Rational Molecular Design of Efficient Heavy-Atom-Free Photosensitizers for Cancer Photodynamic Therapy

Van Nghia Nguyen, Jeongsun Ha, Hyunsun Jeong, Moonyeon Cho, Gyongmi Kim, Juyoung Yoon

Research output: Contribution to journalArticlepeer-review

1 Scopus citations

Abstract

Photodynamic therapy has emerged as a promising modality for treatment of cancer due to its minimal invasiveness and high selectivity. However, development of advanced photosensitizers (PSs) for clinical translation of photodynamic therapy remains challenging. To overcome the limitations of common photosensitizers containing heavy atoms, we herein developed highly effective heavy-atom-free photosensitizers based on strong donor-π-acceptor-type structures (PTZ-CN and PXZ-CN) for bioimaging and photodynamic ablation of cancer. These PSs exhibited bright fluorescence emission with a large Stokes shift as well as considerable reactive oxygen generation capability under specific conditions. Notably, PTZ-CN could produce reactive oxygen species more efficiently than Ru(bpy)32+ (commercial PS) with an approximately 2.2-fold via type I and type II photochemical mechanisms. In addition, their stable nanoparticles were easily formed by self-assembly in an aqueous solution without employing a polymer. More importantly, PTZ-CN/PXZ-CN exhibited bright fluorescence and excellent photodynamic performance with negligible dark cytotoxicity toward HeLa cells. This study demonstrates the promising potential of donor-π-acceptor-type molecule-based PSs in fluorescence image-guided photodynamic therapy.

Original languageEnglish
Article numbere202200086
JournalChemPlusChem
Volume87
Issue number7
DOIs
StatePublished - Jul 2022

Bibliographical note

Funding Information:
This work was supported by a National Research Foundation of Korea (NRF) grant funded by the Korean government (MSIT) (No. 2022R1A2C3005420). This work was supported by Korea Basic Science Institute (National Research Facilities and Equipment Center) grant funded by the Ministry of Education (2020R 1A 6C 101B194).

Funding Information:
This work was supported by a National Research Foundation of Korea (NRF) grant funded by the Korean government (MSIT) (No. 2022R1A2C3005420). This work was supported by Korea Basic Science Institute (National Research Facilities and Equipment Center) grant funded by the Ministry of Education (2020R 1A 6C 101B194).

Publisher Copyright:
© 2022 Wiley-VCH GmbH.

Keywords

  • donor-acceptor structure
  • intersystem crossing
  • photodynamic therapy
  • photosensitizer
  • reactive oxygen species

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