Diabetic retinopathy (DR) remains high incidence and accounts for severe impact on vision in diabetics, but its mechanism is still poorly understood. Abnormal migration and proliferation of endothelial cells (ECs) drive neovascular retinopathies, which has an important role in promoting the occurrence and development of DR. In this study, we designed and synthesized a series of PEDF-derived peptides as angiogenesis inhibitors. Especially, compound G24 significantly inhibited the cell proliferation in VEGF-activated human umbilical vein endothelial cells (HUVECs) with IC₅₀ values of 2.88 ± 0.19 μM. Further biological evaluation demonstrated that compound G24 exhibited strong inducing-effects on cell apoptosis and internalization of 67LR, and advanced inhibitory potency in cell migration and angiogenesis formed by HUVECs in vitro. In summary, the optimal compound G24 as a novel angiogenesis inhibitor showed the potentiality in the further research for the treatment for DR.

糖尿病视网膜病变 (DR) 的发病率仍然很高，对糖尿病患者的视力造成严重影响，但其机制仍知之甚少。内皮细胞（ECs）的异常迁移和增殖驱动新生血管性视网膜病变，这对促进DR的发生和发展具有重要作用。在这项研究中，我们设计并合成了一系列 PEDF 衍生肽作为血管生成抑制剂。特别是，化合物G24显着抑制 VEGF 激活的人脐静脉内皮细胞 (HUVEC) 的细胞增殖，IC ₅₀值为 2.88 ± 0.19 μM。进一步的生物学评估表明，化合物G24对细胞凋亡和 67LR 的内化有很强的诱导作用，对体外HUVECs 形成的细胞迁移和血管生成具有高度抑制作用。综上所述，最佳化合物G24作为一种新型血管生成抑制剂显示出在DR治疗的进一步研究中的潜力。