| 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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| 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6×10-3 L·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。 |
| 关键词: 叶酸受体 靶向 大分子造影剂 体外弛豫性能 |
| 基金项目: |
| 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. |
| Keywords: folate receptor targeting macromolecular contrast agent relaxivity in vitro |
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| 龙娜,项光亚,唐大宗,夏黎明,崔佳,汤军.叶酸介导的靶向性钆造影剂的制备及弛豫性能研究[J].无机化学学报,2007,23(5):759-764. |
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