Single and Combined Impact of Semaglutide, Tirzepatide, and Metformin on β-Cell Maintenance and Function Under High-Glucose-High-Lipid Conditions: A Comparative Study

Int J Mol Sci. 2025 Jan 6;26(1):421. doi: 10.3390/ijms26010421.

Abstract

Type 2 diabetes (T2D), the most common form, is marked by insulin resistance and β-cell failure. β-cell dysfunction under high-glucose-high-lipid (HG-HL) conditions is a key contributor to the progression of T2D. This study evaluates the comparative effects of 10 nM semaglutide, 10 nM tirzepatide, and 1 mM metformin, both alone and in combination, on INS-1 β-cell maintenance and function under HG-HL conditions. INS-1 cells were pretreated for 2 h with single doses of metformin (1 mM), semaglutide (10 nM), tirzepatide (10 nM), or combinations of 1 mM metformin with either 10 nM semaglutide or 10 nM tirzepatide, followed by 48 h of HG-HL stimulation. The results indicate that combining 1 mM metformin with either 10 nM semaglutide or 10 nM tirzepatide significantly enhances the effects of 10 nM semaglutide and 10 nM tirzepatide on HG-HL-induced apoptosis and dysregulated cell cycle. Specifically, the combination treatments demonstrated superior restoration of glucose-stimulated insulin secretion (GSIS) functionality compared to 1 mM metformin, 10 nM semaglutide, and 10 nM tirzepatide.

Keywords: HG-HL conditions; metformin; semaglutide; tirzepatide; β-cells.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Cell Line
  • Diabetes Mellitus, Type 2 / drug therapy
  • Diabetes Mellitus, Type 2 / metabolism
  • Gastric Inhibitory Polypeptide
  • Glucagon-Like Peptide-2 Receptor
  • Glucagon-Like Peptides* / pharmacology
  • Glucose* / metabolism
  • Humans
  • Hypoglycemic Agents / pharmacology
  • Insulin / metabolism
  • Insulin Secretion / drug effects
  • Insulin-Secreting Cells* / drug effects
  • Insulin-Secreting Cells* / metabolism
  • Lipids
  • Metformin* / pharmacology
  • Rats

Substances

  • Metformin
  • semaglutide
  • Glucagon-Like Peptides
  • Glucose
  • tirzepatide
  • Hypoglycemic Agents
  • Lipids
  • Insulin
  • Glucagon-Like Peptide-2 Receptor
  • Gastric Inhibitory Polypeptide

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