A Blood-brain Barrier Permeable Derivative of 5-Fluorouracil: Preparation, Intracellular Localization, and Mouse Tissue Distribution

摘要

5-Fluorouracil (5-FU), an anticancer agent was covalently attached to the recently developed sorbitol-based G8BRtransporter, and the conjugate (STRONG7/STRONG) with FITC was found to have an affinity toward mitochondria and to readilyBRcross BBB to gain an entry into mouse brain. Measured by ICSUB50/SUB, the conjugate (STRONG9/STRONG) without the fluorophoreBRshowed enhanced cytotoxic activity toward two types of multidrug-resistant cell lines. These results stronglyBRsuggest that the sorbitol-based G8 transporter can be utilized as a good CNS delivery vector.