黄酮葡萄糖硫苷分子的设计合成及其辐射防护活性评价

项目名称： 黄酮葡萄糖硫苷分子的设计合成及其辐射防护活性评价

项目编号： No.21272273

项目类型： 面上项目

立项/批准年度： 2013

项目学科： 数理科学和化学

项目作者： 彭涛

作者单位： 中国人民解放军军事医学科学院

项目金额： 80万元

中文摘要： 目前辐射防护药物发展缓慢，可用于临床的药物十分缺乏。清除自由基是治疗辐射损伤的关键，因此急需寻找和发现具有新结构特点的清除自由基活性分子。前期研究中我们发现一些合成的芳香葡萄糖硫苷化合物具有清除二苯基苦基苯肼自由基（DPPH）的作用，且可提高全身8Gy受照小鼠的存活率。此类硫苷的清除自由基活性与抗辐射活性具有相关性，其中清除DPPH自由基活性最强的S01可以提高小鼠的存活率达50%。为了进一步揭示此类葡萄糖硫苷分子清除自由基活性与抗辐射损伤活性的变化规律，并获得新的抗辐射损伤活性分子，我们提出用具有较强清除自由基和抗氧化作用的黄酮类结构取代芳香葡萄糖硫苷化合物中的芳香环部分,会增强其抗辐射损伤活性，并据此设计了四类新型的黄酮葡萄糖硫苷分子。本项目拟开展深入分子设计合成及评价研究，以揭示黄酮葡萄糖硫苷清除自由基与抗辐射损伤活性的变化规律，为创新抗辐射损伤药物研究提供理论和实验依据。

中文关键词： 葡萄糖硫苷；黄酮；辐射防护活性；设计；合成

英文摘要： Currently, there has been very little progress in the research of radioprotectants. The scavenging of free radical is the key point in treatment of radiation damage. So there is an urgent need to find new molecules with free radical scavenging activity and new structural features. In our former research work, some of synthesized aryl thioglucosides had showed 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity and could increase survival rate of 8Gy total body radiation mice. Scavenging free radical activity and antiradiation activity had showed interrelationships in these thioglucosides. The most potent free radical scavenger is S01 in these compounds and S01 can increase survival of the radiated mice to 50%. In order to reveal the relationship between antiradiation activity and free radical scavenging activity, we propose the ideal that substituting structure of flavonoids which usually have free radical scavenging activity and antioxidant activity for aryl in those compounds will improve new molecules' antiradiation activity dramatically. So four classes of novel thioglucosyl flavonoids are designed in this research project. The implementation of the project will provide the theoretical and experimental foundation for radioprotectant research.

英文关键词： thioglucoside；flavonoid；radioprotective activity；design；synthesis