Hanan F Aly, Ghadha Ibrahim Fouad, Wagdy K B Khalil, Nahla N Kamel, Nagy S El-Rigal, Kawkab A Ahmed, Dalia A Taha, Mohamed B Shalaby, Somaia S Abd El-Karim, Doha H Abou Baker, Maha Z Rizk
{"title":"苯并呋喃-胺酮衍生物通过调节细胞凋亡和AD相关基因的表达来评估对大鼠阿尔茨海默病（AD）样病理的治疗效果。","authors":"Hanan F Aly, Ghadha Ibrahim Fouad, Wagdy K B Khalil, Nahla N Kamel, Nagy S El-Rigal, Kawkab A Ahmed, Dalia A Taha, Mohamed B Shalaby, Somaia S Abd El-Karim, Doha H Abou Baker, Maha Z Rizk","doi":"10.1080/01616412.2025.2520021","DOIUrl":null,"url":null,"abstract":"<p><strong>Background: </strong>Alzheimer's disease (AD) is a progressive age-related neurodegenerative disorder. There is currently no promising cure for AD; the available treatments can only alleviate the symptoms.</p><p><strong>Objectives: </strong>The Benzofuran-Enaminone derivative '(E)-1-(benzofuran-2-yl)-3-((2-hydroxyphenyl)amino)prop-2-en-1-one (5)' was synthesized as a potential anti-AD candidate in Aluminum chloride (AlCl<sub>3</sub>)-induced AD in rats.</p><p><strong>Methods: </strong>In vivo and in vitro acute and chronic studies were conducted to examine the potential toxicity, as well as the antioxidant and anti-acetylcholinesterase (AChE) activities of compound 5. Then, rats were divided into four groups: (1) negative control; (2) AD-induced rats; (3) AD-induced rats treated with compound 5; and (4) AD-induced rats treated with Donepezil. Behavioral, biochemical, and molecular investigations were conducted. The expression of insulin 1 gene, apoptotic genes, and the AD-related genes were estimated.</p><p><strong>Results: </strong>The selected dose of compound 5 (10 mg/kg) was based on an acute toxicity test, then it was applied for a chronic study for 1 month; no toxicological features were stimulated. In vitro, compound 5 demonstrated antioxidant and anti-AChE activities. The expression of apoptotic genes (Bcl-2, Bax, and Caspase-3), AD-related genes (Amyloid precursor protein (APP) and Tau), and the insulin 1 gene were altered in AD-induced rats versus control rats. Treatment of AD rats with compound 5 counteracted the AlCl<sub>3</sub>-induced neurotoxicity.</p><p><strong>Conclusion: </strong>This study could be regarded as an initial step in drug discovery for testing this new chemical entity as a potent anti-AD therapeutic agent.</p>","PeriodicalId":19131,"journal":{"name":"Neurological Research","volume":" ","pages":"1-15"},"PeriodicalIF":1.5000,"publicationDate":"2025-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Evaluating the therapeutic efficacy of a Benzofuran-Enaminone derivative for the management of Alzheimer's disease (AD)-like pathology in rats through regulating the expression of apoptosis and AD-related genes.\",\"authors\":\"Hanan F Aly, Ghadha Ibrahim Fouad, Wagdy K B Khalil, Nahla N Kamel, Nagy S El-Rigal, Kawkab A Ahmed, Dalia A Taha, Mohamed B Shalaby, Somaia S Abd El-Karim, Doha H Abou Baker, Maha Z Rizk\",\"doi\":\"10.1080/01616412.2025.2520021\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Background: </strong>Alzheimer's disease (AD) is a progressive age-related neurodegenerative disorder. There is currently no promising cure for AD; the available treatments can only alleviate the symptoms.</p><p><strong>Objectives: </strong>The Benzofuran-Enaminone derivative '(E)-1-(benzofuran-2-yl)-3-((2-hydroxyphenyl)amino)prop-2-en-1-one (5)' was synthesized as a potential anti-AD candidate in Aluminum chloride (AlCl<sub>3</sub>)-induced AD in rats.</p><p><strong>Methods: </strong>In vivo and in vitro acute and chronic studies were conducted to examine the potential toxicity, as well as the antioxidant and anti-acetylcholinesterase (AChE) activities of compound 5. Then, rats were divided into four groups: (1) negative control; (2) AD-induced rats; (3) AD-induced rats treated with compound 5; and (4) AD-induced rats treated with Donepezil. Behavioral, biochemical, and molecular investigations were conducted. The expression of insulin 1 gene, apoptotic genes, and the AD-related genes were estimated.