceae) leaves to investigate neuropharmacological, anticonvulsant, analgesic, antidiarrhoeal activity and effect on gastrointestinal motility. All studies were conducted in mice using doses of 125, 250 and 500 mg/kg of body weight. In the pentobarbitone-induced hypnosis test, the extract statistically reduced the time for the onset of sleep at 500 mg/kg dose and (dose-dependently) increased the total sleeping time at 250 and 500 mg/kg dose. A statistically significant decrease in locomotor activity was observed at all doses in the open-field and hole-cross tests. In the strychnine-induced anticonvulsant test, the extract increased the average survival time of the test animals (statistically significant at 250 and 500 mg/kg). The extract significantly and dose-dependently reduced the writhing reflex in the acetic acid-induced writhing test. Antidiarrhoeal activity was supported by a statistically significant decrease in the total number of stools (including wet stools) in castor oil-induced diarrhoea model. A statistically significant delay in the passage of charcoal meal was observed at 500 mg/kg in the gastrointestinal motility test. The extract was further evaluated in vitro for antioxidant and antibacterial activity. It revealed radical scavenging properties in the DPPH assay (IC(50)=22.36 microg/ml) and antibacterial activity against selected causative agents of diarrhoea and dysentery, including Shigella dysenteriae.  相似文献   

6.
Since a previous study indicated that the water extract of Scutellariae radix (SR) had high affinity for the benzodiazepine (BDZ) binding site of GABA(A) receptors, the present study examined whether SR water extract has an anticonvulsant effect in vivo and an enhancing effect on gamma-amino-n-butyric acid (GABA)-stimulated uptake of 36Cl(-) in cortex preparation in vitro in mice. The results showed that SR water extract had little effect on pentylenetetrazol (PTZ, 85 mg/kg, s.c.)-induced clonic seizures but significantly inhibited maximal electroshock-induced tonic seizures with an ED(50) of 3.6 g/kg. The BDZ agonist chlordiazepoxide (10 mg/kg, i.p.) had anticonvulsant activity on both types of seizures. In 36Cl(-) uptake assay, SR water extract (1-500 microg/ml) had no significant effect on 25 microM GABA-stimulated 36Cl(-) uptake, whereas chlordiazepoxide (10 microM) increased the 36Cl(-) uptake to 125% of control. Therefore, the present results showed for the first time that SR water extract had anticonvulsant activity against maximal electroshock-induced tonic seizures, and suggested that this anticonvulsant effect might be not via the activation of the BDZ binding site of GABA(A) receptors, but probably via the prevention of seizure spread.  相似文献   

7.
Fresh leaves of Baphia nitida supplied by a herbalist were extracted, screened phytochemically and then subjected to various pharmacological tests. The phytochemical tests showed the presence of saponin, flavonoid glycosides and true tannins. In the dose range used, no acute toxicity was observed for the ethanolic extract. The extract showed a dose dependent antinociceptive (analgesic) activity in mice with the analgesic activity of 500 mg/kg extract being comparable to that of 300 mg/kg of acetylsalicylic acid. The extract demonstrated an antidiarrhoeal effect by protecting rats against castor oil induced diarrhoea. This was also dose related but less than the protection afforded by sodium salicylate. The extract did not demonstrate any appreciable anticonvulsant effect against strychnine-induced convulsion in rats.  相似文献   

