Sativex® effects on promoter methylation and on CNR1/CNR2 expression in peripheral blood mononuclear cells of progressive multiple sclerosis patients

J Neurol Sci. 2017 Aug 15:379:298-303. doi: 10.1016/j.jns.2017.06.017. Epub 2017 Jun 15.

Abstract

Multiple sclerosis (MS) is a chronic demyelinating central nervous system (CNS) disease that involve oligodendrocyte loss and failure to remyelinate damaged brain areas causing a progressive neurological disability. Studies in MS mouse model suggest that cannabinoids ameliorate symptoms as spasticity, tremor and pain reducing inflammation via cannabinoid-mediated system. The aim of our study is to investigate the changes in cannabinoid type 1 (CNR1) and 2 (CNR2) receptors mRNA expression levels and promoter methylation in peripheral blood mononuclear cells (PBMCs) of MS secondary progressive (MSS-SP) patients treated with Sativex®. Our cohort included MSS-SP patients, that at the time of Sativex® treatment, are treated (n=7), not treated (n=11) or that had terminated interferon-β-1b (IFN-β-1b) therapy (n=12). By Methylation Sensitive High Resolution Melting (MS-HRM), we characterized the methylation profile of CNR1 and CNR2 promoter region, while the relative mRNA transcript levels of these two genes were evaluated in the same samples by Quantitative Real-Time PCR (qRT-PCR) analysis. We did not find different pattern of cytosine-phosphate-guanine (CpG) methylation in the CNR1/CNR2 promoter region of all MSS-SP patients treated with Sativex®. In addition, CNR1 and CNR2 expression did not significantly differ in MSS-SP patients not treated with IFN-β-1b vs. them that have suspended, while in MSS-SP patients treated with IFN-β-1b during Sativex® therapy we found a specific decrease of the CNR2 expression levels. These results suggest that the different expression of cannabinoid receptors by Sativex® treatment in leukocytes might be regulated through a molecular mechanism that involve interferon modulation.

Keywords: Cannabinoid receptor type 1; Cannabinoid receptor type 2; Interferon-β-1b; Methylation; Sativex®.

Publication types

  • Controlled Clinical Trial

MeSH terms

  • Cannabidiol / pharmacology*
  • Dronabinol / pharmacology*
  • Drug Combinations
  • Female
  • Humans
  • Interferon beta-1b / pharmacology
  • Interferon beta-1b / therapeutic use
  • Leukocytes, Mononuclear / metabolism*
  • Male
  • Methylation / drug effects*
  • Middle Aged
  • Multiple Sclerosis, Chronic Progressive / genetics*
  • Promoter Regions, Genetic / genetics*
  • Receptor, Cannabinoid, CB1 / genetics*
  • Receptor, Cannabinoid, CB2 / genetics*

Substances

  • CNR1 protein, human
  • CNR2 protein, human
  • Drug Combinations
  • Receptor, Cannabinoid, CB1
  • Receptor, Cannabinoid, CB2
  • Interferon beta-1b
  • Cannabidiol
  • Dronabinol
  • nabiximols