https://scholars.lib.ntu.edu.tw/handle/123456789/641336
標題: | Traversal of the Blood-Brain Barrier by Cleavable l-Lysine Conjugates of Apigenin | 作者: | Wong, Tsung-Yun Tsai, Ming-Shian Hsu, Lih-Ching Lin, Shu-Wha PI-HUI LIANG |
關鍵字: | amino acids; apigenin; blood brain barrier; flavonoid; prodrug; water solubility | 公開日期: | 1-八月-2018 | 卷: | 66 | 期: | 30 | 起(迄)頁: | 8124 | 來源出版物: | Journal of agricultural and food chemistry | 摘要: | 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 |
顯示於: | 藥學系 |
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