https://scholars.lib.ntu.edu.tw/handle/123456789/641336
Title: | Traversal of the Blood-Brain Barrier by Cleavable l-Lysine Conjugates of Apigenin | Authors: | Wong, Tsung-Yun Tsai, Ming-Shian Hsu, Lih-Ching Lin, Shu-Wha PI-HUI LIANG |
Keywords: | amino acids; apigenin; blood brain barrier; flavonoid; prodrug; water solubility | Issue Date: | 1-Aug-2018 | Journal Volume: | 66 | Journal Issue: | 30 | Start page/Pages: | 8124 | Source: | Journal of agricultural and food chemistry | Abstract: | Apigenin, a flavone abundant in parsley and celery, is known to act on several CNS receptors, but its very poor water solubility (<0.001 mg/mL) impedes its absorption in vivo and prevents clinical use. Herein, apigenin was directly conjugated with glycine, l-phenylalanine, and l-lysine to give the corresponding carbamate derivatives, all of which were much more soluble than apigenin itself (0.017, 0.018, and 0.13 mg/mL, respectively). The Lys-apigenin carbamate 10 had a temporary sedative effect on the mice within 5 min of intraperitoneal administration (single dose of 0.4 mg/g) and could be detected in the mice brain tissues at a concentration of 0.82 μg/g of intact Lys-apigenin carbamate 10 and 0.42 ug/g of apigenin at 1.5 h. This study accomplished the delivery of apigenin across the BBB in a manner that might be applicable to other congeners, which should inform the future development of BBB-crossing flavonoids. |
URI: | https://scholars.lib.ntu.edu.tw/handle/123456789/641336 | ISSN: | 00218561 | DOI: | 10.1021/acs.jafc.8b01187 |
Appears in Collections: | 藥學系 |
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.