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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。
To compare the liver targeting of hGH-L and hGH-Gal, an ideal receptor-mediated liver-targeting somatomedin (SOM) Enhance the effect of human growth hormone (hGH) on dwarfism. The authors synthesized hGH-L and hGH-Gal and labeled 131I or 125I with hGH-L, hGH-Gal and hGH to compare the in vivo distribution in vivo with that in rabbits, as well as 131I-hGH-L, 131I -hGH-Gal chicken imaging and in vivo competition in rabbits. Results: Both hGH-L and hGH-Gal had a tendency to hepatopancreas. The maximal uptake rates of liver were 68.83% -74.65% and 68.16% -74% Liver binding all have receptor-mediated binding properties. However, the synthesis of hGH-L is more simpler than that of hGH-Gal, and the reaction conditions are mild and the raw materials are much cheaper. This suggests that hGH-L is more likely than hGH-Gal to be a new drug that mediates liver-targeted SOM secretion in order to treat dwarfism.