当前位置: X-MOL 学术Dyes Pigments › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Novel unsymmetrical silicon(IV) phthalocyanines as highly potent anticancer photosensitizers. Synthesis, characterization, and in vitro photodynamic activities
Dyes and Pigments ( IF 4.1 ) Pub Date : 2020-02-16 , DOI: 10.1016/j.dyepig.2020.108286
Bi-Yuan Zheng , Lei Wang , Qing-Yan Hu , Jie Shi , Mei-Rong Ke , Jian-Dong Huang

A series of novel unsymmetrical silicon (IV) phthalocyanines (SiPcs) di-substituted axially with tyramine and different oligomeric ethylene glycol moieties have been synthesized by alkoxy exchange reactions, and their singlet oxygen quantum yields (ΦΔ) and in vitro photodynamic activities have also been evaluated. The unsymmetrical SiPcs 25 show slightly higher photosensitizing efficiency (ΦΔ = 0.08–0.12) than the corresponding symmetrical SiPc 1 (ΦΔ = 0.05), but are less efficient compared to the symmetrical SiPc 6 (ΦΔ = 0.33). All the compounds exhibit high photocytotoxicities against BGC-823 cancer cells with IC50 values ranging from 3 nM to 20 nM. Particularly for the unsymmetrical SiPc 5, the IC50 value toward BGC-823 cells is significantly lower than its corresponding symmetrical SiPcs 1 and 6, which could be attributed to its higher cellular uptake. In addition, SiPc 5 can essentially bind to mitochondria and induces cell death of BGC-823 cells mainly through apoptosis. So SiPc 5 is a highly promising photosensitizer for photodynamic therapy.



中文翻译:

新型不对称硅(IV)酞菁类作为高效抗癌光敏剂。合成,表征和体外光动力活性

一系列新颖不对称硅(IV)酞菁(SiPcs)二取代酪胺和不同的低聚乙二醇部分轴向已经被烷氧基交换反应合成,和它们的单重态氧的量子产率(Φ Δ)和体外光动力活动也被评估。不对称SiPcs 2 - 5显示略高光敏效率(Φ Δ  = 0.08-0.12)比相应的对称SIPC 1Φ Δ  = 0.05),但是效率较低相比对称SIPC 6Φ Δ = 0.33)。所有化合物均对BGC-823癌细胞表现出高光细胞毒性,IC 50值为3 nM至20 nM。特别是对于非对称SiPc 5而言,针对BGC-823细胞的IC 50值明显低于其对应的对称SiPcs 16,这可能归因于其较高的细胞摄取。另外,SiPc 5可以基本上结合线粒体并主要通过凋亡诱导BGC-823细胞的细胞死亡。因此,SiPc 5是用于光动力疗法的非常有前途的光敏剂。

更新日期:2020-02-20
down
wechat
bug