A novel near‐infrared fluorescent probe for monitoring cyclooxygenase‐2 in inflammation and tumor. Issue 6 (6th March 2018)

• Record Type: Journal Article
• Authors: Zhang, Qi; Han, Zhihao; Tao, Ji; Zhang, Wancun; Li, Ping; Tang, Liping; Gu, Yueqing
• Is Part Of: Journal of biophotonics. Volume 11:Issue 6(2018)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2018-03-06
• Subjects: COX‐2 -- fluorescence -- inflammation -- molecular imaging -- tumor; Photonics -- Periodicals; Optical materials -- Periodicals; Optics -- Periodicals; Medical instruments and apparatus -- Periodicals; 621.3605
• DOI: 10.1002/jbio.201700339
• Languages: English
• ISSNs: 1864-063X

Abstract

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. Abstract : We have successfully synthesized a novel near‐infrared (NIR) imaging probe (named celecoxib‐MPA probe [CMP]) for targeting cyclooxygenase‐2 (COX‐2) by combining celecoxib and a water‐soluble NIR dye. This probe possesses good biocompatibility, long‐term observation, satisfying COX‐2 specific targeting ability. For in vivo applications, CMP can bind to locally endogenic COX‐2 and exhibits prominent fluorescence in inflamed or cancerous tissues. The current studies suggest that the probe CMP is useful for monitoring COX‐2 in inflammation and tumor.