乳糖化和半乳糖基人生长激素的肝靶向性比较研究

为比较乳糖化人生长激素（ｈＧＨ－Ｌ）和半乳糖基人生长激素（ｈＧＨ－Ｇａｌ）的肝靶向性，获得较理想的受体介导肝靶向促生长介素（ＳＯＭ），以提高人生长激素（ｈＧＨ）治疗侏儒症的效果。作者合成了ｈＧＨ－Ｌ和ｈＧＨ－Ｇａｌ，并以１３１Ｉ或１２５Ｉ标记ｈＧＨ－Ｌ、ｈＧＨ－Ｇａｌ和ｈＧＨ，进行小鼠体内分布实验和家兔显像实验对比研究，以及１３１Ｉ－ｈＧＨ－Ｌ、１３１Ｉ－ｈＧＨ－Ｇａｌ鸡显像和家兔体内竞争结合实验。结果：ｈＧＨ－Ｌ和ｈＧＨ－Ｇａｌ均具有明显的趋肝性，肝最大摄取率分别为６８．８３％～７４．６５％和６８．１６％～７４％，均约为ｈＧＨ的２倍，与肝脏的结合均具有受体介导结合特性。但ｈＧＨ－Ｌ的合成较ｈＧＨ－Ｇａｌ更为简单，而且反应条件温和，原料便宜得多。由此提示ｈＧＨ－Ｌ较ｈＧＨ－Ｇａｌ更可能成为受体介导肝靶向促ＳＯＭ分泌以治疗侏儒症的新药。

Comparative Study on Livertaxis of Lactosaminated Human Growth Hormone and Galactosyl-Human Growth Hormone

This study was conducted to compare the livertaxis of lactosaminated human growth hormone (hGHL) with that of galactosyl human growth hormone (hGHGal), using radioactive tracer technique. hGHL and hGHGal were first prepared. After hGHL, hGHGal and hGH were labelled with131I or125I, the data on biodistribution in mice, imaging in rabbits and chicken were otabined. hGHL and hGHGal had remarkable livertaxis and their percentages for uptake in liver were 68.83t.65% and 68.18t% respectively, which were about two times as high as that of hGH. All of the hepatic bindings were receptormediated. But, the synthesizing of hGHL was more easytodo, more mild in reaction conditions, and more economical of raw material as compared with the synthesizing of hGHGal. Therefore, hGHL is a more potential receptormediated hepatic targeting secreting somatomedian drug for treating dwarfism.