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<p>Development of novel photosensitizers (PSs) with high biocompatibility and biological uptake is of significance for efficient photodynamic anti-tumor or anti-bacterial. This study presents a smart self-assembly strategy of glyco-photosensitizers with near-infrared (NIR) emission and aggregation-induced generation reactive oxygen species (AIG-ROS) ability for cell imaging and photodynamic therapy (PDT) of both tumor cells and bacteria. Two photosensitizers, <b>KL1</b> and <b>KL2</b>, are based on a “D-π-A” molecular architecture, featuring a tricyanofuran (TCF) acceptor and a tetraphenylethene (TPE) donor bridged by thiophene derivatives. After self-assembling with TPE-based glycoclusters (<b>TPE-Glc</b><sub><b>4</b></sub>), the resulting glyco-nanoparticles (<b>KL1-G</b> and <b>KL2-G</b>) exhibit improved water solubility and AIG-ROS capability, including singlet oxygen (<sup>1</sup>O<sub>2</sub>) and superoxide radicals (·O<sub>2</sub><sup>−</sup>) upon light irradiation. In cellular studies, TPE-glycoclusters facilitate the cellular uptake of PSs, thereby enhancing the NIR fluorescence signal and PDT efficiency for multiple kinds of cells. <b>KL2-G</b> shows superior phototoxicity, reducing cell viability to less than 5% at a low concentration of &lt;5 μM under light irradiation. Additionally, <b>KL2-G</b> exhibits potential for photodynamic anti-bacterial applications against <i>Escherichia coli</i>. This work underscores the importance of glycoclustersmediated delivery in therapeutic efficacy enhancement of PSs and highlights the potential of glyco-nanoparticles in bioimaging and phototherapy applications.</p>

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Smart formation of multifunctional glyco-nanoparticles: glycoclusters delivering NIR photosensitizers for enhanced cell imaging and photodynamic therapy

  • 期刊论文

  • 发表日期：

    2025年8月4日

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  • Kai-Li He,
  • Lu-Lu Sun,
  • Wen-Jia Li,
  • Lei Dong,
  • Cheng-Long Ding,
  • Ming-Chao Tan,
  • Ke-Xin Zhang,
  • Jin Gong,
  • Liping Zhang,
  • Hai-Hao Han

摘要

Development of novel photosensitizers (PSs) with high biocompatibility and biological uptake is of significance for efficient photodynamic anti-tumor or anti-bacterial. This study presents a smart self-assembly strategy of glyco-photosensitizers with near-infrared (NIR) emission and aggregation-induced generation reactive oxygen species (AIG-ROS) ability for cell imaging and photodynamic therapy (PDT) of both tumor cells and bacteria. Two photosensitizers, KL1 and KL2, are based on a “D-π-A” molecular architecture, featuring a tricyanofuran (TCF) acceptor and a tetraphenylethene (TPE) donor bridged by thiophene derivatives. After self-assembling with TPE-based glycoclusters (TPE-Glc4), the resulting glyco-nanoparticles (KL1-G and KL2-G) exhibit improved water solubility and AIG-ROS capability, including singlet oxygen (1O2) and superoxide radicals (·O2−) upon light irradiation. In cellular studies, TPE-glycoclusters facilitate the cellular uptake of PSs, thereby enhancing the NIR fluorescence signal and PDT efficiency for multiple kinds of cells. KL2-G shows superior phototoxicity, reducing cell viability to less than 5% at a low concentration of <5 μM under light irradiation. Additionally, KL2-G exhibits potential for photodynamic anti-bacterial applications against Escherichia coli. This work underscores the importance of glycoclustersmediated delivery in therapeutic efficacy enhancement of PSs and highlights the potential of glyco-nanoparticles in bioimaging and phototherapy applications.