scholarly journals The Potential Antiepileptic Activity of Astaxanthin in Epileptic Rats Treated with Valproic Acid

2021 ◽  
Author(s):  
Yussra Ata Yaseen Abdulqader ◽  
Hala Salah Abdel Kawy ◽  
Huda Mohammed Alkreathy ◽  
Nisreen Abdullah Rajeh
Keyword(s):  
Valproic Acid ◽  
Antiepileptic Activity

scholarly journals Pharmacophoric Analysis of the Structure of a New 1,3,4-Thiadiazolylamide Derivative of Valproic Acid

Medicina ◽  
2020 ◽  
Vol 8 (3) ◽  
pp. 58-66
Author(s):  
A. S. Malygin ◽  
◽  
V. V. Yasnetsov ◽  
Keyword(s):  
Valproic Acid ◽  
Electron Donor ◽  
Amide Group ◽  
Antiepileptic Activity ◽  
Hydrophobic Moiety

Pharmacophoric analysis of the structure of valprazolamide, a 1,3,4-thiadiazolylamide derivative of valproic acid, was carried out. It was shown that the new valproate contains a substituted amide group, hydrophobic and electron-donor domеns – pharmacophores, determining its antiepileptic activity. Valproic acid has only a hydrophobic moiety. Modification of valproic acid by introducing an additional pharmacophore, 1,3,4-thiadiazole, into its structure leads to a decrease in toxicity and an increase in antiepileptic activity.

Synthesis and Antiepileptic Activity Evaluation of Valproic Acid Derivatives by Niche Chemistry

2020 ◽  
Vol 41 (5) ◽  
pp. 558-562
Author(s):  
Ju Hyun Song ◽  
Song Mi Bae ◽  
Whae Ran Bae ◽  
Jin Sun Huh ◽  
Yu Chen ◽  
...  
Keyword(s):  
Valproic Acid ◽  
Antiepileptic Activity ◽  
Activity Evaluation

scholarly journals Synthesis of a novel amide derivative of valproic acid and 1,3,4-thiadiazole with antiepileptic activity

2020 ◽  
pp. 75-80 ◽  
Author(s):  
A.S. Malygin ◽  
M.A. Demidova ◽  
S.Ya. Skachilova ◽  
E.V. Shilova
Keyword(s):  
Valproic Acid ◽  
High Performance ◽  
Therapeutic Index ◽  
Probit Analysis ◽  
Great Promise ◽  
Antiepileptic Activity ◽  
Amide Derivative ◽  
Amide Derivatives ◽  
Derivatives Of ◽  
Acid Structure

Valproates are commonly used to treat various forms of epilepsy. Problems accompanying their clinical application include drug resistance, adverse effects, acute and chronic toxicity. Safer anticonvulsants with improved efficacy can be obtained through the chemical modification of valproic acid structure. Thiadiazole-linked amide derivatives of valproates hold great promise because 1,3,4-thiadiazole can improve the drug’s bioavailability and reduce its toxicity. The aim of this work was to synthesize a novel amide derivative of valproic acid and 1,3,4-thiadiazole exerting antiepileptic activity. The chemical structure of the synthesized valproate was studied by IR, proton NMR and 13С-NMR-spectroscopy, mass spectroscopy and elemental analysis. The purity and individuality of the compound was confirmed by thin-layer and high-performance liquid chromatography. Its antiepileptic activity was assessed in the test with intraperitoneally injected 250 mg/kg isoniazid and subsequent Probit analysis. The synthesized N-(5-ethyl-1,3,4-thiadiazol-2-yl)-2-propyl pentane amide (valprazolamide) had the following characteristics. ESI+MS: m/z 256.1 [M + H]+; MRM transitions: m/z 256.1 — m/z 81.0 and m/z 130.1. The valproate exerted antiepileptic activity against isoniazid-induced seizures in mice. In the test with isoniazid, ED50 of intraperitoneally injected VPZ was 126.8 mg/kg (95% CI: 65.5–245.4). Its therapeutic index was 7.3.

