非酶糖基化对人血清白蛋白磁共振成像造影剂的影响

THE INFLUENCE OF NONENZYMATIC GLYCOSYLATION ON HUMAN SERUM ALBUMIN MAGNETIC RESONANCE LMAGING CONTRAST AGENTS

目的:本研究旨在评估HSA的非酶糖基化可能对一些钆螯合物相对该蛋白的亲和力造成的影响。方法:利用标准的反转恢复序列,在Minispect mq-20磁共振分析仪中(0.47 T和310 K实验条件)测量了纵向的质子弛豫速率。结果:人血清白蛋白(HSA)的非酶糖基化(NEG)会让钆塞酸二钠(1)和MS-325(2)的亲和力稍微降低,但是它对MP2269(3)的的亲和力不造成任何影响。结论:人血清白蛋白(HSA)被糖基化时,钆塞酸二钠(1)和MS-325(2)相对该蛋白的亲和力略微减弱,足以忽略。因此,存在被糖基化人血清白蛋白(HSA)的情况下,所研究的三种造影剂的效能实际上不受影响。糖尿病患者的效能与药物动力学特性不会存在特别明显的差异。

Objective：This study is to evaluate that HAS nonenzymatic glycosylation may have influence on chelate affinity relative to the protein. Methods：Using the standard inversion recovery sequence, measure longitudinal proton relaxation rate by the Minispect mq -20 magnetic resonance analyzer （0.47 T and 310 K experimental condition）. Results：The nonenzymafie glycosylation （NEG） of human serum albumin （HSA） will make the affinity of gadoxetic acid two sodium （ 1 ） and MS -325 （2） decreased slightly, but it does not have any influence on the affinity of MP2269 （ 3 ）. Conclusion： When the human serum albumin （HSA） was glycosylated, the affinity of gadoxetic acid two sodium （ 1 ） and MS - 325 （2） relative to the protein is slightly decreased, but the decrease is less e- nough to ignore. Therefore, the performances of three kinds of contrast agent are actually not affected by the existence of glycosylated human serum albumin （lISA）. The efficacy and pharmacokinetic properties of diabetic will not have clear difference.