An Off鈥揙n COX-2-Specific Fluorescent Probe: Targeting the Golgi Apparatus of Cancer Cells

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• 作者：Hua Zhang ; Jiangli Fan ; Jingyun Wang ; Shuangzhe Zhang ; Bairui Dou ; Xiaojun Peng
• 刊名：The Journal of the American Chemical Society
• 出版年：2013
• 出版时间：August 7, 2013
• 年：2013
• 卷：135
• 期：31
• 页码：11663-11669
• 全文大小：440K
• 年卷期：v.135,no.31(August 7, 2013)
• ISSN：1520-5126

文摘

Identifying cancer cells and quantifying cancer-related events in particular organelles in a rapid and sensitive fashion are important for early diagnosis and for studies on pathology and therapeutics of cancers. Herein a smart 鈥渙ff鈥搊n鈥?cyclooxygenase-2-specific fluorescence probe (ANQ-IMC-6), able to report the presence of cancer cells and to image Golgi-related events, has been designed and evaluated. Cyclooxygenase-2 (COX-2) has been used as imaging target in the probe design, since this enzyme is a biomarker of virtually all cancer cell lines. In the free state in aqueous solution, ANQ-IMC-6 mainly exists in a folded conformation where probe fluorescence is quenched through photoinduced electron transfer between the fluorophore acenaphtho[1,2-b]quinoxaline (ANQ) and the recognition group, indomethacin (IMC). Fluorescence is turned on, by restraining the photoinduced electron transfer, when ANQ-IMC-6 is forced to adopt the unfolded state following binding to COX-2 in the Golgi apparatus of cancer cells. ANQ-IMC-6 provides high signal-to-background staining and has been successfully used to rapidly differentiate cancer cells from normal cells when using flow cytometry and one- and two-photon fluorescence microscopic imaging. Furthermore, ANQ-IMC-6 may be able to visualize dynamic changes of the Golgi apparatus during cancer cell apoptosis, with possible application to early diagnosis.