高等学校化学学报

高等学校化学学报 ›› 2000, Vol. 21 ›› Issue (9): 1399.

• 论文 • 上一篇    下一篇

多羟基甾醇的合成及其结构与抗肿瘤细胞活性关系研究

崔建国1,3, 曾陇梅1, 苏镜娱1, 彭文烈2, 徐安龙2   

  1. 1. 中山大学化学与化学工程学院;
    2. 中山大学生命科学院, 广州 510275;
    3. 广西师范学院化学系, 南宁 530001
  • 收稿日期:1999-08-21 出版日期:2000-09-24 发布日期:2000-09-24
  • 通讯作者: 苏镜娱(1930年出生),女,教授,博士生导师,主要从事天然产物化学研究.
  • 基金资助:

    国家自然科学基金(批准号:29932030);广东省自然科学基金(批准号:970154)资助

Synthesis of Some Polyhydroxysterols and Investigation of Relationship Between Their Structure and Cytotoxicity

CUI Jian-Guo1,3, ZENG Long-Mei1, SU Jing-Yu1, PENG Wen-Lie2, XU An-Long2   

  1. 1. Schoolof Chemistryand Chemical Engineering, Zhongshan University, Guangzhou 510275, China;
    2. Schoolof Life Science, Zhongshan University, Guangz hou 510275, China;
    3. Depa rtment of Chemistry, Guangx i Teachers College, Nanning 530001, China
  • Received:1999-08-21 Online:2000-09-24 Published:2000-09-24

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被引次数

26

摘要： 报道了6个具有类似结构的多羟基甾醇的合成和它们的抗肿瘤细胞活性.发现此类化合物的细胞毒性与其分子中双键存在与否有着密切关系.当甾核或支链中双键被饱和时,其细胞毒性均明显降低.甾醇(5)和(8)对胃癌(MGC)、宫颈癌(HELA)细胞的生长具有一定的抑制作用.

关键词: 多羟基甾醇, 甾醇合成, 细胞毒性, 构效关系

Abstract: In this paper, we have prepared six analogues of 24-methylenecholest-4-en-3β,6β-diol(1) and investigated the relationships between the biological activity and their structures. The results showed that the double bond in the molecule played an impor tant role to the cytotoxicity of these polyhydroxysterols. Their cytotoxicity reduced obviously while the double bond in steroidal nucleus or side-chain was saturated. Compounds 5 and 8 showed a moderate cytotoxic activity against human gastric carcinoma cells(MGC) and cervical carcinoma cells(HELA).

Key words: Polyhydroxysterols, Synthesis of sterols, Cytotoxicity, Structure activity relationship

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