The Effects of Empagliflozin, an SGLT2 Inhibitor, on Pancreatic β-Cell Mass and Glucose Homeostasis in Type 1 Diabetes

PLoS One. 2016 Jan 25;11(1):e0147391. doi: 10.1371/journal.pone.0147391. eCollection 2016.

Abstract

The novel sodium glucose co-transporter 2 (SGLT2) inhibitor empagliflozin has recently been reported to improve glycemic control in streptozotocin-induced type 1 diabetic rats in an insulin-independent manner, via an increase in urinary glucose output. We investigated the potential of empagliflozin to recover insulin pathways in type 1 diabetes by improving pancreatic β-cell mass. Blood glucose homeostasis was assessed by an intraperitoneal glucose tolerance test. Serum insulin levels and insulin mRNA expression were determined using commercial insulin ELISA kits and real-time quantitative polymerase chain reaction, respectively. Immunohistochemistry was used to investigate β-cell areas, β-cell proliferation, apoptosis of pancreatic β-cells, and reactive oxygen species production in the pancreatic β-cells. Results showed that glucose tolerance was significantly improved in streptozotocin-induced type 1 diabetic mice treated with empagliflozin. Empagliflozin-treated mice also showed an increase in insulin mRNA expression. Higher serum insulin levels were detected in mice treated with empagliflozin compared with the vehicle group. Immunohistochemistry indicated that β-cell area/total pancreatic area and the expression of cell proliferation marker Ki-67 (co-stained with insulin) were significantly enhanced by empagliflozin treatment. These effects were due, probably, to a reduction in apoptosis and reactive oxygen species in the pancreatic β-cells. Taken together, the results of this study indicate that empagliflozin may have a beneficial effect on preserving β-cell regeneration, thus improving blood glucose homeostasis in type 1 diabetes mellitus, probably via the protection of pancreatic β-cell from glucotoxicity-induced oxidative stress.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Area Under Curve
  • Benzhydryl Compounds / administration & dosage
  • Benzhydryl Compounds / pharmacology*
  • Benzhydryl Compounds / therapeutic use
  • Diabetes Mellitus, Experimental / drug therapy*
  • Diabetes Mellitus, Experimental / metabolism
  • Diabetes Mellitus, Type 1 / drug therapy*
  • Diabetes Mellitus, Type 1 / metabolism
  • Dose-Response Relationship, Drug
  • Drug Evaluation, Preclinical
  • Glucose / metabolism*
  • Glucose Tolerance Test
  • Glucosides / administration & dosage
  • Glucosides / pharmacology*
  • Glucosides / therapeutic use
  • Homeostasis
  • Hypoglycemic Agents / administration & dosage
  • Hypoglycemic Agents / pharmacology*
  • Hypoglycemic Agents / therapeutic use
  • Insulin / biosynthesis
  • Insulin / blood
  • Insulin / genetics
  • Insulin-Secreting Cells / drug effects*
  • Insulin-Secreting Cells / pathology
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Organ Size / drug effects
  • RNA, Messenger / biosynthesis
  • RNA, Messenger / genetics
  • Sodium-Glucose Transporter 2
  • Sodium-Glucose Transporter 2 Inhibitors

Substances

  • Benzhydryl Compounds
  • Glucosides
  • Hypoglycemic Agents
  • Insulin
  • RNA, Messenger
  • Slc5a2 protein, mouse
  • Sodium-Glucose Transporter 2
  • Sodium-Glucose Transporter 2 Inhibitors
  • empagliflozin
  • Glucose

Grants and funding

This work was supported by Boehringer-Ingelheim Pharma GmbH & Co KG, Biberach, Germany (CUHK Ref. No.: TB127545). Boehringer-Ingelheim Pharma GmbH & Co KG provided support in the form of a salary for author EM, but did not have any additional role in the study design, data collection and analysis, decision to publish, or preparation of the manuscript. The specific role of this author is articulated in the ‘author contributions’ section.