Combinatory FK506 and Minocycline Treatment Alleviates Prion-Induced Neurodegenerative Events via Caspase-Mediated MAPK-NRF2 Pathway

Int J Mol Sci. 2019 Mar 6;20(5):1144. doi: 10.3390/ijms20051144.

Abstract

Transcription factors play a significant role during the symptomatic onset and progression of prion diseases. We previously showed the immunomodulatory and nuclear factor of activated T cells' (NFAT) suppressive effects of an immunosuppressant, FK506, in the symptomatic stage and an antibiotic, minocycline, in the pre-symptomatic stage of prion infection in hamsters. Here we used for the first time, a combinatory FK506+minocycline treatment to test its transcriptional modulating effects in the symptomatic stage of prion infection. Our results indicate that prolonged treatment with FK506+minocycline was effective in alleviating astrogliosis and neuronal death triggered by misfolded prions. Specifically, the combinatory therapy with FK506+minocycline lowered the expression of the astrocytes activation marker GFAP and of the microglial activation marker IBA-1, subsequently reducing the level of pro-inflammatory cytokines interleukin 1 beta (IL-1β) and tumor necrosis factor alpha (TNF-α), and increasing the levels of anti-inflammatory cytokines IL-10 and IL-27. We further found that FK506+minocycline treatment inhibited mitogen-activated protein kinase (MAPK) p38 phosphorylation, NF-kB nuclear translocation, caspase expression, and enhanced phosphorylated cAMP response element-binding protein (pCREB) and phosphorylated Bcl2-associated death promoter (pBAD) levels to reduce cognitive impairment and apoptosis. Interestingly, FK506+minocycline reduced mitochondrial fragmentation and promoted nuclear factor⁻erythroid2-related factor-2 (NRF2)-heme oxygenase 1 (HO-1) pathway to enhance survival. Taken together, our results show that a therapeutic cocktail of FK506+minocycline is an attractive candidate for prolonged use in prion diseases and we encourage its further clinical development as a possible treatment for this disease.

Keywords: astrogliosis; heme oxygenase 1 (HO-1); nuclear factor kappa-b (NF-kB); nuclear factor of activated T-cells (NFAT); nuclear factor–erythroid2-related factor-2 (NRF2); phosphorylated Bcl2-associated death promoter (pBAD); phosphorylated cAMP response element-binding protein (pCREB); phosphorylated mitogen-activated protein kinase (MAPK) p38; transcription factors.

MeSH terms

  • Animals
  • Caspases / metabolism
  • Cell Death / drug effects
  • Cricetinae
  • Disease Models, Animal
  • Down-Regulation
  • Drug Therapy, Combination
  • Glial Fibrillary Acidic Protein / metabolism
  • Minocycline / administration & dosage*
  • Minocycline / pharmacology
  • Mitogen-Activated Protein Kinases / metabolism
  • NF-E2-Related Factor 2 / metabolism
  • Neurons / cytology
  • Neurons / drug effects
  • Prion Diseases / drug therapy*
  • Prion Diseases / immunology
  • Prion Diseases / metabolism
  • Signal Transduction / drug effects*
  • Tacrolimus / administration & dosage*
  • Tacrolimus / pharmacology

Substances

  • Glial Fibrillary Acidic Protein
  • NF-E2-Related Factor 2
  • Mitogen-Activated Protein Kinases
  • Caspases
  • Minocycline
  • Tacrolimus