Trimetazidine potentiates the antiepileptic activity and ameliorates the metabolic changes associated with pentylenetetrazole kindling in rats treated with valproic acid

2017 ◽  
Vol 95 (6) ◽  
pp. 686-696
Author(s):  
Amina Ahmed Sedky ◽  
Osama Mahmoud Hassan El Serafy ◽  
Olfat Ahmed Hassan ◽  
Hala Salah Abdel-kawy ◽  
Amany Helmy Hasanin ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Valproic Acid ◽  
Metabolic Changes ◽  
Anticonvulsant Effect ◽  
Histopathological Changes ◽  
Atherosclerotic Vascular Disease ◽  
Antiepileptic Activity ◽  
Increased Risk ◽  
The Impact ◽  
Oxidative Effect

Oxidative stress is implicated in epileptogenesis as well as in the metabolic changes associated with increased risk of atherosclerotic vascular disease in epilepsy. The present work investigated the impact of the antioxidant trimetazidine (TMZ) on the antiepileptic activity of valproic acid (VPA) and on the metabolic and histological changes in hippocampal, aortic, and hepatic tissues associated with epilepsy and (or) VPA. Rats were divided into non-pentylenetetrazole (non-PTZ) group subdivided into control and VPA-treated groups, and PTZ-treated group subdivided into PTZ, PTZ/VPA, PTZ/TMZ, and PTZ/VPA + TMZ groups. VPA treatment in PTZ rats resulted in an antioxidant effect with improvement in oxidative stress, metabolic and histopathological changes induced by PTZ in hippocampus, aortic, and hepatic tissues. TMZ exhibited anticonvulsant activity and potentiated the anticonvulsant effect of VPA. Combination of TMZ with VPA induced a greater reduction in oxidative stress, improvement in the metabolic and histopathological changes compared to VPA treatment. In contrast, VPA administration in non-PTZ-treated rats induced a pro-oxidative effect, associated with metabolic and histopathological changes in aortic and hepatic tissues. These findings suggest that co-administration of TMZ with VPA in epilepsy might antagonize not only the oxidative stress associated with epilepsy but might also counteract a potential pro-oxidative effect of VPA.

scholarly journals The Effect of Coenzyme Q10 on Liver Injury Induced by Valproic Acid and Its Antiepileptic Activity in Rats

Biomedicines ◽  
2022 ◽  
Vol 10 (1) ◽  
pp. 168
Author(s):  
Fahad Alqarni ◽  
Hala S. Eweis ◽  
Ahmed Ali ◽  
Aziza Alrafiah ◽  
Mohammed Alsieni ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Valproic Acid ◽  
Coenzyme Q10 ◽  
Intraperitoneal Injection ◽  
Therapeutic Potential ◽  
Acid Group ◽  
Control Group ◽  
Anticonvulsant Effect ◽  
Antiepileptic Activity ◽  
Stress Markers

Valproic acid (VPA) has toxic metabolites that can elevate oxidative stress markers, and the hepatotoxicity of VPA has been reported. Coenzyme Q10 (CoQ10) is one of the most widely used antioxidants. The effect of CoQ10 on epileptogenesis and VPA hepatotoxicity were examined. Rats were randomly divided into five groups: the control group received 0.5% methylcellulose by oral gavages daily and saline by intraperitoneal injection three times weekly. The PTZ group received 1% methylcellulose by gavages daily and 30 mg/kg PTZ by intraperitoneal injection three times weekly. The valproic acid group received 500 mg/kg valproic acid by gavage and 30 mg/kg PTZ, as above. The CoQ10 group received 200 mg/kg CoQ10 by gavages daily and 30 mg/kg PTZ, as above. The Valproic acid + CoQ10 group received valproic acid and CoQ10, as above. Results: CoQ10 exhibited anticonvulsant activity and potentiated the anticonvulsant effect of VPA. CoQ10 combined with VPA induced a more significant reduction in oxidative stress and improved the histopathological changes in the brain and liver compared to VPA treatment. In addition, CoQ10 reduced the level of toxic VPA metabolites. These findings suggest that the co-administration of CoQ10 with VPA in epilepsy might have therapeutic potential by increasing antiepileptic activity and reducing the hepatotoxicity of VPA.

794: Valproic Acid Inhibits Prostate Cancer Cell Growth in Vitro and in Vivo

2006 ◽  
Vol 175 (4S) ◽  
pp. 257-257
Author(s):  
Jennifer Sung ◽  
Qinghua Xia ◽  
Wasim Chowdhury ◽  
Shabana Shabbeer ◽  
Michael Carducci ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Valproic Acid ◽  
Cell Growth ◽  
Cancer Cell ◽  
Prostate Cancer Cell ◽  
Cancer Cell Growth

Valproic Acid

2006 ◽  
Vol 36 (7) ◽  
pp. 37
Author(s):  
GIDEON KOREN
Keyword(s):  
Valproic Acid
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