Therapeutic Effects of FK506 on IgA Nephropathy Rat

Kidney Blood Press Res. 2017;42(6):983-998. doi: 10.1159/000485346. Epub 2017 Nov 27.

Abstract

Background/aims: FK506 is an immunosuppressive drug and a calcineurin inhibitor that has been widely used in kidney disease in recent years. FK506 shows a wide range of biological and pharmaceutical effects; however, the mechanism of its anti- proliferative effect has not been well elucidated. An IgA nephropathy (IgAN) model was used to generate a mesangial cell proliferation model. This study aims to examine the effect of FK506 on IgAN rats and the underlying mechanisms.

Methods: Hematuria, proteinuria and renal function were measured. To observe the pathological conditions, we performed HE (hematoxylin - eosin) and PAS (periodic acid - schiff) staining. Transcription and protein expression levels were detected by qRT - PCR (quantitative real-time polymerase chain reaction) and Wb (western blotting). The location and semi-quantitative expression levels of TRPCs, CaN (Calcineurin) and α-SMA were examined by IHC (Immunohistochemical staining).

Results: We found that FK506 could improve hematuria, proteinuria and renal function, especially in the HF (high-dose FK506) groups. Renal pathological changes were ameliorated in the treatment groups. FK506 could significantly decrease TRPCs, CaN, phosphorylation of ERK1/2 and α-SMA expression.

Conclusion: Taken together, these results suggest that the therapeutic effect of FK506 on IgAN might be partially associated with the down-regulated expression of TRPC channels, CaN and phosphorylation of ERK1/2.

Keywords: Calcineurin; ERK1/2; Fk506; IgA nephropathy; TRPC.

MeSH terms

  • Animals
  • Calcineurin / genetics
  • Gene Expression
  • Glomerulonephritis, IGA / drug therapy*
  • Hematuria / diagnosis
  • Immunosuppressive Agents
  • MAP Kinase Signaling System
  • Phosphorylation
  • Proteinuria / diagnosis
  • Rats
  • TRPC Cation Channels / genetics
  • Tacrolimus / pharmacology
  • Tacrolimus / therapeutic use*

Substances

  • Immunosuppressive Agents
  • TRPC Cation Channels
  • Calcineurin
  • Tacrolimus