In Situ Construction Of Piptide-based Ligand Network To Integrin α_vβ₃ For Angiogenesis Inhibition

Angiogenesis occurs during the process of tumor growth,invasion and metastasis,and is essential for the survival of solid tumors.As the main metabolic pathway,blood vessels of tumor provide tumor cells with oxygen and nutrients.Therefore,vascular disrupting agents are often adopted to cut off the nutrition supply and bring about an adjuvant treatment effect to starve tumors in addition to periodic chemotherapy and radiation therapy.As a membrane receptor significantly overexpressed on vascular endothelial cells of tumor,integrin α_vβ₃ is a suitable targeting site for anti-angiogenesis of tumor.We designed and prepared a self-assembling anti-angiogenic peptide（SAP）with the ability to targeting α_vβ₃ and morphology transformation.SAP formed nanoparticles in solution and transformed into nanofibrous network after specifically binding to integrin α_vβ₃ 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.