β-榄香烯三羰基铼配合物的合成、放射化学合成及抗癌活性研究

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在β-榄香烯母体上成功地引入含吡啶基的三齿螯合剂, 并与稳定的三羰基铼配位, 得到了一种新的铼(I)三齿配合物, 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-榄香烯三羰基铼配合物的合成、放射化学合成及体外抗癌活性评价, 为探讨β-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.

Synthesis,Radiosynthesis and Anticancer Activity of β-Elemene Tricarbonyl Rhenium Complex

Starting from the Traditional Chinese Medicine β-elemene, a new kind of β-elemene tricarbonyl rhenium complex was prepared via halogenation and nucleophilic substitution reactions, followed by reaction with tricarbonyl rhenium. Under the similar reaction conditions, the radioactive β-elemene tricarbonyl rhenium complex was synthesized. All the compounds were characterized by IR, ¹H NMR, HRMS, HPLC or elemental analysis. The anticancer activity of the target compound was observed in Hela and LLC lines in vitro. The β-elemene tricarbonyl rhenium complex provides the possibility to explore the anticancer mechanism of β-elemene and furthermore find a new kind of radiopharmaceuticals on basis of β-elemene.