一种新型亚酞菁荧光探针的合成、表征及动物活体成像研究

摘要

Zine amino-sub-phthalocyanine ( NH2-Snb-Pc-Zn) was prepared by solid-state reaction of 4-aminophthalonitrile,anhydrous zinc chloride, folic acid, amidation of the carboxyl.Folic acid ( FA ) modified Pc ( FA-Pc) complexes were obtained by MTT method to evaluate the toxicity to Hela cells with NH2-Sub-Pc-Zn,FA-Pc and four substituted amino-zinc-phthalocyanine(NH2-Pc-Zn).Toxicity test results showed that 2 mg/mL of FA-Pc led to the inhibition rate of Hela cells of more than 60%.The FA-Pc in vivo imaging characteristics were studied,near-infrared fluorescence imaging results showed that FA-Pc gathered directional in nude mice’ s tumor hepatorenal areas was stable for 12 h.FA-Pc could be used for whole-body fluorescence imaging.%以4氨基邻苯二腈、无水ZnCl2、叶酸等为原料，经固相合成法制备了三取代氨基亚酞菁锌（ NH2 Sub Pc Zn），进一步通过酰胺反应合成了叶酸修饰的三取代氨基亚酞菁锌（FA Pc）。采用MTT方法评价了NH2 Sub Pc Zn、FA Pc以及四取代氨基酞菁锌（ NH2 Pc Zn）对Hela细胞的毒性，毒性试验表明，加入2 mg/mL FA Pc，Hela细胞的抑制率超过60％；同时研究了FA Pc的活体成像特性，近红外荧光成像结果表明，FA Pc定向聚集在裸鼠的肿瘤肝肾部位且可以稳定12 h。因此说明FA Pc可用于活体肝癌的选择性成像。