Gregersen S, Langel U, Bartfai T, Ahrén B
Department of Endocrinology and Metabolism C, Aarhus University Hospital, Denmark.
Regul Pept. 1994 Aug 31;53(1):31-7. doi: 10.1016/0167-0115(94)90156-2.
The neuropeptide galanin inhibits insulin secretion and has been suggested to be an adrenergic co-transmitter in the endocrine pancreas. Recently, N-terminally elongated forms of galanin have been identified in both porcine brain and adrenals. Whether these elongated peptides show galanin-like biological effects is not known. We therefore synthesized two N-terminally elongated fragments of galanin(1-16), which contains the active site of galanin. The synthesized peptides were galanin(-9-16) and galanin(-7-16), which correspond to amino acids 24-61 and 26-61 in the galanin precursor molecule. Both these peptides were found to potently inhibit glucose-(11.1 mM)-stimulated insulin secretion from isolated mouse islets of Langerhans in all concentrations studied (1-1000 nM) (P < 0.0001). The potency of the peptides was not different from that of synthetic rat galanin. Thus, at 100 nM, insulin secretion was inhibited by galanin(-7-16) by 83 +/- 7% and by galanin(-9-16) by 71 +/- 17% and by rat galanin by 93 +/- 4% (not statistically different). Furthermore, the galanin receptor antagonist, M35 (10 nM), prevented the inhibitory action of the two N-terminally galanin fragments. This study thus shows that N-terminally elongated galanin-fragments as entire galanin inhibits insulin and thus indicates that the effect of galanin on insulin secretion is not dependent on a free amino-terminus.
神经肽甘丙肽可抑制胰岛素分泌,并且有人提出它在内分泌胰腺中作为一种肾上腺素能共递质。最近,在猪脑和肾上腺中均已鉴定出N端延长形式的甘丙肽。这些延长肽是否具有类似甘丙肽的生物学效应尚不清楚。因此,我们合成了甘丙肽(1-16)的两个N端延长片段,该片段包含甘丙肽的活性位点。合成的肽为甘丙肽(-9-16)和甘丙肽(-7-16),它们分别对应于甘丙肽前体分子中的第24-61位和第26-61位氨基酸。在所有研究浓度(1-1000 nM)下,发现这两种肽均能有效抑制从分离的小鼠胰岛中葡萄糖(11.1 mM)刺激的胰岛素分泌(P <0.0001)。这些肽的效力与合成大鼠甘丙肽的效力没有差异。因此,在100 nM时,甘丙肽(-7-16)抑制胰岛素分泌83±7%,甘丙肽(-9-16)抑制71±17%,大鼠甘丙肽抑制93±4%(无统计学差异)。此外,甘丙肽受体拮抗剂M35(10 nM)可阻止两个N端甘丙肽片段的抑制作用。因此,本研究表明,N端延长的甘丙肽片段与完整的甘丙肽一样可抑制胰岛素,从而表明甘丙肽对胰岛素分泌的作用不依赖于游离的氨基末端。