College of Biomedical Engineering & Instrument Science, Zhejiang University, Hangzhou, 310027, PR China; Zhejiang-Malaysia Joint Research Center for Traditional Medicine, Zhejiang University, Hangzhou, 310027, PR China; Schepens Eye Research Institute of Massachusetts Eye and Ear, Boston, MA, USA; Department of Ophthalmology, Harvard Medical School, Boston, MA, USA.
School of Basic Medical Sciences, Ningxia Medical University, Yinchuan, Ningxia, PR China.
Biomed Pharmacother. 2021 Jan;133:110999. doi: 10.1016/j.biopha.2020.110999. Epub 2020 Nov 21.
Abnormal angiogenesis is associated with intraocular diseases such as proliferative diabetic retinopathy and neovascular age-related macular degeneration, and current therapies for these eye diseases are not satisfactory. The purpose of this study was to determine whether capilliposide B (CPS-B), a novel oleanane triterpenoid saponin derived from Lysimachia capillipes Hemsl, can inhibit vascular endothelial growth factor (VEGF)-induced angiogenesis signaling events and cellular responses in primary human retinal microvascular endothelial cells (HRECs). Our study revealed that the capilliposide B IC for HRECs was 8.5 μM at 72 h and that 1 μM capilliposide B specifically inhibited VEGF-induced activation of VEGFR2 and its downstream signaling enzymes Akt and Erk. In addition, we discovered that this chemical effectively blocked VEGF-stimulated proliferation, migration and tube formation of the HRECs, suggesting that capilliposide B is a promising prophylactic for angiogenesis-associated diseases such as proliferative diabetic retinopathy.
异常血管生成与眼部疾病有关，如增生性糖尿病视网膜病变和新生血管性年龄相关性黄斑变性，而目前这些眼部疾病的治疗方法并不令人满意。本研究旨在确定毛蕊花糖苷 B（CPS-B），一种从过路黄中提取的新型齐墩果烷三萜皂苷，是否可以抑制血管内皮生长因子（VEGF）诱导的原代人视网膜微血管内皮细胞（HRECs）中的血管生成信号事件和细胞反应。我们的研究表明，毛蕊花糖苷 B 对 HRECs 的 IC 在 72 小时时为 8.5 μM，而 1 μM 毛蕊花糖苷 B 可特异性抑制 VEGF 诱导的 VEGFR2 及其下游信号酶 Akt 和 Erk 的激活。此外，我们发现该化合物可有效抑制 VEGF 刺激的 HRECs 增殖、迁移和管腔形成，表明毛蕊花糖苷 B 是一种有前途的增生性糖尿病视网膜病变等血管生成相关疾病的预防药物。
