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anticonvulsant potential of rosuvastatin in combination with carbamazepine and valproate in animal models of epilepsy

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World Journal of Methodology 2025年第2期15卷 137-144页

作者： Vandana Tayal Akash Mandal Ijasul Haque M Akhilesh Mishra Bhupinder S Kalra Vandana Roy Department of Pharmacology Maulana Azad Medical CollegeNew Delhi 110002India Department of Pharmacology MES Medical CollegePerintalmanna 679338KeralaIndia Department of Central Animal Facility Maulana Azad Medical CollegeNew Delhi 110002India

BACKGROUND Epilepsy impacts millions of people,with many not responding to existing *** evidence links neuroinflammatory processes to *** exhibit anti-inflammatory and neuroprotective properties,potentially offering antiepileptic *** To evaluate the anticonvulsant effects of rosuvastatin in animal models of *** Ninety-six albino mice were divided into 16 *** the maximal electroshock seizure(MES)model,eight groups received intraperitoneal vehicle,carbama-zepine,rosuvastatin,or a *** measured included seizure protection[tonic hind limb extension(THLE)],duration of THLE,seizure duration,and *** the pentylenetetrazol(PTZ)model,eight groups were pretreated with vehicle,valproate,rosuvastatin,or a combination,with outcomes measured as seizure latency,seizure duration,and *** In the MES model,rosuvastatin exhibited protection against THLE in a small percentage of *** shortens the duration of THLE in a dose-dependent ***,none of these were statistically significant com-pared to the control *** combination of rosuvastatin 10 mg/kg with carbamazepine 4 mg/kg resulted in a significant reduction in seizure duration compared to the control group,better than carbamazepine alone at 4 mg/kg and 6 mg/*** the PTZ model,rosuvastatin alone showed no significant effects on latency,duration of seizure,or ***,rosuvastatin 10 mg/kg combined with valproate 100 mg/kg significantly delayed the onset of seizures,seizure duration and mortality percentage,better than valproate alone at 100 mg/*** Rosuvastatin enhanced the anticonvulsant effects of carbamazepine and *** studies are required to explore the antiepileptic potential of rosuvastatin at various doses,durations,dosage forms,routes and models.

关键词： Antiepileptic anticonvulsant Statins Rosuvastatin Maximal electroshock seizure Pentylenetetrazol

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anticonvulsant effects of medicinal plants with emphasis on mechanisms of action

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Asian Pacific Journal of Tropical Biomedicine 2017年第2期7卷 166-172页

作者： Zahra Rabiei Medical Plants Research Center Shahrekord University of Medical ScienceShahrekordIran

Epilepsy is a disorder in brain in which clusters of nerve cells, or neurons, occasionally signal abnormally and cause strange emotions, sensations, and behavior, or sometimes muscle spasms, convulsions, and loss of consciousness. Neurotransmitters in central nervous system greatly affect and play a very important part in neuronal *** treatments are still a component of health care system in many communities despite the fact that well-established alternatives are available. In this review article, we addressed epilepsy and its treatments with emphasis on medical plants and introduction of antiepileptic plants and their action mechanisms. Relevant articles published since 2010 were retrieved using the search terms including epileptic seizure, anticonvulsant, medicinal plants, and oxidative stress. Most plants/herbal preparations that are ethnomedically used to treat epilepsy or those which have been tested for anticonvulsant activity were reported. Overall, the results of the published articles show that the symptoms of epilepsy seizure can be inhibited or treated by active ingredients derived from medicinal plants.

关键词： Epileptic seizure anticonvulsant Medicinal plants Oxidative stress

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Evaluation of the anticonvulsant and muscle relaxant effects of the methanol root bark extracts of Annona senegalensis

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Asian Pacific Journal of Tropical Medicine 2010年第1期3卷 25-28页

作者： Okoye TC Akah PA Omeke CP Department of Pharmacology and Toxicology Faculty of Pharmaceutical SciencesUniversity of Nigeria

Objective:To investigate the potentials of the root bark of Annona（A.） senegalensis in the control of seizure and related hypnotic and motor incoordination effects in mice using experimental ***:The methanol extract（ME） of the root bark of *** was studied in mice using pentylenetetrazole（PTZ） induced convulsions,phenobarbitone induced sleeping time and motor coordination test on rota-rod *** toxicity and lethality（LD50） lest as well as phytochemical analysis were also carried ***:The extract（200,400,800 mg/ kg） exhibited a non- dose dependent significant（P50 of 1 2%mg/kg,while the phytochemical studies showed the presence of alkaloids, resins,glycosides,carbohydrate,reducing sugar,flavonoids,terpenoids,saponins and tannins. Conclusion:The extract of A senegalensis possessed anticonvulsant activity with pronounced hypnotic and muscle relaxant effects.

