一种作为肿瘤显像剂的五价锝-二巯基琥珀酸复合物的设计。

The design of a pentavalent 99mTc-dimercaptosuccinate complex as a tumor imaging agent.

作者信息

Yokoyama A, Hata N, Horiuchi K, Masuda H, Saji H, Ohta H, Yamamoto K, Endo K, Torizuka K

出版信息

Int J Nucl Med Biol. 1985;12(4):273-9. doi: 10.1016/0047-0740(85)90180-9.

Abstract

In our search for a technetium-tumor seeking agent, the chemical characteristic of polynuclear Ga-citrate attracted our attention. On this basis, we selected the ligand dimercaptosuccinic acid (DMS) and appropriate labeling conditions in the design of 99mTc(V)-DMS. Chemical characterization was performed by thin layer chromatography, electrophoresis, Sephadex column chromatography and spectrophotometric studies at the chemical concentration (99Tc). Biodistribution in mice bearing Ehrlich ascites tumor and scintigraphic images in VX-2 tumor-bearing rabbit, indicated the great applicability of 99mTc(V)-DMS as a new tumor imaging agent. Its distinctive characteristic, different from the kidney imaging agent (99mTc-DMSA) is demonstrated and the biological implication of hydrolytic polynucleation of pentavalent technetium, through an anionic specie Tc(V)O3-(4), in the tumor cell is discussed.

摘要

在寻找一种锝肿瘤靶向剂的过程中，多核柠檬酸镓的化学特性引起了我们的关注。在此基础上，我们在设计99mTc(V)-二巯基丁二酸（DMS）时选择了配体二巯基丁二酸（DMS）和合适的标记条件。通过薄层色谱、电泳、葡聚糖凝胶柱色谱以及在化学浓度（99Tc）下的分光光度研究进行化学表征。在荷艾氏腹水瘤小鼠中的生物分布以及在荷VX-2肿瘤兔中的闪烁图像表明，99mTc(V)-DMS作为一种新型肿瘤显像剂具有很大的适用性。展示了其与肾脏显像剂（99mTc-二巯基丁二酸）不同的独特特性，并讨论了五价锝通过阴离子物种Tc(V)O3-(4)在肿瘤细胞中的水解多核化的生物学意义。