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Bifunctional reactive pentamethine cyanine dyes for biomedical applications
Dyes and Pigments ( IF 4.5 ) Pub Date : 2018-09-27 , DOI: 10.1016/j.dyepig.2018.09.064
Alex Rozovsky , Leonid Patsenker , Gary Gellerman

New unsymmetrical pentamethine cyanine dyes containing two non-equivalent reactive groups selected from carboxyl, amino and hydroxyl in different combinations were synthesized and their spectral properties investigated. Amino and hydroxy groups were used for binding the dyes to the anticancer drug, chlorambucil (CLB) via biodegradable amide or ester linker while the second reactive functionality could be utilized for attachment at mild conditions to a targeting carrier such as an antibody or peptide. These conjugates can thereby potentially be suitable for fluorescence-based monitoring of drug delivery. The CLB release profiles triggered by biodegradable linker were investigated in buffer solutions and cell medium using LC-MS and spectrofluorimetric methods.



中文翻译:

用于生物医学的双功能反应性五甲胺花青染料

合成了新的不对称五甲胺花青染料,该染料含有两个不同等价的选自羧基,氨基和羟基的非活性基团,并对其光谱特性进行了研究。氨基和羟基用于通过可生物降解的酰胺或酯接头将染料与抗癌药苯丁酸氮芥(CLB)结合,而第二种反应性官能团可用于在温和条件下与靶向载体(例如抗体或肽)结合。这些结合物因此可能潜在地适合于基于荧光的药物递送监测。使用LC-MS和荧光光谱法在缓冲溶液和细胞培养基中研究了由可生物降解的接头触发的CLB释放曲线。

更新日期:2018-09-27
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