有机化学 ›› 2016, Vol. 36 ›› Issue (4): 724-735.DOI: 10.6023/cjoc201510022 上一篇    下一篇

综述与进展

Ocotillol型皂苷的合成与生物活性研究进展

徐阳荣, 王文智, 杨静静, 李新利, 孟庆国   

  1. 烟台大学药学院 烟台 264005
  • 收稿日期:2015-10-19 修回日期:2015-11-10 出版日期:2016-04-25 发布日期:2015-12-10
  • 通讯作者: 孟庆国 E-mail:qinggmeng@163.com
  • 基金资助:

    国家自然科学基金(No.81473104)、山东省自然科学基金(No.ZR2012HM036)资助项目.

Advances in the Synthesis and Biological Activities of Ocotillol-Type Saponins

Xu Yangrong, Wang Wenzhi, Yang Jingjing, Li Xinli, Meng Qingguo   

  1. School of Pharmacy, Yantai University, Yantai 264005
  • Received:2015-10-19 Revised:2015-11-10 Online:2016-04-25 Published:2015-12-10
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 81473104), and the Natural Science Foundation of Shandong Province (No. ZR2012HM036).

Ocotillol型皂苷是一类侧链上含有四氢呋喃环的四环三萜类皂苷,主要存在于人参属植物中,并具有抗炎、抗菌、拮抗吗啡依赖、预防老年痴呆、保护心脑血管及神经系统等功效.天然存在的ocotillol型皂苷较少,近年来,已有较多20(S)-ocotillol型皂苷的半合成、以X射线衍射确证绝对构型、抗心肌缺血和代谢等研究报道,其中差向异构体的抗心肌缺血活性与代谢呈现立体选择性.综述了ocotillol型皂苷的分离、合成、绝对构型确证、药理活性、代谢等方面的研究进展.

关键词: ocotillol型皂苷, 合成, 绝对构型确证, 生物活性, 代谢

Ocotillol-type saponins are a kind of tetracyclic triterpenoid ginsenoside with a tetrahydrofuran ring in the side chain. Ocotillol-type saponins mainly exist in panax plants and possess anti-inflammatory, antibacterial, morphine-antagonis- tic, neuroprotective, cardioprotective effects, etc. There are less ocotillol-type saponins in natural plants. Recently, many studies on the semi-synthesis, absolute configuration confirmation using X-ray diffraction, effect of anti-myocardial ischemic and metabolism of 20(S)-ocotillol-type saponins have been reported. It was found that 24R-epimer and 24S-epimer had stereoselectivity in anti-ischemic effect and pharmacokinetics. In this paper, the advances of the separation, synthesis, absolute configuration confirmation, pharmacological activity, metabolism of ocotillol-type saponins are reviewed.

Key words: ocotillol-type ginsenoside, synthesis, absolute configuration confirmation, biological activities, metabolism