同位素 ›› 2006, Vol. 19 ›› Issue (3): 156-161.DOI: 10.7538/tws.2006.19.03.0156

• 研究简报 • 上一篇    下一篇

利用γ-32P-ATP,51Cr研究蛋白激酶C对血管内皮细胞CD44表达及内皮粘附功能的影响 

郝一文;王佩侠;李亚明   

  1. 上海医药工业研究院药理室
  • 收稿日期:1900-01-01 修回日期:1900-01-01 出版日期:2006-05-20 发布日期:2006-05-20
  • 通讯作者: 郝一文

  1. (Department of Pharmacology, Shanghai Institute of
    Pharmaceutical Industry
  • Received:1900-01-01 Revised:1900-01-01 Online:2006-05-20 Published:2006-05-20

摘要: 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,制备氘、氚标记的aPPD。标记物经板层析(TLC)、质谱(MS)、核磁共振(NMR)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-aPPD作用于人肺腺癌A549细胞,检测不同时间细胞浆及细胞核中氚的活度,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。

关键词: 人参皂甙20(S)-protopanaxadiol(aPPD), 氘标记, 氚标记, 人肺腺癌A549细胞

Abstract: Abstract: 20(s)-protopanaxadiol is labeled with 2H and 3H, respectively. UV absorption spectrum and Rf of tritium labeled 20(s)-protopanaxadiol are the same as authentic sample. The radiochemical purity of 3H-aPPD is more than 95%, and the specific radioactivity is 1.57×108GBq/g. To study the character of aPPD on human lung cancer A549 cell line, the specific radioactivity of cytoplasm and nucleus are detected. It was shew that aPPD reached maximum concentration after 24h both 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. The present study can be served as the base for the further studies of its mechanisms.

Key words: ginsenoside, 20(s)-protopanaxadio, tritium, Ddeuterium, humanlungcancerA549cellline