Glucocorticoid chronopharmacology promotes glucose metabolism in heart through a cardiomyocyte-autonomous transactivation program

JCI Insight. 2024 Nov 22;9(22):e182599. doi: 10.1172/jci.insight.182599.

Abstract

Circadian time of intake gates the cardioprotective effects of glucocorticoid administration in both healthy and infarcted hearts. The cardiomyocyte-specific glucocorticoid receptor (GR) and its cofactor, Krüppel-like factor 15 (KLF15), play critical roles in maintaining normal heart function in the long term and serve as pleiotropic regulators of cardiac metabolism. Despite this understanding, the cardiomyocyte-autonomous metabolic targets influenced by the concerted epigenetic action of the GR/KLF15 axis remain undefined. Here, we demonstrated the critical roles of the cardiomyocyte-specific GR and KLF15 in orchestrating a circadian-dependent glucose oxidation program within the heart. Combining integrated transcriptomics and epigenomics with cardiomyocyte-specific inducible ablation of GR or KLF15, we identified their synergistic role in the activation of adiponectin receptor expression (Adipor1) and the mitochondrial pyruvate complex (Mpc1/2), thereby enhancing insulin-stimulated glucose uptake and pyruvate oxidation. Furthermore, in obese diabetic (db/db) mice exhibiting insulin resistance and impaired glucose oxidation, light-phase prednisone administration, as opposed to dark-phase prednisone dosing, restored cardiomyocyte glucose oxidation and improved diastolic function. These effects were blocked by combined in vivo knockdown of GR and KLF15 levels in db/db hearts. In summary, this study leveraged the circadian-dependent cardioprotective effects of glucocorticoids to identify cardiomyocyte-autonomous targets for the GR/KLF15 axis in glucose metabolism.

Keywords: Cardiology; Epigenetics; Glucose metabolism; Heart failure; Metabolism.

MeSH terms

  • Animals
  • Circadian Rhythm / drug effects
  • Glucocorticoids* / pharmacology
  • Glucose* / metabolism
  • Insulin Resistance
  • Kruppel-Like Transcription Factors* / genetics
  • Kruppel-Like Transcription Factors* / metabolism
  • Male
  • Mice
  • Myocytes, Cardiac* / drug effects
  • Myocytes, Cardiac* / metabolism
  • Receptors, Glucocorticoid* / metabolism
  • Transcriptional Activation / drug effects

Substances

  • Glucose
  • Kruppel-Like Transcription Factors
  • Klf15 protein, mouse
  • Receptors, Glucocorticoid
  • Glucocorticoids