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去酰基 ghrelin 片段和类似物可促进胰岛 β 细胞和人胰岛的存活,并预防链脲佐菌素处理的大鼠糖尿病。

Des-acyl ghrelin fragments and analogues promote survival of pancreatic β-cells and human pancreatic islets and prevent diabetes in streptozotocin-treated rats.

机构信息

Laboratory of Molecular and Cellular Endocrinology, University of Turin, Corso Dogliotti 14, 10126 Turin, Italy.

出版信息

J Med Chem. 2012 Mar 22;55(6):2585-96. doi: 10.1021/jm201223m. Epub 2012 Mar 5.

Abstract

Des-acyl ghrelin, although devoid of binding to ghrelin receptor (GRLN), exerts many biological effects, including regulation of glucose and lipid metabolism. Indeed, des-acyl ghrelin promotes pancreatic β-cell and human islet cell survival and prevents diabetes in streptozotocin (STZ) treated rats. We investigated whether des-acyl ghrelin fragments excluding serine(3), which is essential for binding to GRLN, would display similar actions. Among the different compounds tested, des-acyl ghrelin((6-13)) and des-acyl ghrelin((6-13)) with alanine substitutions or cyclization, but not with d-amino acid substitutions, showed the best survival effect, similar to des-acyl ghrelin. Des-acyl ghrelin((6-13)) even prevented diabetes in STZ-treated rats and protected human circulating angiogenic cells from oxidative stress and senescence, similar to des-acyl ghrelin. These results suggest that not only full-length des-acyl ghrelin but also short des-acyl ghrelin fragments have clear beneficial effects on several tissues in vitro and in vivo.

摘要

去酰基 ghrelin 虽然缺乏与 ghrelin 受体 (GRLN) 的结合,但具有许多生物学效应,包括调节葡萄糖和脂质代谢。事实上,去酰基 ghrelin 可促进胰岛β细胞和人胰岛细胞的存活,并可预防链脲佐菌素 (STZ) 处理的大鼠发生糖尿病。我们研究了是否去酰基 ghrelin 的片段(不包括对与 GRLN 结合至关重要的丝氨酸(3))会显示出类似的作用。在测试的不同化合物中,去酰基 ghrelin((6-13))和带有丙氨酸取代或环化的去酰基 ghrelin((6-13)),但不是 D-氨基酸取代,显示出最好的存活效果,类似于去酰基 ghrelin。去酰基 ghrelin((6-13))甚至可以预防 STZ 处理的大鼠发生糖尿病,并保护人循环血管生成细胞免受氧化应激和衰老,类似于去酰基 ghrelin。这些结果表明,不仅全长去酰基 ghrelin,而且短的去酰基 ghrelin 片段对体外和体内的几种组织都具有明显的有益作用。

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