8.
The present study was undertaken to investigate the putative activity of a methanol extract of Hypericum montbretti (Guttiferae) on the central nervous system. Rutin (1519 ppm) and quercitrin (784 ppm) were identified as the major phenolic compounds in the extract. When administered at 25, 50 and 100 mg/kg doses, the extract decreased the total number of head‐dipping behaviours performed by mice during a hole‐board test. Administration of both the extract and diazepam (2 mg/kg) reduced spontaneous locomotory activity, potentiated hexobarbital (60 mg/kg)‐induced sleeping parameters and prevented pentylenetetrazole (80 mg/kg)‐induced seizures relative to the controls. These findings are the first to indicate the sedative and anticonvulsant activities of H. montbretti extract. Atropine (2 mg/kg) and naloxone (5 mg/kg) pre‐treatment did not reverse the sedative effect, indicating that muscarinic and opioidergic mechanisms did not contribute to the pharmacological action. However, pre‐treatment with flumazenil (a benzodiazepine receptor antagonist) reversed both the sedative and anticonvulsant effects induced by a 100 mg/kg dose of the extract, indicating the involvement of the GABA(A)‐benzodiazepine receptor complex. In conclusion, H. montbretti extract is a novel candidate as a sedative and anticonvulsant drug for the treatment of sleep disorders and for the prevention of epileptic seizures. Copyright © 2012 John Wiley & Sons, Ltd.  相似文献   

9.

Ethnopharmacological relevance

To investigate the anticonvulsant activity of the leaf extract of Justicia extensa T. Anders used traditionally in the treatment of convulsion.

Materials and methods

The anticonvulsant activity of the methanolic extract of Justicia extensa (50, 100 and 200 mg/kg, p.o.) was assessed in strychnine-induced (STR) and picrotoxin-induced (PCT) convulsion models in mice. Diazepam (1 mg/kg) and phenobarbitone (2 mg/kg) were used as reference drugs respectively.

Results

The extract showed no toxicity and significantly prolonged (p < 0.01-0.05) the onset and reduced the duration of the seizures induced by picrotoxin (5 mg/kg, i.p.) in a dose dependent manner. Phenobarbitone completely inhibited the seizures in this model. Similarly, in the seizures induced by strychnine (1 mg/kg, i.p.), the extract also prolonged the onset and reduced the duration of the seizures though not in a dose dependent manner. Diazepam failed to inhibit the strychnine-induced seizures. The plant extract however showed a significantly higher anticonvulsant activity at 100 and 200 mg/kg in comparison with diazepam.

Conclusions

The results obtained from this work suggest that Justicia extensa has anticonvulsant activity and this supports the use of the plant traditionally in the treatment of convulsion.  相似文献   

10.
Anti-inflammatory and analgesic activities as well as the median lethal dose (LD50) of water-ethanolic extract (PHE) of the aerial parts of Pothomorphe umbellata were evaluated in animal models. The ED(50) (oral) for the inhibition of carrageenan-induced rat paw edema assay was determined to be 550 mg/kg, while the LD(50) was higher than 2.0 g/kg. At a dose of 550 mg/kg, PHE inhibited the inflammatory process by 48.7% (P < 0.05) on the third hour of the assay (edema peak) when compared to the untreated control. Indomethacin, the positive control used in this test, inhibited the edema by 58.6% at a dose of 10 mg/kg, when compared to the untreated control (P < 0.05). All three fractions--hexane, methylene chloride and ethyl acetate--obtained by partition of PHE with respective solvents also showed inhibition of the edema induced by carrageenan over a period of 4h but the methylene chloride fraction showed the best activity. The activity shown by the methylene chloride fraction at 200 mg/kg was comparable to that exhibited by indomethacin at a dose of 10mg/kg. The number of writhings induced by a 0.6% acetic acid solution intraperitoneal injection was decreased by 22% (P < 0.05) in the group treated orally with Pothomorphe umbellata crude extract. PHE also inhibited the granulomatous tissue formation in rats by 6.2% (P < 0.05). In the same assay, topically applied dexamethasone decreased the granuloma formation by 14.2%. The above results suggest that Pothomorphe umbellata crude extract has analgesic and anti-inflammatory properties supporting its folkloric use for the treatment of these conditions.  相似文献   

