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Chair-Shaped Indoline Donor Enabling Near-Infrared Imaging-Guided Type I Photodynamic Therapy.

Guofeng Yi1, Qiqi Xu1, Haodong Liu2

  • 1Key Laboratory for Advanced Materials and Joint International Research Laboratory of Precision Chemistry and Molecular Engineering, Feringa Nobel Prize Scientist Joint Research Center, Shanghai Key Laboratory of Functional Materials Chemistry, Institute of Fine Chemicals, East China University of Science and Technology, Shanghai 200237, P. R. China.

ACS Applied Bio Materials
|March 17, 2026
PubMed
Summary

Researchers developed a novel indoline-based photosensitizer (IDL-CPy) for imaging-guided photodynamic therapy (PDT). This aggregation-induced emission agent enhances type I reactive oxygen species (ROS) generation, overcoming limitations of traditional PDT.

Keywords:
aggregation-induced emissionnear-infrared imagingphotodynamic therapyreactive oxygen speciestype I photosensitizer

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Area of Science:

  • Materials Science
  • Chemistry
  • Biomedical Engineering

Background:

  • Photodynamic therapy (PDT) offers precise, minimally invasive cancer treatment.
  • Tumor hypoxia and photosensitizer (PS) aggregation limit current PDT efficacy.
  • Developing novel PSs that overcome these challenges is crucial for clinical translation.

Purpose of the Study:

  • To design and synthesize a novel indoline-based photosensitizer with aggregation-induced emission (AIE) characteristics.
  • To enable effective type I reactive oxygen species (ROS) generation for imaging-guided PDT.
  • To evaluate the anticancer efficacy of the developed photosensitizer.

Main Methods:

  • Synthesis of a chair-shaped indoline donor-based AIE photosensitizer (IDL-CPy).
  • Investigation of intramolecular charge transfer and singlet-triplet energy gap modulation.
  • Assessment of ROS generation mechanisms (Type I predominant).
  • In vitro evaluation of anticancer efficacy.

Main Results:

  • IDL-CPy exhibits aggregation-induced emission (AIE) and a type I ROS-predominant mechanism.
  • The indoline structure facilitates efficient ROS generation by narrowing the singlet-triplet energy gap.
  • IDL-CPy demonstrated potent in vitro anticancer efficacy with a low IC50 value of 0.34 μM.
  • This represents the first indoline-based AIE photosensitizer.

Conclusions:

  • The novel indoline-based AIE photosensitizer (IDL-CPy) effectively generates ROS via a type I mechanism.
  • IDL-CPy overcomes limitations of tumor hypoxia and PS aggregation in PDT.
  • This photosensitizer shows significant promise for advanced imaging-guided type I PDT applications.