Publication in refereed journal
香港中文大学研究人员 ( 现职)
| 左中教授 (药剂学院) |
| 林革教授 (生物医学学院) |
全文
| 数位物件识别号 (DOI) http://dx.doi.org/10.1016/j.ijpharm.2008.08.035 |
引用次数
Web of Sciencehttp://aims.cuhk.edu.hk/converis/portal/Publication/14WOS source URL
其它资讯
摘要Flavonoids have low bioavailabilittes due to extensive intestinal first-pass metabolisms, especially glucuronidation. The present study aimed to evaluate the intestinal glucuronidation of dihydroxyflavones and provide more information on their structure-activity relationships. Seven dihydroxyflavones, namely 3,7-, 5,7-, 6,7-, 7,8-, 2',7-, 3',7-, and 4',7-dihydroxyflaovne and a monohydroxyflavone, 7-hydroxyflavone, were investigated by incubating each hydroxyflavone at various concentrations with either human jejunum microsome or rat intestinal microsome. Two mono-glucoronides were identified for each dihydroxyflavone. For human jejunum Microsome, most of the Studied dihydroxyflavones demonstrated greater glucuronidation activities than that of 7-hydroxyflavone except for 3,7-dihydroxyflavone and 4',7-dihydroxyflavone. 3',7-dihydroxyflavone had the greatest intrinsic clearance which was at least seven times greater than that of all other dihydroxyflavones. In addition, species difference in glucuronidation activity was observed with human jejunum microsome higher than rat intestinal microsome for all hydroxyflavones except for 3,7-dihydroxyflavone. The results further demonstrated that the hydroxyl group positions do affect the intestinal glucuronidation activity of hydroxyflavones. Increasing the number of hydroxyl groups on A- or B-ring (except for 4'-OH) Would enhance the glucuronidation activity of flavones, whereas adding a 3-OH on C-ring might not. Furthermore. existence of hydroxyl group at 3' position may enhance the glucuronidation activity of flavonoids. (C) 2008 Elsevier B.V. All rights reserved.
着者Wong YC, Zhang L, Lin G, Zuo Z
期刊名称International Journal of Pharmaceutics
出版年份2009
月份1
日期21
卷号366
期次1-2
出版社Elsevier
页次http://aims.cuhk.edu.hk/converis/portal/Publication/14 - 20
国际标準期刊号0378-5173
电子国际标準期刊号1873-3476
语言英式英语
关键词Dihydroxyflavones; Glucuronidation; Intestine
Web of Science 学科类别Pharmacology & Pharmacy; PHARMACOLOGY & PHARMACY
