| 基于粘度响应的线粒体靶向铱(Ⅲ)配合物用于肿瘤的光动力治疗 | |
| Viscosity Responsive and Mitochondria Targeted Iridium(Ⅲ) Complexes for Photodynamic Therapy of Tumors | |
| 摘要: 合成了2种含有转动基团的铱配合物Ir1和Ir2。研究发现Ir1和Ir2对粘度具有灵敏的荧光响应，在高粘度环境下，其荧光强度分别提高了35.7倍和1 311.6倍。细胞摄取和共定位实验表明该探针能够轻易地穿过细胞膜并靶向聚集于线粒体中，对线粒体内粘度进行荧光成像检测。另外，通过EPR电子顺磁共振仪检测到Ir1和Ir2在光照下能够产生大量的单线态氧；同时发现配合物在肿瘤细胞中也能够产生高毒性的单线态氧，使Ir1和Ir2对A549细胞和Hep-G2细胞表现出很强的光毒性从而导致细胞死亡。 | |
| 关键词: 金属铱配合物 粘度响应 线粒体靶向 光动力治疗 | |
| 基金项目: 国家自然科学基金（No.22077085，21701113，21671137）、广东省自然科学基金（No.2019A1515011958）、深圳市科技计划（No.JCYJ20190808153209537）、深圳市孔雀人才科研启动（No.827-000389）、深圳大学科研启动经费（No.2018036）资助。 | |
| Abstract: Two novel iridium(Ⅲ) complexes (Ir1 and Ir2) containing rotatable groups were designed and synthesized for viscosity probes and photosensitizers. Firstly, they freely rotated and showed weak phosphorescence in lowviscosity environment, while in viscous media, the phosphorescence intensity increased significantly (35.7-fold for Ir1, 1 311.6 -fold for Ir2). The cellular uptake and co -localization studies indicated that the probes could easily cross the cell membrane and aggregate in mitochondria, and the results showed that they could be used for detection of mitochondrial viscosity. Moreover, Ir1 and Ir2 displayed high potent photo-cytotoxicity to cancer cells (A549 and Hep-G2) under light irradiation but exhibited lower photo-cytotoxicity to normal cells (MRC-5 and LO2). The generation of 1O2 under light irradiation were also measured by electron paramagnetic resonance (EPR) and confocal microscopy. | |
| Keywords: iridium(Ⅲ) complexes viscosity-response mitochondria-targeting photodynamic therapy | |
| 投稿时间：2020-07-27 修订日期：2020-12-17 | |
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| 欧阳艾,罗雨珩,陆农,胡仁涛,张平玉,张黔玲.基于粘度响应的线粒体靶向铱(Ⅲ)配合物用于肿瘤的光动力治疗[J].无机化学学报,2021,37(3):401-411. | |
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