Radiopharmaceutical Unit, National Centre of Sciences and Nuclear Technology, Sidi Thabet 2020, Tunisia.
Nucl Med Biol. 2010 Oct;37(7):821-9. doi: 10.1016/j.nucmedbio.2010.04.139.
A technetium-99m-labeled derivative from sulfanilamide, further referred to as (99m)Tc-N-SFC, targeting infections in experimental animals, has been synthesized. The biological features of this radioactive agent have also been studied. The N-sulfanilamide ferrocene carboxamide (N-SFC) was chemically synthesized and then labeled with technetium-99m. It has been confirmed through this work that it is stable and obtained with radiolabelling yield (>87%). Radiochemical analyses of (99m)Tc-N-SFC revealed that the molecule was labeled rapidly (within 2 min) and effectively with little free pertechnetate in the preparations containing purified compound. Furthermore, in vitro investigations were conducted and the label's stability in serum was observed up to 24 h of testing. Uptake of the tracer with live and heat/killed bacteria was compared in physiological conditions and was about 69% and 61.9% for the Escherichia coli and Staphylococcus aureus strains, respectively. We concluded that synthesis and labeling of Sulfanilamide derivative with (99m-)Tc by this method is rapid, efficient and safe. Biodistribution studies demonstrated that our radiolabeled compound is accumulated rapidly and significantly (P<.05) at infection sites. The comparison of the (99m)Tc-N-SFC accumulation at sites of S. aureus-infected animals, which is expressed as target-to-non-target ratio, (2.88 ± 0.10) with other radiotracers was discussed.
一种基于磺胺的锝-99m 标记衍生物,进一步称为(99m)Tc-N-SFC,用于靶向实验动物的感染,已被合成。该放射性药物的生物学特性也已被研究。通过化学合成 N-磺胺甲恶唑铁羧酰胺(N-SFC),然后用锝-99m 标记。通过这项工作证实,它是稳定的,放射性标记产率(>87%)。(99m)Tc-N-SFC 的放射化学分析表明,该分子在 2 分钟内快速(<2 min)有效地进行标记,且在含有纯化化合物的制剂中几乎没有游离的过锝酸盐。此外,还进行了体外研究,观察到标记物在血清中的稳定性长达 24 小时。在生理条件下比较了活细菌和热/死细菌对示踪剂的摄取,大肠杆菌和金黄色葡萄球菌的摄取率分别约为 69%和 61.9%。我们得出结论,通过这种方法合成和标记磺胺衍生物与(99m)Tc 是快速、高效和安全的。生物分布研究表明,我们的放射性标记化合物在感染部位迅速且显著(P<.05)积累。还讨论了(99m)Tc-N-SFC 在金黄色葡萄球菌感染动物部位的积累情况,以靶标与非靶标比值(2.88 ± 0.10)与其他放射性示踪剂进行了比较。