Shen Jian, Pan Liuhong, Zhang Xujing, Zou Zhenyuan, Wei Bo, Chen Yongchang, Tang Xiaoyan, Zou Dengfeng
Department of Urology, Changshu No. 2 People's Hospital, Changshu, China.
School of Pharmacy, Guilin Medical University, Guilin, China.
Front Bioeng Biotechnol. 2022 Mar 9;10:781766. doi: 10.3389/fbioe.2022.781766. eCollection 2022.
Photodynamic therapy (PDT) utilizes the photogeneration of reactive oxygen species (ROS) with high cytotoxicity to kill cancer cells, holding great promise for cancer treatment. Fractionated delivery of singlet oxygen (O) is a wise approach to relieving hypoxia, thus enhancing the therapeutic efficacy. In this article, an anthracene-functionalized semiconducting compound (DPPA) has been designed and synthesized. With irradiation, the compound is able to undergo efficient intersystem crossing (ISC) and non-radioactive decay for photodynamic/photothermal synergistic therapy. In addition, the anthracene module is able to capture and release O reversibly with or without irradiation. DPPA nanoparticles (NPs) obtained by nanoprecipitation with DSPE-PEG exhibit considerable high phototoxicity on human kidney cancer cells (A498), and the half maximum inhibitory concentration (IC) is 15.8 μg/ml. Furthermore, an study demonstrates that complete tumor suppression was observed when the mice were administered DPPA NPs with the help of laser, compared with the control and dark groups. The H&E analysis of the normal tissues (the heart, liver, spleen, lungs, and kidney) indicates that such NPs cause no side effects, indicating the biosafety of DPPA NPs. The results provide a strategy to design a heavy-atom-free photosensitizer for photothermal and fractionated PDT against kidney tumors.
光动力疗法（PDT）利用具有高细胞毒性的活性氧（ROS）的光生成来杀死癌细胞，在癌症治疗方面具有巨大潜力。单线态氧（O）的分次递送是缓解缺氧从而提高治疗效果的明智方法。在本文中，设计并合成了一种蒽官能化的半导体化合物（DPPA）。在光照下，该化合物能够进行有效的系间窜越（ISC）和非辐射衰变，用于光动力/光热协同治疗。此外，蒽模块能够在有或无光照的情况下可逆地捕获和释放O。通过与DSPE-PEG进行纳米沉淀获得的DPPA纳米颗粒（NPs）对人肾癌细胞（A498）表现出相当高的光毒性，半数最大抑制浓度（IC）为15.8μg/ml。此外，一项研究表明，与对照组和黑暗组相比，在激光辅助下给小鼠施用DPPA NPs时观察到肿瘤完全抑制。对正常组织（心脏、肝脏、脾脏、肺和肾脏）的苏木精-伊红（H&E）分析表明，此类纳米颗粒不会产生副作用，表明DPPA NPs具有生物安全性。这些结果提供了一种策略，用于设计一种无重原子的光敏剂，用于针对肾肿瘤的光热和分次PDT。
