响应性BODIPY组装体的构筑及其在光动力疗法中的应用

项目名称： 响应性BODIPY组装体的构筑及其在光动力疗法中的应用

项目编号： No.21302072

项目类型： 青年科学基金项目

立项/批准年度： 2014

项目学科： 数理科学和化学

项目作者： 王晓军

作者单位： 江苏师范大学

项目金额： 25万元

中文摘要： 光动力疗法（PDT）是以光、光敏剂和氧三者相结合来治疗恶性肿瘤的一种技术；其中，光敏剂是PDT的关键要素。本项目拟从超分子自组装的角度出发，设计合成在近红外有强吸收的两亲性BODIPY光敏剂作为自组装基元，并向其中引入对pH和/或GSH等敏感的作用位点，通过分子自组装构筑具有响应性的超分子组装体（如胶束、囊泡），作为BODIPY光敏剂传递的载体。研究该组装体在不同刺激条件下的结构形貌、光物理性质和单线态氧产率等的变化规律，揭示组装基元、组装体的结构与性能之间的内在联系，实现对组装体单线态氧产率等功能的有效控制。研究该组装体对肿瘤细胞的PDT效能，总结并建立PDT效能与BODIPY光敏剂组装基元的化学结构、组装体的结构形貌之间的构效关系。本项目的研究结果将为开发可用于PDT的、高效低毒的新型BODIPY光敏剂超分子体系提供实验和理论依据，并为实现对癌症的诊断和治疗提供有益探索。

中文关键词： 超分子自组装；BODIPY及衍生物；光敏剂；有机光化学；金属有机骨架材料

英文摘要： Photodynamic therapy (PDT) is a noninvasive technique for the treatment of a variety of cancer tumors by the combined use of visible or near-visible light with a photosensitizing drug and oxygen, in which the photosensitizer is critical for PDT. In this proposal, amphiphilic BODIPY derivatives with long exitation wavelength will be rationally desgined and synthesized as building blocks in supramolecular self-assembly, together with the introduction of pH and/or GSH stimuli-responsive functional groups. The smart stimuli-responsive assemblies, such as micelle and vesicle, would be constructed via self-assembling processes. The morphologies, photophysical properties and quantum yield of singlet oxygen will be investigated to reveal the relationship between the function and structures of building blocks and aggregates, as well as to control the yield of singlet oxygen. The photo-induced cytotoxicity for cancer cells was studied to reveal the relationship among efficacy, chemical structures of BODIPY building blocks and morphologies of aggregates. It is envisaged that these results will provide a fundamental understanding for design and synthesis of effective BODIPY based photosensitizers with low dark cytotoxicity in PDT, along with the promise for the diagnosis and treatment of cancers.

英文关键词： supramolecular self-assembly；BODIPY derivatives；photosensitizer；organic photochemistry；metal-organic frameworks