Studies on the synthesis and anti-fatigue activity of the salidroside derivatives
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摘要: 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。Abstract: 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 3a -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.
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Key words:
- salidroside /
- derivatives /
- anti-fatigue
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[1] 肖妤,李绍平,王一涛.红景天苷药理研究进展[J].实用医院临床杂志,2006,3(3):98-99. [2] 张文生,朱陵群,牛福玲,等.红景天苷对缺氧/缺糖损伤神经细胞的保护作用[J].中国中药杂志,2004,29(5):459-462. [3] 宋月英,齐刚,李亚萍,等.红景天苷对全脑缺血再灌注损伤大鼠脑组织肿瘤坏死因子-α表达的影响[J].中草药,2006,37(6):907-908. [4] 盛长忠,元英进,姜燕.库页红景天的研究进展[J].中草药,2004,35(6):699-702. [5] 许建峰,应佩青.高山红景天资源应用与开发研究进展[J].中草药,1998,29(3):202-205. [6] 纪淑芳,周亚青.红景天甙的合成[J].沈阳药学院学报,1987,3(4):192-194. [7] 郭益冰,郑成,孟颖,等.红景天苷及其类似物的合成[J].南通大学学报(自然科学版),2009,8(4):29-35. [8] 徐利锋,曹迪,姜帆,等.红景天苷合成工艺[J].辽宁大学学报(自然科学版),2014,41(1):71-75. [9] 张翼轩,张昌浩,赵春晖,等.红景天苷的全合成[J].合成化学,2014,22(6):813-816. [10] 陈辉,崔颖,李灵芝.红景天苷类似物的合成[J].第三军医大学学报,2012,34(11):1057-1061. [11] 邓梅,吴振刚,刘雪英,等.红景天苷及其类似物的合成[J].第四军医大学学报,2007,28(16):1501-1502. [12] Li H,Li Q,Cai MS,et al. Synthesis of galactosyl and lactosyl derivatives as potential anti-metastasis compounds[J]. Carbohydr Res,2000,328(4):611-615. [13] Kanth J V B,Periasamy M. Selective reduction of carboxylic acids into alcohols using sodium borohydride and iodine[J]. J Organ Chem,1991,56(20):5964-5965. [14] 谭兴起,郭良君,孔飞飞,等.络石藤三萜总皂苷抗疲劳作用的实验研究[J].解放军药学学报,2011,27(2):128-131. [15] 张俊,吴振刚,王庆伟,等.红景天苷系列类似物的设计合成及抗疲劳活性初筛[J].第四军医大学学报,2009,30(19):1916-1918. -
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