11.
The current study was undertaken to explore the antipyretic and anticonvulsant profile of the Polygonatum verticillatum in established pharmacological paradigms. The crude methanol extract of rhizomes (PR) and aerial parts (PA) of the plant were tested in Brewer's‐yeast‐induced pyrexia and pentylenetetrazole‐induced convulsion test. PR and PA both evoked prominent antipyretic activity (p < 0.01) in a dose‐dependent manner during all assessment times at the dose of 50, 100, and 200 mg/kg intraperitoneally. The protection elicited by PR (82.20%) at 200 mg/kg was comparable with aspirin (88.48%) as a standard drug at 100 mg/kg. However, PA was less potent, and maximum protection was 64% at 200 mg/kg. Both PR and PA were devoid of any anticonvulsant activity. Our results demonstrated prominent evidence of antipyretic activity of P. verticillatum that is consistent with the folk uses of the plant. In addition from a biodiversity point of view, PA of the plant can also be used as an alternate of PR. Copyright © 2012 John Wiley & Sons, Ltd.  相似文献   

12.
Activity-guided fractionation of methanol-chloroform (1:1) extract of Ferula gummosa was carried out to investigate the isolation of the active component(s) responsible for the alleviation of morphine withdrawal syndrome induced by naloxone. Dependence was induced using subcutaneous (s.c.) injections of morphine daily for three days. On day 4, morphine was injected 0.5 h before the interaperitoneal (i.p.) injections of fractions or diazepam (5 mg/kg, i.p.) as positive control. Naloxone was injected (5 mg/kg, s.c.) 2 h after the final dose of morphine. The number of episodes of jumping during 30 min after the injection of naloxone was considered as the intensity of the withdrawal syndrome. The methanol-chloroform (1:1) extract of the aerial parts of plant was prepared and partitioned between water and chloroform. The active chloroform layer was concentrated and partitioned between methanol-water (9:1) and n-hexane. Activity was observed in the hydroalcoholic layer. This layer was concentrated and partitioned further between methanol-water (3:2) and chloroform. The chloroform layer showed a dose-dependent and significant activity. For all fractions the activity was observed at 470 mg/kg. Further purification on silica gel column chromatography gave a pure compound, which was 10 times as effective as the crude extract. The results of this study indicated that the plant extract contained component(s) that could be useful for the alleviation of morphine withdrawal syndrome.  相似文献   

13.

Ethnopharmacological relevance

Ficus religiosa (Moraceae) is reported to have numerous therapeutic utility in folk medicine. Among different biological activities on central nervous system, it has been reported to be used in ethnomedical treatment of epilepsy, which led us to further explore its anticonvulsant activity in various animal models of epilepsy.

Aim of the study

To investigate anticonvulsant activity of methanolic extract of figs of Ficus religiosa in animal models and to determine its possible anticonvulsant mechanism.

Materials and methods

Anticonvulsant activity of figs extract (25, 50 and 100 mg/kg, i.p.) was studied in seizures induced by maximum electroshock (MES), picrotoxin and pentylenetetrazol (PTZ). Cyproheptadine, a nonselective (5HT1/2) serotonin antagonist (4 mg/kg, i.p.) was used to study the reversal of protective effect of extract in the above mentioned models. Acute toxicity, neurotoxicity and potentiation of pentobarbitone induced sleep by extract was also studied.

Results

Extract showed no toxicity, potentiated pentobarbitone induced sleep and inhibited seizures induced by MES and picrotoxin in a dose dependent manner. Anticonvulsant effect of extract was comparable to clinically used antiepileptic drugs (phenytoin and diazepam). However, PTZ induced seizures were not inhibited. Animals pretreated with cyproheptadine showed inhibition of the anticonvulsant effect of extract.

