In situ construction of ligand nano-network to integrin alpha(v)beta(3) for angiogenesis inhibition

Angiogenesis occurs during the process of tumor growth, invasion and metastasis, and is essential for the survival of solid tumors. As an integrin significantly overexpressed in human tumor vascular endothelial cells, alpha(v)beta(3) is a suitable targeting site for anti-angiogenesis of tumor. We designed and prepared a self-assembling peptide (SAP) with the ability to targeting alpha(v)beta(3) and self-assembly. SAP formed nanoparticles in solution and transformed into nanofibrous network once specifically binding to integrin alpha(v)beta(3) on the surface of human umbilical vein endothelial cells (HUVECs). The SAP network stably anchored on HUVECs over 24 h, which consequently resulted in high-efficient inhibition of vascularization. In vitro anti-angiogenesis experiment displayed that the inhibition rate of tube-formation reached 94.9%. In vivo anti-angiogenesis array based on chick chorioallantoic membrane (CAM) model exhibited that the SAP had an inhibition rate up to 63.1%. These results indicated the outstanding anti-angiogenic ability of SAP, potentially for tumor therapy. (C) 2020 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.