红景天苷衍生物的合成及其抗疲劳活性研究

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。...

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Published in药学实践杂志 Vol. 36; no. 1; pp. 61 - 63
Main Author 郑巍;曹旭芳;张开霞;孙亮;金永生;郭良君
Format Journal Article
LanguageChinese
Published 解放军98医院药械科 ,浙江湖州,313000%第二军医大学药学院有机化学教研室 ,上海,200433 2018
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ISSN1006-0111
DOI10.3969/j.issn.1006-0111.2018.01.012

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Summary: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。
Bibliography:salidroside;derivatives ;anti-fatigue
31-1685/R
ZHENG Wei1 ,CAO Xufang1 ,ZHANG Kaixia2 ,SUN Liang1 ,JIN Yongsheng2 ,GUO Liangjun1 (1 . Department of Drug and E-quipment ,No .98 Hospital of PLA ,Huzhou 313000 ,China ? 2 . Department of Organic Chemistry ,School of Pharmacy ,Second Military Medical University ,Shanghai 200433 ,China)
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 l
ISSN:1006-0111
DOI:10.3969/j.issn.1006-0111.2018.01.012