Mao Xinxin, Shi Shuqing, Chen Chunmei, Li Yumeng, Zhang Bingxuan, Song Qingqiao
Department of Internal Medicine, Guang'anmen Hospital, China Academy of Chinese Medical Sciences, Beijing, China.
Front Chem. 2025 Jul 21;13:1617676. doi: 10.3389/fchem.2025.1617676. eCollection 2025.
The Wenpitongluo Decoction (WPTLD) was a classical herbal formula composed of medicinal herbs with both edible and therapeutic properties. It demonstrated clinical efficacy in treating Cardiorenal Syndrome (CRS), though its mechanism of action remained unclear. Although inflammatory and oxidative stress pathways in CRS have been intensively studied, the roles of ferroptosis and anoikis, which may be activated by these pathways, have received little attention.
First, the active components of WPTLD were obtained through the TCMSP and Herb databases, and then identified using UHPLC-HRMS. Subsequently, target prediction of the identified components was carried out via the SwissTargetPrediction platform. While CRS-related targets were retrieved from GEO, GeneCards, and PharmGKB. A gene library of ferroptosis- and anoikis-associated targets was established. Tissue-specific mRNA expression profiles were analyzed via BioGPS. Subsequently, protein-protein interaction (PPI) networks were constructed to identify core targets, followed by Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses using Metascape. Finally, molecular docking assessed binding affinities between active components and core targets, with top-ranked complexes undergoing molecular dynamics (MD) simulations.
Fifteen bioactive components and 39 component-disease interaction targets were identified, predominantly localized in kidney, thymus, lung, adipocytes, adrenal gland, and heart tissues. Topological analysis of PPI networks revealed eight core targets, including ferroptosis-/anoikis-associated SIRT1, PTGS2, and PRKCA. KEGG analysis highlighted critical pathways such as AMPK and PI3K-Akt signaling. Notably, molecular docking and MD simulations demonstrated stable binding between active compounds and core targets.
This study systematically deciphers WPTLD's anti-CRS mechanisms via targeting ferroptosis- and anoikis-related genes through multi-pathway modulation. These findings not only clarify the pathological roles of ferroptosis and anoikis in CRS but also provide a computational framework for developing therapeutic strategies.
温脾通络汤(WPTLD)是一种由具有药食两用特性的草药组成的经典中药方剂。它在治疗心肾综合征(CRS)方面显示出临床疗效,但其作用机制尚不清楚。尽管CRS中的炎症和氧化应激途径已得到深入研究,但可能由这些途径激活的铁死亡和失巢凋亡的作用却很少受到关注。
首先,通过中药系统药理学数据库与分析平台(TCMSP)和中药综合数据库(Herb)获取WPTLD的活性成分,然后使用超高效液相色谱-高分辨质谱(UHPLC-HRMS)进行鉴定。随后,通过瑞士靶点预测平台(SwissTargetPrediction)对鉴定出的成分进行靶点预测。同时,从基因表达综合数据库(GEO)、基因卡片数据库(GeneCards)和药物基因组学知识库(PharmGKB)中检索CRS相关靶点。建立铁死亡和失巢凋亡相关靶点的基因库。通过生物基因图谱数据库(BioGPS)分析组织特异性mRNA表达谱。随后,构建蛋白质-蛋白质相互作用(PPI)网络以识别核心靶点,接着使用Metascape进行基因本体(GO)和京都基因与基因组百科全书(KEGG)富集分析。最后,分子对接评估活性成分与核心靶点之间的结合亲和力,对排名靠前的复合物进行分子动力学(MD)模拟。
鉴定出15种生物活性成分和39种成分-疾病相互作用靶点,主要定位于肾脏、胸腺、肺、脂肪细胞、肾上腺和心脏组织。PPI网络的拓扑分析揭示了8个核心靶点,包括与铁死亡/失巢凋亡相关的沉默信息调节因子1(SIRT1)、前列腺素内过氧化物合酶2(PTGS2)和蛋白激酶Cα(PRKCA)。KEGG分析突出了关键途径,如AMPK和PI3K-Akt信号通路。值得注意的是,分子对接和MD模拟表明活性化合物与核心靶点之间具有稳定的结合。
本研究通过多途径调节靶向铁死亡和失巢凋亡相关基因,系统地解读了WPTLD抗CRS的机制。这些发现不仅阐明了铁死亡和失巢凋亡在CRS中的病理作用,还为开发治疗策略提供了一个计算框架。