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Published on: February 17, 2022
Charge-Regulation Activable Theranostic Probe for Tumor-Specific Fluorescence Imaging and Chemo-Phototherapy
Nana Su1, Yanhong Lin1, Bingling Zhang1
1State Key Laboratory of Chemical Resource Engineering, College of Chemistry, Beijing University of Chemical Technology, Beijing, P. R. China.
Abstract:
Activable theranostic probes offer significant potential for the precise diagnosis and therapy in cancer treatment. The core challenge in realizing this target is how to manipulate therapeutic and imaging activities by a simple yet efficient method. To address this, an exceptional "charge regulation" strategy to furnish an activable theranostic probe, GSH-Cy5 is employed. The probe undergoes tumor-specific activation via glutathione (GSH)-triggered decationization, concurrently enhancing its anti-cancer activity and tumor-imaging contrast. Beyond this theranostic activity, GSH-Cy5 also exhibits synergistic photothermal (PTT) and photodynamic (PDT) effects, which further amplify its therapeutic efficacy by inducing cell death through mitochondria-mediated pathways. In vivo experiments demonstrated the effectiveness of GSH-Cy5, as it successfully enabled tumor visualization and selective therapy in tumor-bearing mouse models. This work establishes GSH-Cy5 as a transformative theranostic platform, while the "charge regulation" strategy opens new avenues for designing activable cyanine probes in precise tumor treatment.
Insights
This study introduces GSH-Cy5, an activable theranostic probe for cancer. It uses a charge regulation strategy for enhanced tumor imaging and therapy, combining photothermal and photodynamic effects for improved treatment outcomes.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Activable theranostic probes are crucial for precise cancer diagnosis and therapy.
- A key challenge is efficiently controlling therapeutic and imaging functions.
- Developing simple, effective strategies for activable probes is essential.
Purpose of the Study:
- To develop an activable theranostic probe using a "charge regulation" strategy.
- To enhance anti-cancer activity and tumor-imaging contrast via glutathione (GSH)-triggered decationization.
- To investigate synergistic photothermal (PTT) and photodynamic (PDT) effects for amplified therapeutic efficacy.
Main Methods:
- Designed and synthesized the GSH-Cy5 probe.
- Utilized a "charge regulation" strategy for tumor-specific activation.
- Evaluated probe performance in vitro and in vivo using tumor-bearing mouse models.
Main Results:
- GSH-Cy5 demonstrated tumor-specific activation via GSH-triggered decationization.
- The probe enhanced anti-cancer activity and tumor-imaging contrast.
- Synergistic PTT and PDT effects were observed, leading to enhanced cell death via mitochondria-mediated pathways.
- In vivo studies confirmed successful tumor visualization and selective therapy.
Conclusions:
- GSH-Cy5 serves as a transformative theranostic platform for precise cancer treatment.
- The "charge regulation" strategy offers a novel approach for designing activable cyanine probes.
- This work advances the development of targeted cancer therapies with improved diagnostic and therapeutic capabilities.

