Quan Hui, Huang Yuying, Xia Jiacheng, Yang Jiawen, Lu Bing, Liu Peisheng, Yao Yong
School of Science, Nantong University, No. 9 Seyuan Road, Chongchuan District, Nantong, Jiangsu, 226019, P. R. China.
College of Chemistry and Chemical Engineering, Nantong University, No. 9 Seyuan Road, Chongchuan District, Nantong, Jiangsu, 226019, P. R. China.
Chembiochem. 2023 Oct 4;24(19):e202300461. doi: 10.1002/cbic.202300461. Epub 2023 Aug 17.
BODIPY photosensitizers have been integrated with a hypoxia-activated prodrug to achieve synergistic photodynamic therapy (PDT) and chemotherapy. A novel BODIPY derivative BDP-CN was designed and synthesized. It had two cyano groups to make it complex well with a water-soluble pillar[5]arene. Their association constant was calculated to be (6.8±0.9)×10 M . After self-assembly in water, regular spherical nanocarriers can be formed; these were used to encapsulate the hypoxia-activated prodrug tirapazamine (TPZ). BDP-CN displayed excellent photodynamic activity to complete PDT. In this process, O can be continuously consumed to activate TPZ to allow it to be converted to a benzotriazinyl (BTZ) radical with high cytotoxicity to complete chemotherapy. As a result, the formed nanoparticles showed excellent synergistic photodynamic therapy and chemotherapy efficacy. The synergistic therapy mechanism is discussed in detail.
硼二吡咯光敏剂已与一种缺氧激活前药相结合，以实现协同光动力疗法（PDT）和化疗。设计并合成了一种新型硼二吡咯衍生物BDP-CN。它有两个氰基，使其能与水溶性柱[5]芳烃很好地络合。计算出它们的缔合常数为(6.8±0.9)×10 M。在水中自组装后，可形成规则的球形纳米载体；这些纳米载体用于包裹缺氧激活前药替拉扎明（TPZ）。BDP-CN表现出优异的光动力活性以完成光动力疗法。在此过程中，O可被持续消耗以激活TPZ，使其转化为具有高细胞毒性的苯并三嗪基（BTZ）自由基以完成化疗。结果，形成的纳米颗粒显示出优异的协同光动力疗法和化疗效果。详细讨论了协同治疗机制。
