Department of Pathological Sciences, AstraZeneca Pharmaceuticals, Macclesfield, Cheshire, UK.
Int J Exp Pathol. 2014 Feb;95(1):29-48. doi: 10.1111/iep.12066.
Antagonism of the effects of glucagon as an adjunct therapy with other glucose-lowering drugs in the chronic treatment of diabetes has been suggested to aggressively control blood glucose levels. Antagonism of glucagon effects, by targeting glucagon secretion or disabling the glucagon receptor, is associated with α-cell hyperplasia. We evaluated the influence of total glucagon withdrawal on islets of Langerhans using prohormone convertase-2 knockout mice (PC2-ko), in which α-cell hyperplasia is present from a young age and persists throughout life, in order to understand whether or not sustained glucagon deficit would lead to islet tumorigenesis. PC2-ko and wild-type (WT) mice were maintained drug-free, and cohorts of these groups sampled at 3, 12 and 18 months for plasma biochemical and morphological (histological, immunohistochemical, electron microscopical and image analytical) assessments. WT mice showed no islet tumours up to termination of the study, but PC2-ko animals displayed marked changes in islet morphology from α-cell hypertrophy/hyperplasia/atypical hyperplasia, to adenomas and carcinomas, these latter being first encountered at 6-8 months. Islet hyperplasias and tumours primarily consisted of α-cells associated to varying degrees with other islet endocrine cell types. In addition to substantial increases in islet neoplasia, increased α-cell neogenesis associated primarily with pancreatic duct(ule)s was present. We conclude that absolute blockade of the glucagon signal results in tumorigenesis and that the PC2-ko mouse represents a valuable model for investigation of islet tumours and pancreatic ductal neogenesis.
已有研究表明,拮抗胰高血糖素的作用可辅助其他降糖药物进行慢性糖尿病治疗,以积极控制血糖水平。通过靶向胰高血糖素分泌或使胰高血糖素受体失活来拮抗胰高血糖素的作用,与α细胞增生有关。我们使用前激素转化酶 2 敲除(PC2-ko)小鼠评估了完全去除胰高血糖素对胰岛的影响,PC2-ko 小鼠从幼年开始就存在α细胞增生,并持续存在于整个生命周期中,以了解持续的胰高血糖素缺乏是否会导致胰岛肿瘤发生。PC2-ko 和野生型(WT)小鼠未使用药物维持,并在 3、12 和 18 个月时对这些组的样本进行了血浆生化和形态学(组织学、免疫组织化学、电子显微镜和图像分析)评估。WT 小鼠在研究结束时未发现胰岛肿瘤,但 PC2-ko 动物的胰岛形态发生了明显变化,从α细胞肥大/增生/非典型增生,到腺瘤和癌,这些变化最早在 6-8 个月时出现。胰岛增生和肿瘤主要由α细胞组成,与其他胰岛内分泌细胞类型存在不同程度的关联。除了胰岛肿瘤显著增加外,还存在与胰腺导管(ule)相关的α细胞新生增加。我们得出结论,完全阻断胰高血糖素信号会导致肿瘤发生,PC2-ko 小鼠是研究胰岛肿瘤和胰腺导管新生的有价值模型。