肿瘤是威胁人类生命健康的重大疾病之一，目前抗肿瘤药物研究呈现出多元化发展的趋势，其中以肿瘤血管生成为靶点，开发血管新生抑制剂，已经成为抗肿瘤研究中1个重要的领域。血管内皮生长因子（vascular endothelial growth factor，VEGF）是血管内皮细胞生长和分化的首要因子，在血管生成过程中非常关键。通常VEGF指的是VEGF-A，其结合受体包括血管内皮生长因子受体1（vascular endothelial growth factor receptor 1，VEGFR1）和VEGFR2。目前研究认为，VEGF/VEGFR途径是介导肿瘤血管生成的关键通路。针对VEGF及其受体的靶向治疗可使肿瘤内新生血管减少，有助于抑制肿瘤的增殖、侵袭和转移。传统的中医药在肿瘤辅助治疗方面颇具特色，从中药中筛选和开发具有血管抑制活性的抗肿瘤药物潜力巨大。对以VEGF/VEGFR为靶点的抗肿瘤天然化合物作用机制研究进展进行综述，以期为该类化合物的研究开发提供参考。

Cancer is one of the major harmful diseases threatening human health and life. Development of angiogenesis inhibitors targeting tumor angiogenesis has become an important topic in the field of antitumor. Vascular endothelial growth factor (VEGF), a primary factor in growth and differentiation of vascular endothelial cell, plays an important role in angiogenesis. VEGF receptors include vascular endothelial growth factor receptor 1 (VEGFR1) and VEGFR2. VEGF/VEGFR2 signaling pathway is a critical pathway in regulating tumor angiogenesis. The amount of new blood vessels in tumor could be reduced and the proliferation, invasion, metastasis of tumor could be inhibited by treatment targeting VEGF/VEGFR. Traditional Chinese medicine possesses characteristic in the treatment of cancer, and it has huge potential in screening and developing tumor-angiogenesis inhibitors. Progress in research of natural products targeting VEGF/VEGFR was reviewed in this paper to provide reference for further study and development of these products.

国家青年自然科学基金项目（81502937）；滨州医学院科研启动基金（BY2016KYQD20）；滨州医学院科技计划项目（BY2015KJ05）