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一种具有作为磁共振成像血管内造影剂特性的钆与顺铂共轭明胶的研发。

Development of a conjugated gadolinium and cisplatin-gelatin possessing properties as an intravascular contrast agent for MR imaging.

作者信息

Sonoda Akinaga, Nitta Norihisa, Ohta Shinichi, Seko Ayumi, Jo Jun-ichiro, Morikawa Shigehiro, Tabata Yasuhiko, Takahashi Masashi, Murata Kiyoshi

机构信息

Department of Radiology, Shiga University of Medical Science, Setatsukinowa-cho, Otsu, Shiga 520-2192, Japan.

出版信息

Eur J Radiol. 2009 Sep;71(3):570-5. doi: 10.1016/j.ejrad.2008.04.009. Epub 2008 May 27.

Abstract

PURPOSE

The purpose of this study is to create a Gd-DTPA-Gel-Cis compound, which made from gadolinum (Gd), diethylenetriaminepentaacetic acid (DTPA)-dianhydride, cis-diamminedichloroplatinum (Cis) and bovine gelatin (Gel), that makes it possible to visualize Cis as intravascular agent under magnetic resonance imaging (MRI).

MATERIALS AND METHODS

The amount of DTPA, Gd, and Cis were titrated to determine the new compound's conjugation ratio with gelatin. Considering these functions, Gd-DTPA-Gel-Cis was synthesized, and its stability in bovine serum was evaluated. In addition, the signal intensity of the diluted sample was measured under 1.5 Tesla MRI.

RESULTS

The synthesized 10mg/ml of Gd-DTPA-Gel-Cis contained 42.84 microg/ml of Gd and 1.53 microg/ml of platinum. Gd-DTPA-Gel-Cis (100 mg/10 ml) enclosed into the cellulose dialysis tubing was placed in 90 ml of bovine serum and shaken reciprocally at 72 stroke/min at 37 degrees C. Partial release of free Pt was shown at 6 and 24 h, but no release of Gd occurred for a 24-h period. And high stability of Gd conjugated to DTPA-Gel-Cis. This result suggests possible anti-tumor effectiveness and high stability of Gd conjugated to DTPA-Gel-Cis. The diluted sample presented high signal intensity under 1.5 Tesla MRI.

CONCLUSION

Gd-DTPA-Gel-Cis has been developed successfully and we have proven its stability and contrast ability in MRI.

摘要

目的

本研究旨在制备一种由钆(Gd)、二乙烯三胺五乙酸二酐(DTPA)、顺二氯二氨铂(Cis)和牛明胶(Gel)制成的Gd-DTPA-Gel-Cis化合物,使其能够在磁共振成像(MRI)下作为血管内造影剂使Cis可视化。

材料与方法

滴定DTPA、Gd和Cis的用量,以确定新化合物与明胶的结合率。基于这些功能,合成了Gd-DTPA-Gel-Cis,并评估了其在牛血清中的稳定性。此外,在1.5特斯拉MRI下测量稀释样品的信号强度。

结果

合成的10mg/ml Gd-DTPA-Gel-Cis含有42.84μg/ml的Gd和1.53μg/ml的铂。将装入纤维素透析管的Gd-DTPA-Gel-Cis(100mg/10ml)置于90ml牛血清中,于37℃以72次/分钟的频率往复振荡。在6小时和24小时时出现了游离Pt的部分释放,但在24小时内未出现Gd的释放。并且Gd与DTPA-Gel-Cis结合具有高稳定性。该结果表明Gd与DTPA-Gel-Cis结合可能具有抗肿瘤效果和高稳定性。稀释样品在1.5特斯拉MRI下呈现高信号强度。

结论

已成功研发出Gd-DTPA-Gel-Cis,并已证明其在MRI中的稳定性和造影能力。

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