Department of TCMs Pharmaceuticals, School of Traditional Chinese Pharmacy, China Pharmaceutical University, No. 639 Longmian Avenue, Nanjing 211198, PR China.
Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, No. 130 Meilong Road, Shanghai 200237, China.
Brief Bioinform. 2024 Jul 25;25(5). doi: 10.1093/bib/bbae362.
Herbal medicines, particularly traditional Chinese medicines (TCMs), are a rich source of natural products with significant therapeutic potential. However, understanding their mechanisms of action is challenging due to the complexity of their multi-ingredient compositions. We introduced Herb-CMap, a multimodal fusion framework leveraging protein-protein interactions and herb-perturbed gene expression signatures. Utilizing a network-based heat diffusion algorithm, Herb-CMap creates a connectivity map linking herb perturbations to their therapeutic targets, thereby facilitating the prioritization of active ingredients. As a case study, we applied Herb-CMap to Suhuang antitussive capsule (Suhuang), a TCM formula used for treating cough variant asthma (CVA). Using in vivo rat models, our analysis established the transcriptomic signatures of Suhuang and identified its key compounds, such as quercetin and luteolin, and their target genes, including IL17A, PIK3CB, PIK3CD, AKT1, and TNF. These drug-target interactions inhibit the IL-17 signaling pathway and deactivate PI3K, AKT, and NF-κB, effectively reducing lung inflammation and alleviating CVA. The study demonstrates the efficacy of Herb-CMap in elucidating the molecular mechanisms of herbal medicines, offering valuable insights for advancing drug discovery in TCM.
草药,特别是中药(TCM),是具有重要治疗潜力的天然产物的丰富来源。然而,由于其多成分组成的复杂性,理解其作用机制具有挑战性。我们引入了 Herb-CMap,这是一个利用蛋白质-蛋白质相互作用和草药扰动基因表达特征的多模态融合框架。利用基于网络的热扩散算法,Herb-CMap 创建了一个连接草药扰动与其治疗靶点的连通性图,从而有助于优先考虑活性成分。作为一个案例研究,我们将 Herb-CMap 应用于苏黄止咳胶囊(Suhuang),一种用于治疗咳嗽变异性哮喘(CVA)的中药配方。通过体内大鼠模型,我们的分析确定了 Suhuang 的转录组特征,并鉴定了其关键化合物,如槲皮素和木犀草素,以及它们的靶基因,包括 IL17A、PIK3CB、PIK3CD、AKT1 和 TNF。这些药物-靶标相互作用抑制了 IL-17 信号通路并使 PI3K、AKT 和 NF-κB 失活,有效减轻了肺部炎症并缓解了 CVA。该研究证明了 Herb-CMap 在阐明草药的分子机制方面的功效,为推进 TCM 中的药物发现提供了有价值的见解。