Carboxylesterase-Cleavable Biotinylated Nanoparticle for Tumor-Dual Targeted Imaging.

Abstract

Near-infrared (NIR) nanoprobes with fluorescence "Turn-On" property are advantageous in cancer diagnosis but, to the best of our knowledge, "smart" nanoprobe that simultaneously targets both biotin receptor and carboxylesterase (CES) for HepG2 tumor-dual targeted imaging has not been reported. Methods: Using CBT-Cys click condensation reaction, we rationally designed a "smart" NIR fluorescence probe H2N-Cys(StBu)-Lys(Biotin)-Ser(Cy5.5)-CBT (NIR-CBT) and used it to facilely prepare the fluorescence-quenched nanoparticle NIR-CBT-NP. Results: In vitro results indicated that, after NIR-CBT-NP was incubated with CES for 6 h, its fluorescence was turned "On" by 69 folds. Cell experiments verified that NIR-CBT-NP was uptaken by HepG2 cells via biotin receptor-assisted endocytosis and its fluorescence was turned "On" by intracellular CES hydrolysis. Moreover, NIR-CBT-NP was successfully applied to image both biotin receptor- and CES-overexpressing HepG2 tumors. Conclusion: Fluorescence-quenched nanoparticle NIR-CBT-NP was facilely prepared to actively target biotin receptor-overexpressing HepG2 cancer cells and turn the fluorescence "On" by intracellular CES hydrolysis for tumor-dual targeted imaging. We anticipate that our fluorescence "Turn-On" nanoparticle could be applied for liver cancer diagnosis in clinic in the near future.

• Authors: Peiyao Chen, Wen Kuang, Zhen Zheng, Shuye Yang, Yaling Liu, Lanhong Su, Kui Zhao, Gaolin Liang
• Journal: Theranostics (Theranostics) Vol. 9 Issue 24 Pg. 7359-7369 ( 2019) ISSN: 1838-7640 [Electronic] Australia
• PMID: 31695773 (Publication Type: Evaluation Study, Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: © The author(s).

Chemical References

• Benzothiazoles
• Fluorescent Dyes
• aminobenzothiazole compound
• Carboxylesterase

Topics

• Animals
• Benzothiazoles (chemistry)
• Biotinylation
• Carboxylesterase (chemistry)
• Fluorescence
• Fluorescent Dyes (chemistry)
• Hep G2 Cells
• Humans
• Infrared Rays
• Mice, Inbred BALB C
• Mice, Nude
• Nanoparticles (chemistry)
• Neoplasms (diagnostic imaging)
• Optical Imaging (instrumentation, methods)