Gebze Institute of Technology, Department of Chemistry, P.O. Box 141, Gebze, 41400, Kocaeli, Turkey.
Dalton Trans. 2011 Apr 28;40(16):4067-79. doi: 10.1039/c0dt01260b. Epub 2010 Dec 14.
Three Zn(II) phthalocyanines substituted by hydroxyl-terminated tetraethylene glycol chains have been synthesized. In order to evaluate the potential of these highly water-soluble phthalocyanines as type II-photosensitisers for photodynamic therapy, their structure-activity relationship was assessed by determining relevant photophysical and photochemical properties, such as their aggregation behaviour in aqueous buffers, their fluorescence properties and their efficiency with regard to the generation of singlet oxygen. In addition, evidence for a negligible interaction with plasma proteins in undiluted human plasma was obtained using a recently developed bioanalytical method and compared with the fluorescence quenching approach. These results combined with in vitro data regarding the phototoxicity of these phthalocyanines against HT-29 cancer cells provide evidence for the relevance of the non-peripherally substituted derivative for further in vivo investigations.
已经合成了三个由羟基封端的四乙二醇链取代的 Zn(II) 酞菁。为了评估这些高度水溶性酞菁作为 II 型光敏剂用于光动力治疗的潜力，通过测定相关的光物理和光化学性质，如在水缓冲液中的聚集行为、荧光性质以及生成单线态氧的效率，评估了它们的结构-活性关系。此外，使用最近开发的生物分析方法并与荧光猝灭方法进行比较，获得了在未稀释的人血浆中与血浆蛋白几乎没有相互作用的证据。这些结果结合这些酞菁对 HT-29 癌细胞的体外光毒性数据，为进一步的体内研究提供了非外周取代衍生物的相关性证据。
