Making Aggregation-Induced Emission Luminogen More Valuable by Gold: Enhancing Anticancer Efficacy by Suppressing Thioredoxin Reductase Activity

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 (ALEgen), TBP-Au, was designed and synthesized by integrating an anticancer Au(I) moiety with an ME-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 ME 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.

Automated summary

TBP-Au, a powerful aggregation-induced emission luminogen, combines an anticancer Au(I) moiety with an ME-active photosensitizer to enhance anticancer efficacy, enabling superior two-photon fluorescence imaging in tumor tissues and efficient facilitation of ROS-determined photodynamic therapy.