Synthesis and in Vitro Photodynamic Activities of Pegylated Distyryl Boron Dipyrromethene Derivatives
Synthesis and in Vitro Photodynamic Activities of Pegylated Distyryl Boron Dipyrromethene Derivatives
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DOI：
10.1021/jm101637g
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发表时间：
2011-04-28
影响因子：
7.3
通讯作者：
Ng, Dennis K. P.
中科院分区：
文献类型：
--
作者：
He, Hui;Lo, Pui-Chi;Ng, Dennis K. P.
合成并表征了一系列聚乙二醇化的二乙烯基硼二吡咯亚甲基。还研究了它们在吐温80乳剂中对HT29人结肠癌细胞的体外光动力学活性。具有五个三甘醇链的衍生物(化合物8)表现出最高的。光细胞毒性，IC50低至7 nM。它也优先定位于细胞的内质网，在光照下可以诱导主要的细胞凋亡。
A series of pegylated distyryl boron dipyrromethenes have been prepared and characterized. Their in vitro photodynamic activities in Tween 80 emulsions have also been investigated against HT29 human colorectal carcinoma cells. The derivative having five triethylene glycol chains (compound 8) exhibits the highest. photocytotoxicity with an IC50 as low as 7 nM. It is also localized preferentially in the endoplasmic reticulum of the cells and can induce predominately apoptosis upon illumination.