Gadolinium complexes of diethylenetriamine-N-oxide pentaacetic acid-bisamide: a new class of highly stable MRI contrast agents with a hydration number of 3†,Dalton Transactions

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Gadolinium complexes of diethylenetriamine-N-oxide pentaacetic acid-bisamide: a new class of highly stable MRI contrast agents with a hydration number of 3†
Dalton Transactions ( IF 3.5 ) Pub Date : 2018-12-21 00:00:00 , DOI: 10.1039/c8dt04478c
BeiBei Zhang _{1,

2,

3,

4,

5} , Likun Cheng _{1,

2,

3,

4,

5} , Bing Duan _{4,

5,

6} , Weijun Tang _{4,

5,

7,

8} , Yuan Yuan _{4,

5,

6} , Yun Ding _{1,

2,

3,

4,

5} , Aiguo Hu _{1,

2,

3,

4,

5}

Affiliation

Complexes of gadolinium(III) have proven to be especially effective magnetic resonance imaging (MRI) contrast agents. One essential strategy to achieve more sensitive small-molecule gadolinium-based MRI contrast agents is to increase the hydration number q in order to improve the relaxivity. In this work, a series of diethylenetriamine-N-oxide pentaacetic acid-bisamide-based Gd(III) complexes with 3 coordinated water molecules have been synthesized, in which the hydration numbers are verified by luminescence measurements. Relaxivities of all the complexes are about triple of those commercial MRI contrast agents, ranging from 12.5 to 18.8 mM⁻¹ s⁻¹ (1.5 T; 25 °C). The formation constants of the Gd(III) complexes were calculated from potentiometric titration data at 25 °C using the HYPERQUAD program, which demonstrate superior stability over the commercial MRI contrast agent Gd-DTPA-BMA (Omniscan®). The kinetic inertness of the complexes was also higher than Omniscan® and comparable to another commercial MRI contrast agent Gd-DTPA (Magnevist®). Meanwhile, the viability of HeLa cells remained unaffected after the exposure to the complexes. The efficacy of these complexes as potential positive contrast agents in MRI was further evaluated using in vivo studies, and the complexes were found to exhibit superb positive contrast.

中文翻译：

二亚乙基三胺-N-氧化五乙酸-双酰胺复合物：水合值为3 †的一类新型高度稳定的MRI造影剂

proven （III）的配合物已被证明是特别有效的磁共振成像（MRI）造影剂。实现更敏感的基于小g的MRI造影剂的一种基本策略是增加水合数q，以提高松弛度。在这项工作中，合成了一系列带有3个配位水分子的二亚乙基三胺-N-氧化物五乙酸-双酰胺基Gd（III）配合物，其中的水合数通过发光测量来验证。所有复合物的弛豫度约为市售MRI造影剂的三倍，范围为12.5至18.8 mM ^-1 s ^-1（1.5 T； 25°C）。使用HYPERQUAD程序在25°C下由电位滴定数据计算出Gd（III）配合物的形成常数，该常数证明了其优于商用MRI造影剂Gd-DTPA-BMA（Omniscan®）的稳定性。配合物的动力学惰性也高于Omniscan®，可与另一种商用MRI造影剂Gd-DTPA（Magnevist®）相提并论。同时，暴露于复合物后，HeLa细胞的活力仍不受影响。使用体内研究进一步评估了这些复合物作为MRI中潜在的阳性对比剂的功效，发现该复合物表现出极好的阳性对比。

更新日期：2018-12-21

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