Nebivolol elicits a neuroprotective effect in the cuprizone model of multiple sclerosis in mice: emphasis on M1/M2 polarization and inhibition of NLRP3 inflammasome activation

Inflammopharmacology. 2022 Dec;30(6):2197-2209. doi: 10.1007/s10787-022-01045-4. Epub 2022 Aug 10.

Abstract

Background and aim: Multiple sclerosis (MS) is a demyelinating neurodegenerative inflammatory disease affecting mainly young adults. Microgliosis-derived neuroinflammation represents a key hallmark in MS pathology and progression. Nebivolol (Neb) demonstrated antioxidant, anti-inflammatory and neuroprotective properties in several brain pathologies. This study was conducted to investigate the potential neuroprotective effect of Neb in the cuprizone (Cup) model of MS.

Methods: C57Bl/6 mice were fed 0.2% Cup mixed into rodent chow for 5 weeks. Neb (5 and 10 mg/kg/day) was administered by oral gavage during the last 2 weeks.

Results: Neb prevented Cup-induced weight loss and motor deficits as evidenced by increased latency to fall in the rotarod test and enhanced locomotor activity as compared to Cup-intoxicated mice. Neb reversed Cup-induced demyelination as confirmed by Luxol fast blue staining and myelin basic protein western blotting. Administration of Neb modulated microglial activation status by suppressing M1 markers (Iba-1, CD86, iNOS, NO and TNF-α) and increasing M2 markers (Arg-1 and IL-10) as compared to Cup-fed mice. Furthermore, Neb hindered NLRP3/caspase-1/IL-18 inflammatory cascade and alleviated oxidative stress by reducing lipid peroxidation, as well as increasing catalase and superoxide dismutase activities.

Conclusion: These findings suggest the potential neuroprotective effect of Neb in the Cup-induced model of MS in mice, at least partially by virtue of shifting microglia towards M2 phenotype, mitigation of NLRP3 inflammasome activation and alleviation of oxidative stress.

Keywords: Cuprizone; M1/M2 polarization; Multiple sclerosis; NLRP3; Nebivolol.

MeSH terms

  • Animals
  • Cell Polarity
  • Cuprizone / adverse effects
  • Demyelinating Diseases* / chemically induced
  • Demyelinating Diseases* / drug therapy
  • Demyelinating Diseases* / metabolism
  • Disease Models, Animal
  • Inflammasomes / metabolism
  • Macrophages
  • Mice
  • Mice, Inbred C57BL
  • Microglia
  • Multiple Sclerosis* / drug therapy
  • Multiple Sclerosis* / metabolism
  • NLR Family, Pyrin Domain-Containing 3 Protein / metabolism
  • Nebivolol* / pharmacology
  • Neuroprotective Agents* / pharmacology

Substances

  • Cuprizone
  • Inflammasomes
  • Nebivolol
  • Neuroprotective Agents
  • NLR Family, Pyrin Domain-Containing 3 Protein
  • Nlrp3 protein, mouse