Chin. J. Org. Chem. ›› 2011, Vol. 31 ›› Issue (05): 646-652. Previous Articles     Next Articles

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积雪草酸衍生物的合成与表征及体外抗癌活性的研究

赵龙铉*,1,2,田明珠1,金礼吉3贺兴隆1,沈平1张晓翠1,杨君微1   

  1. (1辽宁师范大学化学化工学院 大连 116029)
    (2辽宁师范大学生物技术与分子药物研发辽宁省重点实验室 大连 116029)
    (3大连理工大学环境与生命学院 大连 116029)
  • 收稿日期:2010-07-03 修回日期:2010-11-29 发布日期:2010-12-09
  • 通讯作者: 赵龙铉 E-mail:lxzhao@lnnu.edu.cn

Synthesis and Characterization of Derivatives of Asiatic Acid and Primary Study on Anti-cancer Activity

Zhao Longxuan*,1,2 Tian Mingzhu1 Jin Liji3 He Xinglong1 Shen Ping1 Zhang Xiaocui1 Yang Junwei1   

  1. (1 School of Chemistry and Chemical Engineering, Liaoning Normal University, Dalian 116029)
    (2 Liaoning Provincial Key Laboratory of Biotechnology and Drug Discov-ery, Liaoning Normal University, Dalian 116029)
    (3 School of Environmental & Biological Science & Technology, Dalian University of Technology, Dalian 116029)
  • Received:2010-07-03 Revised:2010-11-29 Published:2010-12-09
  • Contact: Zhao LongXuan E-mail:lxzhao@lnnu.edu.cn

In order to develop novel asiatic acid derivatives with high efficiency, low toxicity and good biological activity, we used natural product asiatic acid as the lead compound, which exhibits anti-cancer activity. Nine novel asiatic acid derivatives were designed and synthesized through modification of asiatic acid at C-2, C-3, C-11, C-23 and C-28. Structures of all target compounds were confirmed by 1H NMR, 13C NMR, IR and HRMS techniques. Their in vitro anti-cancer activities towards Hela cell and MCF-7 cell lines were evaluated by a MTT method and the results indicate that the anti-cancer activities of the synthesized asiatic acid derivatives were increased in comparison with asiatic acid.

Key words: asiatic acid, derivative, synthesis, characterization, anti-cancer