综述与进展

银杏内酯衍生物和类似物的合成及PAFR和GlyR拮抗活性研究进展

  • 惠爱玲 ,
  • 吴泽宇 ,
  • 袁媛 ,
  • 周安 ,
  • 潘见
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  • a 合肥工业大学天然药物研究所 合肥 230009;
    b 安徽中医学院 安徽省中药研究与开发重点实验室 合肥 230038

收稿日期: 2012-09-20

  修回日期: 2012-12-19

  网络出版日期: 2012-12-25

基金资助

安徽省科技计划(No.11010401025)资助项目.

Progress in Synthesis and Antagonistic Activities towards PAFR and GlyR of Ginkgolide Derivatives and Analogs

  • Hui Ailing ,
  • Wu Zeyu ,
  • Yuan Yuan ,
  • Zhou An ,
  • Pan Jian
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  • a Institute of Natural Medicine, Hefei University of Technology, Hefei 230009;
    b Anhui Province Key Laboratory of Research and Development of Chinese Medicine, Anhui University of Traditional Chinese Medicine, Hefei 230038

Received date: 2012-09-20

  Revised date: 2012-12-19

  Online published: 2012-12-25

Supported by

Project supported by the Science and Technology Project of Anhui Province (No.11010401025).

摘要

银杏内酯是从银杏树中分离的二萜内酯成分, 它的结构是由6个五元环形成的笼状骨架并嵌有一个独特的叔丁基.研究已证实银杏内酯是血小板活化因子受体(PAFR)和甘氨酸受体(GlyR)的强有力拮抗剂, 它的结构变化将引起生物活性的改变.因此, 为了寻找更优的PAFR和GlyR拮抗剂, 人们合成了许多银杏内酯衍生物及类似物.重点综述了近年来银杏内酯类化合物的构效关系研究.

本文引用格式

惠爱玲 , 吴泽宇 , 袁媛 , 周安 , 潘见 . 银杏内酯衍生物和类似物的合成及PAFR和GlyR拮抗活性研究进展[J]. 有机化学, 2013 , 33(06) : 1263 -1272 . DOI: 10.6023/cjoc201209028

Abstract

Ginkgolides are diterpene trilactones with a cage-like skeleton consisting of six five-membered rings and a unique t-Bu group from Ginkgo biloba tree.Many studies have demonstrated that they are highly potent and selective antagonists of platelet activating factor receptor (PAFR) and glycine receptor (GlyR).Ginkgolide skeleton modifications may conduce to physiological activities variation.Therefore, many ginkgolide derivatives and analogs have been synthesized for the optimal antagonistic activities towards PAFR or GlyR.This review covers the structure-activity relationship studies of ginkgolide derivatives and analogs.

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