State Key Laboratory of Coordination Chemistry, School of Chemistry and Chemical Engineering, Nanjing University, Nanjing 210023, China.
State Key Laboratory of Coordination Chemistry, School of Chemistry and Chemical Engineering, Nanjing University, Nanjing 210023, China; Chemistry and Biomedicine Innovation Center, Nanjing University, Nanjing 210023, China.
J Inorg Biochem. 2021 May;218:111394. doi: 10.1016/j.jinorgbio.2021.111394. Epub 2021 Feb 13.
Photodynamic therapy (PDT) has attracted extensive attention in cancer treatment because of its minimum trauma, less side effects, and so on. Photosensitizers, as one of the core elements of PDT, usually have to face problems such as poor water solubility and light stability, lack of targeting, and other problems, which seriously affect the therapeutic effect. In this work, two BODIPY (boron-dipyrromethene)-based monofunctional Pt (II) complexes, 1a and 2a, were designed and synthesized, and their PDT effect was studied. The Pt atom improved the singlet oxygen quantum yield (0.19 for 1a and 0.14 for 2a, respectively), which effectively improves the efficiency of PDT. MTT assay confirmed that the short time photo-irradiation distinctly promoted antitumor cytotoxicity of Pt (II) compounds against different cell lines. For 1a under irradiation, the IC value of cancer cell lines were 13.1 μM for HeLa cells and 7.6 μM for MCF-7 cells, while those of normal cell lines were 32.4 μM for HBL-100 cells and 48.6 μM for L02 cells. The results demonstrated that 1a showed specific phototoxicity to cancer cells. This specific selectivity could be attributed to the synergistic effect of increased cellular uptake (determined by ICP-MS) and higher ROS generation (detected by Cell ROX Deep Red) in cancer cells after irradiation. This study laid the foundation for the future design and synthesis of effective PDT photosensitizers.
光动力疗法（PDT）因其创伤小、副作用少等优点，在癌症治疗中受到广泛关注。作为 PDT 的核心元素之一，光敏剂通常面临水溶性差、光稳定性差、缺乏靶向性等问题，严重影响了治疗效果。在这项工作中，设计并合成了两种基于 BODIPY（硼二吡咯甲烷）的单功能 Pt（II）配合物 1a 和 2a，并研究了它们的 PDT 效应。Pt 原子提高了单线态氧量子产率（1a 为 0.19，2a 为 0.14），有效提高了 PDT 的效率。MTT 试验证实，短时间光照射明显促进了 Pt（II）化合物对不同细胞系的抗肿瘤细胞毒性。在 1a 的照射下，癌细胞系的 IC 值为 HeLa 细胞为 13.1 μM，MCF-7 细胞为 7.6 μM，而正常细胞系的 IC 值为 HBL-100 细胞为 32.4 μM，L02 细胞为 48.6 μM。结果表明，1a 对癌细胞具有特异性光毒性。这种特异性选择性可以归因于照射后癌细胞中细胞摄取的增加（通过 ICP-MS 确定）和 ROS 生成的增加（通过 Cell ROX Deep Red 检测）的协同作用。这项研究为未来有效 PDT 光敏剂的设计和合成奠定了基础。
