四苯乙烯骨架的光动力学治疗试剂合成及体外抗肿瘤活性  

Synthesis and in vitro antitumor activity of photodynamic therapy reagent based on tetraphene skeleton

作　　者：房可欣 刘海通 王书香[1] FANG Kexin;LIU Haitong;WANG Shuxiang(Key Laboratory of Medicinal Chemistry and Molecular Diagnosis Ministry of Education,College of Chemistry and Materials Science,Hebei University,Baoding 071000,China)

机构地区：[1]河北大学化学与材料科学学院,药物化学与分子诊断教育部重点实验室,河北保定071000

出　　处：《河北大学学报(自然科学版)》2025年第2期176-184,共9页Journal of Hebei University(Natural Science Edition)

基　　金：国家自然科学基金资助项目(22177026)。

摘　　要：以4-溴二苯甲酮、4,4′-二甲氧基二苯甲酮、对硝基苄溴(Br-BNO_(2))和叠氮基乳糖(LT)等为原料,经亲核取代、铃木偶联和click反应等构建了一种四苯乙烯(TPE)为骨架,并能高效产生活性氧(ROS)的光动力学治疗(PDT)试剂LT-TPE-DB-BNO_(2).采用分光光度法和共聚焦荧光显微镜探究LT-TPE-DB-BNO_(2)在血清和不同pH值溶液中的稳定性及细胞内外产生ROS的能力;利用MTT法和活死细胞双染法测定其对HeLa与BRL-3A细胞活力的影响.结果表明:在不同pH值溶液及血清中LT-TPE-DB-BNO_(2)表现出优良的稳定性;在黑暗条件下,LT-TPE-DB-BNO_(2)对HeLa和BRL-3A细胞的活力影响很小;在氙灯辐照下,LT-TPE-DB-BNO_(2)高效产生ROS,使HeLa细胞的活力下降88.3%,表明LT-TPE-DB-BNO_(2)是高效的PDT试剂.A photodynamic therapy(PDT)reagent,LT-TPE-DB-BNO_(2)for reactive oxygen species(ROS)generation based on tetraphene(TPE),was synthesized from 4-bromobenzoylbenzene,4,4’-dimethoxybenzophenone,p-nitrobenzyl bromide(Br-BNO_(2))and azide lactose(LT)by nucleophilic substitution,suzuki coupling and click reaction.The stability of LT-TPE-DB-BNO_(2)in serum and at different pH value,and the ability of ROS generation were investigated by spectrophotometry and confocal fluorescence microscopy.The effects of LT-TPE-DB-BNO_(2)on the viability of HeLa and BRL-3A cells were investigated by MTT method and live and dead cell double staining method.The results showed that LT-TPE-DB-BNO_(2)was stable in serum and at different pH value.In the dark condition,it had a little effect on the activity of HeLa and BRL-3A cells.Under irradiation by xenon lamp,ROS was produced by LT-TPE-DB-BNO_(2),and the activity of HeLa cells was reduced by 88.3%,indicating that LT-TPE-DB-BNO_(2)is a highly efficient PDT reagent.

关 键 词：四苯乙烯骨架 光动力学治疗试剂 抗肿瘤活性 

分 类 号：O632.6[理学—高分子化学]