Evaluation of the Anticonvulsant and Antidepressant Effects of the Aqueous Extract of the Leaves of Ascotheca paucinervia (T. Anderson ex C.B. Clarke) Heine in Mice

The present study was undertaken to evaluate the anticonvulsant and antidepressant effects of Ascotheca paucinervia leaves on mice by using strychnine at 2.5mg/kg to induce convulsions and the forced swimming test to create a stressful situation, respectively. Concerning convulsions, only the 500mg/kg extract significantly increases (p<0.001) the time to onset of convulsions and it non-significantly reduces the duration of convulsions induced by strychnine. In addition, the extract reduces very significantly in a dose-dependent manner the time of immobility and it significantly increases the swimming time as well as the climbing time at both doses. At the same time, the estimation of the acute toxicity of the extract from the leaves of Ascotheca paucinervia according to guideline No. 425 of the OECD (2022) shows that the latter is weakly toxic and its LD50 is greater than 5000mg/kg. In addition, the evaluation of the sedative effect of this extract shows that it produces a dose-dependent sedative effects and at doses of 250m/kg and 500mg/kg, the extract significantly potentiates the sleep induced by phenobarbital. In summary, the results obtained suggest that Ascotheca paucineervia leaves extract possesses anticonvulsant and antidepressant effects.

Evaluation Of Anticonvulsant Activity Of Cow Urine Betel Vine Extract In Mice

The present study was designed to investigate the anticonvulsant activity of Cowurine betel vine extract in rats. Anticonvulsant activity was performed by using the two modelsMaximal Electric Shock (MES) induced convulsions and Pentylene tetrazole (PTZ) inducedconvulsions. The animals were fed with Cow urine betel vine extract at the dose of 250 and500mg/kg b.w orally for a period of 14 days. The pretreated extract reduced the convulsions ina dose dependent manner which was determined by taking the duration of flexion, extensor,clonus and stupor phase and Percentage of inhibition of seizures relative to controls wascalculated.

Synthesis and anticonvulsant activity of 6-methyl-2-thioxo-2, 3-dihydropyrimidin-4(1H)-one acetamides

This research aimed at synthesizing new potential anticonvulsants in the series of 2-(4-methyl-6-oxo-1,6-dihydropyrimidin2-yl)thio-acetamides. An initial intermediate 6-methyl-2-thioxo-2,3-dihydro-pyrimidin-4(1Н)-one was obtained by thereaction of thiourea with an acetoacetic ester in the presence of sodium methoxide. The target 2-(4-methyl-6-oxo-1,6-dihydropyrimidin-2-yl) thioacetamides were synthesized by alkylation of initial 6-methyl-2-thiopyrimidin-4-one withcorresponding 2-chloroacetamides in Dimethylformamide (DMF) in the presence of potassium carbonate. The structureof compounds was confirmed by 1H Nuclear magnetic resonance (NMR)-spectroscopy, LCMS, and elemental analysis.A screening of anticonvulsant activity of synthesized compounds was carried out using the pentylenetetrazole- andmaximal electroshock-induced seizures models. In these studies, the highest anticonvulsant activity demonstrated acompound 5.5 2-[(4-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)thio]-N-(4-bromophenyl)-acetamide, which decreased thelethality, the number and the severity of seizures, and increased their latent period. For these compound parameters ofЕD50, acute (LD50) and neurotoxicity (TD50), as well as therapeutic (TI) and protective (PI) indexes were determined.Logical structure analysis of anticonvulsant activity screening revealed some patterns of “structure–activity” relationship.

Docking studies of biologically active substances from plant extracts with anticonvulsant activity

Virtual screening methods are promising and useful to design new herbal remedies to satisfy the numerous clinicalneeds. Major problem for extensive use of herbs is the lack of information concerning mechanisms of their action.In the previous pharmacological studies using different models of seizures, it was found that some members of theSolanaceae, Fumariaceae, Lamiaceae, Oleaceae, Viscaceae, and Betulaceae families show a high level of anticonvulsantproperties but the role of individual components of these herbs in the realization of antiepileptic activity remainsunknown. The aim of the present research was molecular docking of compounds identified in the studied herbs to findthe binding mechanism with the suitable targets. The study resulted that the given herbal individual substances did notshow any potential anticonvulsant properties. Anticonvulsant activity of the studied herbs is probably due to the factthat in contrast to individual substances they are characterized by a complex chemical composition and synergism ofbiologically active compounds.

