Department of Urology, The Second Hospital of Lanzhou University, Lanzhou, 730000, Gansu, China.
Institute of Urology, The Second Hospital of Lanzhou University, Lanzhou, 730030, Gansu, China.
Naunyn Schmiedebergs Arch Pharmacol. 2024 Nov;397(11):8691-8706. doi: 10.1007/s00210-024-03183-8. Epub 2024 Jun 1.
This study is aimed at exploring the potential mechanisms of melatonin (MT) in treating chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS) using network pharmacology and experimental study. The target genes of MT were acquired from the Swiss Target Prediction, SuperPred, SEA, and PharmMapper databases, and the CP/CPPS targets were collected based on OMIM, DisGeNET, and GeneCards databases. The intersection of MT and CP/CPPS target genes was analyzed. A PPI network was constructed using Cytoscape to identify core targets. The shared targets underwent GO and KEGG enrichment analyses by Using R software. Molecular docking of MT with core targets was performed using AutoDock and PyMOL. GROMACS software was used for molecular dynamics simulation. And using cell experiments to verify the potential effect of MT in CP/CPPS. Network pharmacology analysis reveals 284 shared targets between MT and CP/CPPS, with AKT1, SRC, HSP90AA1, PTGS2, BCL2L1, ALB, CASP3, NFKB1, HIF1A, and ESR1 identified as key targets. Enrichment analysis indicates that MT affects CP/CPPS through various biological processes, and pathway analysis emphasizes the significance of PI3K-Akt, MAPK, Ras, FoxO, HIF-1, EGFR, and apoptosis pathways. Molecular docking confirms strong binding between MT and core targets. It is worth noting that the molecular dynamics simulation showed that the average binding free energy of AKT1, PTGS2, ALB, HSP90AA1 proteins, and MT was - 26.15, - 29.48, - 18.59, and - 20.09 kcal/mol, respectively. These results indicated that AKT1, PTGS2, ALB, and HSP90AA1 proteins were strongly bound to MT. Cell experiments demonstrate that MT can inhibit the secretion of IL-1β, IL-6, and TNF-α in LPS-induced RWPE-1 cells, alleviate inflammation, and suppress cell apoptosis and oxidative stress. Network pharmacology, molecular docking, molecular dynamics simulation, and cell experiments showed that MT could play a role in CP/CPPS by regulating multiple targets and pathways. These findings provide an important scientific basis for further exploration of the molecular mechanism and clinical application of MT in CP/CPPS treatment and are expected to provide new ideas and directions for the development of novel therapeutic strategies.
本研究旨在采用网络药理学和实验研究探讨褪黑素(MT)治疗慢性前列腺炎/慢性骨盆疼痛综合征(CP/CPPS)的潜在机制。MT 的靶基因从 Swiss Target Prediction、SuperPred、SEA 和 PharmMapper 数据库中获得,CP/CPPS 靶基因则基于 OMIM、DisGeNET 和 GeneCards 数据库收集。分析 MT 与 CP/CPPS 靶基因的交集。使用 Cytoscape 构建 PPI 网络以识别核心靶标。使用 R 软件对共享靶标进行 GO 和 KEGG 富集分析。使用 AutoDock 和 PyMOL 对 MT 与核心靶标进行分子对接。使用 GROMACS 软件进行分子动力学模拟。并通过细胞实验验证 MT 在 CP/CPPS 中的潜在作用。网络药理学分析揭示 MT 与 CP/CPPS 之间有 284 个共享靶标,其中 AKT1、SRC、HSP90AA1、PTGS2、BCL2L1、ALB、CASP3、NFKB1、HIF1A 和 ESR1 被鉴定为关键靶标。富集分析表明 MT 通过多种生物过程影响 CP/CPPS,通路分析强调了 PI3K-Akt、MAPK、Ras、FoxO、HIF-1、EGFR 和细胞凋亡通路的重要性。分子对接证实 MT 与核心靶标之间具有强结合性。值得注意的是,分子动力学模拟显示,MT 与 AKT1、PTGS2、ALB、HSP90AA1 蛋白的平均结合自由能分别为-26.15、-29.48、-18.59 和-20.09 kcal/mol。这些结果表明,AKT1、PTGS2、ALB 和 HSP90AA1 蛋白与 MT 具有强结合性。细胞实验表明,MT 可抑制 LPS 诱导的 RWPE-1 细胞中 IL-1β、IL-6 和 TNF-α 的分泌,减轻炎症,抑制细胞凋亡和氧化应激。网络药理学、分子对接、分子动力学模拟和细胞实验表明,MT 可通过调节多种靶标和通路在 CP/CPPS 中发挥作用。这些发现为进一步探讨 MT 在 CP/CPPS 治疗中的分子机制和临床应用提供了重要的科学依据,并有望为新型治疗策略的开发提供新的思路和方向。