Disulfonated tetraphenyl chlorin (TPCS2a), a novel photosensitizer developed for clinical utilization of photochemical internalization
Disulfonated tetraphenyl chlorin (TPCS2a), a novel photosensitizer developed for clinical utilization of photochemical internalization
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DOI：
10.1039/c1pp05128h
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发表时间：
2011-01-01
影响因子：
3.1
通讯作者：
Hogset, Anders
中科院分区：
文献类型：
--
作者：
Berg, Kristian;Nordstrand, Solveig;Hogset, Anders
光化学内化（PCI）是一种将内吞大分子释放到胞质溶胶中的新技术。该技术基于使用位于内吞囊泡中的光敏剂，并且在光激活时诱导大分子从内吞囊泡释放。PCI已显示刺激不容易穿透质膜的多种大分子和其它分子的递送。以酞菁铝二磺酸盐（AlPcS2a）为光敏剂进行了PCI的临床前评价。AlPcS2a由于其大量的异构体可能具有批次间比例变化，因此不是临床使用的最佳光敏剂。因此，通过二酰亚胺还原二磺化四苯基卟啉（TPPS2a），开发了二磺化四苯基二氢卟酚（TPCS 2a）。合成的TPCS 2a含有3个异构体，
Photochemical internalisation (PCI) is a novel technology for release of endocytosed macromolecules into the cytosol. The technology is based on the use of photosensitizers that locate in endocytic vesicles, and that upon activation by light induce a release of macromolecules from the endocytic vesicles. PCI has been shown to stimulate delivery of a large variety of macromolecules and other molecules that do not readily penetrate the plasma membrane. The preclinical evaluation of PCI has been performed with aluminum phthalocyanine disulfonate (AlPcS2a) as photosensitizer. AlPcS2a, due to its large number of isomers potentially with batch-to-batch ratio variations, is not an optimal photosenstizer for clinical use. Disulfonated tetraphenyl chlorin (TPCS2a) has therefore been developed by di-imide reduction of disulfonated tetraphenyl porphine (TPPS2a). The synthesized TPCS2a contains 3 isomers as shown by HPLC with low (