A Blood-brain Barrier Permeable Derivative of 5-Fluorouracil: Preparation, Intracellular Localization, and Mouse Tissue Distribution
A Blood-brain Barrier Permeable Derivative of 5-Fluorouracil: Preparation, Intracellular Localization, and Mouse Tissue Distribution
임정균(순천향대학교); Goutam Biswas(Department of Chemistry, Pohang University of Science and Technology); 김완일(포항공과대학교); 김경태(포항공과대학교); 정성기(포항공과대학교)
32권 3호, 873~879쪽
초록
5-Fluorouracil (5-FU), an anticancer agent was covalently attached to the recently developed sorbitol-based G8transporter, and the conjugate (7) with FITC was found to have an affinity toward mitochondria and to readily cross BBB to gain an entry into mouse brain. Measured by IC_50, the conjugate (9) without the fluorophore showed enhanced cytotoxic activity toward two types of multidrug-resistant cell lines. These results strongly suggest that the sorbitol-based G8 transporter can be utilized as a good CNS delivery vector.
Abstract
5-Fluorouracil (5-FU), an anticancer agent was covalently attached to the recently developed sorbitol-based G8transporter, and the conjugate (7) with FITC was found to have an affinity toward mitochondria and to readily cross BBB to gain an entry into mouse brain. Measured by IC_50, the conjugate (9) without the fluorophore showed enhanced cytotoxic activity toward two types of multidrug-resistant cell lines. These results strongly suggest that the sorbitol-based G8 transporter can be utilized as a good CNS delivery vector.
- 발행기관:
- 대한화학회
- 분류:
- 화학