关键词： Annona senegalensis Hypnosis anticonvulsant Muscle relaxant

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Synthesis and anticonvulsant activity of 1-substituted benzyl- N-substituted-1, 2, 3-triazole-4-formamides

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Progress in Natural Science:Materials International 2006年第9期16卷 925-929页

作者： WANG Junmin, JUN Changsoo, CHAI Kyuyun, KWAK Kyungchell, QUAN Zheshan ( Key Laboratory of Natural Resources of the Changbai Mountain and Functional Molecules, Yanbian University, Yanji 133002, China Henan University of Traditional Chinese Medicine Pharmacy College, Zhengzhou 450003, China Department of Chemistry, Wonkwang University, Iksan 570-749, Korea) [a]Key Laboratory of Natural Resources of the Changbai Mountain and Functional Molecules Yanbian University Yanji China [b]Henan University of Traditional Chinese Medicine Pharmacy College Zhengzhou China [c]Department of Chemistry Wondwang University Iksan Korea

Substituted benzyl azids were synthesized through the reaction of substituted benzyl chloride and sodium azid, which subsequently underwent cyclization with ethyl propiolate and amidation to give thirteen 1-substituted benzyl-N-substituted-1, 2, 3-triazole-4-formamide derivatives (3a-3m) . The structure of the synthesized compounds was confirmed by IR, 1H-NMR, MS and elemental analysis. Their ant icon vulsant activity against maximal electrolshock (MES) induced seizure was tested and the result showed that all these compounds possess anticonvulsant activity in different degrees. Among those, the compounds containing chloro atoms on the phenyl ring were less potent in anticonvulsant activity, while introducing one or two fluorin atoms on benzyl system increased its activity. Furthermore, their activity decreased when there was substituent on the nitrogen atom of carboxamide, and the larger the substituent, the lower the activity.

关键词： 1-substituted benzyl-N-substituted-1 2 3-triazole-4-formamide anticonvulsant synthesis.

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Synthesis and anticonvulsant activity of 7-benzylamino-4,5-dihydro-[1,2,4] triazolo[4,3-a] quinolines

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Progress in Natural Science:Materials International 2007年第9期17卷 1104-1108页

作者： Cui Xiangshu1,2,Guan Liping3,Li Hailan3,Piao Huri3 and Quan Zheshan1,3(1.Key Laboratory of Organic Functional Factors of the Changbai Mountain,Ministry of Education,Yanbian University,Yanji 133002,China 2.College of Basic Medicine,Yanbian University,Yanji 133000,China 3.College of Pharmacy,Yanbian University,Yanji 133000,China) Key Laboratory of Organic Functional Factors of the Changbai Mountain Ministry of Education Yanbian University Yanji 133002 China College of Basic Medicine Yanbian University Yanji 133000 China 3. College of Pharmacy Yanbian University Yanji 133000 China

A series of 7-substituted-benzylamino-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline derivatives was synthesized and evaluated for their anticonvulsant *** subcutaneous pentylenetetrazole test(sc-PTZ)demonstrated that the most effective compound in controlling the sc-PTZ induced seizure was 7-(3-bromine-benzylamino)-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline(4j)with an ED50 of 5.0 mg/kg and the PI of 20.7,which was also safer than the reference *** the maximal electroshock test(MES)demonstrated that among these derivatives,7-(3-fluorobenzylamino)-4,5-dihydro-[1,2,4]trizolo[4,3-a]quinoline(4i),with an ED50 of 15.3 mg/kg and the PI of 7.2,was the safest in MES ***,their neurotoxicities were measured by the rotarod neurotoxicity test,and the results showed that all derivatives possessed lower neurotoxicity.

