scholarly journals Ichnocarpus frutescens Ameliorates Experimentally Induced Convulsion in Rats

2014 ◽  
Vol 2014 ◽  
pp. 1-9
Author(s):  
Narendra Kumar Singh ◽  
Damiki Laloo ◽  
Debapriya Garabadu ◽  
Tryambak Deo Singh ◽  
Virendra Pratap Singh
Keyword(s):  
Anticonvulsant Activity ◽  
Brain Homogenate ◽  
Root Extract ◽  
Maximal Electroshock ◽  
Behavioral Models ◽  
Amino Butyric Acid ◽  
Stress Markers ◽  
Ichnocarpus Frutescens ◽  
The Brain ◽  
And Oxidative Stress

The present study was carried out to evaluate the anticonvulsant activity and probable mechanism of action of the methanol root extract from I. frutescens (MEIF) using different experimental animal models. Anticonvulsant activity of the single dose of MEIF (100, 200, and 400 mg/kg, p.o.) was evaluated in maximal electroshock- (MES-), pentylenetetrazole- (PTZ-), and isoniazid- (INH-) induced convulsions models in rats. The levels of γ-amino butyric acid (GABA), glutamate, GABA-transaminase (GABA-T) activity and oxidative stress markers were measured in pretreated rat’s brain homogenate to corroborate the mechanism of observed anticonvulsant activity. MEIF (200–400 mg/kg, p.o.) protected the animals in all the behavioral models used. Pretreatment of MEIF (200–400 mg/kg, p.o.) and diazepam (1.0 mg/kg, i.p.) to the animals in INH-induced convulsion model showed 100% and 80% protection, respectively, as well as significant restoration of GABA and glutamate level in the rat’s brain. MEIF and vigabatrin (50 mg/kg, i.p.) reduced the PTZ-induced increase in the activity of GABA-T (46%) in the brain. Further, MEIF reversed the PTZ-induced increase in lipid peroxidase (LPO) and decrease in reduced glutathione (GSH), catalase (CAT), and superoxide dismutase (SOD) activities. The findings of this study validate the anticonvulsant activity of I. frutescens.

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 anxiolytic and anticonvulsant potential of Mirabilis jalapa ethanolic extracts on standardized rat models

2021 ◽  
Vol 23 (09) ◽  
pp. 482-495
Author(s):  
M. Kumar ◽  
◽  
G. Thamotharan ◽  
P. Revathi ◽  
S. Shyji ◽  
...  
Keyword(s):  
Anticonvulsant Activity ◽  
Leaf Extract ◽  
Mental Disease ◽  
Root Extract ◽  
Maximal Electroshock ◽  
Indigenous Plants ◽  
Standard Drug ◽  
Rat Models ◽  
Ethanolic Extracts ◽  
Mirabilis Jalapa

Anxiety and Convulsion are the most prominent, crippled and cruel neurological diseases in recent times. There are many indigenous plants have beneficial properties to treat mental disease and psychic complaints. Evaluation of anxiolytic and anticonvulsant activity of leaf and root ethanolic extracts of mirabilis jalapa in rat models were carried out using standardized experimental methods. The dried leaves and root was macerated with ethanol separately and administered the discern dose of 200 mg/k g p.o. and 400mg/kg p.o. from each extract and employed in Elevated Plus Maze test (EPM) and Open field test (OFT) with 2mg/kg i.p of Diazepam as a standard drug to assess the anxiolytic activity. Maximal electroshock induced convulsion (MES) (Phenytoin-20mg/kg i.p as a standard drug) and Pentylenetetrazol (PTZ) induced seizures analyzed where Diazepam (5mg/kg) i.p as a standard drug to assess the anticonvulsant activity. Substantial changes in all tested activities EPM, OFT in anxiety model and MES, PTZ in anticonvulsant model were observed. The results revealed that ethanol leaf extract (400 mg/kg p.o.) was more impetus due to the high amount of flavonoid, phenolic compounds, steroids, terpenoid contents possess tremendous anti-anxiety whereas the ethanol root extract (400 mg/kg p.o.) and ethanol leaf extract (400 mg/kg p.o.) produce significant anticonvulsant potential effect compared to the control and standard drug treatment group. This study suggested that the plant M. jalapa is a much more active compound consistent medicinal plant to derive a potent drug against anxiety and convulsion.

