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Characterization of extracellular and membrane potentials in imeglimin-treated islets

Asuka Tsurumoto1, Ryota Inoue1, Esther Ong Yajima1

  • 1Laboratory of Diabetes and Metabolic Disorders, Institute for Molecular and Cellular Regulation (IMCR), Gunma University, Maebashi, Japan.

Journal of Diabetes Investigation
|February 16, 2026
PubMed

Insights

Imeglimin enhances glucose-stimulated insulin secretion (GSIS) by increasing β-cell electroactivity and membrane depolarization. This oral diabetes agent improves insulin release dynamics at the islet level.

Area of Science:

  • Endocrinology
  • Cellular Electrophysiology
  • Diabetes Therapeutics

Background:

  • Glucose-stimulated insulin secretion (GSIS) is crucial for glucose homeostasis.
  • β-cell electroactivity, particularly membrane depolarization, drives GSIS.
  • The precise electrophysiological effects of imeglimin on β cells are not fully understood.

Purpose of the Study:

  • To investigate the impact of imeglimin on β-cell electroactivity and insulin secretion dynamics.
  • To elucidate the mechanisms by which imeglimin influences islet function.

Main Methods:

  • Utilized microelectrode array (MEA) recordings to assess islet electrophysiology.
  • Employed a plasma membrane potential indicator (PMPI) to measure membrane potential changes.
  • Quantified insulin release and analyzed MEA-derived parameters like the fraction of the plateau phase (FOPP).

Main Results:

  • Imeglimin significantly augmented first-phase insulin release.
  • Imeglimin increased the FOPP, indicating enhanced secretory competence.
  • PMPI fluorescence showed imeglimin potentiated high-glucose-induced membrane depolarization in islets.

Conclusions:

  • Imeglimin enhances GSIS by increasing β-cell electroactivity.
  • The drug facilitates depolarization and improves insulin secretory dynamics at the islet level.
  • Imeglimin shows potential as an effective therapeutic agent for type 2 diabetes by modulating islet cell function.

Keywords:
ImegliminInsulin secretionMicroelectrode array

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