Conclusions

These findings suggested that the methanolic extract of figs of Ficus religiosa had anticonvulsant activity against MES and picrotoxin induced convulsions, with no neurotoxic effect, in a dose dependent manner. Inhibition of the anticonvulsant effect of extract by cyproheptadine substantiates the involvement of serotonergic pathways for the anticonvulsant activity of extract.  相似文献   

14.
The effect of a 50% aqueous ethanol extract of Alchornea cordifolia (Schum and Thonn) Muell. Arg. leaf was investigated in mice which had been infected intraperitoneally with 5.0 x 10(9) cfu of Staphylococcus aureus. Dose-dependent antibacterial activity was demonstrated and the rate of survival of infected mice was improved significantly by doses between 25 and 200 mg/kg of injected extract when compared with untreated infected controls. The intraperitoneal median lethal dose of the extract was found to be 800 mg/kg.  相似文献   

15.
The anti-diarrheal and spasmolytic activities of Soonkijangquebo (SKJQB), a Korean herbal anti-diarrheal formulation, were subjected to pharmacological evaluation. SKJQB, at a dose of 50-200 mg/kg, inhibited castor oil-induced diarrhea in mice. The median effective dose (ED50) for the anti-diarrheal effect was 93 mg/kg. In isolated rabbit jejunum preparations, SKJQB produced a spasmolytic effect by the relaxation of spontaneous contractions in a dose-dependent manner. The median effective concentration (EC50) for the spasmolytic effect was 3.6 mg/ml. In isolated guinea pig ileum preparations, SKJQB also produced a spasmolytic effect by reduction of acetylcholine-induced contractions. When tested against calcium channel blockade in rabbit jejunum, SKJQB caused a dose-dependent rightward shift in the Ca2+ dose-response curves, similar to that produced by verapamil, a well-known calcium antagonist. In an acute toxicity study in Sprague-Dawley rats, the median lethal dose (LD50) of SKJQB was greater than 2000 mg/kg, and no pathological changes were noticed in macroscopic examination by necropsy of rats treated with SKJQB. Thus, SKJQB may be safely used as a spasmolytic as well as an anti-diarrheal agent.  相似文献   

16.
Taxus wallichiana Zucc. (Himalayan Yew) is often used in northern areas of Pakistan for the treatment of pyrexia, acute pains and epilepsy. We have investigated certain pharmacological activities of the methanol leaf extract against convulsion, nociception and pyrexia induced in rodents. The aim was to justify and explore its folk uses in these pathological conditions, on scientific basis. The studies were carried out using acetic acid-induced nociception and pentylenetetrazole-induced convulsions in mice, while formalin test and yeast-induced pyrexia in rats. Significant analgesic (67.77 and 74.29%) effect was found in acetic acid-induced model at doses of 100 and 200mg/kg, i.p. respectively. Crude extract exhibited significant (P<0.05) inhibition of the formalin noxious stimulation on both early and late phases of pain by the extracts (100 and 200mg/kg doses). In case of yeast-induced pyrexia model, 200mg/kg dose showed very significant (P<0.01) inhibition while 50 and 100mg/kg dose caused a significant (P<0.05) inhibition. Plant extract has controlled the pentylenetetrazole-induced convulsions in mice. 100 and 200mg/kg i.p doses of the extract significantly (P<0.05) inhibited the mioclonus and clonus while inhibition of tonus and hind limb tonic extension (HLTE) was highly significant (P<0.01). The anticonvulsant activity of this plant has been reported for the first time throughout the whole genus. The observed pharmacological activities provide the scientific basis for the folkloric use of the plant in treating epilepsy, pyrexia and acute pain.  相似文献   

17.
The antigiardial activity of crude methanolic extracts from Helianthemum glomeratum and Rubus coriifolius, plants used in Mexican traditional medicine for the treatment of diarrhea and dysentery, were demonstrated using experimental infections of Giardia lamblia in suckling female CD-1 mice. In vivo antigiardial activity was studied to determine the dose required to kill 50% of the trophozoites (ED50). Five single-doses between 1.25 and 20 mg extract/kg body weight were tested. Drugs metronidazole and emetine were used as reference. The ED50 (mg/kg) obtained for the extracts and drugs used as reference was 0.125 for Helianthemum glomeratum, 0.506 for Rubus coriifolius, 0.194 for metronidazole and 0.167 for emetine. Both methanolic extracts showed antigiardial activity, the extract of Helianthemum glomeratum was more active than Rubus coriifolius, and its activity is comparable to metronidazole and emetine. Our results hold the perspective for the utilization of the extracts of these plants as an option to develop of novel antigiardial phytodrugs.  相似文献   

18.

