scholarly journals Comparative estimation of anticonvulsant activity of cumarines umbelliferone, obtusifole and Haplofillum obtusifolium grass decoction

2015 ◽  
Vol 13 (2) ◽  
pp. 49-53
Author(s):  
Oleg Dmitrievich Barnaulov
Keyword(s):  
Anticonvulsant Activity ◽  
Maximal Electroshock ◽  
Unconditioned Reflex ◽  
Traditional Medicines ◽  
Enteral Administration ◽  
Low Toxicity

Obtusifole and umbelliferone had low toxicity after enteral administration. Even high obtusifole doses demonstrated weak anticonvulsant activity in the models of maximal electroshock (MES) and pentamethylentetrasole seizures (LD 100). These coumarines were not effective in the models of strychnine- and thiosemycarboside-induced convulsions. They revealed neurotoxical influence, reducing unconditioned reflex, normal adoptive mice behavior and did not prevent the loss of conditioned passive avoiding reflex (CPAR) after MES. These coumarines did not antagonize with synthetic anticonvulsants. The Haplophyllum obtusifolium grass decoction administered enterally was not toxic, because LD minimal might not be fixed. It had no neurotoxical properties, prevented the loss of CPAR and mortality after MES, elevated tolerance to convulsive-mortal pentamethylentetrasole and strychnine action. So this decoction demonstrated cerebroprotective properties. The use of Haplophyllum obtusifolium in traditional medicines of Asiatic states may not be explained by only coumarines. It is based on cerebroprotective properties of this medicine.

Synthesis and Anticonvulsant Activity of 3-(alkylamino, alkoxy)-1,3,4,5- Tetrahydro-2H-benzo [b] azepine-2-one Derivatives

2018 ◽  
Vol 17 (6) ◽  
pp. 448-457 ◽  
Author(s):  
Xia Huang ◽  
Tie Chen ◽  
Rong-Bi Han ◽  
Feng-Yu Piao
Keyword(s):  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Anticonvulsant Activity ◽  
Mass Spectra ◽  
Maximal Electroshock ◽  
Test Compound ◽  
Maximal Electroshock Test ◽  
Mes Test ◽  
Structure Activity

Background & Objective: A series of novel 3-Substituted-1,3,4,5-Tetrahydro-2H-benzo [b] azepine-2-one Derivatives (4, 5, 7, 10, 12, 5a-j, 8a-e) were synthesized from 1,2,3,4-Tetrahydro-1- naphthalenone. The structures of these compounds were confirmed by IR, 1H NMR, 13C NMR, MASS spectra and elemental analysis. Their anticonvulsant activity was evaluated by the maximal electroshock (MES) test, subcutaneous pentylenetetrazol (scPTZ) test, and their neurotoxicity was evaluated by the rotarod neurotoxicity test. Compound 4 showed the maximum anticonvulsant activity against the maximal electroshock test (ED50=26.4, PI =3.2) and against the subcutaneous pentylenetetrazol test (ED50=40.2, PI =2.1). Conclusion: Possible structure-activity relationship was discussed.

scholarly journals Synthesis, Anticonvulsant and Neurotoxicity Screening of Some Novel 2, 5-Disubstituted - 1, 3, 4 � Oxadiazole Derivatives

2017 ◽  
Vol 9 (01) ◽  
Author(s):  
Y. Khatoon ◽  
M. Shaquiquzzaman ◽  
V. Singh ◽  
M. Sarafroz
Keyword(s):  
Sodium Hydroxide ◽  
1H Nmr ◽  
Elemental Analysis ◽  
Neurological Deficit ◽  
Anticonvulsant Activity ◽  
Sodium Hydroxide Solution ◽  
Maximal Electroshock ◽  
Rota Rod Test ◽  
Oxadiazole Derivatives ◽  
Ft Ir

A series of 2, 5-disubstituted - 1, 3, 4 oxadiazoles (4a-o) were synthesized on refluxing hydrazine carbothioamides with iodine and potassium iodide in ethanolic sodium hydroxide solution starting from methyl-3-amino-4-hydroxy benzoate via synthesis of an intermediate methyl-2-substitutedaryl-1, 3-benzoxazole-5-carboxylates and 2-substitutedaryl-1, 3-benzoxazole-5-carbohydrazides. The newly synthesized compounds were characterized on the basis of spectral (FT-IR, 1H-NMR, MS) and elemental analysis. All these compounds were screened for anticonvulsant activity using Maximal Electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) method. Anticonvulsant activity was shown by majority of the synthesized compounds when given i.p. to mice. Among the tested compounds 4e, 4j and 4o were considered to have potent anticonvulsant activity comparable to that of standard drugs Phenytoin and Carbamazepine. Compounds 4e, 4g, 4h, 4i, 4k and 4m passed the rota rod test successfully without any sign of neurological deficit.

