State Key Laboratory of Fine Chemicals , Dalian University of Technology , 2 Linggong Road , High-Tech District, Dalian 116024 , China.
Department School of Life Science and Biotechnology , Dalian University of Technology , 2 Linggong Road , High-Tech District, Dalian 116024 , China.
Anal Chem. 2018 Apr 17;90(8):5187-5193. doi: 10.1021/acs.analchem.7b05337. Epub 2018 Apr 3.
Cyclooxygenase-2 (COX-2) is an enzyme overexpressed in most types of cancers and has been used for an excellent targetable biomarker. Celecoxib is an effective inhibitor of COX-2, used in anti-inflammation. Herein we report a one and two-photon fluorescence probe (NP-C6-CXB) for COX-2, based on the conjugation of naphthalamide with Celecoxib, by using flexible hexylene linker. NP-C6-CXB is nonfluorescent in buffer solution and normal cells, while it shows bright fluorescence in solutions and cancer cells in the presence of COX-2 with an excellent selectivity. Interestingly, NP-C6-CXB can discriminate cancer cells (MCF-7) from normal cells (COS-7) in the single culture medium under confocal microscopy. Due to the selective binding affinity of NP-C6-CXB with a COX-2 enzyme, the intensity is proportional to the level of COX-2 enzyme in cancer cells. In vivo and in vitro experiments proved that NP-C6-CXB is a potential tool for identification of tumor and might be used in surgical resection of COX-2 expressed tumors.
环氧化酶-2(COX-2)在大多数类型的癌症中过度表达,已被用作出色的靶向生物标志物。塞来昔布是一种有效的 COX-2 抑制剂,用于抗炎。本文报告了一种基于萘酰胺与塞来昔布连接的,通过使用柔性己烯 linker 的 COX-2 一和双光子荧光探针(NP-C6-CXB)。NP-C6-CXB 在缓冲液和正常细胞中无荧光,但在存在 COX-2 的情况下,它在溶液和癌细胞中显示出明亮的荧光,具有出色的选择性。有趣的是,NP-C6-CXB 可以在共聚焦显微镜下在单一培养基中区分癌细胞(MCF-7)和正常细胞(COS-7)。由于 NP-C6-CXB 与 COX-2 酶具有选择性结合亲和力,其强度与癌细胞中 COX-2 酶的水平成正比。体内和体外实验证明,NP-C6-CXB 是识别肿瘤的潜在工具,可能用于 COX-2 表达肿瘤的手术切除。