Chem. J. Chinese Universities ›› 2012, Vol. 33 ›› Issue (04): 750.doi: 10.3969/j.issn.0251-0790.2012.04.019

• Organic Chemistry • Previous Articles     Next Articles

Synthesis of A-Ring Functional Derivatives of 18β-Glycyrrhetinic Acid and Their Antiproliferative Effect in Tumor Cells

GAO Zhen-Bei1, HU Jun2, KANG Xiao1, XU Chuan-Lian1, JU Yong2   

  1. 1. College of Life Science, Zhejiang Sci-Tech University, Hangzhou 310018, China;
    2. Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology, Ministry of Education, Department of Chemistry, Tsinghua University, Beijing 100084, China
  • Received:2011-05-06 Online:2012-04-10 Published:2012-04-10
  • Supported by:

    浙江省自然科学基金(批准号: Y4110320)、浙江省生物医学工程"重中之重"学科开放基金(批准号: SWYX0901)和国家自然科学基金(批准号: 20972086)资助.

Abstract: Thirteen analogues of 18β-glycyrrhetinic acid were synthesized using various chemical methods and one of them exhibited certain cytotoxicity against cell-lines of HL60 cells, K562 cells, BEL-7404 cells and MDA-MB-231, respectively, via MTT method. The results show that compound 5 with C=C bond in the A-ring of 18β-glycyrrhetinic acid has markedly antiproliferative effect on these four tumor cells compared with 18β-glycyrrhetinic acid. K562 cells with nuclear apoptotic bodies were observed after staining with Hoechst 33258 and AO/EB with flourescence microscope.

Key words: 18β-Glycyrrhetinic acid, Chemical modification, A-Ring functional derivative, Antiproliferative effect

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