Imaging and inhibiting cyclooxygenase-2 using aspirin-based fluorescent reporter for the treatment of breast cancer

Abstract Combining imaging and treatment of cancer into one molecule has become an efficient strategy for studies on pathology and cancer therapeutics. Herein, a novel highly selective and sensitive green-emitting probe (APLN), which contained a fluorophore (Naphthalimide), a linker, and a COX-2 kinase inhibitor (aspirin) has been designed and evaluated. Cyclooxygenase-2 (COX-2), as one of the typical rate-limiting enzymes, has been utilized as imaging and therapeutic target since this enzyme is overexpressed in various cancer cell lines. Aspirin, a non-steroidal anti-inflammatory drug (NSAID), has been reported to reduce the incidence and risk of cancers by down-regulating the expression of COX-2 in cancer cells. The APLN probe has been proved to successfully label the COX-2 enzyme to identify tumors and significantly inhibit tumor growth in a xenotransplantation model of nude mice. Therefore, this enzyme-targeted fluorescence probe (APLN) is a potential reagent for in situ imaging and fluorescent-visible cancer therapy.