Synthesis and biological evaluation of scopoletin derivatives
Synthesis and biological evaluation of scopoletin derivatives
复制标题
DOI：
10.1016/j.bmc.2012.10.059
复制
发表时间：
2013-01-01
影响因子：
3.5
通讯作者：
Cao, Peng
中科院分区：
文献类型：
--
作者：
Cai, Xueting;Yang, Jie;Cao, Peng
设计并合成了一系列新的东莨菪内酯衍生物。它们的抗增殖作用最初是针对各种人类癌细胞系进行评估的。在所测试的化合物中，A1、A2和D 6显示出显著的抗增殖活性。内皮细胞迁移实验和管腔形成实验检测血管生成。结果表明，A1、A2和D 6在体外抑制血管内皮生长因子（VEGF）刺激的人脐静脉内皮细胞的增殖、迁移和管腔形成。此外，它们在体内抑制绒毛尿囊膜中的血管生长。这种抑制与VEGF触发的ERK 1/2和Akt磷酸化形式的显著减少相关。综上所述，这些研究结果有力地表明，这些东莨菪内酯衍生物可能是结构新颖的血管生成抑制剂。(C)2012爱思唯尔有限公司保留所有权利。
A series of new scopoletin derivatives were designed and synthesized. Their anti-proliferative effect was initially evaluated against various human cancer cell lines. Among the tested compounds, A1, A2, and D6 showed significant anti-proliferative activities. Angiogenesis was detected by endothelial cell migration assay and tube formation study. The results showed that A1, A2, and D6 inhibited the vascular endothelial growth factor (VEGF)-stimulated proliferation, migration, and tube formation of human umbilical vein endothelial cells in vitro. Moreover, they inhibited the vessel growth in the chorioallantoic membrane in vivo. This inhibition was correlated with a significant decrease in the VEGF-triggered phosphorylated forms of ERK1/2 and Akt. In summary, these findings strongly suggested that these scopoletin derivatives might be structurally novel angiogenesis inhibitors. (C) 2012 Elsevier Ltd. All rights reserved.