</p><p><strong>Results: </strong>The selected dose of compound 5 (10 mg/kg) was based on an acute toxicity test, then it was applied for a chronic study for 1 month; no toxicological features were stimulated. In vitro, compound 5 demonstrated antioxidant and anti-AChE activities. The expression of apoptotic genes (Bcl-2, Bax, and Caspase-3), AD-related genes (Amyloid precursor protein (APP) and Tau), and the insulin 1 gene were altered in AD-induced rats versus control rats. Treatment of AD rats with compound 5 counteracted the AlCl<sub>3</sub>-induced neurotoxicity.</p><p><strong>Conclusion: </strong>This study could be regarded as an initial step in drug discovery for testing this new chemical entity as a potent anti-AD therapeutic agent.</p>\",\"PeriodicalId\":19131,\"journal\":{\"name\":\"Neurological Research\",\"volume\":\" \",\"pages\":\"1-15\"},\"PeriodicalIF\":1.5000,\"publicationDate\":\"2025-06-21\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Neurological Research\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1080/01616412.2025.2520021\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CLINICAL NEUROLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Neurological Research","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1080/01616412.2025.2520021","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CLINICAL NEUROLOGY","Score":null,"Total":0}
Evaluating the therapeutic efficacy of a Benzofuran-Enaminone derivative for the management of Alzheimer's disease (AD)-like pathology in rats through regulating the expression of apoptosis and AD-related genes.
Background: Alzheimer's disease (AD) is a progressive age-related neurodegenerative disorder. There is currently no promising cure for AD; the available treatments can only alleviate the symptoms.
Objectives: The Benzofuran-Enaminone derivative '(E)-1-(benzofuran-2-yl)-3-((2-hydroxyphenyl)amino)prop-2-en-1-one (5)' was synthesized as a potential anti-AD candidate in Aluminum chloride (AlCl3)-induced AD in rats.
Methods: In vivo and in vitro acute and chronic studies were conducted to examine the potential toxicity, as well as the antioxidant and anti-acetylcholinesterase (AChE) activities of compound 5. Then, rats were divided into four groups: (1) negative control; (2) AD-induced rats; (3) AD-induced rats treated with compound 5; and (4) AD-induced rats treated with Donepezil. Behavioral, biochemical, and molecular investigations were conducted. The expression of insulin 1 gene, apoptotic genes, and the AD-related genes were estimated.
Results: The selected dose of compound 5 (10 mg/kg) was based on an acute toxicity test, then it was applied for a chronic study for 1 month; no toxicological features were stimulated. In vitro, compound 5 demonstrated antioxidant and anti-AChE activities. The expression of apoptotic genes (Bcl-2, Bax, and Caspase-3), AD-related genes (Amyloid precursor protein (APP) and Tau), and the insulin 1 gene were altered in AD-induced rats versus control rats. Treatment of AD rats with compound 5 counteracted the AlCl3-induced neurotoxicity.
Conclusion: This study could be regarded as an initial step in drug discovery for testing this new chemical entity as a potent anti-AD therapeutic agent.
期刊介绍：
Neurological Research is an international, peer-reviewed journal for reporting both basic and clinical research in the fields of neurosurgery, neurology, neuroengineering and neurosciences. It provides a medium for those who recognize the wider implications of their work and who wish to be informed of the relevant experience of others in related and more distant fields.
The scope of the journal includes:
•Stem cell applications
•Molecular neuroscience
•Neuropharmacology
•Neuroradiology
•Neurochemistry
•Biomathematical models
•Endovascular neurosurgery
•Innovation in neurosurgery.
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