Nestorone® , a 19nor-progesterone derivative boosts remyelination in an animal model of demyelination

CNS Neurosci Ther. 2021 Apr;27(4):464-469. doi: 10.1111/cns.13538. Epub 2020 Dec 24.

Abstract

Introduction: We previously showed that Nestorone® (NES), a synthetic progestin structurally related to progesterone, stimulated remyelination of the corpus callosum in a Cuprizone (CUP) mouse model of demyelination in intact females by promoting replenishment with mature oligodendrocytes (OL) (Glia. 2015;63:104-117). Here, we further investigated the underlying mechanisms of this promyelinating effect.

Methods: We explored whether NES, applied subcutaneously through Alzet mini-osmotic pumps, regulates specific transcription factors involved in oligodendrocyte progenitor cell (OPC) proliferation and their differentiation into mature OL, using RT-qPCR and Western Blot analysis.

Results: Our present data show that in comparison to controls, a one-week treatment with NES, through Alzet mini-osmotic pumps, enhanced the production of three relevant transcription factor mRNAs encoding Olig2, Myt1, and Sox17. After 3 weeks, NES treatment reversed the effect of CUP on the levels of corresponding Olig2, Myt1, and Sox17 proteins. Moreover, in mice receiving NES + Estradiol (E2) co-treatment, levels of Olig2, Myt1, and Sox17 proteins did not change as compared to NES alone.

Conclusion: NES alone or with E2 increased the levels of transcription factors, essential for myelin synthesis.

Keywords: estradiol; multiple sclerosis; nestorone; oligodendrocytes; remyelination.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Demyelinating Diseases / drug therapy*
  • Demyelinating Diseases / metabolism
  • Disease Models, Animal*
  • Female
  • Mice
  • Mice, Inbred C57BL
  • Myelin Sheath / drug effects*
  • Myelin Sheath / metabolism
  • Norprogesterones / pharmacology
  • Norprogesterones / therapeutic use*
  • Remyelination / drug effects*
  • Remyelination / physiology

Substances

  • Norprogesterones
  • ST 1435