College of Chemistry and Chemical Engineering, Fuzhou University, Fuzhou 350108, China.
Dalton Trans. 2013 Aug 7;42(29):10398-403. doi: 10.1039/c3dt50910a.
A series of novel silicon(IV) phthalocyanines conjugated axially with different nucleoside moieties (uridine, 5-methyluridine, cytidine, and 5-N-cytidine derivatives) have been synthesized and evaluated for their photodynamic activities. The uridine-containing compound 1 exhibits the highest photocytotoxicity against HepG2 human hepatocarcinoma cells with an IC50 value as low as 6 nM, which can be attributed to its high cellular uptake and non-aggregated nature in the biological media. This compound shows high affinity toward the mitochondria of HepG2 cells and causes cell death mainly through apoptosis upon illumination. The result indicates that 1 is a highly promising photosensitizer for photodynamic therapy.
一系列新型硅（IV）酞菁与不同核苷部分（尿苷、5-甲基尿苷、胞苷和 5-N-胞苷衍生物）轴向连接的化合物已被合成并评估其光动力活性。含有尿苷的化合物 1 对 HepG2 人肝癌细胞表现出最高的光细胞毒性，IC50 值低至 6 nM，这可以归因于其在生物介质中高的细胞摄取和非聚集性质。该化合物对 HepG2 细胞的线粒体具有高亲和力，并在光照下主要通过细胞凋亡导致细胞死亡。结果表明，1 是一种很有前途的用于光动力治疗的光敏剂。
