Epimerase activity of the human 11beta-hydroxysteroid dehydrogenase type 1 on 7-hydroxylated C19-steroids

J Steroid Biochem Mol Biol. 2009 Mar;114(1-2):57-63. doi: 10.1016/j.jsbmb.2008.12.015. Epub 2009 Jan 9.

Abstract

Cytochrome P4507B1 7alpha-hydroxylates dehydroepiandrosterone (DHEA), epiandrosterone (EpiA) and 5alpha-androstane-3beta,17beta-diol (Adiol). 11beta-Hydroxysteroid dehydrogenase type 1 (11beta-HSD1) interconverts 7alpha- and 7beta-forms. Whether the interconversion proceeds through oxido-reductive steps or epimerase activity was investigated. Experiments using [(3)H]-labelled 7beta-hydroxy-DHEA, 7beta-hydroxy-EpiA and 7beta-hydroxy-Adiol showed the (3)H-label to accumulate in the 7-oxo-DHEA trap but not in 7-oxo-EpiA or 7-oxo-Adiol traps. Computed models of 7-oxygenated steroids docked in the active site of 11beta-HSD1 either in a flipped or turned form relative to cortisone and cortisol. 7-Oxo-steroid reduction in 7alpha- or 7beta-hydroxylated derivatives resulted from either turned or flipped forms. 11beta-HSD1 incubation in H(2)(18)O medium with each 7-hydroxysteroid did not incorporate (18)O in 7-hydroxylated derivatives of EpiA and Adiol independently of the cofactor used. Thus oxido-reductive steps apply for the interconversion of 7alpha- and 7beta-hydroxy-DHEA through 7-oxo-DHEA. Epimerization may proceed on the 7-hydroxylated derivatives of EpiA and Adiol through a mechanism involving the cofactor and Ser(170). The physiopathological importance of this epimerization process is related to 7beta-hydroxy-EpiA production and its effects in triggering the resolution of inflammation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 11-beta-Hydroxysteroid Dehydrogenase Type 1 / chemistry
  • 11-beta-Hydroxysteroid Dehydrogenase Type 1 / genetics
  • 11-beta-Hydroxysteroid Dehydrogenase Type 1 / metabolism*
  • Androstane-3,17-diol / chemistry
  • Androstane-3,17-diol / metabolism
  • Androsterone / chemistry
  • Androsterone / metabolism
  • Catalytic Domain
  • Cytochrome P450 Family 7
  • Dehydroepiandrosterone / chemistry
  • Dehydroepiandrosterone / metabolism
  • Humans
  • Hydroxylation
  • Molecular Structure
  • Oxidation-Reduction
  • Steroid Hydroxylases / genetics
  • Steroid Hydroxylases / metabolism*
  • Steroids* / chemistry
  • Steroids* / metabolism

Substances

  • Steroids
  • Androstane-3,17-diol
  • Dehydroepiandrosterone
  • Androsterone
  • 11-beta-Hydroxysteroid Dehydrogenase Type 1
  • Steroid Hydroxylases
  • Cytochrome P450 Family 7
  • CYP7B1 protein, human