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Three in One: Viscosity-Sensitive Ruthenium(II) Complexes for Photodynamic Anticancer by Activating Pyroptosis with
Xiurong Ma1, Guixi Wang2, Qian Zhou1
1School of Chemical Science and Technology, Key Laboratory of Medicinal Chemistry for Natural Resource of Yunnan, University Ministry of Education, Yunnan University, Kunming, Yunnan 650091, China.
Journal of Medicinal Chemistry
|October 30, 2025
Summary
New ruthenium photosensitizers trigger tumor cell pyroptosis and offer real-time treatment monitoring. This advancement in photodynamic therapy (PDT) allows for precise cancer treatment with visual feedback.
Area of Science:
- Materials Science
- Chemistry
- Biomedical Engineering
Background:
- Precision photodynamic therapy (PDT) requires real-time monitoring for enhanced efficacy.
- Developing photosensitizers (PS) with integrated monitoring capabilities is a key challenge.
Purpose of the Study:
- To design and synthesize novel ruthenium(II)-triphenylamine photosensitizers (Ru1-3).
- To investigate the antitumor mechanisms, focusing on pyroptosis induction and real-time luminescence monitoring.
- To evaluate their photocytotoxicity in 3D multicellular tumor spheroids (MCTSs) and in vivo.
Main Methods:
- Synthesis of three ruthenium(II)-triphenylamine compounds (Ru1-3).
- Antitumor mechanism studies involving caspase-1 activation, GSDMD cleavage, and mitochondrial membrane potential (MMP) depolarization assays.
- Luminescence intensity measurements during pyroptosis.
- Two-photon excitation experiments in 3D MCTSs.
- In vivo efficacy studies of Ru3.
Main Results:
- Ru1 and Ru3 successfully triggered tumor cell pyroptosis by activating caspase-1 and inducing GSDMD cleavage.
- Luminescence intensity of Ru1 and Ru3 increased during pyroptosis, correlating with cytoplasmic viscosity changes.
- Photocytotoxicity was confirmed in 3D MCTSs with luminescence amplification linked to pyroptosis.
- In vivo studies demonstrated superior PDT efficacy for Ru3 with real-time luminescence feedback.
Conclusions:
- Ruthenium(II)-triphenylamine photosensitizers (Ru1-3) can induce tumor cell pyroptosis.
- The luminescence of Ru1 and Ru3 serves as a real-time indicator of pyroptosis progression and treatment response.
- Ru3 shows significant potential for precision PDT with integrated therapeutic monitoring and two-photon imaging capabilities.
