一种基于铂（II）的光敏三脚架，作为通过DNA损伤发挥作用的有效光动力抗癌剂。
A Platinum(II)-based Photosensitive Tripod as an Effective Photodynamic Anticancer Agent through DNA Damage.
作者信息
Zhong Yi-Fang, Zhang Hang, Liu Wen-Ting, Zheng Xiao-Hui, Zhou Yi-Wei, Cao Qian, Shen Yong, Zhao Yong, Qin Peter Z, Ji Liang-Nian, Mao Zong-Wan
机构信息
MOE Key Laboratory of Bioinorganic and Synthetic Chemistry, School of Chemistry, Sun Yat-Sen University, Guangzhou, 510275, China.
School of Life Sciences, Sun Yat-Sen University, Guangzhou, 510006, China.
出版信息
Chemistry. 2017 Nov 21;23(65):16442-16446. doi: 10.1002/chem.201703598. Epub 2017 Oct 26.
Herein, two photosensitive platinum(II)-based tripods were designed and synthesized. Notably, complex 1 ({[Pt(dien)] L}(NO ) , L=tri(4-pyridylphenyl)amine and dien=diethylenetriamine), which mainly accumulated in the cell nucleus, exhibited very low cytotoxicity in the absence of light irradiation, but displayed a remarkable increase in cytotoxicity upon visible light irradiation. Mechanistic investigations revealed that the tripod interacted with DNA in the nucleus, induced ROS generation upon light irradiation, and consequently elicited rapid DNA damage response; thereby triggering cancer cell apoptosis.
在此，设计并合成了两种基于光敏铂（II）的三脚架化合物。值得注意的是，配合物1（{[Pt（二乙三胺）]L}(NO₃)₂，L = 三（4 - 吡啶基苯基）胺，二乙三胺 = 二乙烯三胺）主要积聚在细胞核中，在无光照时表现出非常低的细胞毒性，但在可见光照射下细胞毒性显著增加。机理研究表明，该三脚架化合物与细胞核中的DNA相互作用，光照时诱导活性氧生成，进而引发快速的DNA损伤反应；从而触发癌细胞凋亡。
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