Department of Laboratory Medicine, Nanfang Hospital, Southern Medical University, Guangzhou, 510515, China.
Department of Chemistry, Hong Kong Branch of Chinese National Engineering Research Center for Tissue Restoration and Reconstruction and Institute for Advanced Study, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong 999077, China.
ACS Nano. 2021 May 25;15(5):9176-9185. doi: 10.1021/acsnano.1c02882. Epub 2021 May 3.
Gold complexes have been recognized as potential anticancer agents against various kinds of diseases due to their inherent suppressions of antioxidant thioredoxin reductase (TrxR) activity. Herein, a powerful aggregation-induced emission luminogen (AIEgen), TBP-Au, was designed and synthesized by integrating an anticancer Au(I) moiety with an AIE-active photosensitizer (TBP), in which both the production and consumption routes of reactive oxygen species (ROS) were elaborately considered simultaneously to boost the anticancer efficacy. It has been demonstrated that TBP-Au could realize superior two-photon fluorescence imaging in tumor tissues with high resolution and deep penetration as well as long-term imaging in live animals due to its AIE property. In addition, the introduction of a special Au(I) moiety could tune the organelle specificity and efficiently facilitate the ROS-determined photodynamic therapy (PDT). More impressively, TBP-Au could efficiently eliminate cancer cells under light irradiation through the preconceived synergetic approaches from the PDT and the effective suppression of TrxR, demonstrating that TBP-Au holds great potential for precise cancer theranostics.
金配合物因其内在的抗氧化剂硫氧还蛋白还原酶（TrxR）活性抑制作用，被认为是对抗各种疾病的潜在抗癌药物。本文设计并合成了一种强效的聚集诱导发光体（AIEgen）TBP-Au，它将抗癌的金（I）部分与 AIE 活性的光敏剂（TBP）结合在一起，同时精心考虑了活性氧（ROS）的产生和消耗途径，以提高抗癌效果。由于其 AIE 特性，TBP-Au 能够在肿瘤组织中实现优异的双光子荧光成像，具有高分辨率和深穿透性，以及在活体动物中的长期成像。此外，引入特殊的金（I）部分可以调整细胞器的特异性，并有效地促进 ROS 决定的光动力疗法（PDT）。更令人印象深刻的是，TBP-Au 可以通过 PDT 和有效抑制 TrxR 的协同作用，在光照射下有效地消除癌细胞，这表明 TBP-Au 在精确的癌症治疗中有很大的潜力。
