选定的镓-68和锆-89标记的铁载体的体外和体内比较
In Vitro and In Vivo Comparison of Selected Ga-68 and Zr-89 Labelled Siderophores.
作者信息
Petrik Milos, Zhai Chuangyan, Novy Zbynek, Urbanek Lubor, Haas Hubertus, Decristoforo Clemens
机构信息
Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry, Palacky University, Hnevotinska 5, CZ-77900, Olomouc, Czech Republic.
Clinical Department of Nuclear Medicine, Medical University Innsbruck, Innsbruck, Austria.
出版信息
Mol Imaging Biol. 2016 Jun;18(3):344-52. doi: 10.1007/s11307-015-0897-6.
PURPOSE
Some [(68)Ga]siderophores show promise in specific and sensitive imaging of infection. Here, we compare the in vitro and in vivo behaviour of selected Ga-68 and Zr-89 labelled siderophores.
PROCEDURES
Radiolabelling was performed in HEPES or sodium acetate buffer systems. Radiochemical purity of labelled siderophores was determined using chromatography. Partition coefficients, in vitro stability and protein binding affinities were determined. Ex vivo biodistribution and animal imaging was studied in mice.
RESULTS
Certain differences among studied siderophores were observed in labelling efficiency. Protein binding and stability tests showed highest stabilities and lowest protein binding affinities for Ga-68 and [(89)Zr]triacetylfusarinine C (TAFC). All studied Ga-68 and [(89)Zr]siderophores exhibited a similar biodistribution and pharmacokinetics in mice with the exception of [(89)Zr]ferrioxamine E (FOXE).
CONCLUSIONS
Zr-89 and [(68)Ga]siderophores showed analogous in vitro and in vivo behaviour. Tested [(89)Zr]siderophores could be applied for longitudinal positron emission tomography (PET) studies of fungal infections and especially TAFC for the development of novel bioconjugates.
目的
某些[（68）镓]铁载体在感染的特异性和灵敏成像方面显示出前景。在此，我们比较了选定的镓 - 68和锆 - 89标记的铁载体的体外和体内行为。
程序
在HEPES或醋酸钠缓冲系统中进行放射性标记。使用色谱法测定标记铁载体的放射化学纯度。测定分配系数、体外稳定性和蛋白质结合亲和力。在小鼠中研究了体内生物分布和动物成像。
结果
在所研究的铁载体之间观察到标记效率存在某些差异。蛋白质结合和稳定性测试表明，镓 - 68和[（89）锆]三乙酰fusarinine C（TAFC）具有最高的稳定性和最低的蛋白质结合亲和力。除了[（89）锆]去铁胺E（FOXE）之外，所有研究的镓 - 68和[（89）锆]铁载体在小鼠中均表现出相似的生物分布和药代动力学。
结论
锆 - 89和[（68）镓]铁载体在体外和体内表现出类似的行为。经测试的[（89）锆]铁载体可用于真菌感染的纵向正电子发射断层扫描（PET）研究，特别是TAFC可用于新型生物共轭物的开发。
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