Bakris George L, Fonseca Vivian A, Sharma Kumar, Wright Ernest M
Hypertensive Diseases Unit, Department of Medicine, Pritzker School of Medicine, University of Chicago, Chicago, IL, USA.
Department of Medicine and Pharmacology, Tulane University Health Sciences Center, New Orleans, Los Angeles, USA.
Kidney Int. 2009 Jun;75(12):1272-1277. doi: 10.1038/ki.2009.87. Epub 2009 Apr 8.
The kidneys play a major role in the regulation of glucose in humans, reabsorbing 99% of the plasma glucose that filters through the renal glomeruli tubules. The glucose transporter, SGLT2, which is found primarily in the S1 segment of the proximal renal tubule, is essential to this process, accounting for 90% of the glucose reabsorption in the kidney. Evidence has suggested that selective inhibition of SGLT2 induces glucosuria in a dose-dependent manner and may have beneficial effects on glucose regulation in individuals with type II diabetes. Preclinical data with SGLT2 inhibitors, such as dapagliflozin and sergliflozin, show that these compounds are highly selective inhibitors for SGLT2, have beneficial effects on the glucose utilization rate, and reduce hyperglycemia while having no hypoglycemic adverse effects. Clinical research remains to be carried out on the long-term effects of glucosuria and other potential effects of this class of drug. Nonetheless, these compounds represent a very promising approach for the treatment of diabetes.
肾脏在人体葡萄糖调节中起主要作用,可重吸收经肾小球滤过的99%的血浆葡萄糖。葡萄糖转运体SGLT2主要存在于近端肾小管的S1段,对这一过程至关重要,占肾脏葡萄糖重吸收的90%。有证据表明,选择性抑制SGLT2可剂量依赖性地诱导糖尿,对II型糖尿病患者的血糖调节可能具有有益作用。达格列净和舍格列净等SGLT2抑制剂的临床前数据表明,这些化合物是SGLT2的高度选择性抑制剂,对葡萄糖利用率有有益作用,可降低高血糖,且无低血糖不良反应。关于糖尿的长期影响以及这类药物的其他潜在影响仍有待开展临床研究。尽管如此,这些化合物是治疗糖尿病非常有前景的方法。