SGLT2 inhibitors therapy protects glucotoxicity-induced β-cell failure in a mouse model of human KATP-induced diabetes through mitigation of oxidative and ER stress

PLoS One. 2022 Feb 18;17(2):e0258054. doi: 10.1371/journal.pone.0258054. eCollection 2022.

Abstract

Progressive loss of pancreatic β-cell functional mass and anti-diabetic drug responsivity are classic findings in diabetes, frequently attributed to compensatory insulin hypersecretion and β-cell exhaustion. However, loss of β-cell mass and identity still occurs in mouse models of human KATP-gain-of-function induced Neonatal Diabetes Mellitus (NDM), in the absence of insulin secretion. Here we studied the temporal progression and mechanisms underlying glucotoxicity-induced loss of functional β-cell mass in NDM mice, and the effects of sodium-glucose transporter 2 inhibitors (SGLT2i) therapy. Upon tamoxifen induction of transgene expression, NDM mice rapidly developed severe diabetes followed by an unexpected loss of insulin content, decreased proinsulin processing and increased proinsulin at 2-weeks of diabetes. These early events were accompanied by a marked increase in β-cell oxidative and ER stress, without changes in islet cell identity. Strikingly, treatment with the SGLT2 inhibitor dapagliflozin restored insulin content, decreased proinsulin:insulin ratio and reduced oxidative and ER stress. However, despite reduction of blood glucose, dapagliflozin therapy was ineffective in restoring β-cell function in NDM mice when it was initiated at >40 days of diabetes, when loss of β-cell mass and identity had already occurred. Our data from mouse models demonstrate that: i) hyperglycemia per se, and not insulin hypersecretion, drives β-cell failure in diabetes, ii) recovery of β-cell function by SGLT2 inhibitors is potentially through reduction of oxidative and ER stress, iii) SGLT2 inhibitors revert/prevent β-cell failure when used in early stages of diabetes, but not when loss of β-cell mass/identity already occurred, iv) common execution pathways may underlie loss and recovery of β-cell function in different forms of diabetes. These results may have important clinical implications for optimal therapeutic interventions in individuals with diabetes, particularly for those with long-standing diabetes.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Animals
  • Benzhydryl Compounds / administration & dosage*
  • Blood Glucose / metabolism
  • Diabetes Mellitus / chemically induced
  • Diabetes Mellitus / drug therapy*
  • Diabetes Mellitus / genetics*
  • Diabetes Mellitus / metabolism
  • Disease Models, Animal
  • Endoplasmic Reticulum Stress / drug effects*
  • Female
  • Gain of Function Mutation* / drug effects
  • Glucosides / administration & dosage*
  • Humans
  • Infant, Newborn
  • Infant, Newborn, Diseases / chemically induced
  • Infant, Newborn, Diseases / drug therapy*
  • Infant, Newborn, Diseases / genetics*
  • Infant, Newborn, Diseases / metabolism
  • Insulin-Secreting Cells / drug effects
  • Insulin-Secreting Cells / metabolism*
  • KATP Channels / genetics*
  • Male
  • Mice
  • Mice, Transgenic
  • Oxidative Stress / drug effects*
  • Protective Agents / administration & dosage*
  • Signal Transduction / drug effects
  • Signal Transduction / genetics
  • Sodium-Glucose Transporter 2 Inhibitors / administration & dosage*
  • Treatment Outcome

Substances

  • Benzhydryl Compounds
  • Blood Glucose
  • Glucosides
  • KATP Channels
  • Protective Agents
  • Sodium-Glucose Transporter 2 Inhibitors
  • dapagliflozin