亲脂性取代基对含顺磁性金属离子的乙二胺四乙酸配合物生物学性质的影响。

The effect of lipophilic substituents on the biological properties of EDTA complexes containing paramagnetic metal ions.

作者信息

Baker R J, McLaren A B, Bellen J C, Penglis S

出版信息

Int J Rad Appl Instrum B. 1987;14(2):123-6. doi: 10.1016/0883-2897(87)90142-5.

Abstract

Complexes of the radioactive paramagnetic metal ions 51Cr(III), 54Mn(II), 59Fe(III), 57Co(II), 64Cu(II) and 153Gd(III) were prepared with EDTA and its derivative containing the lipophilic 1-(4-methylphenyl)-group (MPEDTA), together with the corresponding 99mTc-compounds. The formation of these complexes was verified by electrophoresis and they were screened for potential use as MRI hepatobiliary contrast agents by biodistribution studies in mice. In this series, the MPEDTA complexes of 54Mn(II) and 64Cu(II) showed increased urinary excretion compared to the unsubstituted EDTA complexes, while the MPEDTA complexes of 99mTc, 59Fe, 57Co, 153Gd and particularly 51Cr demonstrated improved hepatobiliary excretion. Further lipophilic substitution should enhance this property but the preparation of such ligands is complicated by cyclisation reactions.

摘要

用乙二胺四乙酸（EDTA）及其含亲脂性1-（4-甲基苯基）基团的衍生物（MPEDTA）制备了放射性顺磁性金属离子51Cr(III)、54Mn(II)、59Fe(III)、57Co(II)、64Cu(II)和153Gd(III)的配合物，以及相应的99mTc化合物。通过电泳验证了这些配合物的形成，并通过在小鼠体内的生物分布研究筛选它们作为磁共振成像（MRI）肝胆造影剂的潜在用途。在该系列中，与未取代的EDTA配合物相比，54Mn(II)和64Cu(II)的MPEDTA配合物显示出尿排泄增加，而99mTc、59Fe、57Co、153Gd尤其是51Cr的MPEDTA配合物表现出改善的肝胆排泄。进一步的亲脂性取代应会增强该性质，但此类配体的制备因环化反应而变得复杂。