Screening of Some Novel 4, 5 Disubstituted 1, 2, 4-Triazole-3-thiones for Anticonvulsant Activity

2020 ◽  
Vol 20 (1) ◽  
pp. 41-48 ◽  
Author(s):  
Krishan K. Verma ◽  
Umesh K. Singh ◽  
Jainendra Jain
Keyword(s):  
Drug Administration ◽  
Anticonvulsant Activity ◽  
Motor Coordination ◽  
Docking Study ◽  
Maximal Electroshock ◽  
Gamma Amino Butyric Acid ◽  
Molecular Docking Study ◽  
Amino Butyric Acid ◽  
Mes Test ◽  
Autodock 4.2

Objective: In the present study, we synthesized fifteen 4, 5-disubstituted 1, 2, 4-triazol- 3-thione derivatives and evaluated for anticonvulsant activity with neurotoxicity determination. Method: The synthesized compounds were characterized using FTIR, 1H-NMR and MS. The molecular docking study 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. The anticonvulsant activity was assessed by maximal electroshock (MES) test and subcutaneous pentylenetetrazol (scPTZ) tests. The neurotoxicity was assessed by rotarod ataxia test. Results: In MES test, compounds 5a, 8a and 9a were found active at 100 mg/kg and five compounds were found active at 300 mg/kg dose after 1 hr of administration. After 4 hr of drug administration, only two compounds 8a and 9a exhibited protection at 100 mg/kg. In scPTZ test, three compounds 2a, 6a and 8a were found active at 100 mg/kg and 7a was active at 300 mg/kg after 1 hr of test drug administration. Most of the compounds were found active in MES test with 8a and 9a being the most active among all. In docking study, 2a was found to be best compound based on the binding energy of -6.5 kcal/mol and estimated inhibition constant of 17.2 µM. Conclusion: Majority of synthesized compounds were found active in MES test, whereas only few were found to possess anti scPTZ activity. Among all compounds, only 14a caused motor coordination impairment in rotarod ataxia test at 300 mg/kg 1 hr duration.

scholarly journals Synthesis and Enantioselective Pharmacokinetic/Pharmacodynamic Analysis of New CNS-Active Sulfamoylphenyl Carbamate Derivatives

2021 ◽  
Vol 22 (7) ◽  
pp. 3361
Author(s):  
Reem Odi ◽  
David Bibi ◽  
Bella Shusterman ◽  
Natalia Erenburg ◽  
Chanan Shaul ◽  
...  
Keyword(s):  
Anticonvulsant Activity ◽  
Maximal Electroshock ◽  
Chiral Compounds ◽  
New Class ◽  
Mes Test ◽  
Pharmacodynamic Analysis ◽  
Pharmacokinetic Properties ◽  
Analogous Compound ◽  
Aliphatic Carbon ◽  
The Brain

We recently reported a new class of carbamate derivatives as anticonvulsants. Among these, 3-methylpentyl(4-sulfamoylphenyl)carbamate (MSPC) stood out as the most potent compound with ED50 values of 13 mg/kg (i.p.) and 28 mg/kg (p.o.) in the rat maximal electroshock test (MES). 3-Methylpropyl(4-sulfamoylphenyl)carbamate (MBPC), reported and characterized here, is an MSPC analogous compound with two less aliphatic carbon atoms in its structure. As both MSPC and MBPC are chiral compounds, here, we studied the carbonic anhydrase inhibitory and anticonvulsant action of both MBPC enantiomers in comparison to those of MSPC as well as their pharmacokinetic properties. Racemic-MBPC and its enantiomers showed anticonvulsant activity in the rat maximal electroshock (MES) test with ED50 values in the range of 19–39 mg/kg. (R)-MBPC had a 65% higher clearance than its enantiomer and, consequently, a lower plasma exposure (AUC) than (S)-MSBC and racemic-MSBC. Nevertheless, (S)-MBPC had a slightly better brain permeability than (R)-MBPC with a brain-to-plasma (AUC) ratio of 1.32 (S-enantiomer), 1.49 (racemate), and 1.27 (R-enantiomer). This may contribute to its better anticonvulsant-ED50 value. The clearance of MBPC enantiomers was more enantioselective than the brain permeability and MES-ED50 values, suggesting that their anticonvulsant activity might be due to multiple mechanisms of action.

