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Tumor Stimulus-Activatable Pretheranostic Agent: One Key to Three Locks
Yize Zhang1, Yingyong Ni1, Xuan Zhao1
1School of Chemistry and Chemical Engineering, School of Materials Science and Engineering, Institutes of Physical Science and Information Technology, Center of Free Electron Laser & High Magnetic Field, Key Laboratory of Structure and Functional Regulation of Hybrid Materials Ministry of Education, Key Laboratory of Functional Inorganic Materials Chemistry of Anhui Province, and Key Laboratory of Chemistry for Inorganic/Organic Hybrid Functionalized Materials of Anhui Province, Anhui University, Hefei 230601, P. R. China.
Abstract:
The uncontrollable distribution of antitumor agents remains a large obstacle for specific and efficient cancer theranostics; thus, efficient construction of tumor-specific systems is highly desirable. In this work, a general design of tumor stimulus-activatable pretheranostic agents was put forward via a series of structures-tunable triphenylamine derivatives (TPA-2T-FSQ, TPA-2T-BSZ, and TPA-2T-ML) with phenothiazine, benzothiazine, and thiomorpholine as identifying groups of hypochlorite (HClO), respectively. Notably, the sulfur atom in phenothiazine of TPA-2T-FSQ was more easily oxidized to sulfoxide groups by HClO, transforming into an electron acceptor to form an excellent push-pull electronic system, which was beneficial to a large redshift of absorbance and emission wavelengths. Based on this, TPA-2T-FSQ resorted to a key of overexpressed HClO in the tumor to open "three locks", viz, NIR fluorescence, photothermal, and photoacoustic signals for multimodal diagnostic and treatment of the tumor. This study provided an elegant design to adopt tumor stimulus-triggerable pretheranostic for improving theranostic accuracy and efficiency, which was regarded as a promising candidate for precision medicine.
Insights
Researchers developed a novel tumor-specific system using triphenylamine derivatives that activate upon detecting hypochlorite (HClO). This system enhances cancer theranostics by enabling precise multimodal diagnosis and treatment.
Area of Science:
- Biomedical Engineering
- Materials Science
- Oncology
Background:
- Uncontrolled distribution of antitumor agents hinders effective cancer theranostics.
- Development of tumor-specific systems is crucial for improving therapeutic specificity and efficiency.
Purpose of the Study:
- To design and synthesize tumor stimulus-activatable pretheranostic agents for enhanced cancer theranostics.
- To create a general platform using triphenylamine derivatives for targeted tumor detection and treatment.
Main Methods:
- Synthesized triphenylamine derivatives (TPA-2T-FSQ, TPA-2T-BSZ, TPA-2T-ML) with specific identifying groups for hypochlorite (HClO).
- Investigated the oxidation of the sulfur atom in phenothiazine by HClO and its effect on electronic properties.
- Utilized the overexpressed HClO in tumors to trigger multimodal signals (NIR fluorescence, photothermal, photoacoustic).
Main Results:
- TPA-2T-FSQ demonstrated efficient oxidation by HClO, leading to a significant redshift in absorbance and emission wavelengths.
- The developed system successfully activated NIR fluorescence, photothermal, and photoacoustic signals in response to tumor-specific HClO.
- The agent enabled multimodal diagnosis and treatment of tumors, showcasing its theranostic potential.
Conclusions:
- A general design for tumor stimulus-triggerable pretheranostic agents was successfully established.
- The TPA-2T-FSQ agent offers improved theranostic accuracy and efficiency by leveraging tumor-specific hypochlorite.
- This approach represents a promising strategy for precision medicine in cancer treatment.
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