Table_8_Mapping Pharmacological Network of Multi-Targeting Litchi Ingredients in Cancer Therapeutics.xlsx

Considerable pharmacological studies have demonstrated that the extracts and ingredients from different parts (seeds, peels, pulps, and flowers) of Litchi exhibited anticancer effects by affecting the proliferation, apoptosis, autophagy, metastasis, chemotherapy and radiotherapy sensitivity, stemness, metabolism, angiogenesis, and immunity via multiple targeting. However, there is no systematical analysis on the interaction network of “multiple ingredients-multiple targets-multiple pathways” anticancer effects of Litchi. In this study, we summarized the confirmed anticancer ingredients and molecular targets of Litchi based on published articles and applied network pharmacology approach to explore the complex mechanisms underlying these effects from a perspective of system biology. The top ingredients, top targets, and top pathways of each anticancer function were identified using network pharmacology approach. Further intersecting analyses showed that Epigallocatechin gallate (EGCG), Gallic acid, Kaempferol, Luteolin, and Betulinic acid were the top ingredients which might be the key ingredients exerting anticancer function of Litchi, while BAX, BCL2, CASP3, and AKT1 were the top targets which might be the main targets underling the anticancer mechanisms of these top ingredients. These results provided references for further understanding and exploration of Litchi as therapeutics in cancer as well as the application of “Component Formula” based on Litchi’s effective ingredients.

大量药理学研究已证实，荔枝（Litchi）不同部位（种子、果皮、果肉及花）的提取物与活性成分可通过多靶点作用，调控肿瘤细胞增殖、凋亡、自噬、转移、化疗与放疗敏感性、干细胞干性、代谢、血管生成及免疫应答，从而发挥抗癌功效。然而，目前尚无针对荔枝抗癌作用的“多成分-多靶点-多通路”相互作用网络的系统性分析。本研究基于已发表文献，梳理了已被证实的荔枝抗癌活性成分与分子靶点，并运用网络药理学（network pharmacology）方法，从系统生物学视角探究此类抗癌作用的潜在复杂机制。本研究通过网络药理学方法，筛选得到各抗癌功能对应的核心活性成分、核心靶点与核心通路。进一步交集分析显示，表没食子儿茶素没食子酸酯（Epigallocatechin gallate, EGCG）、没食子酸（Gallic acid）、山奈酚（Kaempferol）、木犀草素（Luteolin）及白桦脂酸（Betulinic acid）为介导荔枝抗癌作用的核心活性成分；而BAX、BCL2、CASP3及AKT1则为上述核心成分发挥抗癌机制的主要靶点。本研究结果可为进一步理解与开发荔枝作为癌症治疗候选药物，以及基于荔枝有效成分的“组分复方”应用提供参考依据。