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Improved chemoenzymatic radiosynthesis of fluorine-18 labeled sakebiose for microPET-CT imaging of Staphylococcus aureus

Abstract

Staphylococcus aureus (S. aureus) is a gram-positive bacterium that can cause severe infections such as pneumonia, osteomyelitis, and endocarditis when it breaches the skin. This study aimed to enhance the chemoenzymatic radiosynthesis of 2-deoxy-2-[18F]-fluoro-sakebiose ([18F]FSK), a radiotracer potentially useful for imaging S. aureus infections. By optimizing the synthesis of 2-deoxy-2-[19F]-fluoro-sakebiose ([19F]FSK), we identified key factors—such as increased enzyme concentration and decreased precursor levels—that significantly improved the yield. Applying these optimized conditions to the synthesis of [18F]FSK resulted in a 30% increase in the radiochemical yield (RCY%) from the control experiment. In vitro evaluation showed that [18F]FSK was successfully incorporated into two strains of S. aureus, suggesting its potential utility for imaging bacterial infections in vivo. This work lays the groundwork for using [18F]FSK in PET/CT imaging to diagnose and monitor S. aureus infections.

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