Molecular imaging of human tumor cells that naturally overexpress type 2 cannabinoid receptors using a quinolone-based near-infrared fluorescent probe

Zhiyuan Wu; Pin Shao; Shaojuan Zhang; Xiaoxi Ling; Mingfeng Bai

doi:10.1117/1.JBO.19.7.076016

18 July 2014 Molecular imaging of human tumor cells that naturally overexpress type 2 cannabinoid receptors using a quinolone-based near-infrared fluorescent probe

Zhiyuan Wu, Pin Shao, Shaojuan Zhang, Xiaoxi Ling, Mingfeng Bai

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Journal of Biomedical Optics, Vol. 19, Issue 7, 076016 (July 2014). https://doi.org/10.1117/1.JBO.19.7.076016

Abstract

Cannabinoid CB2 receptors (CB₂R) hold promise as therapeutic targets for treating diverse diseases, such as cancers, neurodegenerative diseases, pain, inflammation, osteoporosis, psychiatric disorders, addiction, and immune disorders. However, the fundamental role of CB₂R in the regulation of diseases remains unclear, largely due to a lack of reliable imaging tools for the receptors. The goal of this study was to develop a CB₂R-targeted molecular imaging probe and evaluate the specificity of the probe using human tumor cells that naturally overexpress CB₂R. To synthesize the CB₂R-targeted probe (NIR760-Q), a conjugable CB₂R ligand based on the quinolone structure was first prepared, followed by bioconjugation with a near-infrared (NIR) fluorescent dye, NIR760. In vitro fluorescence imaging and competitive binding studies showed higher uptake of NIR760-Q than free NIR760 dye in Jurkat human acute T-lymphoblastic leukemia cells. In addition, the high uptake of NIR760-Q was significantly inhibited by the blocking agent, 4-quinolone-3-carboxamide, indicating specific binding of NIR760-Q to the target receptors. These results indicate that the NIR760-Q has potential in diagnostic imaging of CB₂R positive cancers and elucidating the role of CB₂R in the regulation of disease progression.

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Zhiyuan Wu, Pin Shao, Shaojuan Zhang, Xiaoxi Ling, and Mingfeng Bai "Molecular imaging of human tumor cells that naturally overexpress type 2 cannabinoid receptors using a quinolone-based near-infrared fluorescent probe," Journal of Biomedical Optics 19(7), 076016 (18 July 2014). https://doi.org/10.1117/1.JBO.19.7.076016

Published: 18 July 2014

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