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为有效提高半乳糖基化合物的糖密度以增加其趋肝性 ,作者采用分枝化合物 3,5 -二羟基苯甲酸为偶联桥 ,将半乳糖与胰岛素偶联 ,得到糖密度较单链桥法高一倍的双糖密度半乳糖基胰岛素 ,而后用 1 31 分别标记双糖密度半乳糖基胰岛素、单链桥偶联半乳糖基胰岛素和普通胰岛素 ,通过家兔体内示踪实验对比研究它们的肝靶向性。结果显示 :双糖密度偶联物的趋肝性最大 ,单糖偶联物次之 ,普通胰岛素最差 ,其肝最大摄取率分别为5 9.5 %、43.8%和 2 1 .5 %。而 3种标记物的鸡全身显像皆未见肝脏特异性浓聚 ,从而证明以分枝化合物为偶联桥 ,可以有效地提高半乳糖基化合物的糖密度 ,大幅度提高其趋肝性。并提示这是一条制备高趋肝性肝受体显像剂和高肝靶向性药物的有效途径
In order to effectively increase the sugar content of galactosyl compounds to increase their hepatic degeneration, the authors used the branched compound 3,5 - dihydroxybenzoic acid as the coupling bridge to couple galactose to insulin to obtain a higher sugar density than single - Method twice as high as double sugar density galactosyl insulin, and then using 1 31 labeled double sugar density galactosyl insulin, single chain bridge coupling of galactosyl insulin and normal insulin, comparative study of their rabbit tracer experiments Liver targeting. The results showed that the conjugate with double sugar density had the highest tendency to hepatopancreas, followed by monosaccharide conjugate with the lowest normal insulin, and the maximum hepatic uptake rates were 5 9.5%, 43.8% and 21.5% respectively. However, no chicken liver specific enrichment was found in the three kinds of markers of chicken whole body imaging, which proves that using the branched compound as the coupling bridge can effectively improve the sugar density of the galactosyl compound and greatly enhance the hepatotanning. And suggested that this is an effective way to prepare high-hepatic hepatic receptor imaging agent and high-liver targeting drug