11种黄酮类化合物清除超氧阴离子的构效关系研究  

Study on structure-activity relationship of eleven natural flavonoids scavenging superoxide anion

作　　者：陈季武[1] 胡天喜[1] 朱大元[2] 

机构地区：[1]华东师范大学生命科学学院,上海200062 [2]中国科学院上海药物研究所,上海200031

出　　处：《中国药学杂志》2002年第1期57-58,共2页Chinese Pharmaceutical Journal

摘　　要：目的　研究了 11种高纯度的天然黄酮类化合物清除超氧阴离子 (O-·2 )的构效关系 ,试图找出某些规律 ,为其进一步开发利用提供参考依据。方法　采用高灵敏度的化学发光法。结果　 9种天然黄酮类化合物能有效地清除O-·2 ,其清除O-·2 能力大小顺序依次为 :黄芩苷 >泽漆新苷 >槲皮素 >芸香苷 >金丝桃苷 >山奈素 >甘草查尔酮 >橙皮苷 >石吊兰素 ,而川陈和补甲 Ac无效。结论　①A环上羟基和 /或B环上羟基是清除O-·2 2的主要活性基团 ;②A环上具有邻位羟基和 /或B环上具有邻位羟基可大大增强清除O-·2 能力 ;③A环上 6位羟基和B环上 3′、4′位羟基清除O-·2 的活性都很强 ;④糖苷对清除O-·2 也有贡献 ,其作用因糖苷种类而异 ;⑤酚羟基化合物往往具有清除O-·2 作用。OBJECTIVE: The structure-activity relationship of eleven pure and natural flavonoids scavenging superoxide anion (O2.-)were studied so as to find some regularities, which may provide the foundation for their further exploitation and utility. METHODS: The sensitive chemiluminescence system was used. RESULTS: Nine natural flavonoids effectively scavenged O2.-. The ability of scavenging O2.- in turn was: baicalin > heliosin > quercetin > rutin > hyperoside > kaempferol > licochalcone > hesperidin > nevadensin, whereas nobilitin and corylifolin-Ac did not scavenge O2.-. CONCLUSION: 1. Hydroxyl groups in the A ring and/or B ring were main active groups scavenging O2.-. 2. A ring and/or B ring with adjacent hydroxyl groups greatly increased their ability of scavenging O2.-. 3. The hydroxyl group in the 6 position on the A ring and the hydroxyl groups in 3′, 4′ position on the B ring possessed the high activity of scavenging O2.-. 4. The glucoside contributed to scavenge O2.-, which varied with sort of the glucoside. 5. The phenolic hydroxyl compounds usually have activity scavenging O2.-.

关 键 词：黄酮类化合物 构效关系 超氧阴离子 药物化学 

分 类 号：R914[医药卫生—药物化学]