Differential Responses to Sigma-1 or Sigma-2 Receptor Ablation in Adiposity, Fat Oxidation, and Sexual Dimorphism

Int J Mol Sci. 2022 Sep 16;23(18):10846. doi: 10.3390/ijms231810846.

Abstract

Obesity is increasing at epidemic rates across the US and worldwide, as are its co-morbidities, including type-2 diabetes and cardiovascular disease. Thus, targeted interventions to reduce the prevalence of obesity are of the utmost importance. The sigma-1 receptor (S1R) and sigma-2 receptor (S2R; encoded by Tmem97) belong to the same class of drug-binding sites, yet they are genetically distinct. There are multiple ongoing clinical trials focused on sigma receptors, targeting diseases ranging from Alzheimer's disease through chronic pain to COVID-19. However, little is known regarding their gene-specific role in obesity. In this study, we measured body composition, used a comprehensive laboratory-animal monitoring system, and determined the glucose and insulin tolerance in mice fed a high-fat diet. Compared to Sigmar1+/+ mice of the same sex, the male and female Sigmar1-/- mice had lower fat mass (17% and 12% lower, respectively), and elevated lean mass (16% and 10% higher, respectively), but S1R ablation had no effect on their metabolism. The male Tmem97-/- mice exhibited 7% lower fat mass, 8% higher lean mass, increased volumes of O2 and CO2, a decreased respiratory exchange ratio indicating elevated fatty-acid oxidation, and improved insulin tolerance, compared to the male Tmem97+/+ mice. There were no changes in any of these parameters in the female Tmem97-/- mice. Together, these data indicate that the S1R ablation in male and female mice or the S2R ablation in male mice protects against diet-induced adiposity, and that S2R ablation, but not S1R deletion, improves insulin tolerance and enhances fatty-acid oxidation in male mice. Further mechanistic investigations may lead to translational strategies to target differential S1R/S2R regulations and sexual dimorphism for precision treatments of obesity.

Keywords: fat mass and lean mass; fatty acid oxidation; insulin tolerance; obesity; sexual dimorphism; sigma receptors.

MeSH terms

  • Adiposity
  • Animals
  • COVID-19*
  • Carbon Dioxide / pharmacology
  • Diet, High-Fat
  • Female
  • Glucose / pharmacology
  • Insulins* / metabolism
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Obesity / genetics
  • Receptors, sigma / genetics
  • Receptors, sigma / metabolism*
  • Sex Characteristics
  • Sigma-1 Receptor

Substances

  • Insulins
  • Receptors, sigma
  • sigma-2 receptor
  • Carbon Dioxide
  • Glucose