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一种用于靶向磁共振成像的新型胆酸基造影剂。

A novel cholic acid-based contrast enhancement agent for targeted MRI.

作者信息

Chong Hyun-Soon, Song Hyun A, Lim Sooyoun, Macrenaris Keith, Ma Xiang, Lee Haisung, Bui Phuong, Meade Thomas

机构信息

Chemistry Division, Biological, Chemical, and Physical Sciences Department, Illinois Institute of Technology, 3101 S. Dearborn St., LS 182, Chicago, IL 60616, USA.

出版信息

Bioorg Med Chem Lett. 2008 Apr 1;18(7):2505-8. doi: 10.1016/j.bmcl.2008.01.044. Epub 2008 Jan 18.

DOI:10.1016/j.bmcl.2008.01.044
PMID:18337094
Abstract

The novel Gd(III) complexes of heptadentate ligands NE3TA and NE3TA-Bn were prepared, and their relaxivities were measured and favorably compared to the commercially available MRI contrast enhancement agent Gd(DOTA). NE3TA was conjugated with cholic acid (CA) to produce CA-NE3TA. TEM images of Gd(CA-NE3TA) indicate that the complex self-assembles forming nano-sized micelles and displays an over threefold increased relaxivity compared to Gd(DOTA). The new cholic acid-conjugated nanoparticle MR contrast enhancement agent, Gd(CA-NE3TA) possesses great promise for use in targeted MRI.

摘要

制备了七齿配体NE3TA和NE3TA-Bn的新型钆(III)配合物,并测定了它们的弛豫率,与市售的磁共振成像(MRI)造影增强剂钆(DOTA)相比效果良好。NE3TA与胆酸(CA)共轭生成CA-NE3TA。钆(CA-NE3TA)的透射电子显微镜(TEM)图像表明,该配合物自组装形成纳米尺寸的胶束,与钆(DOTA)相比,弛豫率提高了三倍多。新型胆酸共轭纳米颗粒MRI造影增强剂钆(CA-NE3TA)在靶向MRI应用方面具有巨大潜力。

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