Research progress on biological activities and synthesis of alkaloids in plants from Chimonanthus Lindl / 中草药

The plants of Chimonanthus Lindl. are endemic traditional medicinal plants in China. As the important components of these plants, the Chimonanthus alkaloids showed biological activities such as hypotensive activity, anticonvulsant, antifungal, antiviral, analgesia, antitumor, and melanogenesis inhibitory properties. In this paper, the types, bioactivities, and synthesis of alkaloids in plants of Chimonanthus Lindl. were reviewed systematically for providing reference in the further research and development of Chimonanthus alkaloids.

Neuropharmacological effects of the ethanolic extract of Sida acuta

ABSTRACT Sida acuta Burm. f., Malvaceae, is regarded as astringent, tonic and useful in treating urinary diseases and blood disorders, bile, liver and as treatment for nervous diseases. Different methods were developed: sodium pentobarbital-induced sleeping time, anxiolytic activity, test for muscle-effects, pentylenetetrazole (PTZ)-induced seizures, effect on normal body temperature. All experiments were performed in an isolated room with 12/12 h light/dark cycles at 22 ± 1 ºC. The effects described in this work for Sida acuta are according to what is known in traditional medicine, where is used as sedative agent. At the higher doses used in this work (500 and 1000 mg/kg), the Sida acuta extract reduced the latency time (T1) and increased the sleeping time (T2) induced by pentobarbital, indicating a sedative and hypnotic effect of the plant's extract. The extract of Sida acuta shows an increase in open arm exploration (anxiolytic activity). Results obtained in the rota-rod test showed that only the elevated dose (750 mg/kg) of Sida acuta extract, acutely administered, promotes significant changes, at 60 and 120 min post-administration, in the time of permanence in the rod. The ethanolic extract from the leaves and stems of Sida acuta, causes effects on the central nervous system in experimental animals.

Pharmacognostic and phytopharmacology study of Anacyclus pyrethrum: An insight.

Anacyclus pyrethrum an amazing medicinal plant is one of the most widely growing species of the family Asteraceae. The present review endow with significant information about its phytochemical investigations, pharmacological activities and medicinal properties as a folk medicine to treat several disease like anti-rheumatic, analgesic, antibacterial, antiviral, carminative, anti-catarrh, improve digestion, emmenagogue, febrifuge, nervine, vermifuge, and sialagogue. The plant has been reported several pharmacological actions such as antidiabetic, immunostimulating effect, inhibitory effects, antidepressant activity, anticonvulsant activity, memory-enhancing activity, aphrodisiacs, antimicrobial activity, antioxidant, local anesthetic effect, insecticidal effect, action on COX and LOX, interactions with testosterone, interaction with libido, and it interaction with testicles. Mainly the root portion has beneficial properties that can serve the mankind. The entire plant can be extensively studied for further future prospective.

EFFECT OF NICORANDIL ON PENTYLENETETRAZOLE (PTZ) INDUCED CONVULSIONS IN MICE

Aims & Objectives: To evaluate or screen the anticonvulsant effect of Nicorandil a potassium channel opener in Pentylenetetrazole(PTZ) induced convusions in albino mice. Materials & Methods: Mice of either sex weighing 20-25gms were selected for the present study. The animals were divided into 6 groups with each group consisting of 6 albino mice. Group 1 mice received placebo (0.2ml of distilled water) intraperitoneally (i.p), group 2 received sodium valproate 200 mg/kg/i.p. as positive control, while groups 3,4, 5 and 6 were administered Nicorandil 5, 10, 20 and 40 mg/kg i.p respectively. Pentylenetetrazole (PTZ) was administered in the dose of 100mg/kg i.p, 30mins after Nicorandil/ control drug pre-treatment. Onset and duration of clonic convulsion were recorded. Results: Nicorandil pretreatment in the dose of 5mg/kg increased onset time and significantly decreased the duration of convulsions,while the doses of 10, 20, 40mg/kg prevented the convulsions. Conclusion: Nicorandil possesses significant anticonvulsant activity comparable to sodium valproate on PTZ induced seizure in albino mice.

