Massey Iona, Yadav Sandeep, Kumar Durgesh, Maharia Ram Swaroop, Kumari Kamlesh, Singh Prashant
Department of Chemistry, Atma Ram Sanatan Dharma College, University of Delhi, Delhi, India.
Amity Institute of Biotechnology, Amity University, Noida, India.
Mol Divers. 2025 Feb;29(1):439-455. doi: 10.1007/s11030-024-10865-1. Epub 2024 May 17.
In the contemporary landscape, anxiety and seizures stand as major areas of concern, prompting researchers to explore potential drugs against them. While numerous drugs have shown the potential to treat these two neurological conditions, certain adverse effects emphasize the need for development of safer alternatives. This study seeks to employ an in silico approach to evaluate natural compounds, particularly curcumins, as potential inhibitors of GABA-AT to mitigate anxiety and seizures. The proposed methodology includes generating a compound library, minimizing energy, conducting molecular docking using AutoDock, molecular dynamics simulations using Amber, and MM-GBSA calculations. Remarkably, CMPD50 and CMPD88 exhibited promising binding affinities of - 9.0 kcal/mol and - 9.1 kcal/mol with chains A and C of GABA-AT, respectively. Further, MM-GBSA calculations revealed binding free energies of - 10.88 kcal/mol and - 10.72 kcal/mol in CMPD50 and CMPD88, respectively. ADME analysis showed that these compounds contain drug-likeness properties and might be considered as potential drug candidates. The findings from this study will have practical applications in the field of drug discovery for the development of safer and effective drugs for treatment of anxiety and seizures. Overall, this study will lay the groundwork for providing valuable insights into the potential therapeutic effects of curcumins in alleviating anxiety and seizures, establishing a computational framework for future experimental validation.
在当代环境中,焦虑和癫痫是主要关注领域,促使研究人员探索针对它们的潜在药物。虽然许多药物已显示出治疗这两种神经疾病的潜力,但某些不良反应凸显了开发更安全替代品的必要性。本研究旨在采用计算机模拟方法评估天然化合物,特别是姜黄素,作为γ-氨基丁酸转氨酶(GABA-AT)的潜在抑制剂,以减轻焦虑和癫痫。所提出的方法包括生成化合物库、能量最小化、使用AutoDock进行分子对接、使用Amber进行分子动力学模拟以及MM-GBSA计算。值得注意的是,化合物CMPD50和CMPD88分别与GABA-AT的A链和C链表现出有前景的结合亲和力,分别为-9.0千卡/摩尔和-9.1千卡/摩尔。此外,MM-GBSA计算分别揭示了CMPD50和CMPD88的结合自由能为-10.88千卡/摩尔和-10.72千卡/摩尔。ADME分析表明这些化合物具有类药物性质,可能被视为潜在的药物候选物。本研究的结果将在药物发现领域具有实际应用,用于开发更安全有效的治疗焦虑和癫痫的药物。总体而言,本研究将为深入了解姜黄素在减轻焦虑和癫痫方面的潜在治疗作用奠定基础,为未来的实验验证建立一个计算框架。