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Development of next generation of photosensitizer for fluorescent imaging and photodynamic therapy of cancer

开发用于癌症荧光成像和光动力治疗的下一代光敏剂

基本信息

批准号：
23790063
负责人：
KAMINO Shinichiro
金额：
$ 2.66万
依托单位：
The Institute of Physical and Chemical Research
依托单位国家：
日本
项目类别：
Grant-in-Aid for Young Scientists (B)
财政年份：
2011
资助国家：
日本
起止时间：
2011 至 2012
项目状态：
已结题

项目摘要

We have designed and synthesized a new class of rhodamine dyes with an extended ?-conjugated system, named 3’,3’’-bis(oxospiroisobenzofuran)-3,7-bis(diethylamino)benzopyrano-xanthene (ABPX01) dye. In this study, the investigations were carried out to reveal the relationships among the chemical species of ABPX01, the color, and the fluorescence emission in various solutions. ABPX01 had various forms: the spirolactone form (ABPX01^0), which is colorless; and the monocationic form (ABPX01H^+) and the dicationic form (ABPX01H_2^<2+>), which are colored. ABPX01H_2^<2+> was identified to be a red fluorescent species. Detailed spectroscopic and electron microscopic investigations led to the assumption that the ABPX01H_2^<2+> formed ion associates with Cl^- as counter anions in HCl aqueous solution, and the nanoand submicrometer-sized colloidal aggregates of ABPX01 hydrochloride exhibit fluorescence emission. Good performance in fluorescent imaging demands large fluorescence quantum yields, and solubility in hydrosoluble media of the markers. We design and synthesize new ABPX derivatives in which the amino groups are incorporated into rigid six-membered rings. The relative fluorescence quantum yields of ABPX101H_2^<2+>, ABPX102H_2^<2+>, and ABPX103H_2^<2+>were drastically increased relative to that of ABPX01H_2^<2+>. All ABPX derivatives commonly exhibited the well-developed bimodal fluorescence emission spectra over a wide range including red and NIR region. The intrinsic solubility of the ABPX dyes is favorable for the photosensitizers of fluorescent imaging and photodynamic therapy.

我们设计并合成了一类新的罗丹明染料。-偶联体系，命名为3′，3′”-二（二乙基氨基）-3,7-二（二）苯并吡喃-杂蒽（ABPX01）染料。本研究揭示了ABPX01在不同溶液中的化学种类、颜色和荧光发射之间的关系。ABPX01有多种形式：螺内酯形式（ABPX01^0），无色；单位形（ABPX01H^+）和单位形（ABPX01H_2^<2+>）为彩色。ABPX01H_2^<2+>为红色荧光物质。详细的光谱和电镜研究表明，ABPX01H_2^<2+>在HCl水溶液中与Cl^-作为反阴离子结合，ABPX01盐酸盐的纳米和亚微米级胶体聚集体表现出荧光发射。良好的荧光成像性能要求大的荧光量子产率和标记物在水溶性介质中的溶解性。我们设计并合成了新的ABPX衍生物，其中的氨基被纳入刚性六元环。与ABPX01H_2^<2+>相比，ABPX101H_2^<2+>、ABPX102H_2^<2+>和ABPX103H_2^<2+>的相对荧光量子产率显著提高。所有ABPX衍生物普遍表现出良好的双峰荧光发射光谱在广泛的范围内，包括红色和近红外区。ABPX染料的固有溶解度有利于作为荧光成像和光动力治疗的光敏剂。