Issue 36, 2024

A thiol-triggered croconaine–chromene integration to induce ferroptosis and photothermal synergistic efficient tumor ablation

Abstract

Theranostic probes, combining diagnostic and treatment capabilities, have emerged as promising tools in tumor precision medicine. However, existing probes with constant fluorescence and photothermal activity can result in low signal-to-background ratios and phototoxicity. In this study, we introduced CM-Croc, a novel probe comprised of chromene and croconaine, selectively triggered by thiol. CM-Croc exhibited turn-on fluorescence and released croconaine for photothermal therapy. The croconaine moiety possesses high photothermal conversion efficiency up to 55%. Besides, it demonstrated potent activity against various cancer cell lines at low micromolar concentrations, including drug-resistant variants, through enhanced photothermal therapy combined with the ferroptosis effect. What's more, CM-Croc was proved to inhibit the activity of GPX4 to induce ferroptosis. Finally, CM-Croc was demonstrated to be the first croconaine-derived SOP, which targeted tumors and significantly inhibited tumor growth in vivo following intravenous administration with irradiation. This study showed CM-Croc's potential for enhancing tumor precision medicine.

Graphical abstract: A thiol-triggered croconaine–chromene integration to induce ferroptosis and photothermal synergistic efficient tumor ablation

Supplementary files

Article information

Article type
Edge Article
Submitted
05 Jun 2024
Accepted
09 Aug 2024
First published
16 Aug 2024
This article is Open Access

All publication charges for this article have been paid for by the Royal Society of Chemistry
Creative Commons BY-NC license

Chem. Sci., 2024,15, 14924-14930

A thiol-triggered croconaine–chromene integration to induce ferroptosis and photothermal synergistic efficient tumor ablation

X. Niu, H. Yang, X. Wu, F. Huo, K. Ma and C. Yin, Chem. Sci., 2024, 15, 14924 DOI: 10.1039/D4SC03688C

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