scholarly journals Effect of Ellagic Acid on Seizure Threshold in Two Acute Seizure Tests in Mice

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4841
Author(s):  
Mateusz Pieróg ◽  
Katarzyna Socała ◽  
Elżbieta Wyska ◽  
Ewa Poleszak ◽  
Piotr Wlaź
Keyword(s):  
Animal Models ◽  
Ellagic Acid ◽  
Motor Coordination ◽  
Clonic Seizure ◽  
Seizure Threshold ◽  
Maximal Electroshock ◽  
Maximal Electroshock Seizure ◽  
Neuroprotective Effects ◽  
Total Brain ◽  
Acute Seizure

Ellagic acid (EA) is a natural dietary polyphenol that has many beneficial properties, including anti-inflammatory, antioxidant, antiviral, antibacterial, and neuroprotective effects. Studies have revealed that EA may modulate seizure activity in chemically induced animal models of seizures. Therefore, the aim of the present study was to investigate the effect of EA on the seizure threshold in two acute seizure tests in male mice, i.e., in the intravenous (i.v.) pentylenetetrazole (PTZ) seizure test and in the maximal electroshock seizure threshold (MEST) test. The obtained results showed that EA (100 mg/kg) significantly elevated the threshold for both the first myoclonic twitch and generalized clonic seizure in the i.v. PTZ seizure test. At the highest dose tested (200 mg/kg), EA increased the threshold for tonic hindlimb extension in the MEST test. EA did not produce any significant changes in motor coordination (assessed in the chimney test) or muscular strength (investigated in the grip-strength test). The plasma and total brain concentration-time profiles of EA after intraperitoneal and oral administration were also determined. Although further studies are necessary to confirm the anticonvulsant activity of EA, our findings suggest that it may modulate seizure susceptibility in animal models.

scholarly journals Salvinorin A Does Not Affect Seizure Threshold in Mice

Molecules ◽  
2020 ◽  
Vol 25 (5) ◽  
pp. 1204
Author(s):  
Katarzyna Socała ◽  
Urszula Doboszewska ◽  
Piotr Wlaź
Keyword(s):  
Opioid Receptor ◽  
Muscular Strength ◽  
Motor Coordination ◽  
Clonic Seizure ◽  
Seizure Threshold ◽  
Salvinorin A ◽  
Maximal Electroshock ◽  
Threshold Test ◽  
Opioid Receptor Agonist ◽  
Chimney Test

The κ-opioid receptor has recently gained attention as a new molecular target in the treatment of many psychiatric and neurological disorders including epilepsy. Salvinorin A is a potent plant-derived hallucinogen that acts as a highly selective κ-opioid receptor agonist. It has unique structure and pharmacological properties, but its influence on seizure susceptibility has not been studied so far. Therefore, the aim of the present study was to investigate the effect of salvinorin A on seizure thresholds in three acute seizure tests in mice. We also examined its effect on muscular strength and motor coordination. The obtained results showed that salvinorin A (0.1–10 mg/kg, i.p.) did not significantly affect the thresholds for the first myoclonic twitch, generalized clonic seizure, or forelimb tonus in the intravenous pentylenetetrazole seizure threshold test in mice. Likewise, it failed to affect the thresholds for tonic hindlimb extension and psychomotor seizures in the maximal electroshock- and 6 Hz-induced seizure threshold tests, respectively. Moreover, no changes in motor coordination (assessed in the chimney test) or muscular strength (assessed in the grip-strength test) were observed. This is a preliminary report only, and further studies are warranted to better characterize the effects of salvinorin A on seizure and epilepsy.

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 Fluoxetine enhances maximal electroshock seizure threshold in Albino rat model when compared to phenytoin

2017 ◽  
Vol 7 (1) ◽  
pp. 138 ◽  
Author(s):  
Tanmoy Gangopadhyay ◽  
Ananya Mandal ◽  
Uma Shanker Keshri
Keyword(s):  
Seizure Threshold ◽  
Albino Rats ◽  
P Value ◽  
Anticonvulsant Effect ◽  
Maximal Electroshock ◽  
Maximal Electroshock Seizure ◽  
Albino Rat ◽  
Co Morbidity ◽  
Significant Difference ◽  
Electroconvulsive Seizure

