Wu Xuanjun, Yu Mingzhu, Lin Bijuan, Xing Hongjie, Han Jiahuai, Han Shoufa
Department of Chemical Biology , College of Chemistry and Chemical Engineering , the Key Laboratory for Chemical Biology of Fujian Province , The MOE Key Laboratory of Spectrochemical Analysis & Instrumentation , and Innovation Center for Cell Biology , Xiamen University , Xiamen , 361005 , China . Email:
State Key Laboratory of Cellular Stress Biology , Innovation Center for Cell Biology , School of Life Sciences , Xiamen University , Xiamen , 361005 , China.
Chem Sci. 2015 Jan 1;6(1):798-803. doi: 10.1039/c4sc02248c. Epub 2014 Sep 25.
Agents enabling tumor staging are valuable for cancer surgery. Herein, a targetable sialic acid-armed near-infrared profluorophore (SA-pNIR) is reported for fluorescence guided tumor detection. SA-pNIR consists of a sialic acid entity effective for tumor targeting and a profluorophore which undergoes lysosomal acidity-triggered fluorogenic isomerization. SA-pNIR displays a number of advantageous biomedical properties in mice, high tumor-to-normal tissue signal contrast, long-term retention in tumors and low systemic toxicity. In addition, SA-pNIR effectively converts NIR light into cytotoxic heat in cells, suggesting tumor-activatable photothermal therapy. With high performance tumor illumination and lysosome-activatable photothermal properties, SA-pNIR is a promising agent for detection and photothermal ablation of surgically exposed tumors.
能够实现肿瘤分期的试剂对于癌症手术很有价值。在此，报道了一种可靶向的唾液酸修饰的近红外前体荧光团（SA-pNIR）用于荧光引导的肿瘤检测。SA-pNIR由对肿瘤具有靶向作用的唾液酸实体和一种前体荧光团组成，该前体荧光团会经历溶酶体酸性触发的荧光异构化。SA-pNIR在小鼠中表现出许多有利的生物医学特性，如肿瘤与正常组织的信号对比度高、在肿瘤中长期保留以及全身毒性低。此外，SA-pNIR能在细胞中将近红外光有效转化为细胞毒性热，提示其具有肿瘤激活的光热疗法作用。凭借高性能的肿瘤照明和溶酶体激活的光热特性，SA-pNIR是用于手术暴露肿瘤检测和光热消融的一种有前景的试剂。
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