11β-HSD1 is the major regulator of the tissue-specific effects of circulating glucocorticoid excess

Proc Natl Acad Sci U S A. 2014 Jun 17;111(24):E2482-91. doi: 10.1073/pnas.1323681111. Epub 2014 Jun 2.

Abstract

The adverse metabolic effects of prescribed and endogenous glucocorticoid (GC) excess, Cushing syndrome, create a significant health burden. We found that tissue regeneration of GCs by 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), rather than circulating delivery, is critical to developing the phenotype of GC excess; 11β-HSD1 KO mice with circulating GC excess are protected from the glucose intolerance, hyperinsulinemia, hepatic steatosis, adiposity, hypertension, myopathy, and dermal atrophy of Cushing syndrome. Whereas liver-specific 11β-HSD1 KO mice developed a full Cushingoid phenotype, adipose-specific 11β-HSD1 KO mice were protected from hepatic steatosis and circulating fatty acid excess. These data challenge our current view of GC action, demonstrating 11β-HSD1, particularly in adipose tissue, is key to the development of the adverse metabolic profile associated with circulating GC excess, offering 11β-HSD1 inhibition as a previously unidentified approach to treat Cushing syndrome.

Keywords: HSD11b1; cortisol; endocrinology; hypercortisolemia; steroids.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 11-beta-Hydroxysteroid Dehydrogenase Type 1 / genetics
  • 11-beta-Hydroxysteroid Dehydrogenase Type 1 / metabolism*
  • Adipose Tissue / metabolism*
  • Animals
  • Anti-Inflammatory Agents / chemistry
  • Blood Pressure
  • Cushing Syndrome / blood*
  • Cushing Syndrome / genetics*
  • Disease Models, Animal
  • Fatty Acids, Nonesterified / blood
  • Gene Expression Regulation
  • Glucocorticoids / blood*
  • Glucose Intolerance
  • Glucose Tolerance Test
  • Hydrocortisone / blood*
  • Liver / metabolism
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Regeneration / drug effects
  • Triglycerides / blood

Substances

  • Anti-Inflammatory Agents
  • Fatty Acids, Nonesterified
  • Glucocorticoids
  • Triglycerides
  • 11-beta-Hydroxysteroid Dehydrogenase Type 1
  • Hydrocortisone