摘要
通过化学合成得到一种由ZnPc(酞菁锌)和TAP(12个二甲氨甲基基团)构成的高灵敏pH响应光敏剂ZnPc(TAP)4。实验表明ZnPc(TAP)4在生理pH条件下处于聚集状态,毒性较低,有利于保持药物的稳定性和体内运输的安全性;当药物处于偏酸性环境时(肿瘤微环境),ZnPc(TAP)4能够从聚集体转变成单体,产生的单线态氧约是聚集状态的5倍,从而实现更好的细胞毒性。细胞实验证明ZnPc(TAP)4光敏剂对在同浓度条件下对肿瘤细胞MCF-7的细胞毒性约是正常细胞HELF的2~3倍;同时,ZnPc(TAP)4光敏剂在pH6.0时发射的荧光强度是pH8.0的30倍,有利于对肿瘤的实现光学诊断,具有良好的应用潜力。
A pH-sensitive photosensitizer was prepared with zinc phthalocyanine (ZnPc) and 2,4,6-tris (N,N-dimethylaminomethyl) phenoxy (TAP) with efficient tumor cytotoxicity.The yield of singlet-oxygen from ZnPc(TAP)4 was found extremely low at physiological pH,while dramatically increased at pH 6.0 (under slightly acidic conditions).ZnPc(TAP)4 can produce five-fold singlet-oxygen in pH 6.0 than pH 8.0.The tumor cells MCF-7 showed enhanced cellular uptake of ZnPc(TAP)4 than HELF cells (more than 2-3 folds),resulting in that ZnPc(TAP)4 not only exhibited better phototoxicity in tumor cells MCF-7,but also present stronger fluorescence (increased by 30 times).Such efficient photosensitizer showed an improved anti-tumor capability and clinical applying foreground with fluorescence imaging.
作者
鄢树枫
黄晓晨
邢建宏
刘希华
张君诚
YAN Shu-feng;HUANG Xiao-chen;XING Jian-hong;LIU Xi-hua;ZHANG Jun-cheng(Engineering Research Center of Medicinal plant Exploration and Utilization in Colleges and Universities of Fujian Province,Sanming 365004,China;School of Resources and Chemical Engineering,Sanming University,Sanming 365004,China;Fujian Institute of Research on the Structure of Matter,Chinese Academy of Sciences,Fuzhou 350002,China)
出处
《三明学院学报》
2019年第4期7-12,共6页
Journal of Sanming University
基金
福建省高校青年自然基金重点项目(JZ160477)
三明学院引进高层次人才科研启动经费资助(18YG04)
关键词
光敏剂
光动力治疗
PH响应
单线态氧
肿瘤细胞毒性
photosensitizer
photodynamic therapy
pH-sensitive
singlet-oxygen
tumor cytotoxicity
