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基于光活化诊疗一体试剂的靶向荧光成像及对 H₂O₂高表达癌细胞的光毒性作用

Target-Selective Fluorescence Imaging and Photocytotoxicity against H O High-Expressing Cancer Cells Using a Photoactivatable Theranostic Agent.

机构信息

Department of Applied Chemistry, Faculty of Science and Technology, Keio University, 3-14-1 Hiyoshi, Kohoku-ku, Yokohama, 223-8522, Japan.

出版信息

Chem Asian J. 2017 Oct 18;12(20):2656-2659. doi: 10.1002/asia.201701004. Epub 2017 Sep 21.

DOI:10.1002/asia.201701004
PMID:28834271
Abstract

A purpose-designed and synthesized H O -reactive and photoactivatable theranostic agent 1 consisting of 1) an arylboronic acid moiety, 2) pro-fluorophore moiety, and 3) photoactivatable moiety (photosensitizer), selectively and effectively reacted with H O while simultaneously releasing resorufin for fluorescence detection under neutral aqueous conditions. In addition, 1 was cell-permeable, and exhibited effective photocytotoxicity against fluorescently visualized cells only upon photoirradiation. The results also showed that 1 produced a selective fluorescence response to H O , even in living cultured cells.

摘要

一种专门设计和合成的 H2O2-反应性和光活化治疗剂 1,由 1)芳基硼酸部分,2)前荧光团部分和 3)光活化部分(光敏剂)组成,在中性水条件下选择性和有效地与 H2O2反应,同时释放用于荧光检测的 Resorufin。此外,1 具有细胞通透性,并仅在光照下表现出对荧光可视化细胞的有效光细胞毒性。结果还表明,1 对 H2O2产生了选择性荧光响应,即使在活的培养细胞中也是如此。

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