Design, Synthesis and Biological Activity of Some 4, 5-Disubstituted-2, 4- Dihydro-3H-1, 2, 4- Triazole-3-Thione Derivatives

2019 ◽  
Vol 19 (3) ◽  
pp. 197-205 ◽  
Author(s):  
Krishan Kumar Verma ◽  
Umesh Kumar Singh ◽  
Jainendra Jain
Keyword(s):  
Biological Activity ◽  
1H Nmr ◽  
Anticonvulsant Activity ◽  
Maximal Electroshock ◽  
Gamma Amino Butyric Acid ◽  
Rotarod Test ◽  
Design Synthesis ◽  
Amino Butyric Acid ◽  
Mes Test ◽  
Autodock 4.2

Background: In the present study, 4, 5-disubstituted triazol-3-thione derivatives were synthesized and evaluated for anticonvulsant activity along with neurotoxicity determination. Materials and Methods: The synthesized compounds were characterized using FTIR, 1H-NMR and MS. The anticonvulsant activity was assessed by Maximal Electroshock (MES) test and subcutaneous Pentylenetetrazole (scPTZ) tests and neurotoxicity was assessed by rotarod test. Docking was also performed to study the interactions of compounds with LYS329 residue of gamma amino butyric acid aminotransferase (GABA-AT) using Autodock 4.2 software. Results: The compounds 7a and 9a with significant pharmacological activity were also found to interact with LYS329 residue of GABA-AT by H-bond with a docking score of -5.92 kcal/mol (Ki = 41.99 μM) and -5.87 kcal/mol (Ki = 49.83 μM) respectively. Conclusion: Most of the compounds were found to be active in MES test but only seven showed protection in scPTZ test.

Evaluation of the Anticonvulsant Activity of Terpinen-4-ol

2009 ◽  
Vol 64 (1-2) ◽  
pp. 1-5 ◽  
Author(s):  
Damião P. de Sousa ◽  
Franklin F. F. Nóbrega ◽  
Liana C. S. L. de Morais ◽  
Reinaldo N. de Almeida
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Animal Models ◽  
Motor Activity ◽  
Anticonvulsant Activity ◽  
Maximal Electroshock ◽  
Aromatic Plants ◽  
Depressant Effect ◽  
Maximal Electroshock Seizure ◽  
The Central Nervous System

Terpinen-4-ol is a monoterpenoid alcohol and component of the essential oils of several aromatic plants. Similarly to terpinen-4-ol, other monoterpenoid alcohols have shown anticonvulsant activity in convulsion animal models. The present study aimed to investigate the anticonvulsant activity of terpinen-4-ol. Treatment of mice with terpinen-4-ol ( 200 mg/kg) caused a signifi cant decrease in the spontaneous motor activity at 30, 60 and 120 min after administration. Terpinen-4-ol (100 and 200 mg/kg) produced a significant dosedependent increase in the duration of sleeping in mice. Pretreatment of mice with terpinen-4- ol at doses of 100, 200 and 300 mg/kg significantly increased the latency of pentylenetetrazole -induced convulsions. Terpinen-4-ol (200 and 300 mg/kg) also inhibited the induced seizures of picrotoxin. In another model, maximal electroshock seizure, terpinen-4-ol decreased the tonic hind convulsions percentage at the dose of 300 mg/kg. From the overall results we can conclude that terpinen-4-ol showed a depressant effect on the central nervous system and significant anticonvulsant activity.

scholarly journals Evaluation of Anticonvulsant and Antioxidant Activity of Senna occidentalis Seeds Extracts

