检索结果-南通市图书馆

Comprehensive Assessment of Anxiolytic Properties in 4-HPAA Derivatives: Bridging in Vivo Validation and Molecular Docking Analyses

引用

Open Journal of Medicinal Chemistry 2024年第3期14卷 29-44页

作者： Kawthar Alhussieni Rami Ayoub Jamal Jilani Qais Jarrar Othman Alhussinei Vetriselvan Subramaniyan Esra Nasraldin Khalil Sharafaldin Harshini Muruganantham Jureerat Kijsomporn Ling Shing Wong Department of Applied Pharmaceutical Sciences and Clinical Pharmacy Faculty of Pharmacy Isra University Amman Jordan Department of Pharmaceutical Chemistry Faculty of Pharmacy Universiti Malaya Kuala Lumpur Malaysia Department of Medicinal Chemistry and Pharmacognosy Faculty of Pharmacy Jordan University of Science and Technology Irbid Jordan Department of Allied Medical Sciences Zarqa Private University Zarqa Jordan Department of Medical Sciences School of Medical and Life Sciences Sunway University Bandar Sunway Malaysia Department of Clinical Pharmacy and Pharmacy Practice Faculty of Pharmacy Universiti Malaya Kuala Lumpur Malaysia Center for Global Research Saveetha Medical College Saveetha Institute of Medical and Technical Sciences Saveetha University Chennai India School of Nursing Metharath University Bangtoey Thailand Faculty of Health and Life Sciences INTI International University Nilai Malaysia

Anxiety is a significant mental health issue that substantially affects an individual’s quality of life. Feelings of uneasiness, irritability, and sleep disturbances characterize it. 4-Hydroxyphenyl acetic acid (4-HPAA) is identified in brain cells as a physiological byproduct of tyramine. This study hypothesizes that 4-HPAA may regulate anxiety due to its anxiolytic properties, acting as a modulator of the GABAergic system, which plays a crucial role in the pathophysiology of anxiety disorders. Our study aims to enhance the anxiolytic effects of 4-HPAA through chemical modification to improve its pharmacokinetic properties. Three derivatives, namely Isopropyl-4-hydroxy-[phenyl] acetate (IHPA), Isopropyl-4-hydroxy-[phenyl] acetate (MPAA), and 4-methoxyphenyl acetate (MPHA), have been synthesized from 4-HPAA. This assessment will use well-established animal models, specifically the Elevated Plus-maze (EPM) and zero maze (EZM) tests, selected for their validity in replicating anxiety-like symptoms in animals. Chronic caffeine administration via drinking water (0.3 g/l for 14 days) was employed to induce an anxiety state for testing purposes. IHPA and MPAA demonstrated significant anxiolyticactivity when tested in the EPM and EZM experiments. Molecular docking simulations using AutoDock Vina indicated that 4-HPAA derivatives had docking scores ranging from −5.8 to −4.8 kcal/mol, compared to the standard anxiolytic medication Diazepam, which scored −7.1 kcal/mol. These scores suggest a potential for 4-HPAA derivatives to interact effectively with the Gamma-aminobutyric acid (GABA_A) receptor. In conclusion, our in vivo and in silico analyses indicate a promising anxiolytic potential for 4-HPAA derivatives.

关键词： Anxiolytics 4-HPAA Molecular Docking Elevated Plus-maze zero maze tests

来源：

维普期刊数据库评论

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

欢迎您,

建议与咨询留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

时间限定

文献类型

馆藏选择

核心期刊

语言

文献类型

帮助

文字说明：

检索规则说明：

检索范例：

分类表

所选分类

限定检索结果

文献类型

馆藏范围

日期分布

学科分类号

主题

机构

作者

语言

在线全文

请选择保存的检索档案：

请选择收藏分类：

通借通还

欢迎您,

建议与咨询 留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

时间限定

文献类型

馆藏选择

核心期刊

语言

文献类型

帮助

文字说明：

检索规则说明：

检索范例：

分类表

所选分类

限定检索结果

文献类型

馆藏范围

日期分布

学科分类号

主题

机构

作者

语言

在线全文

请选择保存的检索档案： 新增检索档案 确定 取消

请选择收藏分类： 新增自定义分类 确定 取消

通借通还

建议与咨询留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

请选择保存的检索档案：

请选择收藏分类：