葛根素衍生物的合成及抗缺氧活性研究  

Synthesis of puerarin derivatives and their anti-hypoxic effects

作　　者：张首国[1] 王林[1] 朱晓伟[1] 彭涛[1] 温晓雪[1] 

机构地区：[1]军事医学科学院放射与辐射医学研究所,北京100850

出　　处：《中国药物化学杂志》2008年第2期90-95,共6页Chinese Journal of Medicinal Chemistry

基　　金：国家自然科学基金项目(30472081);北京市自然科学基金项目(7012030)

摘　　要：目的设计并合成新的葛根素衍生物。方法针对葛根素水溶性差的缺点,在其4′位羟基引入烷胺基烷基,得到新的葛根素衍生物。通过小鼠抗缺氧试验和离体动脉条试验,评价了目标化合物的抗缺氧活性和扩血管活性。结果与结论合成了12个新的葛根素衍生物,初步药理实验结果显示,大多数化合物的抗缺氧活性等于或略强于葛根素,化合物P1、P2、P4、P5和P6均具有明显的扩血管活性,活性随剂量增加而增大,其中P1和P2扩血管活性强于葛根素。Aim To design and synthesize new derivatives of puerarin. Methods Target compounds were designed to improve the water-solubility of puerarin, whose 4＇-hydroxy were substituted by alkyl-amino-alkyl groups. The anti-hypoxic effects of the target compounds were evaluated in mice, and their vasodilator effects were evaluated in the trial on rat isolated aortic rings. Results and conclusion 12 Target compounds were synthesized. The results of primary pharmacological tests indicate that the anti-hypoxic effects of most compounds are equal to or slightly stronger than that of puerarin. Five compounds（P1, P2, P4, P5 and P6） have significant dosage-dependent vasodilator effects and the effects of P1 and P2 are stronger than that of puerarin.

关 键 词：葛根素 衍生物 合成 抗缺氧 

分 类 号：R284[医药卫生—中药学] R285[医药卫生—中医学]