在杯[4]芳烃支架上具有快速水交换的密集包裹的 Gd(III)-螯合物：一种有潜力的 MRI 造影剂。

Densely packed Gd(III)-chelates with fast water exchange on a calix[4]arene scaffold: a potential MRI contrast agent.

机构信息

Biocatalysis and Organic Chemistry, Department of Biotechnology, Delft University of Technology, Julianalaan 136, 2628, BL Delft, The Netherlands.

出版信息

Dalton Trans. 2010 Jan 7(1):185-91. doi: 10.1039/b917673j. Epub 2009 Oct 26.

DOI:10.1039/b917673j

PMID:20023949

Abstract

A pyridine-N-oxide functionalized DOTA analogue has been conjugated to a calix[4]arene and the corresponding Gd-complex was characterized with respect to its suitability as MRI contrast agent. The compound forms spherical micelles in water with a cmc of 35 microM and a radius of 8.2 nm. The relaxivity of these aggregates is 31.2 s(-1) mM(-1) at 25 degrees C and 20 MHz, which corresponds to a molecular relaxivity of 125 s(-1) mM(-1). The high relaxivity mainly originates from the short tau(M) (72.7 ns) and the size of the micelles. The interaction with bovine serum albumin (BSA) was studied and an observed relaxivity of up to 40.8 s(-1) mM(-1) (163.2 s(-1) mM(-1) per binding place) at 20 MHz and 37 degrees C was found in the presence of 2.0 mM protein.

摘要

一种吡啶-N-氧化物功能化的 DOTA 类似物已与杯[4]芳烃连接，相应的 Gd 配合物的特性与其作为 MRI 造影剂的适用性有关。该化合物在水中形成具有 cmc 为 35 μM 和半径为 8.2 nm 的球形胶束。这些聚集体的弛豫率在 25°C 和 20 MHz 下为 31.2 s(-1) mM(-1)，对应于分子弛豫率为 125 s(-1) mM(-1)。高弛豫率主要源于短驰豫时间（tau(M)）（72.7 ns）和胶束的大小。与牛血清白蛋白（BSA）的相互作用进行了研究，在存在 2.0 mM 蛋白质的情况下，在 20 MHz 和 37°C 下观察到高达 40.8 s(-1) mM(-1)（每个结合位 163.2 s(-1) mM(-1)）的弛豫率。