高等学校化学学报

高等学校化学学报

• 研究论文 • 上一篇    下一篇

β-榄香烯-TEG-Re(CO)3配合物的合成、放射性标记及初步生物活性

任云峰1,2, 刘贵锋1,2, 孙艳红1, 沈玉梅1   

    1. 中国科学院上海应用物理研究所放射药物研究中心, 上海 201800;
    2. 中国科学院研究生院, 北京 100049
  • 收稿日期:2008-01-29 修回日期:1900-01-01 出版日期:2008-09-10 发布日期:2008-09-10
  • 通讯作者: 沈玉梅

Synthesis, Radiolabelling and Preliminary Bioactivity of β-Elemene-TEG-Re(CO)3 Complex

REN Yun-Feng1,2, LIU Gui-Feng1,2, SUN Yan-Hong1, SHEN Yu-Mei1

  

    1. Radiopharmaceutical Centre, Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai 201800, China;
    2. Graduate School of the Chinese Academy of Sciences, Beijing 100049, China
  • Received:2008-01-29 Revised:1900-01-01 Online:2008-09-10 Published:2008-09-10
  • Contact: SHEN Yu-Mei

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摘要： 以中草药有效成分β-榄香烯为起始原料, 经烯丙位的氯代反应及亲核取代反应, 成功地合成一种含水溶性基团TEG的三齿吡啶螯合剂, 并与稳定的三羰基铼配位, 得到了一种新的三羰基铼配合物, 在此基础上利用铼的放射性同位素Re-188进行了放射性标记. 反应中间体及最终化合物分别用IR, 1H NMR, HRMS, HPLC或元素分析等技术进行表征, 并对该化合物进行了初步的体外抗癌活性研究. β-Elemene-TEG-Re(CO)3配合物的合成、放射化学合成及体外抗癌活性评价, 为探讨榄香烯体内靶点和作用机制提供了可能, 并为最终开发基于β-榄香烯的放射性药物奠定了基础.

关键词: β-榄香烯, 三羰基铼, Re-188, 放射性标记, 生物活性

Abstract: β-Elemene, (5S,7R,10S)-(-)-(1-methyl-1-vinyl-2,4-diisopropenyl-cyclohexane) is an anti-cancer agent from the Traditional Chinese Herb Medicinal. Accordingly, we synthesized β-Elemene-TEG-Re(CO)3 complexe and evaluated it as a potential radiopharmaceuticals. The structures and properties of the intermediate were indentified via IR, 1H NMR and HRMS. Good radioactive yield(above 90%) and radioactive chemical purity with Re-188(above 97%) were obtained. The antiproliferative activity of non-radioactive β-Elemene-TEG-Re(CO)3 derivatives on LLC and Hela cell lines were evaluated by WST-1 methods. The result shows a substantial decrease of IC50 values compared with that of the parent compound β-elemene.

Key words: β-Elemene, Re(CO)3, Re-188, Radiolabelling, Bioactivity

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