肾上腺髓质素对大鼠血糖及其调节激素的构效关系  

The relationship between molecular structure and bioactivities of adrenomedullin on glucose and its regulating hormones in rat blood

作　　者：盛树力[1] 郭育红[1] 齐红伟[1] 姬志娟[1] 赵咏梅[1] 赵志炜[1] 

机构地区：[1]首都医科大学宣武医院多肽研究室

出　　处：《中国糖尿病杂志》1996年第3期145-147,共3页Chinese Journal of Diabetes

摘　　要：已有研究表明，肾上腺髓质素（ＡＭ）对血糖和胰岛激素的分泌有明显影响。为了解ＡＭ结构和功能的关系，我们合成了ＡＭ１－１３、ＡＭ１６－５２、ＡＭ２３－５２和ＡＭ４０－５２四个多肽片段，并观察在大鼠静脉滴注时其对血糖、胰岛素和胰升糖素浓度的影响。实验结果表明：ＡＭ１６－５２和ＡＭ２３－５２均可使血糖降低、胰岛素分泌增加，但这４个片段对胰升糖素浓度均无影响。ＡＭ１－１３无降糖作用，但滴注２小时后能使血胰岛素升高。说明完整的ＡＭ分子存在一个较长的多肽片段，它可促进胰岛素分泌，定位在ＡＭ２３－４０左右。而ＡＭ分子中能抑制胰升糖素分泌的有效片段较短，在分段合成时被分割而失去活性。但对ＡＭ１６－５２和ＡＭ２３－５２的促胰岛素分泌作用的机理尚需进一步研究。Significant effect of Adrenomedullin(AM) on the concentration of blood sugar and its regulating hormones was demonstrated in our previous research. In order to understand the relationship between the biological activity and molecular structure, we synthesized four fragments of AM (AM1-13, AM16-52,AM23-52 and AM40-52) to observe the function of each peptide fragment on sugar, insulin and glucagon levels in the rat blood. By iv infusion, AM16-52 and AM23-52 could cause the blood sugar decline and insulin increase but no effect on glucagon was found for all the four peptide fragments.AM1-13 increased the insulin concentration at the end of experiment. However, it was surprising to find that the blood sugar was still normal. These results,suggest that the intact AM molecule probably contains a longer region and a shorter region, the main longer one located about AM23-40 can accelerate the insulin secretion while the shorter one may inhibit the glucagon secretion. But it is possible that this potential region may be divided from the intact peptide into different fragments with losing of the biological activity. The conclusion is that about 23￣40 amino acid sequence of AM is associated with promotion of insulin secretion and decline of blood glucose concentration.

关 键 词：肾上腺髓质素 血糖 激素 构效关系 药理学 

分 类 号：R977[医药卫生—药品]