红景天苷衍生物的合成及其抗疲劳活性研究

Studies on the synthesis and anti-fatigue activity of the salidroside derivatives

目的设计并合成系列4-取代的新型红景天苷衍生物并研究其抗疲劳作用。方法通过五乙酰基葡萄糖与不同的4-取代苄基酪醇,经过糖苷化、脱乙酰基合成红景天苷衍生物;采用小鼠负重游泳为实验模型,通过观察测定小鼠的负重游泳时间研究合成衍生物的抗疲劳作用。结果合成了10个新型红景天苷衍生物;小鼠负重游泳实验显示:阳性对照组(红景天苷)和3a-1组(苯乙基-β-D-葡萄糖苷)的小鼠游泳时间明显高于空白对照组(P<0.05),差异有统计学意义;其余组均与空白对照组小鼠负重游泳时间相近,差异无统计学意义。结论本实验设计的红景天苷衍生物合成方法简便、可行;红景天苷及其衍生物苯环上的4位羟基可能与其抗疲劳活性密切相关。

Objective A series of 4 substituted salidroside derivatives were designed and synthesized.Their anti-fatigue effects were investigated.Methods With five-acetyl glucose and different 4-substituted benzyl tyrosols as the starting materials,salidroside derivatives were synthesized through glycosidation and deacetylation reactions.The exercise exhaustive mice model was used to study the anti-fatigue effects of those synthesized derivatives by comparing the loading swimming time of mice.Results 10 novel salidroside derivatives were synthesized.The loading swimming tests showed that the swimming time of the mice in the positive group（salidroside）and 3 a-1 group（phenethyl-β-D-glucoside）was longer than that in the control group with statistically significant difference（P〈0.05）.The swimming times for other groups were similar to control group with no statistically significant difference.Conclusion This synthetic method for salidroside derivatives was convenient and feasible for large production.The 4-hydroxyl groups on the benzene ring of salidroside and its derivatives may be the active site responsible for their anti-fatigue activity.