Synthesis, potential anticonvulsant and antidepressant effects of 2-(5-methyl-2,3-dioxoindolin-1-yl)acetamide derivatives

A new series of 2-(5-methyl-2,3-dioxoindolin-1-yl)acetamide derivatives were synthesized and evaluated for their anticonvulsive activity in a pentylenetetrazole (PTZ)-evoked convulsion model and antidepressant activity in the forced swimming test (FST) model. Eleven synthesized compounds were found to be protective against PTZ-induced seizure and showed the anticonvulsant activity. In addition, four of the synthesized compounds (4l, 4m, 4p and 4q) showed potent antidepressant-like activity. Among these compounds, compound 4l was found to have the most potent antidepressant-like activity, and significantly reduced the duration of immobility time at 100 mg/kg dose level when compared to the vehicle control, which is similar to the reference drug fluoxetine.

Isolation of compound and CNS depressant activities of Mikania scandens Willd with special emphasis to brain biogenic amines in mice.

Mikania scandens, a twining herb that grows as a weed in India and Bangladesh is used as vegetables and is a good source of vitamin A, C, B complex, mikanin, sesquiterpenes, betasitosterin, stigmasterol and friedelin. The present communication reports CNS depressant activities with special emphasis to brain biogenic amines in mice. Ethanol extract of leaves of M. scandens (EEMS) was prepared by Soxhalation and analyzed chemically. EEMS potentiated sleeping time induced by pentobarbitone, diazepam and meprobamate and showed significant reduction in the number of writhes and stretches. EEMS caused significant protection against pentylene tetrazole-induced convulsion and increased catecholamines and brain amino acids level significantly. Results showed that EEMS produced good CNS depressant effects in mice.

Anticonvulsant and antioxidant activity of aqueous leaves extract of Desmodium triflorum in mice against pentylenetetrazole and maximal electroshock induced convulsion

The present investigation was aimed to study an anticonvulsant activity of aqueous extract of Desmodium triflorum (L.) DC., Fabaceae, in mice. Animal models of epilepsy namely the pentylenetetrazole, and maximal electroshock induced convulsion were used to evaluate the anticonvulsant effects of the extracts. The biochemical estimation was done by measuring the lipid peroxidation and reduced glutathione. In the pentylenetetrazole induced convulsion, aqueous extract of D. triflorum 800 mg/kg significant delayed the onset of convulsion, reduced the duration of convulsion (p<0.05) and reduced mortality. The aqueous extract of D. triflorum 800 mg/kg dose reduced hind limb tonic extension phase of maximal electroshock induced convulsion induced convulsion in mice (p<0.05). The pretreated aqueous extract of D. triflorum showed significant inhibition of lipid peroxidation and increases the reduced glutathione level in mice brain tissue (p<0.001). The results revealed that D. triflorum possesses a significant dose dependent anticonvulsant activity.

Anxiolytic and anticonvulsant activity of methanol extract of leaves of Alternanthera brasiliana (L.) Kuntze (Amaranthaceae) in laboratory animals.