Background: Individuals with epilepsy have a higher incidence of psychiatric disorders than person without epilepsy. Epidemiological studies have shown that the co-morbidity of epilepsy and depression to be high as 50%. The conventional anti-depressants are believed to lower the seizure threshold making it difficult to treat the co-morbid depression, but animal studies have shown SSRIs, a common anti-depressant, to have anti-convulsant properties. So, we propose to study the anticonvulsant effects of fluoxetine, a SSRI, in albino rats against maximal electroshock seizure and to compare against a standard antiepileptic drug phenytoin.Methods: The anticonvulsant effect of fluoxetine was observed in model of maximal electroconvulsive seizure threshold in albino rats. The animals were divided into 3 groups having 6 animals each, receiving distilled water, fluoxetine and phenytoin respectively. The drugs were given orally, and the effect was observed on day 7, 14 and 21. Tonic hind-limb extension was taken as the parameter of electroshock seizure. The effects were compared against a standard anti-seizure drug phenytoin.Results: Fluoxetine showed significant elevation of the seizure threshold following 14 days of administration (P value 0.031). The effect was comparable to phenytoin with no significant difference after 7, 14 and 21 days of treatment (P-value 0.485, 0.699 and 0.818 respectively) though phenytoin showed significant anti-seizure effect since day 7 of treatment.Conclusions: Fluoxetine showed significant anti-seizure activity against electroconvulsive seizure in albino rats.

Discovery of novel substituted N-(6-Chloro-3-cyano-4-phenyl-4H-chromen-2-yl)-2-(4-chloro-phenoxy)-acetamide for biphasic anticancer and anticonvulsant activities

2019 ◽  
Vol 15 ◽  
Author(s):  
Divya Chauhan ◽  
Syed Riaz Hashim ◽  
Priyanka Rani ◽  
Sushil Kumar ◽  
Navratan Shrimal ◽  
...  
Keyword(s):  
Wistar Rats ◽  
Computational Study ◽  
Colon Adenocarcinoma ◽  
Human Colon ◽  
Pharmacokinetic Profile ◽  
Seizure Threshold ◽  
Anticonvulsant Effect ◽  
Maximal Electroshock ◽  
Maximal Electroshock Seizure ◽  
Ht 29

Background : Privileged 4H-chromenes possess the potent anticancer and anticonvulsant actives. By inspiring potency of 4H-chromenes and demands of present era of scaffold, discovery of effective molecule was carried out for the treatment of cancer and conversant. Objective : Designed and synthesized a novel series of 4H-chromene derivatives from one port synthesis for the treatment of cancer and conversant. Method : Substitution of side amide chain was formed in multiple steps on amine group of chromene. Later, anticancer activity of synthesized compounds was investigated against human colon adenocarcinoma cell line (HT-29) using sulforhodamine B (SRB) assay. Moreover, anticonvulsant activity was also screened out by using maximal electroshock seizure (MES) model and subcutaneous Metrazol Seizure Threshold Test (scMET) in albino Wistar rats. Neurotoxicity was evaluated using by rotarod test. Before the synthesis, docking studies were performed using various molecular targets. Subsequently, the computational study of the titled compounds was performed to predict the pharmacokinetic profile. Result: Among the fifteen tested compounds, A4 and A9 were found to be active against HT-29 cells (growth inhibitory dose 50% (GI50) <11µM). Moreover, compounds A4 showed the protection at 300mg/kg in scMET (h) for albino Wistar rats and compounds A9, A11, A15 exhibited the anticonvulsant effect at the doses 100, 300 and 300 mg/kg, respectively in MES screen(h). Conclusion : Due to these encouraging results, we concluded that both A4 and A9 may be effective against colon cancer. While compound A9 may be used as a considerable effective molecule for the treatment of epilepsy.

scholarly journals EVALUATION OF ANTI-SEIZURE ACTIVITY OF SIDA RHOMBIFOLIAALONE AND IN COMBINATION WITH ANTI-SEIZURE DRUGS IN SWISS ALBINO MICE

2020 ◽  
pp. 1-3
Author(s):  
Ruchika Kalra ◽  
Bhargav Purohit ◽  
Ashish Anovadiya
Keyword(s):  
Sodium Valproate ◽  
Seizure Activity ◽  
Antioxidant Property ◽  
Clonic Seizure ◽  
High Dose ◽  
Absence Seizure ◽  
Maximal Electroshock ◽  
Maximal Electroshock Seizure ◽  
Tonic Extension ◽  
Sida Rhombifolia

