乳糖化、99mTc 螯合白蛋白的合成与应用：用于肝功能测定。

Synthesis and application of lactosylated, 99mTc chelating albumin for measurement of liver function.

机构信息

Universite Paris-Sud 11, EA4046, Kremlin-Bicetre, F-94275, AP-HP, CHU de Bicetre, Le Kremlin-Bicetre, F-94275, Unite de Pharmacologie Chimique et Genetique, U640 INSERM, UMR8151 CNRS, Universite Paris Descartes, Paris, France.

出版信息

Bioconjug Chem. 2010 Apr 21;21(4):589-96. doi: 10.1021/bc900275f.

DOI:10.1021/bc900275f

PMID:20201600

Abstract

Neogalactosylated and neolactosylated albumins are currently used as radiopharmaceutical agents for imaging the liver asialoglycoprotein receptors, which allows the quantification of hepatic liver function in various diseases and also in healthy liver transplant donors. We developed an original process for synthesizing a chelating neolactosylated human albumin using maleimidopropyl-lactose and maleimidopropyl-diethylene triamine pentaacetic acid (DTPA) derivatives. The lactosylated protein (LACTAL) conjugate showed excellent liver uptake compared to nonlactosylated protein and a very high signal-to-noise ratio, based on functional assessment of biodistribution in mice using (99m)Tc-scintigraphy.

摘要

目前，半乳糖基化和新半乳糖基化白蛋白被用作放射性药物，用于成像肝脏去唾液酸糖蛋白受体，这使得可以在各种疾病和健康的肝移植供体中定量评估肝功能。我们开发了一种使用马来酰亚胺丙基乳糖和马来酰亚胺丙基二乙烯三胺五乙酸（DTPA）衍生物合成螯合新半乳糖基化人白蛋白的原始方法。基于使用（99m）Tc 闪烁扫描术在小鼠中进行的生物分布功能评估，与非半乳糖基化蛋白相比，该乳糖基化蛋白（LACTAL）缀合物显示出优异的肝脏摄取率和非常高的信噪比。