磁共振对比剂Gd-DTPA-DG的制备及动物实验研究  

Preparation and animal experimental study in MRI contrast agent Gd-DTPA-DG

作　　者：黄占文[1] 张伟[1] 陈跃[1] 蔡亮[1] 曹丰[1] 丁志凌[1] 何菱[2] 

机构地区：[1]泸州医学院附属医院核医学科,四川646000 [2]四川大学华西药学院,成都610041

出　　处：《重庆医学》2010年第21期2866-2868,2871,F0002,共5页Chongqing medicine

基　　金：2009年国家自然科学基金资助项目(30970858);2009年四川省高等学校科技创新重大培育项目(2009-07);2008年四川省医学重点学科建设项目(2008-17);四川省杰出青年学科带头人基金资助项目(2008-46-386)

摘　　要：目的合成一种顺磁性脱氧葡萄糖类MR对比剂——二乙三胺五乙酸-脱氧葡萄糖钆盐(Gd-DTPA-DG),并探讨其在荷瘤裸鼠体内肿瘤信号改变的规律。方法首先合成DTPA-DG,再与氧化钆(Gd2O3)螯合,制得Gd-DTPA-DG。采用荷瘤裸鼠体内实验模型,将裸鼠随机分成实验组(n=10)与对照组(n=10),前者尾静脉注射Gd-DTPA-DG,后者尾静脉注射含相同钆离子(Gd3+)浓度(0.1 mmol/kg)的Gd-DTPA,测量SEW1 WI平扫及引入对比剂30 s、2 min、5 min、10 min、20 min、30 min、45 min、1 h、2 h后瘤体信号强度,并计算对比度信噪比(CNR)。将右侧前肢肌肉组织信号变化作为参照物,并进行统计分析。结果 Gd-DTPA-DG比Gd-DTPA在肿瘤组织内表现为更强且更持久的强化。注射对比剂30 s后,实验组裸鼠瘤体信号增加与扫描前差异无统计意义(P=0.171),在30 min左右差异最大(P<0.001),且持续时间长。对照组5 min前后差异最大(P<0.001),但2 h时即与注射前差异无统计学意义(P=0.28)。结论 Gd-DTPA-DG可在肺癌模型活体内起到肿瘤强化作用,是一种新型顺磁性钆类MR对比剂。Objective To synthesize a paramagnetic deoxy-glucose-type MR contrast agent diethylenetriamine pentaacetic acid-gadolinium salt deoxy-glucose（Gd-DTPA-DG） and to study the tumor signal intensity pattern in vivo MR imang in tumor-bearing nude mice model.Methods After successfully synthesized diethylenetriamine pentaacetic acid glucosamine（DTPA-DG）,Gd2O3 was added to conjugate with it,and Gd-DTPA-DG,an MR contrast agent,was thus preparated.We conducted in vitro studies using nude mice with transplanted human adenocarcinoma of lung as experimental model.The mice were divided into study group（n=10） and control group（n=10）.The animals in the experimental group were injected with Gd-DTPA-DG via vena caudalis,whereas the routine Gd-DTPA was used in the control group at the same dosage of gadolinium with the same amount of 0.1 mmol/kg as the experimental group.The tumor signal intensities（SI） on T1W1 was measured at 30 s,2 min,5 min,10 min,20 min,30 min,45 min,1 h,2 h respectively after injection of contrast agents with SI of the anterior limb muscles on the same side as control.Then all of the results were statistically analyzed.The CNR（contrast to noise ratio） was calculated as wel1.Results Gd-DTPA-DG compared with Gd-DTPA in tumor tissue showed a stronger and more durable reinforced.Consequently,there was no statistically significant difference on the SI in the experimental group before and after injection of the specific contrast agents at 30 s（P=0.171）.In comparison with the pre-contrast imaging,SI of tumor and musc1es in the experimental group increased greatly at 30 min after injection of Gd-DTPA-DG with significant difference（P〈0.001）.In control group,there was statistically significant difference on SI before and after injection of Gd-DTPA at 5 min（P〈0.001）,and the contrast in the tumors almost entirely washed out at 2 h after injection of Gd-DTPA（P=0.28）.Conclusion Gd-DTPA-DG can produce a greatly signal intensity enhancement of the transplanted human adenocarcinoma of

关 键 词：Gd-DTPA-DG 顺磁性对比剂 葡萄糖代谢 肿瘤靶向性 分子影像 

分 类 号：R981.1[医药卫生—药品] R445.2[医药卫生—药学]