Lin Shengying, Tang Roy Wai-Lun, Ye Yutong, Xia Chenxi, Wu Jiahui, Duan Ran, Leung Ka-Wing, Dong Tina Ting-Xia, Tsim Karl Wah-Keung
Center for Chinese Medicine, Division of Life Science, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, China.
State Key Laboratory of Molecular Neuroscience, Division of Life Science, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, China.
Molecules. 2025 Jan 10;30(2):257. doi: 10.3390/molecules30020257.
Vascular endothelial growth factor (VEGF), also known as VEGF-A, has been linked to various diseases, such as wet age-related macular degeneration (wAMD) and cancer. Even though there are VEGF inhibitors that are currently commercially available in clinical applications, severe adverse effects have been associated with these treatments. There is still a need to develop novel VEGF-based therapeutics against these VEGF-related diseases. Here, we established a series of VEGF-based computational docking analyses and cell models, such as a wound healing assay in HaCaT cells and an evaluation of NF-κB performance in macrophages, to screen a large library of flavonoid-type phytochemicals. Three flavonoids, namely, farrerol, ononin and (-)-epicatechin, were shown to express binding affinities to VEGF protein and inhibit VEGF-mediated biological activities. The investigation evidently suggested that the three flavonoids above could be considered potential anti-VEGF agents for the following drug development against VEGF-mediated diseases.
血管内皮生长因子（VEGF），也被称为VEGF - A，与多种疾病有关，如湿性年龄相关性黄斑变性（wAMD）和癌症。尽管目前在临床应用中有市售的VEGF抑制剂，但这些治疗方法已出现严重的不良反应。仍然需要开发新型的基于VEGF的疗法来对抗这些与VEGF相关的疾病。在此，我们建立了一系列基于VEGF的计算对接分析和细胞模型，如在HaCaT细胞中的伤口愈合试验以及对巨噬细胞中NF - κB性能的评估，以筛选大量黄酮类植物化学物质库。三种黄酮类化合物，即杜鹃素、鹰嘴豆芽素A和（ - ） - 表儿茶素，显示出与VEGF蛋白的结合亲和力，并抑制VEGF介导的生物学活性。该研究显然表明，上述三种黄酮类化合物可被视为潜在的抗VEGF药物，用于后续针对VEGF介导疾病的药物开发。
