FTY720 ameliorates acute ischemic stroke in mice by reducing thrombo-inflammation but not by direct neuroprotection

Stroke. 2013 Nov;44(11):3202-10. doi: 10.1161/STROKEAHA.113.002880. Epub 2013 Sep 12.

Abstract

Background and purpose: Lymphocytes are important players in the pathophysiology of acute ischemic stroke. The interaction of lymphocytes with endothelial cells and platelets, termed thrombo-inflammation, fosters microvascular dysfunction and secondary infarct growth. FTY720, a sphingosine-1-phosphate receptor modulator, blocks the egress of lymphocytes from lymphoid organs and has been shown to reduce ischemic neurodegeneration; however, the underlying mechanisms are unclear. We investigated the mode of FTY720 action in models of cerebral ischemia.

Methods: Transient middle cerebral artery occlusion (tMCAO) was induced in wild-type and lymphocyte-deficient Rag1(-/-) mice treated with FTY720 (1 mg/kg) or vehicle immediately before reperfusion. Stroke outcome was assessed 24 hours later. Immune cells in the blood and brain were counted by flow cytometry. The integrity of the blood-brain barrier was analyzed using Evans Blue dye. Thrombus formation was determined by immunohistochemistry and Western blot, and was correlated with cerebral perfusion.

Results: FTY720 significantly reduced stroke size and improved functional outcome in wild-type mice on day 1 and day 3 after transient middle cerebral artery occlusion. This protective effect was lost in lymphocyte-deficient Rag1(-/-) mice and in cultured neurons subjected to hypoxia. Less lymphocytes were present in the cerebral vasculature of FTY720-treated wild-type mice, which in turn reduced thrombosis and increased cerebral perfusion. In contrast, FTY720 was unable to prevent blood-brain barrier breakdown and transendothelial immune cell trafficking after transient middle cerebral artery occlusion.

Conclusions: Induction of lymphocytopenia and concomitant reduction of microvascular thrombosis are key modes of FTY720 action in stroke. In contrast, our findings in Rag1(-/-) mice and cultured neurons argue against direct neuroprotective effects of FTY720.

Keywords: FTY720; MCAO; inflammation; ischemic stroke; microvascular dysfunction; thrombo-inflammation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Brain Ischemia / therapy*
  • Enzyme Inhibitors / pharmacology
  • Fingolimod Hydrochloride
  • Homeodomain Proteins / genetics
  • Hypoxia
  • Immunosuppressive Agents / pharmacology*
  • Inflammation / therapy*
  • Lymphocytes / drug effects
  • Lymphopenia / pathology
  • Male
  • Mice
  • Mice, Transgenic
  • Middle Cerebral Artery / pathology
  • Neurons / pathology
  • Neuroprotective Agents / therapeutic use
  • Propylene Glycols / pharmacology*
  • Sphingosine / analogs & derivatives*
  • Sphingosine / pharmacology
  • Stroke / therapy*
  • Thrombosis / therapy*

Substances

  • Enzyme Inhibitors
  • Homeodomain Proteins
  • Immunosuppressive Agents
  • Neuroprotective Agents
  • Propylene Glycols
  • RAG-1 protein
  • Fingolimod Hydrochloride
  • Sphingosine