Graduate Institute of Biomedical Engineering, National Chung Hsing University , 250 Kuo Kuang Road, Taichung, 402, Taiwan, R.O.C.
ACS Appl Mater Interfaces. 2013 Dec 26;5(24):12935-43. doi: 10.1021/am403593m. Epub 2013 Dec 11.
We introduce a new class of photostable, efficient photosensitizers based on boron-dipyrromethene (BODIPY) derivatives that can generate singlet oxygen and super oxide simultaneously under irradiation. For compound preparation, appropriate regulation of the reaction conditions and control of specifically substituted BODIPY derivatives have been achieved. After biologically evaluating the intracellular uptake, localization, and phototoxicity of the compounds, we conclude that 3,5-dianiline-substituted BODIPY is a potentially selective photodynamic therapy candidate because its photodamage is more efficient in cancer cells than in normal cells, without apparent dark toxicity. Furthermore, direct comparison of photodamage efficacy revealed that our compound has better efficacy than Foscan and nearly equal efficacy to that of methylene blue.
我们介绍了一类新的光稳定、高效的基于硼二吡咯甲烷（BODIPY）衍生物的光敏剂，它们在光照下可以同时产生单线态氧和超氧化物。为了制备化合物，我们已经实现了对反应条件的适当调节和对特定取代的 BODIPY 衍生物的控制。在对化合物的细胞内摄取、定位和光毒性进行生物评价后，我们得出结论，3,5-二苯胺取代的 BODIPY 是一种潜在的选择性光动力治疗候选物，因为其光损伤在癌细胞中比在正常细胞中更有效，而没有明显的暗毒性。此外，光损伤功效的直接比较表明，我们的化合物比 Foscan 更有效，与亚甲蓝的功效几乎相等。