2019 ◽  
Vol 9 (2) ◽  
pp. 183-187
Author(s):  
Vijay Vikram Singh ◽  
Jainendra Jain ◽  
Arun Kumar Mishra
Keyword(s):  
Antioxidant Activity ◽  
Ascorbic Acid ◽  
Anticonvulsant Activity ◽  
Future Research ◽  
Maximal Electroshock ◽  
Formulation Development ◽  
Dpph Method ◽  
Dose Dependent Fashion ◽  
Seizure Model ◽  
Dose Dependent

Aim: The aim of present work was to determine the anticonvulsant and antioxidant activity of Senna occidentalis L. ethanolic seed extract by different mod­els. Methods: For evaluation of anticonvulsant activity, Pentylenetetrazole (PTZ) seizure model and Maximal electroshock (MES) seizure model were used. For antioxidant activity, (1, 1-diphenyl - 2-picryl hydrazine (DPPH) and hydrogen peroxide (H2O2) method were used. Results: The finding suggested that the ethanolic extract (EAE) of Senna occidentalis in the dose 400 mg/kg body weight posses potent anticonvulsant activity. The EAE showed anticonvulsant action in dose dependent fashion. It was observed that upon increasing the concentration of extract, it showed reduced absorbance and increased free radical inhibition, and when comparison was made with Ascorbic acid, it showed marked antioxidant property in DPPH as well as H2O2 method. The IC50 of Ascorbic acid and EAE by DPPH method were found to be 14.56 and 14.8 respectively whereas the IC50 of Ascorbic acid and EAE by H2O2 method were found that 14.3and 14.8 respectively. Conclusion: The results of the present study concluded hat the EAE of Senna occidentalis L. possesses significant antioxidant and anticonvulsant activity. The activity was in dose dependent fashion. This study will assist in future research associated with formulation development of seeds of Senna occidentalis L. Keyword: Senna occidentalis L., Anticonvulsant, Antioxidant, DPPH model

scholarly journals A Review on anti-epileptic activity of seaweed Ecklonia cava

2019 ◽  
Vol 9 (1-s) ◽  
pp. 425-432 ◽  
Author(s):  
Samiat Abimbola Owoalade ◽  
Diana Moria Martin Lou ◽  
Kashikant Yadav ◽  
Sumitra Poudel
Keyword(s):  
Anticonvulsant Activity ◽  
Wistar Rats ◽  
Wistar Rat ◽  
Epileptic Activity ◽  
Ecklonia Cava ◽  
Laboratory Animals ◽  
Maximal Electroshock ◽  
Antiepileptic Activity ◽  
Chemically Induced ◽  
Experimental Laboratory

The Present study was undertaken to investigate the Anticonvulsant activity of sea weed extract of Ecklonia cava on electrically and chemically induced seizures in wistar rat. The methanolic seaweed extract was studied for its anticonvulsant activity by using experimental paradigms like Maximal electroshock-induced seizures (MES). Expected to exhibited protection against tonic convulsions induced by MES in wistar rats. Objective of these studies were designed to screen the antiepileptic activity of the seaweed Ecklonia cava in experimental laboratory animals. Keywords: Antiepileptic Activity, Ecklonia cava (E.C), seizures, Flexon, Hind Limb Extension, Electroencephalography (EEG)

scholarly journals EVALUATION OF ANTICONVULSANT ACTIVITY OF CALLISTEMON CITRINUS (CURTIS) SKEELS (MYRTACEAE) VOLATILE OIL

2021 ◽  
Vol 2 (2) ◽  
pp. 117-125
Author(s):  
R. O. Imade ◽  
A. M. Akhigbemen ◽  
A. Uchendu ◽  
C. L. Onyeagoro
Keyword(s):  
Anticonvulsant Activity ◽  
Conventional Medicine ◽  
Volatile Oil ◽  
Positive Control ◽  
Maximal Electroshock ◽  
Acute Toxicity Test ◽  
Orthodox Medicine ◽  
Leg Extension ◽  
Model C ◽  
Dose Dependent

