Synthesis and in Vitro Photodynamic Activity of Oligomeric Ethylene Glycol–Quinoline Substituted Zinc(II) Phthalocyanine Derivatives
作者:Xiao Jia、Feng-Feng Yang、Jun Li、Jian-Yong Liu、Jin-Ping Xue
DOI:10.1021/jm400722d
日期:2013.7.25
J·cm–2). The high photodynamic activities of these compounds are in accordance with their low aggregation tendency and high cellular uptake. Their structure–activity relationship was assessed by determining the photophysical properties, cellular uptake, and in vitro photodynamic activities of this series of compounds. As shown by confocal microscopy, monosubstituted phthalocyanines can target the mitochondria
合成和表征了一系列新的锌(II)酞菁衍生物。这些大环化合物在DMF的红色可见区域显示出清晰的吸收带,这表明它们溶解得很好,几乎没有在该溶剂中聚集。与未取代的酞菁锌(II)相比,所有这些酞菁均具有红移的Q波段(在678–699对670 nm),并且荧光发射相对较弱,并且产生单线态氧的效率更高。单取代的光敏剂还具有对HepG2人肝癌细胞的高光细胞毒性,IC 50值低至0.02–0.05μM(λ= 670 nm,80 mW·cm –2,1.5 J·cm –2)。这些化合物的高光动力活性与其低聚集趋势和高细胞摄取相一致。通过确定该系列化合物的光物理性质,细胞摄取和体外光动力活性,评估了它们的结构活性关系。如共聚焦显微镜所示,单取代的酞菁可以靶向细胞的线粒体和溶酶体,而四取代的酞菁则倾向于靶向细胞的溶酶体。