一种亲骨剂DO2A2P的反式和顺式异构体的对比研究。
A comparative study of trans- and cis-isomers of a bone-seeking agent, DO2A2P.
作者信息
Hao Guiyang, Liu Wei, Hassan Gedaa, Öz Orhan K, Kovacs Zoltan, Sun Xiankai
机构信息
Department of Radiology, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA.
Department of Radiology, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA; Institute of Crystal Materials, Shandong University, Jinan, Shandong, China.
出版信息
Bioorg Med Chem Lett. 2015 Feb 1;25(3):571-4. doi: 10.1016/j.bmcl.2014.12.016. Epub 2014 Dec 13.
The macrocyclic bone-seeking agent, DO2A2P, bears a cyclen core and two pairs of peripheral phosphonate and carboxylate groups. The geometric disposition of the peripheral functionalities gives arise to a pair of geometric isomers: cis-DO2A2P and trans-DO2A2P. In order to compare the biological behavior of the isomer pair, cis-DO2A2P was synthesized. Both isomers were successfully radiolabeled with (177)Lu, which might potentiate their applications in both radiotherapy and imaging of bone diseases. Through a set of biological assays including the hydroxyapatite binding, in vitro stability, and in vivo distribution, we demonstrated that the geometric pair of DO2A2P had virtually identical biological properties.
大环亲骨剂DO2A2P具有一个环烯核心以及两对外围膦酸酯和羧酸酯基团。外围官能团的几何排布产生了一对几何异构体：顺式-DO2A2P和反式-DO2A2P。为了比较这对异构体的生物学行为，合成了顺式-DO2A2P。两种异构体均成功用（177）Lu进行了放射性标记，这可能会增强它们在骨疾病放疗和成像中的应用。通过一系列生物学试验，包括羟基磷灰石结合、体外稳定性和体内分布，我们证明了DO2A2P的几何异构体对具有几乎相同的生物学特性。
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