银杏叶（Ginkgo Folium）是银杏（Ginkgo biloba L.）的叶片，在中医药中因其有效性和安全性而享有盛名。银杏叶富含多种具有生物活性的成分，具有多种药理活性。最近的研究显示，银杏叶中的活性物质在不同类型的癌细胞中显示出了有希望的抗肿瘤效果，突显了其作为天然抗肿瘤剂的潜力。进一步的研究需要阐明其作用机制并优化其治疗潜力。 为了深入了解银杏叶的药理活性及其对癌症患者的潜在治疗益处，本研究在多个在线数据库，包括PubMed、Web of Science和Medline等，进行了全面和系统的检索。相关关键词包括“银杏叶”、“黄酮类”、“萜类”、“银杏叶提取物”和“抗肿瘤”，以涵盖广泛的研究，从而为我们的综述提供信息。此外，我们遵循严格的选择过程，以确保所选研究符合预定的纳入标准。 银杏叶的活性成分主要由黄酮类和萜类组成，其中主要化合物包括槲皮素、山奈酚、异槲皮素、银杏内酯和银杏苷内酯。这些活性成分通过调节多样的信号通路，通过关键的生物事件，如凋亡、细胞周期停滞、自噬以及通过调节多样化的信号通路抑制侵袭和转移，发挥其抗肿瘤效应。在凋亡过程中，活性成分主要通过调节半胱氨酸蛋白酶-8介导的死亡受体通路和半胱氨酸蛋白酶-9介导的线粒体通路来发挥作用，从而调节特定的信号通路。此外，通过调节多条信号通路，活性成分可以有效诱导细胞在G1期、G0/G1期、G2期和G2/M期停滞。其中，与G2/M期停滞相关的通路尤其广泛，而与这些通路最相关的是细胞周期依赖性激酶（CDKs）。此外，活性成分主要通过调节特定的炎症因子和应激物质介导自噬，促进自噬体与溶酶体的融合阶段。此外，通过调节特定的趋化因子和基质金属蛋白酶，活性成分可以有效抑制上皮-间质转化（EMT）和血管生成的过程，对细胞侵袭和迁移产生显著影响。尤其是槲皮素和山奈酚等活性成分之间表现出协同作用。 来自银杏叶的活性成分在各个层面和通路上展示了全面的抗肿瘤效应，为新药开发提供了有力的证据。然而，为了促进它们在临床的广泛和适应性应用，还需要进一步的广泛实验研究，以全面探索它们的疗效、安全性和作用机制。 版权所有 © 2023。由Elsevier B.V.出版。

Ginkgo biloba L. is a well-known and highly regarded resource in Chinese traditional medicine due to its effectiveness and safety. Ginkgo Folium, the leaf of Ginkgo biloba L., contains biologically active constituents with diverse pharmacological activities. Recent studies have shown promising antitumor effects of the bioactive constituents found in Ginkgo Folium against various types of cancer cells, highlighting its potential as a natural source of antitumor agents. Further research is needed to elucidate the underlying mechanisms and optimize its therapeutic potential.To provide a detailed understanding of the pharmacological activities of Ginkgo Folium and its potential therapeutic benefits for cancer patients.In this study, we conducted a thorough and systematic search of multiple online databases, including PubMed, Web of Science, Medline, using relevant keywords such as "Ginkgo Folium," "flavonoids," "terpenoids," "Ginkgo Folium extracts," and "antitumor" to cover a broad range of studies that could inform our review. Additionally, we followed a rigorous selection process to ensure that the studies included in our review met the predetermined inclusion criteria.The active constituents of Ginkgo Folium primarily consist of flavonoids and terpenoids, with quercetin, kaempferol, isorhamnetin, ginkgolides, and bilobalide being the major compounds. These active constituents exert their antitumor effects through crucial biological events such as apoptosis, cell cycle arrest, autophagy, and inhibition of invasion and metastasis via modulating diverse signaling pathways. During the process of apoptosis, active constituents primarily exert their effects by modulating the caspase-8 mediated death receptor pathway and caspase-9 mediated mitochondrial pathway via regulating specific signaling pathways. Furthermore, by modulating multiple signaling pathways, active constituents effectively induce G1, G0/G1, G2, and G2/M phase arrest. Among these, the pathways associated with G2/M phase arrest are particularly extensive, with the cyclin-dependent kinases (CDKs) being most involved. Moreover, active constituents primarily mediate autophagy by modulating certain inflammatory factors and stressors, facilitating the fusion stage between autophagosomes and lysosomes. Additionally, through the modulation of specific chemokines and matrix metalloproteinases, active constituents effectively inhibit the processes of epithelial-mesenchymal transition (EMT) and angiogenesis, exerting a significant impact on cellular invasion and migration. Synergistic effects are observed among the active constituents, particularly quercetin and kaempferol.Active components derived from Ginkgo Folium demonstrate a comprehensive antitumor effect across various levels and pathways, presenting compelling evidence for their potential in new drug development. However, in order to facilitate their broad and adaptable clinical application, further extensive experimental investigations are required to thoroughly explore their efficacy, safety, and underlying mechanisms of action.Copyright © 2023. Published by Elsevier B.V.