Y. B. Chavan College of Pharmacy, Dr. Rafiq Zakaria Campus, Aurangabad, Maharashtra, India.
Metab Brain Dis. 2024 Jun;39(5):763-782. doi: 10.1007/s11011-024-01356-1. Epub 2024 May 29.
The present investigation delved into the pharmacological mechanisms underlying the management of depression through Flavan-3-ols and Aromatic Resins, employing in silico and in vivo methodologies. Network pharmacology was utilized to identify targets associated with the antidepressant activity of Flavan-3-ols and Aromatic Resins. Protein-protein interaction and KEGG analyses were conducted to enrich and explore key pathways. Molecular docking and simulation studies were executed to assess the targets. The antidepressant effects were studied using the Forced Swim Test and Tail Suspension Test on both unstressed mice and those subjected to the chronic unpredictable mild stress (CUMS) paradigm. The Compound-Target network analysis revealed a substantial impact of the components on numerous targets, with 332 nodes and 491 edges. Protein-protein interaction analysis indicated significant interactions with targets implicated in depression. KEGG analysis highlighted major pathways, including neuroactive ligand-receptor interaction, dopaminergic synapse, and long-term depression. Docking studies on EGCG demonstrated binding energies of -7.2 kcal/mol for serotonin 1 A (5-HT1A), -7.9 kcal/mol for D2, and - 9.6 kcal/mol for MOA-A. Molecular dynamics simulation indicated minute fluctuation, hence suggesting stable complexes formed between small molecules and proteins. The combination of Flavan-3-ols and Aromatic Resins significantly increased mobility time (p < 0.05) in the Forced Swim Test and Tail Suspension Test, while significantly decreasing immobility time and time freezing (p < 0.05) in both unstressed and CUMS mice. This study demonstrated the antidepressant characteristics of Flavan-3-ols and Aromatic Resins, underscoring the need for further research to develop a novel antidepressant medication.
本研究采用网络药理学方法和体内方法,探讨了黄烷-3-醇和芳香树脂治疗抑郁症的药理学机制。利用网络药理学方法鉴定与黄烷-3-醇和芳香树脂抗抑郁活性相关的靶点。进行蛋白质-蛋白质相互作用和 KEGG 分析以丰富和探索关键途径。执行分子对接和模拟研究以评估靶点。采用强迫游泳试验和悬尾试验对未应激小鼠和慢性不可预测轻度应激(CUMS)模型小鼠进行抗抑郁作用研究。化合物-靶点网络分析表明,这些成分对许多靶点具有显著影响,共有 332 个节点和 491 个边。蛋白质-蛋白质相互作用分析表明,与涉及抑郁的靶点存在显著相互作用。KEGG 分析突出了主要途径,包括神经活性配体-受体相互作用、多巴胺能突触和长时程抑郁。EGCG 的对接研究表明,其与 5-HT1A(血清素 1A)的结合能为-7.2 kcal/mol,与 D2 的结合能为-7.9 kcal/mol,与 MOA-A 的结合能为-9.6 kcal/mol。分子动力学模拟表明,小分子和蛋白质之间形成了稳定的复合物,仅存在微小的波动。黄烷-3-醇和芳香树脂的组合显著增加了强迫游泳试验和悬尾试验中小鼠的移动时间(p < 0.05),同时显著减少了未应激和 CUMS 小鼠的不动时间和冻结时间(p < 0.05)。本研究证明了黄烷-3-醇和芳香树脂的抗抑郁特性,强调需要进一步研究以开发新型抗抑郁药物。