基于[12]aneN_(3)的近红外AIE活性非病毒基因载体的合成及基因递送  

Synthesis and gene delivery properties of [12]aneN_(3)-based nonviral gene vector with near infrared AIE activity

作　　者：唐芳 高仪楠 张曦 张雨杉 卢忠林 Fang Tang;Yi-Nan Gao;Xi Zhang;Yu-Shan Zhang;Zhong-Lin Lu(Key Laboratory of Radiopharmaceuticals,Ministry of Education,College of Chemistry,Beijing Normal University,Beijing 100875,China)

机构地区：[1]北京师范大学化学学院,放射性药物教育部重点实验室,北京100875

出　　处：《中国科学：化学》2022年第6期956-962,共7页SCIENTIA SINICA Chimica

基　　金：国家自然科学基金(批准号:21372032,21778012)资助项目。

摘　　要：荧光非病毒基因载体具有可示踪载物基因释放和载体在细胞内命运的功能,在实现基因递送可视化和诊疗一体化等领域具有重要意义.本文基于双[12]aneN_(3)设计合成了一种三苯胺衍生物TPAH,作为近红外(NIR)聚集诱导发射(AIE)荧光型非病毒基因载体. TPAH和辅助脂质二油酰磷脂酰乙醇胺(DOPE)混合后形成的脂质体能够将核酸压缩成纳米颗粒进行基因递送,在多种细胞系中能够观察到质粒DNA (pDNA)和小干扰RNA (siRNA)的高效转染,转染效率(TE)和商业的转染试剂lipofectamine 2000相近.载体的荧光清楚地显示了载物基因的摄取、运输和细胞内释放,提供了有关基因转染的重要时空信息.Fluorescent nonviral gene vectors have drawn increasing research interest in trackable gene delivery, which could furnish important spatiotemporal information regarding the translocation and intracellular fate of gene cargoes,thus benefiting to understand the critical steps in determining the transfection efficiency. Herein, we report a triphenylamine derivative, TPAH, modified with [12]aneN_(3)and a long hydrocarbon chain as a nonviral gene vector.TPAH bears typical near-infrared(NIR) aggregation-induced emission(AIE), and the resulting TPAH/dioleoylpho-sphatidylethanolamine(DOPE) liposome possesses strong DNA binding ability, capable of compacting nucleic acids into nanoparticles for gene delivery. High transfection efficiency of both plasmid DNAs(pDNAs) and small interfering RNAs(siRNAs) was observed in various cell lines. Under optimal conditions, the best transfection efficiency is comparable to that of commercial transfection agent lipofectamine 2000. The vector as a deliver tracker showing ondemand reporting property was successfully applied to monitor the entire gene delivery process, providing spatiotemporal information regarding the translocation and intracellular fate of gene cargoes. This study suggests that integrating NIR AIE molecules into [12]aneN_(3)is a promising strategy to achieve trackable gene delivery.

关 键 词：aneN_(3) 非病毒基因载体 近红外发光 聚集诱导发光 生物显像 

分 类 号：Q78[生物学—分子生物学] O657.3[理学—分析化学]