Chang Rui, Nikoloudakis Emmanouil, Zou Qianli, Mitraki Anna, Coutsolelos Athanassios G, Yan Xuehai
State Key Laboratory of Biochemical Engineering, Institute of Process Engineering, Chinese Academy of Sciences, Beijing 100190, China.
University of Chinese Academy of Sciences, Beijing 100049, China.
ACS Appl Bio Mater. 2020 Jan 21;3(1):2-9. doi: 10.1021/acsabm.9b00558. Epub 2019 Sep 10.
Two hybrid materials were designed by conjugating peptide nucleic acids (PNAs) to porphyrin or boron-dipyrromethene, generating PNA-porphyrin (PNA-TPP) and PNA-BODIPY (PNA-BDP) conjugates, respectively. Because of the combination of the supramolecular characteristics of PNAs and photosensitizers, the two hybrid conjugates readily self-assemble in aqueous solutions and produce well-defined nanoparticles with uniform particle sizes. The resulting two kinds of nanoparticles show good stability in biological solutions and upon dilution. Importantly, the nanoparticles can efficiently interact with cancer cells and the internalized nanoparticles are mainly distributed in the cytoplasm without discernible cytotoxicity in the dark, enabling them to be applied as photodynamic nanoagents for selective killing cells. Hence, self-assembly of PNA-photosensitizer conjugates may hold promise for advancing the rational design and construction of photodynamic nanoagents for cancer therapy.
通过将肽核酸（PNA）与卟啉或硼二吡咯亚甲基共轭，设计了两种杂化材料，分别生成了PNA-卟啉（PNA-TPP）和PNA-硼二吡咯（PNA-BDP）共轭物。由于PNA和光敏剂的超分子特性相结合，这两种杂化共轭物在水溶液中易于自组装，并产生粒径均匀、定义明确的纳米颗粒。所得的两种纳米颗粒在生物溶液和稀释时均表现出良好的稳定性。重要的是，纳米颗粒可以与癌细胞有效相互作用，内化的纳米颗粒主要分布在细胞质中，在黑暗中没有明显的细胞毒性，使其能够作为光动力纳米剂用于选择性杀伤细胞。因此，PNA-光敏剂共轭物的自组装可能为推进用于癌症治疗的光动力纳米剂的合理设计和构建带来希望。
