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  • 标题:Design, Preparation and Studies Regarding Cytotoxic Properties of Glycyrrhetinic Acid Derivatives
  • 本地全文:下载
  • 作者:Qing-Xuan Zheng ; Rui Wang ; Yan Xu
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2020
  • 卷号:43
  • 期号:1
  • 页码:102-109
  • DOI:10.1248/bpb.b19-00615
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:Glycyrrhetinic acid (GA) is a natural product with certain antitumor activity. In order to enhance the cytotoxicity, a total of eighteen derivatives of GA were designed and synthesized. Their cytotoxicity against MDA-MB-231cells (human breast cancer cells) and HeLa cells (human cervical cancer cells), were evaluated by the MTT method (3-(4,5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide). The results indicated that these target compounds have a wide molar activity range and some of them show better activity than the commercial drugs gefitinib and doxorubicin. Compound 6g induces apoptosis of 7, 10 and 44% of MDA-MB-231 cells at 5, 10, and 20 µM, respectively.
  • 关键词:glycyrrhetinic acid;cytotoxicity;MDA-MB-231;apoptosis
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