Anxiety related disorders are the most common mental illnesses and major cause of disability in man. Anxiolytic activity of methanol extract of leaves of A. brasiliana (L.) Kuntze (MEAB) was evaluated using hole board (HB), open field (OF), elevated plus maze (EPM) and light/dark exploration test (LDE) in mice. Its locomotor activity was studied using actophotometer and anticonvulsant effect was studied using maximal electroshock-induced seizures and pentylenetetrazole-induced seizures in mice. Single oral administration of MEAB at different doses (100, 300 and 600 mg/kg, ip) significantly increased the number and duration of head poking in the HB test; rearing, assisted rearing and number of square traveled in the OF test; entries and time spent in open arm in the EPM test; time spent in lighted box, and numbers of crossings and transfer latency time in the LDE test. There was significant reduction in the time spent in close arm in the EPM test and time spent in dark box in LDE test. In the actophotometer, the activity count was reduced in MEAB and diazepam treated group than control group. All the three doses of the extract significantly reduced the duration of seizures induced by pentylenetetrazole (chemoshock convulsion). However, the extract did not show any appreciable effect in electroshock convulsion model. The results of the present study suggest promising anxiolytic and anticonvulsant activity of MEAB which might be accredited to different phytoconstituents like alkaloids, steroids and triterpenes present in the methanol extract of A. brasiliana.

Pharmacological justification for the ethnomedical use of Clausena anisata root-bark extract in the management of epilepsy.

Various morphological parts of the tropical plant, Clausena anisata (Wild) Hook [family: Rutaceae], have ethnomedical claim for use in the management of epilepsy. This study examined the antiepileptic activity of Clausena anisata root bark, stem bark and leaf ethanolic extracts (i.e. CARE, CASE and CALE respectively) against pentylenetetrazole (PTZ) induced seizures in mice. Phytochemical and acute toxicity tests were performed on the extracts followed by oral administration of graded doses of CASE (500, 750 and 1000 mg/kg), CARE and CALE (400, 600 and 800 mg/kg) to the mice, thirty minutes before the administration of PTZ (90 mg/kg i.p.). The anticonvulsant effect of the extracts and diazepam (4 mg/kg) were compared. CALE was found to possess large amount of saponins, CARE large amounts of tannins and saponins, CASE large amounts of flavonoids, alkaloids and tannins. While CARE at the dose level of 800 mg/kg significantly (p<0.05) delayed the onset of convulsions and afforded 33.33 % protection, neither CALE nor CASE could exert any significant protective effect on PTZ induced convulsions, whereas diazepam totally abolished the episodes of convulsions. This study suggests that the ethanolic root bark extract of Clausena anisata contains bioactive constituents that may be beneficial in petit mal epilepsy and lend pharmacological credence to the ethnomedical claim for the use of the plant in the management of epilepsy. Abbreviations: NMDA= N-methyl-D-aspartate, SCMC= sodium carboxy methyl cellulose, CARE= Clausena anisata root bark ethanolic extract, CASE= Clausena anisata stem bark ethanolic extract, CALE= Clausena anisata leaf ethanolic extract, PTZ= pentylenetetrazole.

Evaluation of anticonvulsant activity of ethanolic leaves extract of Desmodium triflorum in mice

The present investigation was aimed to study an anticonvulsant activity of ethanolic extract of Desmodium triflorum (L.) DC., Fabaceae, in mice. Animal models of epilepsy namely the pentylenetetrazole (PTZ), isoniazid or isonicotinic hydrazide (INH) and maximal electroshock induced convulsion (MES) were used to evaluate the anticonvulsant effects of the extracts. The biochemical estimation was done by measuring the lipid peroxidation and reduced glutathione (GSH). In the PTZ induced convulsion, ethanolic extract of D. triflorum (EEDT) 400 mg/kg significant delayed the onset of convulsion, reduced the duration of convulsion and reduced mortality. Similarly a dose of 800 mg/kg of EDDT significantly delayed the onset of convulsion, reduced the duration of convulsion and showed 33.33% protection in mice against INH induced convulsion. Further no mortality was found. Both the doses reduced hind limb tonic extension (HLTE) phase of MES induced convulsion in mice. The pretreated EEDT showed significant inhibition of lipid peroxidation and increases the reduced glutathione level in mice brain tissue. The results revealed that D. triflorum possesses a significant dose dependent anticonvulsant activity.

Pharmacological screening of Dikamaliartane-A, A cycloartane isolated from gum resin, Dikamali.

