Amartey J K, Esguerra C, Al-Otaibi B, Al-Jammaz I, Al-Qahtani M, Parhar R S
Cyclotron and Radiopharmaceuticals Department, King Faisal Specialist Hospital and Research Centre, MBC-03, P.O. Box 3354, Riyadh 11211, Kingdom of Saudi Arabia.
Appl Radiat Isot. 2005 Jan;62(1):39-47. doi: 10.1016/j.apradiso.2004.06.006.
Numerous molecular entities with diverse structures have been radiolabeled and investigated as potential infection and inflammation detection agents. However, none of these molecules have gained the acceptance of gallium citrate or radiolabeled autologous white blood cells. We have radioiodinated interleukin-8 using two different methods and tested the biological behavior of the products in mice. As expected, the direct radioiodinated material displayed extensive in vivo deiodination. The use of pyridine-based prosthetic label yielded a product with better kinetics than the direct radioiodination method and showed a better target to non-target ratio. Nonetheless, this method is not suited for labeling of bioactive peptides such as the title peptide because of the very high specific activity required to prevent cytotoxic effects in a human application.
许多结构各异的分子实体已被放射性标记,并作为潜在的感染和炎症检测剂进行了研究。然而,这些分子中没有一种能获得枸橼酸镓或放射性标记的自体白细胞那样的认可。我们使用两种不同方法对白细胞介素-8进行了放射性碘化,并在小鼠体内测试了产物的生物学行为。正如预期的那样,直接放射性碘化的物质在体内表现出广泛的脱碘作用。使用基于吡啶的辅助标记产生的产物比直接放射性碘化方法具有更好的动力学,并且显示出更好的靶标与非靶标比率。尽管如此,由于在人体应用中防止细胞毒性作用所需的比活度非常高,这种方法不适用于标记诸如标题肽这样的生物活性肽。