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.

将癌症的成像和治疗结合到一个分子中已成为进行病理学和癌症治疗方法研究的有效策略。在此，已经设计并评估了一种新型的高选择性和灵敏的绿色发射探针（APLN），该探针包含荧光团（萘二甲酰亚胺），连接子和COX-2激酶抑制剂（阿司匹林）。作为典型的限速酶之一，环氧合酶2（COX-2）已被用作成像和治疗靶标，因为该酶在各种癌细胞系中过表达。阿司匹林是一种非甾体类抗炎药（NSAID），据报道可通过下调癌细胞中COX-2的表达来降低癌症的发生率和风险。该APLN在裸鼠的异种移植模型中，已证明该探针可成功标记COX-2酶以鉴定肿瘤并显着抑制肿瘤生长。因此，这种酶靶向的荧光探针（APLN）是用于原位成像和荧光可见的癌症治疗的潜在试剂。