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Programmed Aggregation of Lipidated Nitrobenzoselenadiazole as a Photo-Activatable Pyroptosis Inducer

Jong Min An1, Hyunyoung Choi2, Hyo In Kim3

  • 1College of Medicine, Kyung Hee University, Seoul, 02447, Republic of Korea.

Advanced Healthcare Materials
|August 5, 2025
PubMed

Insights

This study introduces novel nitrobenzoselenadiazole (NBSD) photosensitizers that enhance photodynamic therapy (PDT) through programmed aggregation. NBSD-NOc shows superior performance in tumor treatment and preventing recurrence.

Area of Science:

  • Biochemistry
  • Materials Science
  • Oncology

Background:

  • Photosensitizers are crucial for photodynamic therapy (PDT) against tumors.
  • Photosensitizer aggregation in aqueous solutions reduces reactive oxygen species (ROS) generation and therapeutic efficacy.

Purpose of the Study:

  • To develop a programmed aggregation system using nitrobenzoselenadiazole (NBSD) scaffolds with varying alkyl chain lengths.
  • To investigate the potential of these NBSD derivatives as photo-activable pyroptosis inducers for cancer therapy.

Main Methods:

  • Synthesis of NBSD scaffolds with C1, C3, and C8 alkyl chains.
  • Evaluation of photophysical properties, cellular uptake, and ROS generation.
  • Assessment of pyroptosis induction and biocompatibility in vitro and in vivo.

Main Results:

  • NBSD derivatives demonstrated controlled aggregation and enhanced PDT effects.
  • NBSD-NOc exhibited superior cellular uptake, pyroptosis induction, and biocompatibility.
  • Programmed aggregation significantly improved photophysical properties and therapeutic outcomes.

Conclusions:

  • Molecular design of NBSD scaffolds can control aggregation and optimize photophysical properties for enhanced PDT.
  • NBSD-NOc presents a promising strategy for implantable photosensitizers in post-surgical tumor management.
  • This approach offers a novel method to combat tumor recurrence by inducing programmed cell death.
Keywords:
aggregationlipidationphotodynamic therapyphotosensitizerpyroptosis

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