人参皂甙20（S）-protopanaxadiol的^2H、^3H标记及其在A549细胞内的浓度

Perparation of Labeled 20 （S）-protopanaxadiol With ^3 H and 3H and Its Concentration in A549 Cell Line

分别用钠硼氘、钠硼氚还原人参皂甙Rh1的活性形式20(S)-protopanaxadiol(aPPD)的氧化前体aPPD=O,制备2H3、H标记的aPPD。标记物经薄层层析(TLC)、质谱(MS)、核磁共振(1HNMR)分析鉴定,结果与标准品的测量数据一致;氚标记的aPPD放化纯度为98%,放射性比活度为7.64×1011Bq/g。将3H-aP-PD作用于人肺腺癌A549细胞,检测不同时间细胞浆及细胞核中3H的活度,结果提示aPPD在A549细胞浆、核内均于24 h达到最高浓度,表明aPPD作为一个与甾体类激素结构相类似的药物,可以进入细胞甚至细胞核发挥药理作用。

20（s）-protopanaxadiol is labeled with 2H and ^3H, respectively. UV absorption spectrum and Rf of ^2H labeled 20（s）-protopanaxadiol are the same as stand and product. The radiochemical purity of ：^3H-aPPD is 98%, and the specific radioactivity is 7.64× 10^11 Bq/g. To study the character of aPPD on human lung cancer A549 cell line, the specific ra dioactivity of cytoplasm and nucleus are detected. The resuls show that aPPDreached maximum concentration after 24 hboth in cytoplasm and nucleus. The results provide the direct evidence that aPPD, which structure looks like the steroid, can enter the nucleus to play its pharmacological effects.