A sialic acid-targeted near-infrared theranostic for signal activation based intraoperative tumor ablation.
A sialic acid-targeted near-infrared theranostic for signal activation based intraoperative tumor ablation.
复制标题
用于基于信号激活的术中肿瘤消融的唾液酸靶向近红外治疗诊断
DOI：
10.1039/c4sc02248c
复制
发表时间：
2015-01-01
期刊：
影响因子：
8.4
通讯作者：
Han S
中科院分区：
文献类型：
--
作者：
Wu X;Yu M;Lin B;Xing H;Han J;Han S
开发了一种具有pH响应性荧光和光热特性的唾液酸靶向近红外profluorophore，用于手术期间暴露的存活肿瘤的荧光引导分期和光热治疗。使肿瘤分期成为可能的试剂对于癌症手术是有价值的。本文报道了一种可靶向的唾液酸臂近红外荧光团（SA-pNIR）用于荧光引导的肿瘤检测。SA-pNIR由对体内肿瘤靶向有效的唾液酸实体和经历溶酶体酸度触发的荧光异构化的前荧光团组成。SA-pNIR在小鼠中显示出许多有利的生物医学性质，例如高肿瘤与正常组织信号对比度、在肿瘤中的长期保留和低全身毒性。此外，SA-pNIR在细胞中有效地将NIR光转化为细胞毒性热，这表明肿瘤可激活的光热疗法。由于具有高性能的肿瘤照明和溶酶体可激活的光热特性，SA-pNIR是一种有前途的用于手术暴露肿瘤的检测和光热消融的试剂。
A sialic acid-targeted near-infrared profluorophore with pH-responsive fluorescence and photothermal properties was developed for fluorescence-guided staging and photothermal therapy of viable tumors exposed during surgery. 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 in vivo tumor targeting and a profluorophore which undergoes lysosomal acidity-triggered fluorogenic isomerization. SA-pNIR displays a number of advantageous biomedical properties in mice, e.g. 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.