Protection of MPTP-induced neuroinflammation and neurodegeneration by rotigotine-loaded microspheres

Life Sci. 2015 Mar 1:124:136-43. doi: 10.1016/j.lfs.2015.01.014. Epub 2015 Jan 30.

Abstract

Aims: The aim of the study is to evaluate the neuroprotective effects of continuous dopaminergic stimulation (CDS) by rotigotine-loaded microspheres (RoMS) in a mouse model of MPTP-induced Parkinson's disease (PD) and to elucidate the potential mechanism underlying these effects.

Main methods: Male C57BL/6 mice were treated either intramuscularly once with RoMS or twice daily for two weeks with rotigotine, and from the 9th day, MPTP (30 mg/kg, i.p.) was injected for the last 5 days. Following treatment, Parkinsonism scores were calculated and oxidative stress-related indicators in the striatum were performed. Neuroinflammatory cytokines, such as tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), and interleukin-6 (IL-6) were detected in the striatum. Expression of apoptosis-related proteins B-cell leukemia/lymphoma 2 (Bcl-2) and Bcl-2-associated X protein (BAX) was measured in the striatum by Western blot. Nigral tyrosine hydroxylase (TH)-positive neurons and microglial cell markers, i.e., ionized calcium binding adaptor molecule-1 (Iba-1) and neuronal synaptosomes, were quantified to assess the neuroprotective efficacy of RoMS.

Key findings: The administration of rotigotine significantly improved the Parkinsonism score, protected dopaminergic neurons with antioxidants, reduced microglial cell activation and the release of neuroinflammatory cytokines, and balanced the expression of Bcl-2 and Bax in MPTP-treated mice. Interestingly, the neuroprotective properties of rotigotine were remarkably amplified by CDS treatment with RoMS.

Significance: These results suggest that CDS therapy can play a neuroprotective role in an MPTP mouse model. Neuroprotective disease-modifying therapy may have the potential benefits of early treatment by normalizing compensatory mechanisms and may also help to delay dyskinesia in the later stages of PD.

Keywords: Continuous dopaminergic stimulation; Neuroprotection; Parkinson's disease; Rotigotine-loaded microspheres.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antioxidants / metabolism
  • Blotting, Western
  • Corpus Striatum / drug effects
  • Corpus Striatum / pathology
  • Cytokines / metabolism
  • Disease Models, Animal
  • Dopamine Agonists / pharmacology*
  • Dopaminergic Neurons / drug effects
  • Dopaminergic Neurons / pathology
  • Gene Expression Regulation / drug effects
  • MPTP Poisoning / prevention & control*
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Microspheres
  • Neuroprotective Agents / pharmacology*
  • Oxidative Stress / drug effects
  • Parkinsonian Disorders / drug therapy*
  • Parkinsonian Disorders / physiopathology
  • Tetrahydronaphthalenes / pharmacology*
  • Thiophenes / pharmacology*

Substances

  • Antioxidants
  • Cytokines
  • Dopamine Agonists
  • Neuroprotective Agents
  • Tetrahydronaphthalenes
  • Thiophenes
  • rotigotine