光敏剂能否被肿瘤细胞高效吸收是影响光动力治疗效率的重要因素。亲脂性光敏剂易于被肿瘤组织摄取, 但会使光敏剂发生自猝灭; 亲水性光敏剂则有利于光敏剂在体内的转运, 但肿瘤细胞摄取率会下降。本工作通过亲酯性的乙二醇缩合支链和亲水性季膦基团与卟啉相连接, 成功制备一种新型两亲性卟啉锌化合物 (ZnTP-TP), 实验表明该化合物具有较高的单线态氧量子产率和良好的两亲性, 可被细胞快速摄取, 并表现出较低的细胞毒性和良好的肿瘤光动力治疗效应。

Cellular uptake efficiency of photosensitizers plays crucial role in the tumor photodynamic therapy (PDT). The increased hydrophobicity, which will impart better cellular uptake, might lead to self-aggregation of the photosensitizer, resulting in a reduced 1O2 yield. On the other hand, increased hydrophilicity of the photosensitizer will lead to improved drug loading and delivery, whereas it will also reduce its transport across the cell membrane. In this work, we reported the successful synthesis of a new amphiphilic porphyrin (ZnTP-TP) bearing two triethylene glycol chains and two tetraethylene glycol chain bridged cationic triphenylphosphonium groups with significant hydrophobic/hydrophilic balance. And ZnTP-TP was further demonstrated low-toxic, rapid cellular uptake and thus potentially as new effective tumor PDT agent.