Time-Dependent Photodynamic Therapy for Multiple Targets: A Highly Efficient AIE-Active Photosensitizer for Selective Bacterial Elimination and Cancer Cell Ablation

Angew Chem Int Ed Engl. 2020 Jun 8;59(24):9470-9477. doi: 10.1002/anie.201909706. Epub 2019 Oct 22.

Abstract

Pathogen infections and cancer are two major human health problems. Herein, we report the synthesis of an organic salt photosensitizer (PS), called 4TPA-BQ, by a one-step reaction. 4TPA-BQ presents aggregation-induced emission features. Owing to the aggregation-induced reactive oxygen species generated and a sufficiently small ΔEST , 4TPA-BQ shows a satisfactorily high 1 O2 generation efficiency of 97.8 %. In vitro and in vivo experiments confirmed that 4TPA-BQ exhibited potent photodynamic antibacterial performance against ampicillin-resistant Escherichia coli with good biocompatibility in a short time (15 minutes). When the incubation duration persisted long enough (12 hours), cancer cells were ablated efficiently, leaving normal cells essentially unaffected. This is the first reported time-dependent fluorescence-guided photodynamic therapy in one individual PS, which achieves ordered and multiple targeting simply by varying the external conditions. 4TPA-BQ reveals new design principles for the implementation of efficient PSs in clinical applications.

Keywords: aggregation-induced emission; anion-π+ interactions; antibacterial; cancer cells; multiple and ordered targeting.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • A549 Cells
  • Ablation Techniques*
  • Animals
  • COS Cells
  • Chlorocebus aethiops
  • Escherichia coli / drug effects
  • Escherichia coli / radiation effects
  • Humans
  • Molecular Targeted Therapy*
  • Photochemotherapy*
  • Photosensitizing Agents / pharmacology*

Substances

  • Photosensitizing Agents