Dual-Responsive Molecular Probe for Tumor Targeted Imaging and Photodynamic Therapy
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Xiaoqing Meng1,2, Yueting Yang1, Lihua Zhou1,3
1Guangdong Key Laboratory of Nanomedicine, CAS Key Lab of Health Informatics, Shenzhen Institutes of Advanced Technology, Chinese Academy of Sciences, Shenzhen 518055, China.
Abstract:
The precision oncology significantly relies on the development of multifunctional agents to integrate tumor targeting, imaging and therapeutics. In this study, a first small-molecule theranostic probe, RhoSSCy is constructed by conjugating 5'-carboxyrhodamines (Rho) and heptamethine cyanine IR765 (Cy) using a reducible disulfide linker and pH tunable amino-group to realize thiols/pH dual sensing. In vitro experiments verify that RhoSSCy is highly sensitive for quantitative analysis and imaging intracellular pH gradient and biothiols. Furthermore, RhoSSCy shows superb tumor targeted dual-modal imaging via near-infrared fluorescence (NIRF) and photoacoustic (PA). Importantly, RhoSSCy also induces strongly reactive oxygen species for tumor photodynamic therapy (PDT) with robust antitumor activity both in vitro and in vivo. Such versatile small-molecule theranostic probe may be promising for tumor targeted imaging and precision therapy.
Insights
A novel small-molecule theranostic probe, RhoSSCy, enables dual sensing of pH and biothiols. It achieves precise tumor imaging and effective photodynamic therapy, advancing precision oncology.
Area of Science:
- Oncology
- Biomedical Engineering
- Chemical Biology
Background:
- Precision oncology demands integrated agents for tumor targeting, imaging, and therapy.
- Existing theranostic agents often lack multifunctionality or small-molecule design.
Purpose of the Study:
- To develop a novel small-molecule theranostic probe for dual sensing, imaging, and therapy in precision oncology.
- To evaluate the probe's efficacy in vitro and in vivo for tumor targeting and treatment.
Main Methods:
- Conjugation of 5'-carboxyrhodamines (Rho) and heptamethine cyanine IR765 (Cy) via a reducible disulfide linker and pH-tunable amino group.
- In vitro assessment of dual sensing capabilities for pH and biothiols.
- In vitro and in vivo evaluation of tumor-targeted dual-modal imaging (NIRF and PA) and photodynamic therapy (PDT).
Main Results:
- RhoSSCy demonstrated high sensitivity for quantitative analysis and imaging of intracellular pH gradients and biothiols.
- The probe exhibited excellent tumor-targeted dual-modal imaging via near-infrared fluorescence (NIRF) and photoacoustic (PA) imaging.
- RhoSSCy effectively induced reactive oxygen species, leading to robust in vitro and in vivo antitumor activity via photodynamic therapy (PDT).
Conclusions:
- RhoSSCy is a versatile small-molecule theranostic probe with dual sensing, imaging, and therapeutic capabilities.
- This probe shows significant promise for advancing tumor-targeted imaging and precision therapy in oncology.
