Reno-protective effect of linagliptin against gentamycin nephrotoxicity in rats

Pharmacol Rep. 2019 Dec;71(6):1133-1139. doi: 10.1016/j.pharep.2019.06.017. Epub 2019 Jul 2.

Abstract

Background: Recent studies demonstrated the reno-protective effects of two dipeptidyl peptidase-4 (DPP-4) inhibitors, saxagliptin and sitagliptin, against gentamycin-induced renal injury. However, none of these studies investigated whether renal DPP-4 contributes to the pathogenesis of this nephrotoxicity or not. This prompted us to test this hypothesis and to assess, for the first time, the potential reno-protective effect of linagliptin and whether this action is related or not to DPP-4 inhibition. Lingliptin was chosen since it is mainly excreted through a non-renal pathway and can therefore be used safely in individuals with renal injury.

Methods: Male Sprague-Dawley rats were administered gentamycin (100 mg/kg/day, ip for 10 days) alone or combined with linagliptin (3 mg/kg/day, orally for 14 days). Gentamycin was administered once daily during the last ten days of the linagliptin treatment.

Results: Linagliptin administration ameliorated gentamycin-induced renal injury and restored renal functional, oxidative, inflammatory, apoptotic and histopathological changes. Furthermore, the current study highlighted the role of increased plasma and renal DPP-4 in the pathogenesis of gentamycin renal insults and showed that the potential reno-protective effect of linagliptin is partly, mediated via inhibition of DPP-4, in addition to other antioxidant, anti-inflammatory and anti-apoptotic actions.

Conclusion: Linagliptin may serve as a beneficial adjutant to reduce gentamycin-induced renal injury.

Keywords: Dipeptidyl peptidase-4; Gentamycin; Linagliptin; Nephrotoxicity.

MeSH terms

  • Adamantane / analogs & derivatives
  • Adamantane / pharmacology
  • Animals
  • Dipeptides / pharmacology
  • Dipeptidyl Peptidase 4 / metabolism
  • Dipeptidyl-Peptidase IV Inhibitors / pharmacology
  • Disease Models, Animal
  • Gentamicins / pharmacology*
  • Kidney / drug effects
  • Kidney / metabolism
  • Kidney Diseases / chemically induced*
  • Kidney Diseases / drug therapy*
  • Kidney Diseases / metabolism
  • Linagliptin / pharmacology*
  • Male
  • Rats
  • Rats, Sprague-Dawley
  • Sitagliptin Phosphate / pharmacology

Substances

  • Dipeptides
  • Dipeptidyl-Peptidase IV Inhibitors
  • Gentamicins
  • Linagliptin
  • saxagliptin
  • Dipeptidyl Peptidase 4
  • Adamantane
  • Sitagliptin Phosphate