title: In vivo near-infrared imaging and phototherapy of tumors using a cathepsin B-activated fluorescent probe.
abstract: The development of multifunctional reagents for simultaneous specific near-infrared (NIR) imaging and phototherapy of tumors is of great significance. This work describes the design of a cathepsin B-activated fluorescent probe (CyA-P-CyB) and its applications as an NIR imaging probe for tumor cells and as a phototherapy reagent for tumors. In vitro experiments demonstrated that CyA-P-CyB was activated via the cleavage of a peptide linker by cathepsin B in tumor cells to produce fluorescence in the NIR region based on a FRET mechanism. MTT assays showed that the phototoxicity of CyA-P-CyB toward cells depended on the activity of cathepsin B, and the probe exhibited specific phototoxicity toward tumor cells. CyA-P-CyB was also successfully applied to the in vivo imaging and phototherapy of tumors. Histological analysis indicated that CyA-P-CyB had no cytotoxic effects on seven mouse tissues (lung, liver, heart, kidney, pancreas, spleen and brain) after the CyA-P-CyB treatment and laser irradiation.
authors.affiliation: Department of Chemistry and Nano Science, Ewha Womans University, Seoul 120-750, South Korea; State Key Laboratory of Materials-Oriented Chemical Engineering, College of Chemical Engineering, Jiangsu National Synergetic Innovation Center for Advanced Materials (SICAM), Nanjing Tech University, Nanjing 210009, China.
authors.forename: Xiaoqiang
authors.initials: X
authors.lastname: Chen
authors.affiliation: Department of Chemistry and Nano Science, Ewha Womans University, Seoul 120-750, South Korea.
authors.forename: Dayoung
authors.initials: D
authors.lastname: Lee
authors.affiliation: Severance Biomedical Science Institute, Brain Korea 21 PLUS Project for Medical Science, Yonsei University College of Medicine, Seoul 120-752, South Korea.
authors.forename: Sungsook
authors.initials: S
authors.lastname: Yu
authors.affiliation: Department of Chemistry and Nano Science, Ewha Womans University, Seoul 120-750, South Korea.
authors.forename: Gyoungmi
authors.initials: G
authors.lastname: Kim
authors.affiliation: Department of Chemistry and Nano Science, Ewha Womans University, Seoul 120-750, South Korea.
authors.forename: Songyi
authors.initials: S
authors.lastname: Lee
authors.affiliation: Severance Biomedical Science Institute, Brain Korea 21 PLUS Project for Medical Science, Yonsei University College of Medicine, Seoul 120-752, South Korea.
authors.forename: Yejin
authors.initials: Y
authors.lastname: Cho
authors.affiliation: Severance Biomedical Science Institute, Brain Korea 21 PLUS Project for Medical Science, Yonsei University College of Medicine, Seoul 120-752, South Korea.
authors.forename: Haengdueng
authors.initials: H
authors.lastname: Jeong
authors.affiliation: Severance Biomedical Science Institute, Brain Korea 21 PLUS Project for Medical Science, Yonsei University College of Medicine, Seoul 120-752, South Korea. Electronic address: kitaek@yuhs.ac.
authors.forename: Ki Taek
authors.initials: KT
authors.lastname: Nam
authors.affiliation: Department of Chemistry and Nano Science, Ewha Womans University, Seoul 120-750, South Korea. Electronic address: jyoon@ewha.ac.kr.
authors.forename: Juyoung
authors.initials: J
authors.lastname: Yoon
mesh_terms: D000818:Animals; D002401:Cathepsin B; D045744:Cell Line, Tumor; D005456:Fluorescent Dyes / Q000138:chemical synthesis; D006801:Humans; D007259:Infrared Rays; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D008856:Microscopy, Fluorescence / Q000379:methods*; D009374:Neoplasms, Experimental / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology*; D009842:Oligopeptides / Q000737:chemistry / Q000493:pharmacokinetics*; D010778:Photochemotherapy / Q000379:methods*; D017319:Photosensitizing Agents / Q000008:administration & dosage; D000068936:Theranostic Nanomedicine / Q000379:methods*; D016896:Treatment Outcome
chemical_list: D005456:Fluorescent Dyes; C504380:Gly-Phe-Leu-Gly; D009842:Oligopeptides; D017319:Photosensitizing Agents; D002401:Cathepsin B
keywords: Enzyme-activated fluorescence; Multiple functional probe; NIR bioimaging; Specific phototherapy