Enzyme activatable photodynamic therapy agents targeting melanoma
Imran Verirsen1, Busra Uyar1, Nezahat Gokce Ozsamur1
1Konya Food and Agriculture University, Faculty of Science, Department of Biotechnology, 42080, Konya, Turkey. sundus.erbascakmak@gidatarim.edu.tr.
Abstract:
Cell-selective activity regulation of therapeutics is necessary for efficient personalized treatments with minimal off-target effects. Here, the first example of a structurally simple, pyridinium BODIPY-based, tyrosinase activatable photosensitizer is developed and the cytotoxic singlet oxygen generation capacity is analysed. Singlet oxygen quantum yields of active and inactive forms are determined to be 0.64 and 0.02, respectively. Selective photo-induced cell death in mouse melanoma cells over mammary and hepatocellular carcinoma proved the potential of the photosensitizer in tissue-selective therapies.
Insights
Researchers developed a novel pyridinium BODIPY photosensitizer for targeted cancer therapy. This tyrosinase-activated compound selectively kills melanoma cells, showing promise for personalized treatments with reduced side effects.
Area of Science:
- Biochemistry
- Organic Chemistry
- Photodynamic Therapy
Background:
- Targeted drug delivery is crucial for effective cancer treatment with minimal side effects.
- Developing activatable photosensitizers offers a strategy for localized therapeutic action.
Purpose of the Study:
- To develop and characterize a novel, structurally simple pyridinium BODIPY-based photosensitizer.
- To investigate its tyrosinase-activatable properties and singlet oxygen generation capacity.
- To evaluate its potential for cell-selective photodynamic therapy.
Main Methods:
- Synthesis of a pyridinium BODIPY-based photosensitizer.
- Analysis of singlet oxygen quantum yields for active and inactive forms.
- Assessment of selective photo-induced cell death in various cancer cell lines (melanoma, mammary, hepatocellular carcinoma).
Main Results:
- The developed photosensitizer is tyrosinase-activatable.
- Singlet oxygen quantum yields were determined to be 0.64 for the active form and 0.02 for the inactive form.
- Selective photo-induced cell death was observed in mouse melanoma cells compared to mammary and hepatocellular carcinoma cells.
Conclusions:
- A novel pyridinium BODIPY photosensitizer with tyrosinase-activatable properties has been successfully developed.
- The photosensitizer demonstrates efficient singlet oxygen generation upon activation.
- This compound shows significant potential for tissue-selective photodynamic therapy, particularly against melanoma.
