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Dual-dye systems comprising activatable fluorescein dye and hydrophobic or hydrophilic Cy5 reference fluorophore for ratiometric drug delivery monitoring
Journal of Photochemistry and Photobiology A: Chemistry ( IF 4.1 ) Pub Date : 2021-01-03 , DOI: 10.1016/j.jphotochem.2020.113113
Dvir Poplinger , Andrii Bazylevich , Maksym Bokan , Gary Gellerman , Leonid Patsenker

Ratiometric fluorescence detection in biological samples in vitro and in vivo mitigates several issues in conventional single-signal measurements such as light absorption and scattering, dye photobleaching, and instrumental parameters. Herein, two new systems for ratiometric monitoring of drug delivery are synthesized and investigated. These systems comprise a non-fluorescent fluorescein-based dye, Flu, bound to the anticancer drug, azatoxin (Aza), through a hydrolytically cleavable acrylate ester linker and either hydrophobic (Cy5h) or hydrophilic (Cy5s) pentamethine cyanine dye providing a red-light reference signal. Upon drug release, the green Flu fluorescence notably increases enabling ratiometric tracking of drug release events. The spectral properties of the developed conjugates and fluorescently monitored drug release rates are investigated in biologically relevant media with respect of the Cy5 dye hydrophilicity.



中文翻译:

双染料系统,包括可激活的荧光素染料和疏水或亲水的Cy5参考荧光团,用于比例式药物输送监测

体外体内生物样品中的比率荧光检测可减轻常规单信号测量中的几个问题,例如光吸收和散射,染料光漂白和仪器参数。在此,合成并研究了两种新的用于药物输送的比例监控的系统。这些系统包含一种非荧光素荧光染料Flu,通过可水解裂解的丙烯酸酯接头与抗癌药氮杂毒素(Aza)结合,以及疏水性(Cy5h)或亲水性(Cy5s)五甲meth菁菁染料提供红色光参考信号。药物释放后,绿色流感荧光显着增加,使得能够按比例跟踪药物释放事件。在Cy5染料的亲水性方面,在生物学相关的介质中研究了开发的结合物的光谱特性和荧光监测的药物释放速率。

更新日期:2021-01-07
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