Aim of the study

The objective of this study is to investigate the anticonvulsant, anxiolytic and sedative activities of the aqueous root extract of Securidaca longepedunculata.

Materials and methods

The anticonvulsant effect of the aqueous root extract (100, 200 and 400 mg/kg) was evaluated in mice using the strychnine- and picrotoxin-induced seizure models. Its anxiolytic activity was evaluated using the elevated plus maze (EPM) and the Y maze (YM) methods (14 and 32) while the hexobarbitone induced sleep and the hole board models were used to evaluate the sedative and exploratory activities in mice respectively. The acute toxicity studies and phytochemical analysis of the extract were also carried out.

Results

The extract (100–400 mg/kg) produced a significant (P < 0.01) dose dependent increase in onset of convulsion compared to the control for strychnine- and picrotoxin-induced seizures. It also produced a significant (P < 0.01) dose dependent prolongation of the cumulative time spent in the open arms of the elevated plus maze and Y maze compared with the control. The extract (100–400 mg/kg) produced significant (P < 0.01) reduction in the time of onset of sleep induced by hexobarbitone. The prolongation of hexobarbitone sleeping time by the extract (200 mg/kg) was comparable to that produced by diazepam (3 mg/kg). At doses of 100–400 mg/kg, the extract produced a dose dependent decrease in exploratory activity of the mice. The reduction in exploratory activity produced by the extract (400 mg/kg) was greater than that of chlorpromazine (1 mg/kg). The results obtained from the experiments indicate that the extract has central nervous system depressant and anxiolytic activities. The LD50 obtained for the acute toxicity studies using both oral and intraperitoneal routes of administration were 1.74 g/kg and 19.95 mg/kg respectively.

Conclusion

These findings justify the use of Securidaca longepedunculata in traditional medicine for the management of convulsion and psychosis.  相似文献   

19.
The methanol extract of the leaves of P. incarnata was evaluated for its antiasthmatic effects against acetylcholine chloride (Ach)-induced-bronchospasm in guinea-pigs at doses of 50, 100 and 200 mg/kg. Using a 7-day treatment regimen, significant prevention of dyspnoea-related-convulsions was noted in the animals treated with a 100 mg/kg dose of this extract. No preventive effect was exhibited by the 50 mg/kg dose and at a higher dose, i.e. 200 mg/kg, the preventive effects against Ach-chloride-induced-dyspnoea were also reduced. This may be due to defective alpha-adrenoceptor function reported after excessive or continuous administration of an alpha-receptor agonist.  相似文献   

20.
An ethanol extract of the leaves of Brazilian Casearia sylvestris, given orally, inhibited gastric secretion in pylorus-ligated rats. At a prophylactic dose of 57.5 mg/kg, the extract showed a reduction of gastric juice more effective than misoprostol (500 micrograms/kg). In reducing hydrochloric acid output, the extract was less effective than misoprostol, cimetidine (32.0 mg/kg) and atropine (5.3 mg/kg). With the extract, the pH of the stomach contents was not significantly different from that of controls. Stress-induced lesions produced by restraint and water immersion were significantly prevented by the extract for all levels of severity when compared with the controls. The extract appeared more effective than misoprostol in suppressing light lesions, was equivalent to cimetidine and misoprostol for moderate lesions, and less effective than cimetidine and misoprostol for severe lesions. Toxicological experiments indicated a low acute toxicity, confirmed by subchronic daily testing. The oral LD50 value of greater than 1840 mg/kg was over 32 times higher than the antiulcerogenic ED50 (57.5 mg/kg).  相似文献   

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