Department of Cardiovascular Medicine, Shanghai Institute of Hypertension, Shanghai Key Laboratory of Hypertension, National Research Centre for Translational Medicine, Ruijin Hospital, Shanghai Jiaotong University School of Medicine, Shanghai, China.
J Clin Hypertens (Greenwich). 2024 Sep;26(9):1024-1038. doi: 10.1111/jch.14833. Epub 2024 Jul 11.
Hypertension has become a major contributor to the morbidity and mortality of cardiovascular diseases worldwide. Despite the evidence of the anti-hypertensive effect of gastrodia-uncaria granules (GUG) in hypertensive patients, little is known about its potential therapeutic targets as well as the underlying mechanism. GUG components were sourced from TCMSP and HERB, with bioactive ingredients screened. Hypertension-related targets were gathered from DisGeNET, OMIM, GeneCards, CTD, and GEO. The STRING database constructed a protein-protein interaction network, visualized by Cytoscape 3.7.1. Core targets were analyzed via GO and KEGG using R package ClusterProfiler. Molecular docking with AutodockVina 1.2.2 revealed favorable binding affinities. In vivo studies on hypertensive mice and rats validated network pharmacology findings. GUG yielded 228 active ingredients and 1190 targets, intersecting with 373 hypertension-related genes. PPI network analysis identified five core genes: AKT1, TNF-α, GAPDH, IL-6, and ALB. Top enriched GO terms and KEGG pathways associated with the anti-hypertensive properties of GUG were documented. Molecular docking indicated stable binding of core components to targets. In vivo study showed that GUG could improve vascular relaxation, alleviate vascular remodeling, and lower blood pressure in hypertensive animal models possibly through inhibiting inflammatory factors such as AKT1, mTOR, and CCND1. Integrated network pharmacology and in vivo experiment showed that GUG may exert anti-hypertensive effects by inhibiting inflammation response, which provides some clues for understanding the effect and mechanisms of GUG in the treatment of hypertension.
高血压已成为全球心血管疾病发病率和死亡率的主要原因。尽管天麻钩藤颗粒(GUG)在高血压患者中的降压作用已有证据,但对其潜在的治疗靶点以及潜在机制知之甚少。GUG 的成分来源于 TCMSP 和 HERB,筛选出了生物活性成分。从 DisGeNET、OMIM、GeneCards、CTD 和 GEO 中收集了与高血压相关的靶点。STRING 数据库构建了一个蛋白质-蛋白质相互作用网络,通过 Cytoscape 3.7.1 可视化。使用 R 包 ClusterProfiler 对核心靶点进行了 GO 和 KEGG 分析。分子对接利用 AutodockVina 1.2.2 揭示了有利的结合亲和力。高血压小鼠和大鼠的体内研究验证了网络药理学的发现。GUG 产生了 228 种活性成分和 1190 个靶点,与 373 个与高血压相关的基因相交。PPI 网络分析确定了五个核心基因:AKT1、TNF-α、GAPDH、IL-6 和 ALB。记录了与 GUG 抗高血压特性相关的 GO 术语和 KEGG 途径的顶级富集。分子对接表明核心成分与靶点的结合稳定。体内研究表明,GUG 可能通过抑制 AKT1、mTOR 和 CCND1 等炎症因子,改善血管舒张、减轻血管重构并降低高血压动物模型的血压。综合网络药理学和体内实验表明,GUG 可能通过抑制炎症反应发挥抗高血压作用,为理解 GUG 治疗高血压的作用和机制提供了一些线索。