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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
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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.
出处 《中国糖尿病杂志》 CAS CSCD 1996年第3期145-147,共3页 Chinese Journal of Diabetes
关键词 肾上腺髓质素 血糖 激素 构效关系 药理学 Adrenomedullin Insulin Relationship between structure and function
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