有机化学 ›› 2018, Vol. 38 ›› Issue (4): 919-925.DOI: 10.6023/cjoc201711016 上一篇    下一篇

研究论文

薯蓣皂苷元抗肿瘤衍生物的合成及其生物活性的研究

罗卓玛a, 胡越高a, 王璐红b, 尹祥健c, 马晓东b, 杨鸿均a, 赵志刚a   

  1. a 西南民族大学化学与环境保护工程学院 成都 610041;
    b 大连医科大学药学院 大连 116044;
    c 四川川大华西药业股份有限公司 成都 610014
  • 收稿日期:2017-11-08 修回日期:2018-01-05 出版日期:2018-04-24 发布日期:2018-01-18
  • 通讯作者: 杨鸿均 E-mail:yanghj@swun.cn
  • 基金资助:

    国家自然科学基金(No.21602083)、西南民族大学研究生创新型科研(No.CX2016SZ045)、四川省教育厅研究(No.15ZB0487)资助项目.

Study on the Synthesis and Bioactivity of Diosgenin Antitumor Derivatives

Luo Zhuomaa, Hu Yuegaoa, Wang Luhongb, Yin Xiangjianc, Ma Xiaodongb, Yang Hongjuna, Zhao Zhiganga   

  1. a College of Chemistry and Environmental Protection Engineering, Southwest University for Nationalities, Chengdu 610041;
    b College of Pharmacy, Dalian Medical University, Dalian 116044;
    c Sichuan Chuanda Huaxi Pharmaceutical Co., Ltd., Chengdu 610014
  • Received:2017-11-08 Revised:2018-01-05 Online:2018-04-24 Published:2018-01-18
  • Contact: 10.6023/cjoc201711016 E-mail:yanghj@swun.cn
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 21602083), the Southwest University for Nationalities Graduate Student Innovative Project (No. CX2016SZ045), and the Sichuan Provincial Department of Education Research Project (No. 15ZB0487).

以薯蓣皂苷元为先导物,设计并合成了9个新的薯蓣皂苷元含氮衍生物,其结构经过1H NMR,13C NMR,IR和HRMS鉴定.所有衍生物采用噻唑蓝(MTT)法进行抗肿瘤活性(A549,A431,H1975,HCT-116,Aspc-1,Ramos)的测定以及细胞毒性(HBE,LO-2)的研究.研究结果表明,大部分薯蓣皂苷元衍生物具有显著的抗肿瘤活性和低细胞毒性.

关键词: 薯蓣皂苷元, 衍生物, 抗肿瘤活性, 酰胺

Nine novel diosgenin derivatives were designed and synthesized by using diosgenin as a precursor. Their structures were identified by 1H NMR, 13C NMR, IR and HRMS. Antitumor activity (A549, A431, H1975, HCT-116, Aspc-1, Ramos) and cytotoxicity (HBE, LO-2) were measured for all derivatives using thiazolyl blue tetrazolium bromide (MTT). The results show that most diosgenin derivatives have significant anti-tumor activity and low cytotoxicity.

Key words: diosgenin, derivative, antitumor activity, amide