The use of medicinal plants is on the rise due to the increase of various diseases and shortcomings of orthodox medicine. For many ailments including convulsion, conventional medicine has not been able to find a lasting solution. This study was directed towards assessing the ethnomedicinal use of Callistemon citrinus leaves in the management of convulsion. The volatile oil of the leaves was extracted and an acute toxicity test was carried out following Lorke’s description. Maximal electroshock (MES), strychnine and pentylenetetrazol anticonvulsant methods were used. Separate groups of albino mice were given 200, 400 and 800 mg/kg doses of the volatile oil. Drug solutions; 30 mg/kg phenobarbitone for MES and 2 mg/kg diazepam for strychnine and pentylenetetrazol models were administered as a positive control. The start of tonic leg extension, duration and percentage mortality was recorded. Doses of 200 and 400 mg/kg significantly (P<0.05) inhibited seizure in the mice with scores of 40 % each in the MES model. There was a dose-dependent reduction in the duration of seizures with 68.47, 70.27 and 81.08 % reductions in the pentylenetetrazol model. No significant coverage was given in the strychnine model. C. citrinus oil protected the mice against pentylenetetrazol and maximal electroshock-induced convulsion hence could contribute to the medical treatment of epilepsy.

scholarly journals Adenosine receptor agonists differentially affect the anticonvulsant action of carbamazepine and valproate against maximal electroshock test-induced seizures in mice

2017 ◽  
Vol 25 (1-2) ◽  
pp. 21-29
Author(s):  
Mirosław Jasiński ◽  
Magdalena Chrościńska-Krawczyk ◽  
Stanisław J. Czuczwar
Keyword(s):  
Adenosine Receptor ◽  
Anticonvulsant Activity ◽  
Pharmacokinetic Interaction ◽  
Maximal Electroshock ◽  
Protective Activity ◽  
Adenosine Receptor Agonists ◽  
Brain Concentration ◽  
Receptor Agonists ◽  
Adenosine Agonists ◽  
Free Plasma

SummaryBackground.Adenosine is regarded as an endogenous anticonvulsant and its agonists have been proved to affect the anticonvulsant activity of a number of antiepileptic drugs (AEDs) in animal models of seizures.Aim.To evaluate effects of adenosine agonists on carbamazepine (CBZ) and valproate (VPA) in mouse model of generalized tonic-clonic convulsions.Methods.The following adenosine receptor agonists were used: A1– cyclohexyladenosine, A2A– CGS 21 680, A3– N6-benzyl-NECA and A1(preferentially) and A2– 2-chloroadenosine. Their possible anticonvulsant effects were studied in a threshold electroconvulsive test for maximal electroconvulsions. The protective activity of AEDs alone or in combinations with adenosine agonists was evaluated in the form of their respective ED50values necessary to protect 50% of mice against tonic extension of the hind limbs, following maximal electroshock, delivered through ear electrodes. The specificity of interactions between AEDs and adenosine agonists was challenged with an adenosine receptor A1and A2antagonist, aminophylline (5 mg/kg). The effects of AEDs alone or with adenosine agonists were tested for the occurrence of adverse effects (AE) (impairment of motor coordination) in a chimney test. All combinations with an enhancement the protective activity of CBZ or VPA were verified with the free plasma or brain concentration of these AED.Results.Adenosine receptor agonists (cycloheksyladenosine up to 4 mg/kg; CGS 21 680 – 8 mg/kg; N6-benzyl-NECA – 1 mg/kg; 2-chloroadenosine – 2 mg/kg) did not significantly affect the threshold for maximal electroconvulsions. Cycloheksyladenosine (1 mg/kg), N6-benzyl-NECA (0.5 and 1 mg/kg) and 2-chloroadenosine (1 mg/kg) potentiated the anticonvulsant activity of CBZ. Valproate’s protective action was enhanced by one adenosine agonist – cycloheksyladenosine (1 mg/kg). Only the combination of CBZ + N6-benzyl-NECA (1 mg/kg) was resistant to aminophylline (5 mg/kg). Pharmacokinetic interactions were evident in case of the combination of CBZ + N6-benzyl-NECA (1 mg/kg) and resulted in an increased free plasma concentration of this CBZ. Interestingly, total brain concentration of CBZ confirmed the pharmacokinetic interaction as regards CBZ + N6-benzyl-NECA (1 mg/kg).Conclusion.The best profile was shown by the combination of CBZ + 2-chloroadenosine which involved no AE or a pharmacokinetic interaction. The remaining positive combinations in terms of anticonvulsant activity were associated with general profound AE and pharmacokinetic interactions in some of them.

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