Design, synthesis and biological evaluation of glucose-containing scutellarein derivatives as neuroprotective agents based on metabolic mechanism of scutellarin in vivo
Design, synthesis and biological evaluation of glucose-containing scutellarein derivatives as neuroprotective agents based on metabolic mechanism of scutellarin in vivo
复制标题
基于灯盏乙素体内代谢机制的含葡萄糖灯盏乙素衍生物神经保护剂的设计、合成及生物学评价
DOI：
10.1016/j.bmcl.2012.11.002
复制
发表时间：
2013-01-01
影响因子：
2.7
通讯作者：
Duan, Jian-Ao
中科院分区：
文献类型：
--
作者：
Li, Nian-Guang;Shen, Min-Zhe;Duan, Jian-Ao
基于灯盏花乙素在体内被β-葡萄糖苷酸酶水解为灯盏花乙素的代谢机制，通过糖苷键在灯盏花乙素C-7位引入葡萄糖部分，设计并合成了一些含葡萄糖的灯盏花乙素衍生物。生物活性评价表明，这些含葡萄糖的灯盏乙素衍生物表现出有效的DPPH自由基清除活性。此外，通过引入葡萄糖，还实现了抗凝和神经保护活性以及水溶性等理化性质的改善。这些发现表明，将葡萄糖部分引入到灯盏花素瓦特中进一步开发了此类化合物作为神经保护剂的作用。 (C) 2012 Elsevier Ltd. 保留所有权利。
Based on metabolic mechanism of scutellarin in vivo that scutellarin could be hydrolyzed into scutellarein by beta-glucuronide enzyme, some glucose-containing scutellarein derivatives were designed and synthesized through the introduction of glucose moiety at C-7 position of scutellarein via a glucosidic bond. Biological activity evaluation showed that these glucose-containing scutellarein derivatives exhibited potent DPPH radical scavenging activities. Furthermore, the improvement of physicochemical properties such as anticoagulant and neuroprotective activities alongside with the water solubility was achieved by introducing glucose. These findings suggest that the introduction of the glucose moiety to scutellarein wattants further development of this kind of compounds as neuroprotective agents. (C) 2012 Elsevier Ltd. All rights reserved.