Synthesis and evaluation of a novel BODIPY fluorescent probe targeting integrin αvβ3 for cancer diagnosis.

A series of integrin α v β 3 targeting BODIPY-RGD conjugate were designed and synthesized. Their in vitro and in vivo fluorescence imaging behaviors were investigated. The small molecule compound was designed as an optical imaging near-infrared fluorescent dye which was combined RGD peptide with the meso -amide BODIPYs using succinic moiety as a spacer. The construction alleviated the traditional BODIPY problems including poor water solubility, aggregate caused quench (ACQ) effect, low biocompatibility, etc. In cellular research, BDP-RGD-2 showed rapid, selective uptake in 3 highly expressing integrin α v β 3 cell lines MDA-MB-231, A549, U87MG at different extent rather than an integrin α v β 3 low level expression cell MCF-7. In animal study, fluorescence imaging of U87MG model targeted by BDP-RGD-2 displayed a highest tumor uptake level and T/N ratio up to 6 h after tail-intravenous injection, which demonstrated BDP-RGD-2 was a promising probe for tracing integrin α v β 3 overexpressing tumors. [Display omitted] • Meso Carboxylic amide BODIPY is an excellent platform for imaging applications. • RGD bearing meso carboxylic amide BODIPY exhibited favorable imaging property. • BDP-RGD-2 is a promising probe for tracing α v β 3 overexpressing tumors. [ABSTRACT FROM AUTHOR]