A novel near-infrared fluorescent probe for monitoring cyclooxygenase-2 in inflammation and tumor.

Abstract

Targeting cyclooxygenase-2 (COX-2) for molecular imaging is an attractive approach applicable for its overexpression in inflammation and many malignancies. Herein, for monitoring COX-2, we synthesize a specific COX-2 probe celecoxib-MPA probe (CMP), based on celecoxib and a water-soluble near-infrared dye dye ICG-Der-02 (MPA). Its high affinity for binding to COX-2 is verified by molecular docking, dynamics simulation and inhibition assay. At cellular level, CMP selectively accumulates in cytoplasm of COX-2-positive cells. in vivo assays, probe guided-imaging in inflamed or cancerous tissues confirms that CMP can bind to the locally endogenic COX-2 and exhibit intense fluorescence. Importantly, we further prove the targeting specificity of CMP as the fluorescence is significantly reduced by blocking COX-2 active site through preinjection with celecoxib. The results suggest that the probe CMP, with favorable hydrophilic property, good biocompatibility, long-term observation, excellent targeting ability and optical imaging capability, could serve as a promising probe for real-time monitoring COX-2 in inflammation and tumor.

• Authors: Qi Zhang, Zhihao Han, Ji Tao, Wancun Zhang, Ping Li, Liping Tang, Yueqing Gu
• Journal: Journal of biophotonics (J Biophotonics) Vol. 11 Issue 6 Pg. e201700339 (06 2018) ISSN: 1864-0648 [Electronic] Germany
• PMID: 29341436 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: © 2018 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Chemical References

• Carbocyanines
• Fluorescent Dyes
• ICG-Der-02-2DG
• Water
• Cyclooxygenase 2
• Celecoxib
• Glucosamine

Topics

• Animals
• Carbocyanines (chemistry)
• Celecoxib (chemistry)
• Cyclooxygenase 2 (chemistry, metabolism)
• Female
• Fluorescent Dyes (chemical synthesis, chemistry, metabolism)
• Glucosamine (analogs & derivatives, chemistry)
• HCT116 Cells
• Hep G2 Cells
• Humans
• Infrared Rays
• Mice
• Molecular Docking Simulation
• Molecular Dynamics Simulation
• Protein Conformation
• Solubility
• Water (chemistry)