A fast tumora??targeting neara??infrared fluorescent probe based on bombesin analog for in vivo tumor imaging

摘要

Bombesin (BBN), an analog of gastrina??releasing peptide (GRP), of which the receptors are overa??expressed on various tumor cells, is able to bind to GRP receptor specifically. In this study, a neara??infrared fluorescent dye (MPA) and polyethylene glycol (PEG) were conjugated to BBN analog to form BBN[7a??14]a??MPA and BBN[7a??14]a??SAa??PEGa??MPA. The successful synthesis of the two probes was proved by the characterization via sodium dodecylsulfatea??polyacrylamide gel electrophoresis, infrared and optical spectra. Cellular uptakes studies indicated that BBNa??based probes were mediated by gastrina??releasing peptide receptors (GRPR) on tumor cells and the PEG modified probe had higher affinity. The dynamic distribution and clearance investigations showed that the BBNa??based probes were eliminated by the livera??kidney pathway. Furthermore, both of the BBNa??based probes displayed tumora??targeting ability in GRPR overa??expressed tumora??bearing mice. The PEG modified probe exhibited faster and higher tumor targeting capability than BBN[7a??14]a??MPA. The results implied that BBN[7a??14]a??SAa??PEGa??MPA could act as an effective fluorescence probe for tumor imaging. Copyright ?? 2014 John Wiley & Sons, Ltd.