Molecular Imaging Program, Center for Cancer Research, National Cancer Institute, and NIH Library, National Institutes of Health, Bethesda, MD, USA.
Mol Imaging. 2009 Dec;8(6):341-54.
Fluorophores are potentially useful for in vivo cancer diagnosis. Using relatively inexpensive and portable equipment, optical imaging with fluorophores permits real-time detection of cancer. However, fluorophores can be toxic and must be investigated before they can be administered safely to patients. A review of published literature on the toxicity of 19 widely used fluorophores was conducted by searching 26 comprehensive biomedical and chemical literature databases and analyzing the retrieved material. These fluorophores included Alexa Fluor 488 and 514, BODIPY FL, BODIPY R6G, Cy 5.5, Cy 7, cypate, fluorescein, indocyanine green, Oregon green, 8-phenyl BODIPY, rhodamine 110, rhodamine 6G, rhodamine X, rhodol, TAMRA, Texas red, and Tokyo green. Information regarding cytotoxicity, tissue toxicity, in vivo toxicity, and mutagenicity was included. Considerable toxicity-related information was available for the Food and Drug Administration (FDA)-approved compounds indocyanine green and fluorescein, but published information on many of the non-FDA-approved fluorophores was limited. The information located was encouraging because the amounts of fluorophore used in molecular imaging probes are typically much lower than the toxic doses described in the literature. Ultimately, the most effective and appropriate probes for use in patients will be determined by their fluorescent characteristics and the safety of the conjugates.
荧光团在癌症的体内诊断中具有潜在的应用价值。使用相对廉价且便携的设备，荧光团的光学成像是实时检测癌症的可能手段。然而，荧光团可能具有毒性，在安全地应用于患者之前必须进行研究。通过搜索 26 个全面的生物医学和化学文献数据库并分析检索到的材料，对 19 种广泛使用的荧光团的毒性进行了文献综述。这些荧光团包括 Alexa Fluor 488 和 514、BODIPY FL、BODIPY R6G、Cy 5.5、Cy 7、cypate、荧光素、吲哚菁绿、Oregon 绿、8-苯基 BODIPY、若丹明 110、若丹明 6G、若丹明 X、若丹明红、TAMRA、Texas 红和 Tokyo 绿。包括细胞毒性、组织毒性、体内毒性和致突变性的信息。对于美国食品和药物管理局（FDA）批准的化合物吲哚菁绿和荧光素，有相当多的与毒性相关的信息，但许多非 FDA 批准的荧光团的已发表信息是有限的。所找到的信息令人鼓舞，因为在分子成像探针中使用的荧光团的量通常远低于文献中描述的毒性剂量。最终，最有效和最合适的探针将取决于它们的荧光特性和缀合物的安全性。
