γ-硫脲基丙基锗倍半硫化物的合成,~(99)Tc~m标记及生物分布研究

    SYNTHESIS, ~(99)Tc~m-LABELED AND BIODISTRIBUTION STUDY OF γ-THIOUREIDOPROPYL GERMANIUM SESQUISULFIDE

    • 摘要: 合成了γ 硫脲基丙基锗倍半硫化物 ,进行了99Tcm的标记 ,在配体量为 0 5mg,SnCl2 量为 0 .1mg ,pH =8.0 ,反应温度为 2 0℃ ,反应时间为 2 0min时 ,标记率可达 84 2 %。配合物在小鼠体内的生物分布实验结果表明 ,配合物主要浓集在肺中 ,其次是肝脏。在标记物质量浓度为 5 0 μg/mL时 ,测得它对KB(人鼻咽癌 ) ,HCT(人结肠癌 )和Bel(人肝癌 )细胞的抑制率分别为 69 0 % ,76 9% ,4 4 7%。

       

      Abstract: A new organogermanium sesquisulfide is synthesized and identified by IR spectrum and elemental analysis method.The new compound is labeled by 99Tc m and the labeling yield is 84.2% under the best condition (ligand, 0.5 mg; SnCl 2, 0.1 mg; pH≈8.0; reaction temperature, 20 ℃; reaction time, 20 min). The biodistribution experiments in mice of the 99Tc m labeled compound show that it is mainly concentrated in lung,next in liver.When the mass concentration of the labeled compound is 50 μg/mL,its antitumor activity against KB,HCT and Bel cells in vitro is 69.0%,76.9% and 44.7%,respectively.

       

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