BODIPY 类新型光敏剂的合成与构效研究

项目名称： BODIPY 类新型光敏剂的合成与构效研究

项目编号： No.81202415

项目类型： 青年科学基金项目

立项/批准年度： 2013

项目学科： 药物学、药理学

项目作者： 陆丽

作者单位： 中国医学科学院

项目金额： 23万元

中文摘要： 光动力治疗(PDT)是一种治疗各种肿瘤的新兴无创或微创技术。在特定波长光的照射下激发光敏剂，光敏剂受激发获得能量后可以把能量转给周围的分子氧并经过一系列的能量转换，最终具有极高反应活性的反应氧族产生，导致细胞死亡。目前已报道和开发的光敏剂存在着组分不明、光稳定性差、对红光吸收小等缺点，限制了该项医学新疗法的临床推广，研制开发更符合理想条件的光敏药物已成为光动力治疗的当务之急。 BODIPY类染料高摩尔消光系数、高荧光量子产率、波长范围大、不易受环境极性和PH的影响及良好的光、氧、热稳定和不易光漂白等特点，而且对结构的微小修饰对改变荧光性质显著。本项目对其加以一系列修饰改造，通过研究其结构与光疗效果之间的构效关系，筛选得到高效低毒的一类新型光敏剂。BODIPY光敏剂不仅用于光动力治疗，还可用于在体成像的光动力诊断,将光动力治疗与诊断相结合，更有利于患者的治疗。

中文关键词： BODIPY；光敏治疗；光敏剂；构效关系；

英文摘要： Photodynamic therapy (PDT) is a noninvasive technique for the treatment of a variety of cancer tumor types。Photosensitizers are produce reactive oxygen species (ROS) upon light illumination , and ROS are commonly used to cause physiological damage and death of cell. There are many reported or commercially available photosensitizers, but most have limitations, such as structural instability, low photostability, or a limited usable range of solvent conditions. The development of novel photosensitizers, which are highly efficient, photostable, and widely applicable under various conditions, would be extremely useful. BODIPYs generally have high extinction coefficients (ε) and high quantum efficiencies of fluorescence (Φ), which are relatively insensitive to environment (i.e., solvent polarity or pH), and they are also resistant to photobleaching. Small modifications to their structures enable tuning of their fluorescence characteristics. We prepared some substituted BODIPYs. We have been interested in trying to find a novel photosensitizer by finding the relation between the structure and efficient of photosensitizers, which are not restricted solely to therapeutic generation of singlet oxygen and are useful for in vivo imaging. A fluorescently detectable photosensitizer is beneficial for aiding in defining and

英文关键词： BODIPY；potodynamic therapy；photosensitizer；structure-activity relationship；