| 叶酸介导的靶向性钆造影剂的制备及弛豫性能研究 |
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| 引用本文： | 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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| 作者姓名： | 龙娜 项光亚 唐大宗 夏黎明 崔佳 汤军 |
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| 作者单位： | 1. 华中科技大学同济医学院药学院,武汉,430030
2. 华中科技大学同济医学院附属同济医院放射科,武汉,430030 |
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| 基金项目： | 国家自然科学基金;湖北省自然科学基金 |
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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。
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| 关 键 词： | 叶酸受体； 靶向； 大分子造影剂； 体外弛豫性能 |
| 文章编号： | 1001-4861(2007)05-0759-06 |
| 修稿时间： | 2006-09-05 |
Preparation and Relaxivity of Folate-mediated Targeting Gd3+ Contrast Agent |
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| LONG N,XIANG Guang-Y,TANG Da-Zong,XIA Li-Ming,CUI Jia and TANG Jun. Preparation and Relaxivity of Folate-mediated Targeting Gd3+ Contrast Agent[J]. Chinese Journal of Inorganic Chemistry, 2007, 23(5): 759-764 |
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| Authors: | LONG N XIANG Guang-Y TANG Da-Zong XIA Li-Ming CUI Jia TANG Jun |
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| Affiliation: | Tongji Pharmaceutical College, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430030,Tongji Pharmaceutical College, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430030,Department of Radiology, Tongji Hospital Affiliated Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430030,Department of Radiology, Tongji Hospital Affiliated Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430030,Tongji Pharmaceutical College, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430030 and Tongji Pharmaceutical College, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430030 |
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| 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. |
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| Keywords: | folate receptor targeting macromolecular contrast agent relaxivity in vitro |
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