Kim Dong Yoon, Hong Seong-Min, Cho Jeong-Seok, Lee Sae-Byuk, Cho Hyun-Dong
Department of Food and Nutrition, Sunchon National University, Jeonnam 57922, Korea.
College of Pharmacy, Gachon University, Incheon 21936, Korea.
Prev Nutr Food Sci. 2024 Sep 30;29(3):321-331. doi: 10.3746/pnf.2024.29.3.321.
Age-related macular degeneration (AMD), often triggered by endothelial barrier disruption through vascular endothelial growth factor (VEGF), is a leading cause of blindness. This study investigated the inhibitory effects of phenolic compounds on VEGF-induced endothelial cell proliferation, migration, angiogenesis, and permeability using human retinal microvascular endothelial cells (hRECs). Thirty-seven polyphenolic compounds were selected from various databases based on their antioxidant properties, abundance in food, and solubility. These compounds significantly reduced migration, tube formation, and endothelial permeability in VEGF-stimulated hRECs. Notably, formononetin, eriodictyol, biochanin A, and p-coumaric acid were more effective in suppressing VEGF-induced angiogenesis and endothelial permeability than lutein. Molecular docking simulations revealed that formononetin, eriodictyol, and biochanin A had relatively lower binding energies with VEGF receptor 2 (VEGFR2) than lutein and sorafenib. These findings highlight the potential of phenolic compounds to be used as VEGFR2 inhibitors and an alternative strategy for preventing AMD.
年龄相关性黄斑变性（AMD）通常由血管内皮生长因子（VEGF）导致的内皮屏障破坏引发，是失明的主要原因。本研究使用人视网膜微血管内皮细胞（hRECs），调查了酚类化合物对VEGF诱导的内皮细胞增殖、迁移、血管生成和通透性的抑制作用。基于其抗氧化特性、在食物中的丰度和溶解性，从各种数据库中选择了37种多酚化合物。这些化合物显著降低了VEGF刺激的hRECs中的迁移、管形成和内皮通透性。值得注意的是，芒柄花黄素、圣草酚、鹰嘴豆芽素A和对香豆酸在抑制VEGF诱导的血管生成和内皮通透性方面比叶黄素更有效。分子对接模拟显示，芒柄花黄素、圣草酚和鹰嘴豆芽素A与VEGF受体2（VEGFR2）的结合能比叶黄素和索拉非尼相对更低。这些发现突出了酚类化合物用作VEGFR2抑制剂的潜力以及预防AMD的替代策略。
