【摘 要】
：
L-Ascorbic acid(AA,vitamin C) exhibits a high concentration in the brain.The transportation of AA in brain is mainly mediated by the glucose transporter 1(GLUT_
【机 构】
：
College of Pharmacy,Chengdu University of Traditional Chinese Medicine,Key Laboratory of Drug Target
【出 处】
：
Chinese Chemical Letters
论文部分内容阅读
L-Ascorbic acid(AA,vitamin C) exhibits a high concentration in the brain.The transportation of AA in brain is mainly mediated by the glucose transporter 1(GLUT_1) and the Na~+-dependent vitamin C transporter SVCT_2.While L-ascorbic acid C6-O conjugation has been investigated as a tool to enhance brain drug delivery,C5-O conjugation and C5-O & C6-O conjugation as brain targeting tools have not been reported.In this letter,ibuprofen was linked directly to C5-O,C6-O and C5-O & C6-O positions of L-ascorbic acid with eater bonds,providing prodrug 1,2 and 3,respectively,to improve their targeting abilities in the brain.Prodrug 1,2 and 3 were synthesized in facile ways with good yields.And the preliminary evaluation in vivo illustrated that prodrug 2 had a better targeting ability than prodrug 1. Moreover,prodrug 3,whose C5-O & C6-O positions were both modified,had good targeting ability for brain which will provide an important evidence for our further study on C5-0- & C6-0- di-derivatives of L-ascorbic acid.
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