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叶酸介导的靶向性钆造影剂的制备及弛豫性能研究

Preparation and Relaxivity of Folate-mediated Targeting Gd3+ Contrast Agent

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【作者】 龙娜; 项光亚; 唐大宗; 夏黎明; 崔佳; 汤军;

【Author】 LONG Na1 XIANG Guang-Ya*,1 TANG Da-Zong2 XIA Li-Ming2 CUI Jia1 TANG Jun1 (1Tongji Pharmaceutical College, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430030) (2Department of Radiology, Tongji Hospital Affiliated Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430030)

【机构】 华中科技大学同济医学院药学院; 华中科技大学同济医学院附属同济医院放射科; 华中科技大学同济医学院药学院 武汉430030; 武汉430030;

【摘要】 在弱碱性的条件下,叶酸活化酯与牛血清白蛋白(BSA)反应生成叶酸-牛血清白蛋白偶联物(叶酸-BSA),该偶联物再与二乙三胺五乙酸(DTPA)的酸酐反应,最后与GdCl3进行螯合制得叶酸-BSA-(Gd-DTPA)n。配合物的结构通过紫外光谱法进行了鉴定,并定量测定了配合物中叶酸、Gd-DTPA对BSA的偶联率。通过测定配合物的体外弛豫时间T1,进一步分析其弛豫性能R1。结果表明本研究制得的叶酸-BSA-(Gd-DTPA)n配合物中叶酸的偶联率约为5,体外弛豫性能R1约为6×10-3L·mmol-1·ms-1,与未偶联叶酸的BSA-(Gd-DTPA)n的弛豫性能无显著性差异,且比小分子Gd-DTPA的弛豫性能提高了3倍左右。

【Abstract】 Under weak base condition, Bovine serum albumin (BSA) was reacted with the activated folate firstly; then the conjugates were coupled with Diethylene triamine pentaacetic dianhydride (cDTPAA) to form Folate-BSA-DTPA; finally, these coupled compounds were chelated with GdCl3. All complexes were characterized by UV, the ratios of folate and Gd-DTPA to BSA were determined by UV and ICP-AES methods, respectively. The spin-lattice relaxivity of the Gd complexes in vitro was analyzed. As a result, the ratio of folate to BSA was about 5, and the relaxivity was about 6×10-3 L·mmol-1·ms-1 enhanced three times compared to the small molecular Gd-DTPA, though there was no difference in relaxivity between folate-BSA-(Gd-DTPA)n and BSA-(Gd-DTPA)n.

【基金】 国家自然科学基金(No.30300430);湖北省自然科学基金(No.2006ABA123)资助项目。
  • 【文献出处】 无机化学学报 ,Chinese Journal of Inorganic Chemistry , 编辑部邮箱 ,2007年05期
  • 【分类号】TQ421.7
  • 【被引频次】9
  • 【下载频次】332
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