The biological activitites of Dikamaliartane-A, a cycloartane isolated from gum resin Dikamali of Gardenia gummifera/Gardenia lucida was screened for some pharmacological actions. The study was carried out using albino mice (20-25gr). It reduced locomotor activity and potentiated pentobarbitone-induced sleeping time in mice indicating Central Nervous System depressant activity. It protected mice from strychnine and electro shock–induced convulsions indicating that it has anti-convulsant activity. All these activities were statistically significant. The LD50 (Lethal Dose) was carried out in mice according to Organization for Environmental Cooperation and Development (OECD) Guidelines 423. The LD50 was tested in three mices for each dose with doses from 5mg/kg, 50mg/kg, 300mg/kg and 2000mg/kg. The LD50 was found to be 500mg/kg.

Bioassay-guided evaluation of central nervous system effects of citronellal in rodents

The central nervous system (CNS) depressant and anticonvulsant activities of citronellal (CT) were investigated in animal models. The CT in doses of 100, 200 and 400 mg/kg injected by i.p. route in mice caused a significant decrease in the motor activity of animals when compared with the control group. The highest dose of CT significantly reduced the remaining time of the animals on the Rota-rod apparatus up to 2 h. Additionally, CT at doses 100, 200 and 400 mg/ kg (i.p.) was also capable to promote an increase of latency for development of convulsions induced by pentylenetetrazole (PTZ). It was efficient in prevents the tonic convulsions induced by maximal electroshock (MES) in doses of 200 and 400 mg/kg, resulting in 30 and 40 percent of protection, respectively. This compound was also capable to promote an increase of latency for development of convulsions induced by picrotoxin (PIC) at 400 mg/kg. In the same way, the anticonvulsant effect of CT was affected by pretreatment with flumazenil, a selective antagonist of benzodiazepine site of GABA A receptor. These results suggest a possible CNS depressant and anticonvulsant activities.

Anticonvulsant activity of thymoquinone and its structural analogues

It has been widely reported that the crude oil of Nigella sativa L., Ranunculaceae, seeds and its major chemical component thymoquinone present anticonvulsant activity. These facts led us to verify the pharmacological potential of five structurally related para-benzoquinones on the pentylenotetrazol-induced seizures model, and establish the structural characteristics that influence the anticonvulsant activity of thymoquinone. The unsubstituted para-benzoquinone was the compound that exhibited the highest potency, while 2-methyl-p-benzoquinone was inactive. It was found that the presence of alkyl groups attached to the ring influence the pharmacological activity of the para-benzoquinones. In addition, the number, position, and size of these groups change the anticonvulsant potency of the compounds.

Anticonvulsant Activity of Carissa carandas Linn. Root Extract in Experimental Mice

Purpose: The aim of the present study was to investigate anticonvulsant effect of the ethanolic extract of the roots of Carissa carandas (ERCC) on electrically and chemically induced seizures. Methods: The ethanolic extract of the roots of C. carandas (100, 200 and 400 mg/kg, i.p.) was studied for its anticonvulsant effect on maximal electroshock-induced seizures and pentylenetetrazole-, picrotoxin-, bicuculline- and N-methyl-dl-aspartic acid-induced seizures in mice. The latency of tonic convulsions and the number of animals protected from tonic convulsions were noted. Results: ERCC (100-400 mg/kg) significantly reduced the duration of seizures induced by maximal electroshock (MES). However, only 200 and 400mg/kg of the extract conferred protection (25 and 50%, respectively) on the mice. The same doses also protected animals from pentylenetetrazole-induced tonic seizures and significantly delayed the onset of tonic seizures produced by picrotoxin and N-methyl-dl-aspartic acid. The extract had no effect on bicuculline-induced seizures. Conclusion: The data suggest that the ethanolic root extract of C. carandas may produce its anticonvulsant effects via non-specific mechanisms since it reduced the duration of seizures produced by maximal electroshock as well as delayed the latency of seizures produced by pentylenetetrazole and picrotoxin