Yang Wenjiang, Mou Tiantian, Zhang Xianzhong, Wang Xuebin
Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
Appl Radiat Isot. 2010 Jan;68(1):105-9. doi: 10.1016/j.apradiso.2009.09.015. Epub 2009 Sep 15.
A novel bifunctional coupling agents-biomolecular compound DMP-NGA was prepared by coupling the SATP with galactosyl-neoglycoalbumin (NGA). The DMP-NGA was labeled with technetium-99m, and the radiochemical purity in excess of 98% after purified with HPLC. In vivo biodistribution showed that (99m)Tc-DMP-NGA had very high initial liver uptake with good retention. The liver accumulated 99.35+/-9.77%, 74.25+/-3.03%, 52.47+/-7.58% of the injected dose per gram at 5, 30 and 120min after injection, respectively. It had relative higher initial liver uptake and much lower blood uptake than that of (99m)Tc-GSA. The liver/blood ratio reached 83.4 at 30min post-injection, while the ratio of liver/kidney was 14.4. The uptakes in other organs in the abdomen were also slightly low. In addition, the hepatic uptake of (99m)Tc-DMP-NGA was blocked by preinjecting free GSA as blocking agent. The result indicates that (99m)Tc-DMP-NGA has specific binding to ASGP receptor. Images acquired with Kodak In-Vivo Imaging System FX Pro showed significant difference before and after inhibition. The promising biological properties of (99m)Tc-DMP-NGA afford potential applications in liver receptor imaging for assessment of hepatocyte function.
通过将SATP与半乳糖基新糖白蛋白（NGA）偶联，制备了一种新型双功能偶联剂-生物分子化合物DMP-NGA。用99m锝标记DMP-NGA，经高效液相色谱纯化后放射化学纯度超过98%。体内生物分布显示，99mTc-DMP-NGA具有非常高的初始肝脏摄取率且滞留良好。注射后5、30和120分钟时，肝脏每克分别累积注射剂量的99.35±9.77%、74.25±3.03%、52.47±7.58%。与99mTc-GSA相比，它具有相对较高的初始肝脏摄取率和低得多的血液摄取率。注射后30分钟时肝/血比达到83.4，而肝/肾比为14.4。腹部其他器官的摄取也略低。此外，预先注射游离GSA作为阻断剂可阻断99mTc-DMP-NGA的肝脏摄取。结果表明，99mTc-DMP-NGA与ASGP受体具有特异性结合。用柯达体内成像系统FX Pro采集的图像显示抑制前后有显著差异。99mTc-DMP-NGA有前景的生物学特性为评估肝细胞功能的肝脏受体成像提供了潜在应用。
