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Updated: Sep 16, 2025
Near Infrared Photoimmunotherapy for Mouse Models of Pleural Dissemination
Published on: February 9, 2021
Efficient radical generator with NIR emission by donor modulation for mitochondria-targeted photodynamic therapy
Lixin Ma1, Yingcui Bu2, Mingdi Yang3
1School of Chemistry and Chemical Engineering, Anhui University, Key Laboratory of Functional Inorganic Materials Chemistry of Anhui Province, Key Laboratory of Chemistry for Inorganic/Organic Hybrid Functionalized Materials of Anhui Province, Key Laboratory of Structure and Functional Regulation of Hybrid Materials (Anhui University) Ministry of Education, Hefei 230601, PR China.
Researchers developed new near-infrared type I photosensitizers for photodynamic therapy. One compound, TPA-IN, effectively targets mitochondria, inducing cancer cell death upon light activation.
Area of Science:
- Photodynamic Therapy
- Organic Chemistry
- Cancer Research
Background:
- Developing targeted near-infrared (NIR) type I photosensitizers (PSs) for specific organelle targeting in photodynamic therapy (PDT) is challenging.
- Existing PSs often lack specificity and efficiency in generating reactive oxygen species (ROS).
Purpose of the Study:
- To design and synthesize novel D-π-A type I PSs with enhanced NIR emission and improved ROS generation.
- To investigate the subcellular targeting capabilities, particularly mitochondrial accumulation, and the mechanism of action of these PSs.
- To evaluate their efficacy in inducing cancer cell apoptosis via PDT.
Main Methods:
- Synthesis of two D-π-A PSs, TPE-IN and TPA-IN, by modifying donor groups.
- Spectroscopic analysis to determine photophysical properties, including emission wavelength and singlet-triplet energy gap (ΔEST).
- Mechanistic studies on ROS generation (superoxide anion radical O2- and hydroxyl radical OH) via Haber-Weiss reaction.
- Cellular uptake studies using electrostatic interaction assessment (Pr=0.81) for mitochondrial targeting.
- Assessment of mitochondrial membrane potential and apoptosis induction (95.8%) upon light exposure.
Main Results:
- Replacing the tetraphenylethylene (TPE) donor with triphenylamine (TPA) in TPA-IN extended emission into the NIR-I region.
- TPA-IN exhibited a narrowed ΔEST (0.53 eV), promoting efficient generation of O2- and OH radicals.
- TPA-IN demonstrated specific accumulation in mitochondria via electrostatic interactions.
- Light exposure of TPA-IN treated cells led to decreased mitochondrial membrane potential and high late apoptosis rates (95.8%).
Conclusions:
- The developed D-π-A PSs, particularly TPA-IN, show promise as efficient NIR-I agents for photodynamic cancer therapy.
- TPA-IN's specific mitochondrial targeting and ROS generation capabilities offer a precise approach for cancer cell elimination.
- This work provides a foundation for designing advanced optical theranostic agents for targeted cancer treatment.
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