Neuroprogression in post-traumatic stress disorder

2019 ◽  
pp. 107-128
Author(s):  
Ryan M. Cassidy ◽  
Ives Cavalcante Passos ◽  
Márcia Kauer-Sant’Anna
Keyword(s):  
Post Traumatic Stress Disorder ◽  
Traumatic Stress ◽  
Stress Disorder ◽  
Cognitive Impairments ◽  
Post Traumatic Stress ◽  
Stress Markers ◽  
Post Traumatic ◽  
The Brain ◽  
And Oxidative Stress

Post-traumatic stress disorder (PTSD) has a lifetime prevalence of 10–12% in women and 5–6% in men. Patients with PTSD are at greater risk for obesity, type 2 diabetes mellitus, atherosclerosis, and myocardial infarction. In addition, a subset of these patients develops cognitive impairments unattributable to age or disease comorbidity alone, with hippocampal and prefrontal cortex atrophy. This chapter aims to review the evidence for neuroprogression in PTSD. This concept has been proposed as the pathological rewiring of the brain that takes place in parallel with the clinical and neurocognitive deterioration in the course of some psychiatric disorders. We will also review the biological pathways underlying neuroprogression in PTSD, including changes in inflammatory cytokines, corticosteroids, neurotrophins, and oxidative stress markers.

Protective role of peroxiredoxin-4 in heart failure

2020 ◽  
Vol 134 (1) ◽  
pp. 71-72
Author(s):  
Naseer Ahmed ◽  
Masooma Naseem ◽  
Javeria Farooq
Keyword(s):  
Heart Failure ◽  
Cardiac Fibroblasts ◽  
Protective Role ◽  
Oxidative Stress Markers ◽  
Stress Markers ◽  
Total Antioxidant ◽  
Galectin 3 ◽  
Consequent Increase ◽  
And Oxidative Stress

Abstract Recently, we have read with great interest the article published by Ibarrola et al. (Clin. Sci. (Lond.) (2018) 132, 1471–1485), which used proteomics and immunodetection methods to show that Galectin-3 (Gal-3) down-regulated the antioxidant peroxiredoxin-4 (Prx-4) in cardiac fibroblasts. Authors concluded that ‘antioxidant activity of Prx-4 had been identified as a protein down-regulated by Gal-3. Moreover, Gal-3 induced a decrease in total antioxidant capacity which resulted in a consequent increase in peroxide levels and oxidative stress markers in cardiac fibroblasts.’ We would like to point out some results stated in the article that need further investigation and more detailed discussion to clarify certain factors involved in the protective role of Prx-4 in heart failure.

Comparison of Salivary Antioxidants and Oxidative Stress Status in Gestational Diabetes Mellitus and Healthy Pregnant Women

2020 ◽  
Vol 20 ◽  
Author(s):  
Fatemeh Ahmadi-Motamayel ◽  
Shima Fathi ◽  
Mohammad Taghi Goodarzi ◽  
Shiva Borzouei ◽  
Jalal Poorolajal ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Diabetes Mellitus ◽  
Gestational Diabetes ◽  
Pregnant Women ◽  
Oxidative Stress Markers ◽  
Blood Samples ◽  
Stress Markers ◽  
Total Antioxidant ◽  
Total Oxidative Stress ◽  
And Oxidative Stress

Background: One of the most common complications of pregnant women is gestational diabetes mellitus (GDM). Oxidative stress can play an important role in GDM. Objective: The aim of this study was to evaluate salivary antioxidants and oxidative stress markers in GDM. Method: Twenty pregnant women with GDM and 20 healthy pregnant women with normal blood glucose test participated in this study. Five mL of unstimulated saliva samples were collected. Spectrophotometric assay was carried out for sialochemical analysis. Stata software was used for data analysis. Results: The GDM group exhibited no significant difference in salivary total antioxidant capacity and malondialdehyde compared to the healthy control group. All of antioxidants markers, the uric acid, total antioxidant, peroxidase and catalase, decreased in GDM group that the difference of peroxidase and catalase was statistically significant. All of oxidative stress markers, the salivary malondyaldehid, total oxidative stress and total thiol, increased in GDM group. GDM group exhibited significantly higher salivary total oxidative stress levels. Conclusion: Catalase level was significantly lower and total oxidative stress was significantly higher. These two markers might have significant importance and might exhibit early changes compared to other factors in GDM. . Some of salivary antioxidants might have diagnostic, prognostic or therapeutic implications in GDM. Other studies with large sample size on salivary and blood samples need to be done to confirm this properties and salivary samples using instead of blood samples in GDM biomarkers changes.

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.

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