Roscovitine Attenuates Microglia Activation and Monocyte Infiltration via p38 MAPK Inhibition in the Rat Frontoparietal Cortex Following Status Epilepticus

Cells. 2019 Jul 19;8(7):746. doi: 10.3390/cells8070746.

Abstract

Under physiological conditions, microglia are unique immune cells resident in the brain that is isolated from the systemic immune system by brain-blood barrier. Following status epilepticus (SE, a prolonged seizure activity), microglia are rapidly activated and blood-derived monocytes that infiltrate the brain; therefore, the regulations of microglia activation and monocyte infiltration are one of the primary therapeutic strategies for inhibition of undesirable consequences from SE. Roscovitine, a potent (but not selective) cyclin-dependent kinase 5 (CDK5) inhibitor, has been found to exert anti-inflammatory and microglia-inhibiting actions in several in vivo models, although the underlying mechanisms have not been clarified. In the present study, roscovitine attenuated SE-induces monocyte infiltration without vasogenic edema formation in the frontoparietal cortex (FPC), accompanied by reducing expressions of monocyte chemotactic protein-1 (MCP-1) and lysosome-associated membrane protein 1 (LAMP1) in resident microglia, while it did not affect microglia transformation to amoeboid form. Furthermore, roscovitine ameliorated the up-regulation of p38 mitogen-activated protein kinase (p38 MAPK) phosphorylation, but not nuclear factor-κB-S276 phosphorylation. Similar to roscovitine, SB202190, a p38 MAPK inhibitor, mitigated monocyte infiltration and microglial expressions of MCP-1 and LAMP1 in the FPC following SE. Therefore, these findings suggest for the first time that roscovitine may inhibit SE-induced neuroinflammation via regulating p38 MAPK-mediated microglial responses.

Keywords: CCR2; CD68; IB4; Iba-1; LAMP1; NFκB; SB202190; epilepsy; seizure.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blood-Brain Barrier
  • Chemokine CCL2 / metabolism
  • Frontal Lobe / drug effects
  • Lysosomal Membrane Proteins / metabolism
  • Male
  • Microglia / drug effects*
  • Microglia / metabolism
  • Monocytes / cytology
  • Monocytes / drug effects*
  • Monocytes / metabolism
  • Rats
  • Rats, Sprague-Dawley
  • Roscovitine* / pharmacokinetics
  • Roscovitine* / pharmacology
  • Roscovitine* / therapeutic use
  • Status Epilepticus / drug therapy*
  • p38 Mitogen-Activated Protein Kinases / metabolism*

Substances

  • Ccl2 protein, rat
  • Chemokine CCL2
  • Lamp1 protein, rat
  • Lysosomal Membrane Proteins
  • Roscovitine
  • p38 Mitogen-Activated Protein Kinases