可激活抗癌光敏剂

Activatable Photodynamic Anticancer Photosensitizers

光动力治疗(Photodynamic therapy,PDT)是利用光敏剂在光照下促使分子氧转为具有细胞毒性的活性氧,从而达到破坏靶细胞和靶组织效应的一种治疗手段。可激活光敏剂(Activatable photosensitizers,aPSs)是指事先屏蔽了光敏效应的光敏剂,只在特定因素下,如与肿瘤相关的特异性酶、酸性pH、核酸等的激活下,光敏剂转为激活状态,从而发挥诊断或者治疗的作用。可激活光敏剂由于具有更高的选择性而备受瞩目,成为医用光敏剂领域的研究前沿热点。本文将总结和分析近年来可激活抗癌光敏剂的研究现状和构效关系,以期为后续的相关研究提供参考。

Photodynamic therapy（PDT） is a cancer therapeutic modality that utilizes photosensitizers（PSs） and molecular oxygen upon irradiation with light to generate cytotoxic reactive oxygen species leading to damage of the target tissues and cells. Activatable photosensitizers（aPSs）that are inactivated initially, can only be activated by tumor-associated stimuli, such as tumor-associated specific enzymes, acidic pH, nucleic acid, to achieve targeting diagnosis and treatment. The aPSs have become a hot spot in the field of medical photosensitizers because of its higher selectivity. In this paper, we will summarize the recent development of aPSs, and analyze their structure-activity relationships, expecting to provide a reference for the future studies.