Background-Anti-seizure activity of Sida Rhombifolia in low (300mg/kg) and high doses(600mg/kg) and its combination with Phenytoin(50mg/kg) and Sodium valproate(300mg/kg) were studied in chronic model (14 days) of Maximal Electroshock Seizure (MES) and Pentylenetetrazole (PTZ) induced seizure respectively. Methods- Anti-seizure activity of Sida Rhombifolia on generalized tonic-clonic seizure and absence seizure was evaluated using standard maximal electroshock seizure method and pentylenetetrazole test. Results- In MES induced seizures Sida Rhombifolia in high dose prevented both tonic extension and tonic flexion. In PTZ induced seizures Sida Rhombifolia in high dose significantly (p<0.001) increase the latency of onset of seizures and both high and low dose Sida Rhombifolia significantly decrease the duration of seizure (p<0.01) as compared to vehicle control, however, there was no significant effect on onset of 1st myoclonic jerk (p>0.05). The addition of Sida Rhombifolia to the sub- therapeutic dose of sodium valproate and phenytoin showed a synergistic effect. Conclusion- Inhibition of seizure by Sida Rhombifolia could be due to the presence of flavonoids that acts as a partial positive allosteric modulator at GABAA (γ-aminobutyric acid) receptors, penetrates the blood-brain barrier and possess the anti-convulsant activity and also because of its antioxidant property. Sida Rhombifolia can be effective in generalized tonic-clonic seizures alone and as add on with sodium valproate for absence seizures.

Synthesis and Anticonvulsant Activity of α-Amino Acid Amide Derivatives

2019 ◽  
Vol 15 (5) ◽  
pp. 547-561
Author(s):  
Valerie Currier ◽  
Maryam Molki ◽  
Katelyn Fryman ◽  
Lacey D. Rodgers ◽  
A. Michael Crider
Keyword(s):  
Amino Acid ◽  
Side Effects ◽  
Anticonvulsant Activity ◽  
Acid Amide ◽  
New Drugs ◽  
Seizure Threshold ◽  
Maximal Electroshock ◽  
Maximal Electroshock Seizure ◽  
Maximal Electroshock Seizure Test ◽  
Amide Derivatives

Background: Epilepsy is a disease of the central nervous system that affects approximately 50 million individuals worldwide. Although several new drugs have been marketed in the last 25 years, almost one-third of patients are not protected. In many cases, currently available drugs produce undesirable side effects. As a result, a need exists for novel anticonvulsants with unique mechanisms of action and minimal side effects. Methods: A mixed anhydride coupling procedure and standard deprotection procedures were utilized to prepare 36 α-amino acid amides. All final products were evaluated in mice and rats utilizing a standard battery of anticonvulsant tests. Results: α-Amino acids containing a 2,6-dimethylanilide group exhibited anticonvulsant activity in the maximal electroshock seizure test and 6 Hz test in mice and rats. A small, branched-chain on the α- carbon generally maintained or enhanced anticonvulsant activity in the maximal electroshock seizure test. The (R)-α-amino acid amides were typically more potent and slightly more neurotoxic than the corresponding (S)-enantiomers. The valine dimethylanilide (R)-42 was highly active in the MES test in mice (ED50 = 3.6mg/kg) and rats (ED50 = 3.8 mg/kg). (R)-42 also demonstrated excellent anticonvulsant activity in the 6 Hz, picrotoxin, and corneal kindled mouse tests. Furthermore, (R)-42 did not lower seizure threshold when evaluated in the intravenous metrazol seizure test. Conclusion: α-Amino acid 2,6-dimethylanilides exhibited potent activity in a variety of anticonvulsant tests in mice and rats. The valine derivative (R)-42 represents a promising compound for potential use in complex partial seizures.

scholarly journals Design, synthesis and anticonvulsant-analgesic activity of new N-[(phenoxy)alkyl]- and N-[(phenoxy)ethoxyethyl]aminoalkanols

MedChemComm ◽  
2017 ◽  
Vol 8 (1) ◽  
pp. 220-238 ◽  
Author(s):  
Anna Rapacz ◽  
Anna M. Waszkielewicz ◽  
Katarzyna Pańczyk ◽  
Karolina Pytka ◽  
Paulina Koczurkiewicz ◽  
...  
Keyword(s):  
Analgesic Activity ◽  
Anticonvulsant Activity ◽  
Seizure Threshold ◽  
Maximal Electroshock ◽  
Maximal Electroshock Seizure ◽  
Design Synthesis ◽  
Electroshock Seizure Threshold

New aminoalkanols have been synthesized and evaluated for their anticonvulsant activity in maximal electroshock (MES), maximal electroshock seizure threshold (MEST) and pentylenetetrazol (PTZ) tests, and show promising activity.

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