title: A fast tumor-targeting near-infrared fluorescent probe based on bombesin analog for in vivo tumor imaging.
abstract: Bombesin (BBN), an analog of gastrin-releasing peptide (GRP), of which the receptors are over-expressed on various tumor cells, is able to bind to GRP receptor specifically. In this study, a near-infrared fluorescent dye (MPA) and polyethylene glycol (PEG) were conjugated to BBN analog to form BBN[7-14]-MPA and BBN[7-14]-SA-PEG-MPA. The successful synthesis of the two probes was proved by the characterization via sodium dodecylsulfate-polyacrylamide gel electrophoresis, infrared and optical spectra. Cellular uptakes studies indicated that BBN-based probes were mediated by gastrin-releasing peptide receptors (GRPR) on tumor cells and the PEG modified probe had higher affinity. The dynamic distribution and clearance investigations showed that the BBN-based probes were eliminated by the liver-kidney pathway. Furthermore, both of the BBN-based probes displayed tumor-targeting ability in GRPR over-expressed tumor-bearing mice. The PEG modified probe exhibited faster and higher tumor targeting capability than BBN[7-14]-MPA. The results implied that BBN[7-14]-SA-PEG-MPA could act as an effective fluorescence probe for tumor imaging.
authors: Department of Biomedical Engineering, School of Life Science and Technology, State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjia Lane, Gulou District, Nanjing, 210009, China.
authors: Haiyan
authors: H
authors: Chen
authors: Shunan
authors: S
authors: Wan
authors: Fenxia
authors: F
authors: Zhu
authors: Chuan
authors: C
authors: Wang
authors: Sisi
authors: S
authors: Cui
authors: Changli
authors: C
authors: Du
authors: Yuxiang
authors: Y
authors: Ma
authors: Yueqing
authors: Y
authors: Gu
mesh_terms: D000818:Animals; D001839:Bombesin; D045744:Cell Line, Tumor; D005456:Fluorescent Dyes; D006801:Humans; D051379:Mice; D009369:Neoplasms / Q000175:diagnosis* / Q000473:pathology; D049268:Positron-Emission Tomography / Q000379:methods; D019275:Radiopharmaceuticals; D023041:Xenograft Model Antitumor Assays
chemical_list: D005456:Fluorescent Dyes; D019275:Radiopharmaceuticals; D001839:Bombesin
keywords: PEG; bombesin; gastrin-releasing peptide; near-infrared imaging; target; tumor