期刊
JOURNAL OF FUNCTIONAL FOODS
卷 35, 期 -, 页码 635-640出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.jff.2017.06.027
关键词
Daidzein sulfonic acid ester; Lipid/water partition coefficient; Caco-2 epithelial cell; Anti-inflammatory activity; JNK
资金
- A-Base research of Agriculture & Agri-Food Canada [RBPI 1004]
- National Science Foundation of China [81160412, 81660541]
- Natural Science Foundation of Jiangxi, China [20132BAB204003]
- Special Fund for Young Teacher Development Plan (visiting scholars) in Universities of Jiangxi Province, China
To improve the activity of the isoflavone daidzein (1) and to explore its structure-activity relationship, new daidzein sulfonic acid ester derivatives (2-4) were synthesized. All three derivatives showed significantly enhanced anti-inflammatory activities by 100-10,000-fold over that of the parent daidzein in TNF-alpha-stimulated Caco-2 cells. Daidzein derivatives 2 and 3 showed the same anti-inflammatory effect at 1 mu M and derivative 4 had at 0.01 mu M as 100 mu M daidzein. Compound 3 also showed significant anti -oxidative effect at 100 mu M in H2O2-treated caco-2 cells. Treatment with daidzein and its derivatives significantly inhibited TNF-alpha-induced phosphorylation of JNK. Results suggest that sulfonic acid esterification at 4'- and/or 7-position of daidzein can significantly improve its physicochemical and pharmaceutical properties, consequently the cellular uptake or absorption and ultimately the biological activities. (C) 2017 Elsevier Ltd. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据