Goldfine I D, Iwamoto Y, Pezzino V, Trischitta V, Purrello F, Vigneri R
Diabetes Care. 1984 May-Jun;7 Suppl 1:54-8.
The effects of the two groups of oral agents on insulin receptors were studied in several types of cells in tissue culture: MCF-7 human breast cancer cells, IM-9 human lymphocytes, human fibroblasts, and H-35 rat hepatoma cells. In none of these cells did the four sulfonylureas tested, tolbutamide, glibenclamide (glyburide), gliclazide, and glisolamide, have any significant effects on insulin binding to its receptor. In contrast the two biguanides tested, phenformin and metformin, increased insulin binding in all cell types by 44 to 101%. These studies raise the possibility, therefore, that biguanides may have a direct effect on insulin receptors and this effect may account for the known effects of biguanides to lower elevated blood sugar levels in diabetic patients.
MCF-7人乳腺癌细胞、IM-9人淋巴细胞、人成纤维细胞和H-35大鼠肝癌细胞。在所测试的四种磺脲类药物（甲苯磺丁脲、格列本脲（优降糖）、格列齐特和格列索胺）中，没有一种对胰岛素与其受体的结合有任何显著影响。相比之下，所测试的两种双胍类药物（苯乙双胍和二甲双胍）使所有细胞类型中的胰岛素结合增加了44%至101%。因此，这些研究提出了一种可能性，即双胍类药物可能对胰岛素受体有直接作用，并且这种作用可能解释了双胍类药物降低糖尿病患者升高血糖水平的已知作用。
