Ravindran Sreenithya, Munusamy Shankar
Reagents and Assay Development R&D, BD Biosciences, San Jose, California, USA.
Department of Pharmaceutical and Administrative Sciences, Drake University College of Pharmacy and Health Sciences, Des Moines, Iowa, USA.
J Cell Physiol. 2022 Feb;237(2):1182-1205. doi: 10.1002/jcp.30621. Epub 2021 Oct 29.
Sodium-glucose co-transporter 2 inhibitors (SGLT2-Is) have emerged as a promising class of antidiabetic drugs with cardioprotective and renoprotective effects in patients with type 2 diabetes (T2D). The sodium-glucose co-transporters 1 and 2 (SGLT 1 and SGLT2) located in the renal proximal tubules are responsible for glucose reabsorption from the glomerular filtrate back into the systemic circulation. Inhibition of SGLT2, which accounts for about 90% of the glucose reabsorption, leads to a significant reduction in blood glucose levels and a concomitant increase in the urinary excretion of glucose (glycosuria). Multiple mechanisms contribute to the nephroprotective effects of SGLT2-Is in T2D patients. These include: (1) Restoration of the tubuloglomerular feedback by increasing sodium delivery at macula densa, leading to afferent arteriolar constriction and reduced glomerular hyperfiltration, (2) Decreased activation of the intra-renal renin-angiotensin-aldosterone system, which also contributes to reducing glomerular hyperfiltration, (3) Increased production of ketone bodies, which serves as an alternate fuel for adenosine triphosphate production in mitochondria, which helps in attenuating inflammation, and (4) Protection against hypoxia, oxidative stress, and fibrosis. This review elaborates on the key mechanisms that underlie the nephroprotective effects and the adverse effects of SGLT2-Is in T2D patients with progressive diabetic kidney disease.
钠-葡萄糖协同转运蛋白2抑制剂(SGLT2-Is)已成为一类很有前景的抗糖尿病药物,对2型糖尿病(T2D)患者具有心脏保护和肾脏保护作用。位于肾近端小管的钠-葡萄糖协同转运蛋白1和2(SGLT1和SGLT2)负责将肾小球滤过液中的葡萄糖重吸收回体循环。抑制约占葡萄糖重吸收90%的SGLT2,会导致血糖水平显著降低,同时尿葡萄糖排泄量增加(糖尿)。多种机制促成了SGLT2-Is对T2D患者的肾脏保护作用。这些机制包括:(1)通过增加致密斑处的钠输送来恢复管球反馈,导致入球小动脉收缩并减少肾小球高滤过;(2)减少肾内肾素-血管紧张素-醛固酮系统的激活,这也有助于减少肾小球高滤过;(3)增加酮体生成,酮体可作为线粒体中三磷酸腺苷生成的替代燃料,有助于减轻炎症;(4)防止缺氧、氧化应激和纤维化。本综述阐述了SGLT2-Is对患有进展性糖尿病肾病的T2D患者肾脏保护作用和不良反应的关键机制。