具备亚甲基紫结构的BODIPY类自组装纳米粒子制备及其光治疗应用  

Self-assembled nanoparticles with 3RAX-based BODIPY structure and their phototherapeutic applications

作　　者：梅田恬 董鑫 李享 崔敏 王凯[1] MEI Tiantian;DONG Xin;LI Xiang;CUI Min;WANG Kai(School of Health Science and Engineering,Hubei University,Wuhan 430062,China;Wuhan Asia Heart Disease General Hospital,Wuhan 430050,China)

机构地区：[1]湖北大学健康科学与工程学院,湖北武汉430062 [2]武汉亚洲心脏病总医院,湖北武汉430050

出　　处：《湖北大学学报（自然科学版）》2024年第4期445-452,共8页Journal of Hubei University：Natural Science

基　　金：国家自然科学基金(20902071)资助。

摘　　要：光治疗主要包括光动力治疗(PDT)、光热治疗(PTT),已经发展成为当今癌症治疗的重要备选方法;光治疗的核心涉及光触发光敏剂产生高活性的单线态氧或产生热量。氟硼二吡咯(BODIPY)类荧光母体由于其良好的光热和化学稳定性、易于构建功能分子等优势,已被广泛用于有机分子型或纳米型光敏剂的构建;另一方面,亚甲基紫也是一类重要荧光染料,被用于光治疗等领域。在此,将亚甲基紫与聚乙二醇(PEG)化的共轭增强型BODIPY偶联,制备有机分子BDP-2,并自组装为纳米粒子BDP-2NPs,旨在通过亚甲基紫(3RAX)和BODIPY结构,高效提升光治疗效率。实验结果表明:BDP-2NPs的平均粒径分布为118.5 nm,多分散指数为0.204,具备良好分散性质;光照时(680 nm, 1 W/cm^(2),10 min),BDP-2NPs的单线态氧量子产率为0.16,光热转化效率为30.2%,具备同步产生单线态氧和光热的能力,且该粒子具备较好的光稳定性;最后,HeLa细胞的毒性分析发现,BDP-2NPs光敏剂对癌细胞具有较低的暗毒性和显著的光毒性。因此,本文中开发的具备亚甲基紫结构的BODIPY类自组装纳米粒子BDP-2NPs,可协同触发癌细胞中PDT和PTT过程,具备潜在的抗癌应用前景。Phototherapy,which mainly includes photodynamic therapy(PDT)and photothermal therapy(PTT),is an important method of cancer treatment.The hub of phototherapy involves light-activated photosensitizers that produce singlet oxygen or heat to efficiently kill cancer cells.Currently,BODIPY has been widely used in the construction of photosensitizers due to the excellent photothermal and chemical stabilities,the easy construction for functional molecules and other advantages.On the other hand,3RAX is also an important class of fluorescent dyes that are used in phototherapy.Here,BDP-2 was prepared by coupling 3RAX with conjugate-enhanced BODIPY center,which could self-assembly into nanoparticles BDP-2 NPs to efficiently enhance the phototherapeutic efficiency through 3RAX and BODIPY structures.BDP-2 NPs has a particle diameter of 118.5 nm,and a PDI value of 0.204,which shows the well dispersion.Under light irradiation(680 nm,1 W/cm^(2),10 min),the singlet oxygen quantum yield of BDP-2 NPs is 0.16,and the photothermal conversion efficiency is 30.2%.BDP-2 NPs has both photostability and ability to generate single-line oxygen and photothermal simultaneously.Finally,cytotoxicity analysis of HeLa cells reveales low dark toxicity and significant phototoxicity of BDP-2 NPs.Therefore,our self-assembled nanoparticles with 3RAX-based BODIPY structure can synergistically trigger the PDT and PTT processes in cancer cells,and have potential anti-cancer applications.

关 键 词：亚甲基紫 氟硼二吡咯 光动力治疗 光热治疗 

分 类 号：O626.13[理学—有机化学] R73[理学—化学]