Laquinimod exerts anti-inflammatory and antiapoptotic effects in retinal ischemia/reperfusion injury

Int Immunopharmacol. 2020 Nov:88:106989. doi: 10.1016/j.intimp.2020.106989. Epub 2020 Sep 18.

Abstract

Retinal ischemia/reperfusion (I/R) occurs in various vision disabled ocular diseases, involved in acute glaucoma, diabetic retinopathy, ischemic optic neuropathy, hypertensive retinopathy and retinal vascular occlusion. Laquinimod (LQ), a new type of immunosuppressant, has been reported to exert anti-inflammatory effects on autoimmune diseases. This research aims to investigate the protective effect of LQ on I/R damage by focusing on inhibiting dysregulated neuroinflammation and neuronal apoptosis. In our study, mice were treated with LQ after high intraocular pressure (IOP)-induced retinal I/R injury. The data showed that LQ significantly attenuated high IOP-induced retinal ganglion cell (RGC) death and inner plexiform layer (IPL) thinning and inhibited microglial activation. The results of qRT-PCR, flow cytometry and Luminex multiplex assays demonstrated the anti-inflammatory action of LQ in BV2 cells stimulated with lipopolysaccharide (LPS). In addition, primary RGC apoptosis induced by oxygen-glucose deprivation/reperfusion (OGD/R) was also directly suppressed by LQ. Importantly, LQ inhibited the expression of cleaved caspase-8 and the downstream NLRP3 inflammasome and IL-1β. In conclusion, our findings offer the first evidence that LQ treatment prevents retinal I/R damage. Furthermore, LQ could directly inhibit RGC apoptosis. Caspase-8 activation and subsequent inflammation can also be suppressed by LQ, which suggests that LQ may act through inhibiting the caspase-8 pathway. This study demonstrates a new mechanism of LQ and provides beneficial preclinical data for the clinical application of LQ.

Keywords: Apoptosis; Caspase-8; Ischemia reperfusion; Laquinimod; Laquinimod (PubChem CID: 54677946); Microglia; Neuroinflammation.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / pharmacology*
  • Apoptosis / drug effects*
  • Cells, Cultured
  • Cytokines / genetics
  • Cytokines / metabolism
  • Inflammation / drug therapy
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Quinolones / pharmacology*
  • Reperfusion Injury*
  • Retina / pathology
  • Retinal Diseases / drug therapy*
  • Retinal Diseases / pathology
  • Retinal Neurons / drug effects
  • Retinal Vessels

Substances

  • Anti-Inflammatory Agents
  • Cytokines
  • Quinolones
  • laquinimod