Neuroprotective effect of epalrestat mediated through oxidative stress markers, cytokines and TAU protein levels in diabetic rats

Life Sci. 2018 Aug 15:207:364-371. doi: 10.1016/j.lfs.2018.06.021. Epub 2018 Jun 21.

Abstract

Aims: Type-2 diabetes mellitus (DM) is associated with cognitive impairment. Increasing evidence establishes that neuro-inflammatory and oxidative stress condition plays a main role in the development of neurodegeneration. Epalrestat, an aldose reductase inhibitor is commonly prescribed for the treatment of diabetic peripheral neuropathy. Its beneficial effects for antioxidant, anti-inflammatory potential and being rhodanine structure containing compound suggests possible role for treatment of DM associated with cognitive dysfunction.

Main methods: In the present study, we evaluated the effect of epalrestat (54, 27, 13.5 mg/kg, p.o.) and donepezil (1 mg/kg, p.o.) on Tau protein levels, oxidative stress and inflammatory markers in high fat diet (HFD) and Streptozotocin (STZ; 35 mg/kg, i.p.) induced cognitive impairment in diabetic rats.

Key findings: The epalrestat - 54, 27 mg/kg p.o. and donepezil treatment significantly increased CAT (p < 0.001, p < 0.01, p < 0.001) and GSH (p < 0.001, p < 0.01, p < 0.001) activities respectively as compared to diabetic control rats. In addition, similar dose of epalrestat treatment indicated considerably lowered TAU protein levels (p < 0.001, p < 0.05) while no significant effect was noted with donepezil. These treatments significantly decreased gene expression of TNF-α (1.6, 1.6, 1.7 fold change) and IL-6 (2.5, 1.9, 1.7 fold change). Histopathological examination indicated that epalrestat could attenuate apoptosis of neurons, vacuolations and clumped processes, disorganization and thinning of all the layers.

Significance: Our findings suggest that diabetic rats treated with epalrestat could ameliorate the cognition deficits and might act as a beneficial agent for prevention and treatment of cognitive impairment in diabetes.

Keywords: Cognitive impairment; Cytokine; Epalrestat; Oxidative stress; TAU protein; Type-2 diabetes.

MeSH terms

  • Animals
  • Antioxidants / chemistry
  • Blood Glucose / metabolism
  • Body Weight
  • Cognition Disorders / drug therapy
  • Cytokines / metabolism
  • Diabetes Mellitus, Experimental / drug therapy*
  • Diabetic Neuropathies / drug therapy*
  • Diet, High-Fat
  • Hippocampus / metabolism
  • Inflammation
  • Male
  • Neuroprotective Agents / pharmacology*
  • Oxidative Stress*
  • Rats
  • Rats, Wistar
  • Rhodanine / analogs & derivatives*
  • Rhodanine / chemistry
  • Rhodanine / pharmacology
  • Thiazolidines / pharmacology*
  • tau Proteins / metabolism*

Substances

  • Antioxidants
  • Blood Glucose
  • Cytokines
  • Neuroprotective Agents
  • Thiazolidines
  • tau Proteins
  • epalrestat
  • Rhodanine