关键词： quinoline triazole synthesis anticonvulsant epilepsia

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Synthesis and evaluation of 4-substituted semicarbazones of levulinic acid for anticonvulsant activity

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Journal of Zhejiang University-Science B(Biomedicine & Biotechnology) 2005年第7期6卷 617-621页

作者： AGGARWAL Navneet MISHRA Pradeep Lachoo Memorial College of Science and Technology Pharmacy Wing Jodhpur Rajasthan 342003 IndiaDepartment of Pharmaceutical Sciences Dr. Hari Singh Gour University Sagar M.P. 470003 India

Objective: A series of 4-aryl substituted semicarbazones of levulinic acid (4-oxo pentanoic acid) was designed and synthesized to meet the structural requirements essential for anticonvulsant activity. Methods: All the compounds were evaluated for anticonvulsant activity. anticonvulsant activity was determined after intraperitoneal (i.p.) administration to mice by maximal electroshock (MES) and subcutaneous metrazol (ScMet) induced seizure methods and minimal motor impairment was determined by rotorod test. Results: A majority of the compounds exhibited significant anticonvulsant activity after intraperitoneal administration. In the present study 4-(4'-fluoro phenyl) levulinic acid semicarbazone emerged as the most active molecule, showing broad spectrum of activity with low neurotoxicity. Unsubstituted levulinic acid semicarbazone was found to be inactive in all the screens. Conclusion: The results obtained validate the hypothesis that presence of an aryl group near the semicarbazone moiety is essential for anticonvulsant activity. The results also indicate that the hydrophilic-hydrophobic site can accommodate hydrophilic groups.

关键词： Substituted semicarbazones anticonvulsant Levulinic acid

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Antipyretic and anticonvulsant activity of n-hexane fraction of viola betonicifolia

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Asian Pacific Journal of Tropical Biomedicine 2013年第4期3卷 280-283页

作者： Naveed Muhammad Muhammad Saeed Haroon Khan Naila Raziq Syed Muhammad Ashhad Halimi Department of Pharmacy University of Peshawar-25120 PeshawarPakistan Gandhara College of Pharmacy Gandhara UniversityPeshawarPakistan

Objective:To investigate the antipyretic and anticonvulsant activities of n-hexane fraction of Viola betonicifolia(***).Methods:The antipyretic effect was scrutinized using brewer's yeast induced pyrexia and anticonvlsion effect was tested using pentylenetetrazol and strychnine induced convulsion in ***:N-hexane fraction of *** demonstrated highly significant antipyretic activity during various assessment times(1-5 h)when challenged in yeast induced pyrexia *** effect was in a dose dependent manner with maximum attenuation(82.50%)observed at 300 mg/kg *** tested in pentylenetetrazol induced convulsion test,the 1st stage(Ear and facial twitching)and 2nd stage(Convulsive wave through the body)was 100%protected during 24 h at all the test doses(300,400 and 500 mg/kg i.p.),while the latency time of remaining stages was significantly *** maximum effect was observed by n-hexane fraction of *** at 400 and 500 mg/kg i.p.,as the latency time for generalized clonic-tonic seizure(5th stage)was increased up to 25.34 ***,n-hexane fraction of *** had no protection in strychnine induced convulsion ***:In conclusion,phytopharmacological studies provide scientific foundation to the folk uses of the plant in the treatment of pyrexia and neurological disorders.

关键词： Viola betonicifolia N-hexane fraction Antipyretic anticonvulsant

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anticonvulsant, Sedative and Antidepressant Effects of Aqueous Extract of Costus afer Stems in Mice

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Journal of Biosciences and Medicines 2022年第12期10卷 22-31页

作者： Bassoueka D’Avila Judicaël Peneme Bonaventure Max Lazard Ondele Radar Ahoudi Jered Abena Ange Antoine Laboratory of Pharmacodynamics and Experimental Physiopathology (L2PE) Faculty of Sciences and Techniques Marien Ngouabi University Brazzaville Republic of the Congo Biochemistry and Pharmacology Laboratory Faculty of Health Sciences Marien Ngouabi University Brazzaville Republic of the Congo

