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Updated: Dec 2, 2025

Radionuclide-fluorescence Reporter Gene Imaging to Track Tumor Progression in Rodent Tumor Models
Published on: March 13, 2018
Tumor-specific fluorescence activation of rhodamine isothiocyanate derivatives
Shiqi Hu1, Haiping Jiang2, Jianqiang Zhu3
1Key Laboratory of Biomass Chemical Engineering of Ministry of Education and Center for Bionanoengineering, College of Chemical and Biological Engineering, Zhejiang University, Hangzhou 310027, China.
Abstract:
Fluorescence is routinely used for in vivo tracking and imaging of molecules and nanostructures with assuming that the fluorescence intensity is proportional to the dye concentration. Herein, we report the unique tumor-specific fluorescence character of rhodamine B isothiocyanate derivatives (RBITCs), which emits fluorescence selectively in cancerous tissues, including small metastatic tumors, but is quenched in blood and healthy tissues. A preliminary mechanism study shows that binding of the thiourea group in the RBITCs on hemoglobin quenches their fluorescence, but the oxidation of the thiourea by the elevated reactive oxygen species in tumor activates the fluorescence. Thus, the fluorescent intensity of RBITCs is associated with the microenvironment of tissues and positively correlates with the cancer stages. These findings suggest that the RBITCs are not suitable for tracking of cargos in the presence of red blood cells but may be useful for cancer imaging and early diagnosis, and probing the tumor microenvironment.
Insights
Rhodamine B isothiocyanate derivatives (RBITCs) show unique tumor-specific fluorescence, quenched in healthy tissues but activated in tumors. This property holds potential for cancer imaging and diagnosis.
Area of Science:
- Biochemistry
- Organic Chemistry
- Medical Imaging
Background:
- Fluorescence is commonly used for in vivo tracking, assuming intensity correlates with dye concentration.
- Existing methods lack specificity for certain biological environments.
Purpose of the Study:
- To investigate the tumor-specific fluorescence of rhodamine B isothiocyanate derivatives (RBITCs).
- To explore the potential of RBITCs for cancer imaging and diagnosis.
Main Methods:
- Synthesis and characterization of RBITCs.
- In vitro and in vivo fluorescence imaging studies in cancerous and healthy tissues.
- Preliminary mechanistic studies involving hemoglobin and reactive oxygen species.
Main Results:
- RBITCs exhibit fluorescence selectively in cancerous tissues, including metastatic tumors.
- Fluorescence is quenched in blood and healthy tissues due to hemoglobin binding.
- Elevated reactive oxygen species in tumors activate RBITC fluorescence.
- Fluorescence intensity correlates positively with cancer stages.
Conclusions:
- RBITCs are not suitable for cargo tracking in the presence of red blood cells.
- RBITCs show promise for cancer imaging, early diagnosis, and probing the tumor microenvironment.
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