Nauck M A, Bartels E, Orskov C, Ebert R, Creutzfeldt W
Department of Medicine, Georg August University, Göttingen, Germany.
J Clin Endocrinol Metab. 1993 Apr;76(4):912-7. doi: 10.1210/jcem.76.4.8473405.
Gastric inhibitory polypeptide (GIP) and glucagon-like peptide-1-(7-36) amide (GLP-1) are glucose-dependent insulinotropic gut hormones that may explain the greater insulin secretory response with oral compared to i.v. glucose (incretin effect). To study their individual and combined contributions, in eight healthy volunteers, on separate occasions, synthetic human GIP (1 pmol/kg.min) and/or GLP-1 (0.3 pmol/kg.min) or placebo were infused i.v. (-30 to 120 min), while at 0 min, a glucose infusion "isoglycemic" to the profile after an oral glucose load of 50 g/400 mL was started. After the administration of 50 g oral glucose, immunoreactive GIP rose several-fold to 337 +/- 43 pmol/L, while there was only a transient (10-30 min) and moderate increment in immunoreactive GLP-1 (from basal, 25-30, to 41 +/- 4 pmol/L). Isoglycemic i.v. glucose infusions led to smaller B-cell responses (estimated incretin effect, 41 +/- 5%). With single infusions of GIP or GLP-1 (circulating concentrations, 464 +/- 73 and 54 +/- 3 pmol/L, respectively), B-cell responses were significantly augmented compared to i.v. glucose alone and were no longer significantly different from those after oral glucose. The combination of GIP and GLP-1 led to B-cell responses that were significantly higher than those with either hormone alone (additive mode of cooperation). Plasma GIP concentrations were similar after endogenous secretion (oral glucose) and i.v. infusion, while exogenously administered GLP-1 led to plasma levels that were maintained at an elevated level for a longer period during exogenous infusion than after stimulation by oral glucose. When, in seven volunteers, a lower dose (0.15 pmol/kg.min) of GLP-1 was infused during isoglycemic glucose infusion experiments only for the duration of elevated plasma levels in the oral glucose challenges (0-30 min), a significant, but transient, increment in insulin and C-peptide concentrations was observed, which was equivalent to 26 +/- 10% of the estimated incretin effect. Therefore, in conclusion, circulating GIP seems to make a major contribution to the incretin effect after oral glucose, and GLP-1 appears to mediate a smaller proportion. GIP and GLP-1 can interact in an additive manner in normal man.
胃抑制多肽(GIP)和胰高血糖素样肽-1(7-36)酰胺(GLP-1)是葡萄糖依赖性促胰岛素肠激素,这可能解释了口服葡萄糖相比静脉注射葡萄糖时更大的胰岛素分泌反应(肠促胰岛素效应)。为了研究它们各自的作用以及联合作用,在8名健康志愿者身上,在不同时间分别静脉输注合成人GIP(1 pmol/kg·min)和/或GLP-1(0.3 pmol/kg·min)或安慰剂(-30至120分钟),而在0分钟时,开始静脉输注葡萄糖,使其血糖水平与口服50 g/400 mL葡萄糖负荷后的血糖水平“等血糖”。口服50 g葡萄糖后,免疫反应性GIP升高数倍至337±43 pmol/L,而免疫反应性GLP-1仅有短暂(10 - 30分钟)且适度的升高(从基础值25 - 30升高至41±4 pmol/L)。等血糖静脉输注葡萄糖引起的B细胞反应较小(估计肠促胰岛素效应为41±5%)。单独静脉输注GIP或GLP-1(循环浓度分别为464±73和54±3 pmol/L)时,与单独静脉输注葡萄糖相比,B细胞反应显著增强,且与口服葡萄糖后的反应不再有显著差异。GIP和GLP-1联合使用导致的B细胞反应显著高于单独使用任何一种激素时(协同作用的相加模式)。内源性分泌(口服葡萄糖)和静脉输注后血浆GIP浓度相似,而外源性给予GLP-1导致的血浆水平在外源输注期间比口服葡萄糖刺激后维持在较高水平的时间更长。在7名志愿者的等血糖葡萄糖输注实验中,仅在口服葡萄糖激发试验中血浆水平升高的持续时间内(0 - 30分钟)输注较低剂量(0.15 pmol/kg·min)的GLP-1,观察到胰岛素和C肽浓度有显著但短暂的升高,相当于估计肠促胰岛素效应的26±10%。因此,总之,循环中的GIP似乎对口服葡萄糖后的肠促胰岛素效应起主要作用,而GLP-1似乎介导的比例较小。在正常人体内,GIP和GLP-1可以相加的方式相互作用。