Epilepsy is a disorder in the nervous system which often causes a loss of consciousness. Traditional treatments are quiet a component of health care system in various populations in spite of the fact that well-established options are available. Most plants are used to treat epilepsy or those which have been verified for anticonvulsant activity were reported. Then, Costus afer is a plant of the Congolese flora used in traditional medicine for its many virtues. Therefore, the anticonvulsant activity of Costus afer was assessed with the strychnine convulsion induction test. Two tests were used for sedative activity such as the barbiturate sleep induction test and motor activity and finally the forced swimming test was also used to assess antidepressant activity. The results showed that the aqueous extract of Costus afer stems had no effects on strychnine-induced seizures at doses of 250 mg/kg and 500 mg/kg compared to the control group. However, the extract of Costus afer stems caused a very significant decrease in motricity at a dose of 500 mg/kg, showing a decrease in the onset time and a very significant increase in sleep duration like the reference molecule such as Diazepam. The aqueous extract of Costus afer stems also caused a decrease in immobility time in mice at a dose of 500 mg/kg.

关键词： Epilepsy Sedative Traditional Medicine Antidepressant anticonvulsant

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anticonvulsant potentials of ethanolic extract of Eleusine indica

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Journal of Coastal Life Medicine 2016年第12期 965-968页

作者： Ette Okon Ettebong Edidiong Etukakpan Augustine Bassey Department of Clinical Pharmacology and Therapeutics Faculty of Clinical SciencesCollege of Health SciencesUniversity of UyoUyoNigeria Department of Pharmacology and Toxicology Faculty of PharmacyCollege of Health ScienceUniversity of UyoUyoNigeria

Objective:To assess the anticonvulsant potentials of ethanolic extract of Eleusine ***:Albino Wistar mice were separated into five groups with six animals in each group and thereafter pretreated with distilled water,various doses of the extract(200-600 mg/kg)and standard drug diazepam(0.5 mg/kg).Thirty minutes later,pentylenetetrazole(70 mg/kg),aminophylline(280 mg/kg)and isoniazid(250 mg/kg)were used to induce convulsions by intraperitoneal *** mice were then placed in plexiglas cages and monitored for the occurrence of seizures over a thirty-minute time *** latency of convulsions,duration of tonic convulsions and mortality protection were *** obtained were analyzed using GraphPad InStat ***:The results showed that the extract exhibited a dose-dependent increase in the latency of clonic convulsions and decrease in duration of tonic convulsions as compared to the control and these effects were statistically significant(Panticonvulsant activity and corroborate with the claims of the traditional use of the plant as an anticonvulsant remedy.

关键词： Extract anticonvulsant Eleusine indica Convulsions

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Synthesis and Evaluation of anticonvulsant Activity of 6,8-Dimethoxy-3-methyl-1,2,3,4-tetrahydroisoquinoline in PTZ-Induced Seizure Model in Mice

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Open Journal of Medicinal Chemistry 2012年第3期2卷 72-77页

作者： Yothawathorn Pariyawongsakul Chamnan Patarapanich Chantana Boonyarat Ploenthip Puthongking Faculty of Pharmaceutical Sciences Burapha University Chonburi Thailand Faculty of Pharmaceutical Sciences Khon Kaen University Khon Kaen Thailand Graduate School of Pharmaceutical Sciences Khon Kaen University Khon Kaen Thailand

This study we describe the synthesis of a novel structure of anticonvulsant agent as 6,8-dimethoxy-3-methyl-1,2,3,4- tetrahydroisoquinoline by using GYKI52466, which was the potent anticonvulsant agent, as the lead molecule. Com-pound IV was synthesized and anticonvulsant effects was evaluated against Pentylenetetrazole (PTZ)-induced seizure model in mice. The acute anticonvulsant effect was tested with a single dose of 25 and 75 μmol/kg of the synthesis compound. Sodium valproate and normal saline were used as the reference standard and control, respectively. All compounds were injected intraperitoneally to each mouse an hour prior to seizure induced by injection of 60 mg/kg PTZ and observed their behavior for 30 minutes. The result showed that the IV at 75 μmol/kg could delay the latency to first twitch and decrease percent mortality compared to control group.

关键词： anticonvulsant Pentylenetetrazole Tetrahydroisoquinoline

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