Precise Detection and Visualization of Cyclooxygenase-2 for Golgi Imaging by a Light-Up Aggregation-Induced Emission-Based Probe

Abstract

Precision-targeted detection of cancer in a rapid and sensitive fashion remains a significant challenge in prevention, management, and in particular, treatment. Herein, we have designed and synthesized a unique cyclooxygenase-2 (COX-2) fluorescence probe, dimethylamine-9,10-distyrylanthracene-indomethacin (NDSA-IMC), that could visualize the site of highly expressed COX-2 in the Golgi apparatus of cancer cells, using 9,10-diatyrylanthracene derivative as the luminous unit and a selective inhibitor, indomethacin (IMC), as the recognizing moiety for COX-2. In an aqueous solution, the free state NDSA-IMC showed a weak emission in the absence of COX-2 but enhanced emission in the presence of the enzyme due to the restriction of intramolecular motion of aggregation-induced emission-active NDSA-IMC when bound to COX-2. Cell imaging and flow cytometry experiments indicated that NDSA-IMC could discriminate between cancer and normal cells and visualize the Golgi apparatus of cancer cells via specific targeting of COX-2. Therefore, NDSA-IMC might potentially detect early cancer lesions and ultimately mitigate the population of cancer burden in society.