AI Article Synopsis
- BNCT is a promising treatment for tumors but faces challenges like low boron accumulation in tumors and poor tumor-to-blood/tumor-to-normal tissue ratios.
- Researchers developed fluorinated BPA derivatives to improve boron delivery, leading to better tumor accumulation and enhanced T/B and T/N ratios compared to existing boron drugs.
- In tests with mice, these derivatives showed effectiveness at half the clinical dose, suggesting they could be strong candidates for BNCT treatment in melanoma.
Article Abstract
Boron neutron capture therapy (BNCT) is an emerging approach for treating malignant tumors with binary targeting. However, its clinical application has been hampered by insufficient B accumulation in tumors and low B concentration ratios of tumor-to-blood (T/B) and tumor-to-normal tissue (T/N). Herein, we developed fluorinated BPA derivatives with different fluorine groups as boron delivery agents for enabling sufficient B accumulation in tumors and enhancing T/B and T/N ratios. Our findings demonstrated that fluorinated BPA derivatives had good biological safety. Furthermore, fluorinated BPA derivatives showed improved B accumulation in tumors and enhanced T/B and T/N ratios compared to the clinical boron drug fructose-BPA (f-BPA). In particular, in B16-F10 tumor-bearing mice, fluorinated BPA derivatives met the requirements for clinical BNCT even at half of the clinical dose. Thus, fluorinated BPA derivatives are potentially effective boron delivery agents for clinical BNCT in melanoma.
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| http://dx.doi.org/10.1039/d4tb00846d | DOI Listing |
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