Lin Shengying, Guo Maggie Suisui, Tang Roy Wai-Lun, Ye Yutong, Wu Jiahui, Ho Yuen Man, Duan Ran, Leung Ka Wing, Dong Tina Ting-Xia, Tsim Karl Wah-Keung
Center for Chinese Medicine R & D, Division of Life Science, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, China.
Molecules. 2025 May 27;30(11):2345. doi: 10.3390/molecules30112345.
Vascular endothelial growth factor (VEGF), also known as VEGF-A, has been reported to mediate various diseases, including cancer and wet age-related macular degeneration (wAMD). Despite the fact that VEGF inhibitors are commercially available and appear to be effective in clinical applications, adverse effects have been caused by these treatments. There is an unmet need for developing novel VEGF-targeted treatments against these diseases. Resveratrol, a phytochemical derived from fruits and vegetables, has shown promising potency in suppressing VEGF-mediated bioactivities through a series of in vitro and in vivo testing models. Herein, we report that RE-1, a synthetic resveratrol-type analog, displays robust inhibitory activities against VEGF and its downstream signaling pathways, surpassing its parental molecule, resveratrol. In addition, the drug capabilities of RE-1 were evaluated. As a newly synthesized chemical, RE-1 could be considered for subsequent pharmacological development targeting VEGF-related diseases.
血管内皮生长因子（VEGF），也称为VEGF - A，据报道可介导多种疾病，包括癌症和湿性年龄相关性黄斑变性（wAMD）。尽管VEGF抑制剂已在市场上有售且在临床应用中似乎有效，但这些治疗方法也会引起不良反应。开发针对这些疾病的新型VEGF靶向治疗方法仍存在未满足的需求。白藜芦醇是一种源自水果和蔬菜的植物化学物质，通过一系列体外和体内测试模型，已显示出在抑制VEGF介导的生物活性方面具有可观的效力。在此，我们报告一种合成的白藜芦醇型类似物RE - 1对VEGF及其下游信号通路具有强大的抑制活性，超过其母体分子白藜芦醇。此外，还评估了RE - 1的药物性能。作为一种新合成的化学物质，RE - 1可考虑用于后续针对VEGF相关疾病的药理学开发。
