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首页> 外文期刊>Journal of biological inorganic chemistry: JBIC: a publication of the Society of Biological Inorganic Chemistry >A new ditopic Gd~(III) complex functionalized with an adamantyl moiety as a versatile building block for the preparation of supramolecular assemblies
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A new ditopic Gd~(III) complex functionalized with an adamantyl moiety as a versatile building block for the preparation of supramolecular assemblies

机译：一种新型的双价Gd〜（III）配合物，其功能为金刚烷基部分，作为制备超分子组装体的通用构建基块

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摘要

A dimeric GdAAZTA-like complex (AAZTA is 6-amino-6-methylperhydro-1,4-diazepinetetraacetic acid) bearing an adamantyl group (Gd_2L1) able to form strong supramolecular adducts with specific hosts such as β-cyclodextrin (β-CD), poly-β-CD, and human serum albumin (HSA) is reported. The relaxometric properties of Gd_2L1 were investigated in aqueous solution by measuring the ~1H relaxivity as a function of pH, temperature, and magnetic field strength. The relaxivity of Gd_2L1 (per Gd atom) at 40 MHz and 298 K is 17.6 mM~(-1) s~(-1), a value that remains almost constant at higher fields owing to the great compactness and rigidity of the bimetallic chelate, resulting in an ideal value for the rotational correlation time for high-field MRI applications (1.5-3.0 T). The noncovalent interaction of Gd_2L1 with β-CD, poly-β-CD, and HSA and the relaxometric properties of the resulting host-guest adducts were investigated using ~1H relaxometric methods. Relaxivity enhancements of 29 and 108 % were found for Gd_2L1-β-CD and Gd_2L1-poly-β-CD, respectively. Binding of Gd2L1 to HSA (K_A = 1.2 × 10~4 M~(-1)) results in a remarkable relaxivity of 41.4 mM~(-1) s~(-1) for the bound form (+248 %). The relaxivity is only limited by the local rotation of the complex within the binding site, which decreases on passing from Gd_2L1-β-CD to Gd_2L1-HSA. Finally, the applicability of Gd_2L1 as tumortargeting agent through passive accumulation of the HSAbound adduct was evaluated via acquisition of magnetic resonance images at 1 T of B16-tumor-bearing mice. These experiments indicate a considerable signal enhancement (+160 %) in tumor after 60 min from the injection and a very low hepatic accumulation.
机译：带有金刚烷基（Gd_2L1）的二聚体GdAAZTA样复合物（AAZTA是6-氨基-6-甲基过氢-1,4-二氮杂四乙酸），能够与诸如β-环糊精（β-CD）的特定主体形成强超分子加合物，poly-β-CD和人血清白蛋白（HSA）的报道。通过测量〜1H弛豫度随pH，温度和磁场强度的变化，研究了Gd_2L1在水溶液中的弛豫特性。 Gd_2L1（每个Gd原子）在40 MHz和298 K时的弛豫率为17.6 mM〜（-1）s〜（-1），由于双金属螯合物的紧密性和刚度大，该值在较高的场上几乎保持恒定，从而为高场MRI应用（1.5-3.0 T）产生了理想的旋转相关时间。使用〜1H弛豫法研究了Gd_2L1与β-CD，聚β-CD和HSA的非共价相互作用以及所得主客体加合物的弛豫特性。发现Gd_2L1-β-CD和Gd_2L1-poly-β-CD的弛豫度分别提高了29％和108％。 Gd2L1与HSA的结合（K_A = 1.2×10〜4 M〜（-1））导致结合形式（+248％）的弛豫率为41.4 mM〜（-1）s〜（-1）。弛豫性仅受结合位点内复合物的局部旋转限制，该旋转在从Gd_2L1-β-CD传递至Gd_2L1-HSA时降低。最后，通过采集B16荷瘤小鼠的1 T磁共振图像，评估了Gd_2L1通过HSA结合加合物的被动积累作为肿瘤靶向剂的适用性。这些实验表明，从注射开始60分钟后，肿瘤中的信号明显增强（+160％），并且肝堆积非常低。

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