Drug Testing for Residual Progression of Diabetic Kidney Disease in Mice Beyond Therapy with Metformin, Ramipril, and Empagliflozin

J Am Soc Nephrol. 2020 Aug;31(8):1729-1745. doi: 10.1681/ASN.2019070703. Epub 2020 Jun 23.

Abstract

Background: Progression of CKD in type 2 diabetes, despite dual inhibition of sodium-glucose transporter-2 and the renin-angiotensin system, remains a concern. Bromoindirubin-3'-oxime (BIO), previously reported to promote podocyte survival and regeneration, is a candidate additional drug to elicit renoprotective effects beyond therapy with metformin, ramipril, and empagliflozin (MRE). Evaluating a drug with standard therapeutics more closely mimics the clinical setting than evaluating the drug alone.

Methods: Uninephrectomized BKS-Lepr-/- (db/db) mice treated with or without MRE served as a model of progressive CKD in type 2 diabetes. Mice on or off MRE were randomized to only 4 weeks of add-on BIO or vehicle. The primary end point was slope of GFR (ΔGFR).

Results: Four weeks of MRE treatment alone did not affect ΔGFR, but significantly attenuated hyperglycemia, albuminuria, and glomerulosclerosis and increased podocyte filtration slit density, as assessed by STED super-resolution microscopy upon tissue clearing. BIO alone improved albuminuria, podocyte density in superficial and juxtamedullary nephrons, and podocyte filtration slit density. MRE+BIO combination therapy had additive protective effects on ΔGFR, glomerulosclerosis, podocyte density in juxtamedullary nephrons, and filtration slit density.

Conclusions: Add-on treatment with BIO for only 4 weeks attenuates progression of CKD beyond MRE therapy in mice with type 2 diabetes. Additional drug combinations may help to further delay ESKD in type 2 diabetes.

Keywords: diabetic kidney disease; diabetic nephropathy; glomerulosclerosis; regeneration; translational research.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzhydryl Compounds / administration & dosage*
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Diabetes Mellitus, Type 2 / physiopathology
  • Diabetic Nephropathies / physiopathology
  • Diabetic Nephropathies / prevention & control*
  • Disease Progression
  • Drug Therapy, Combination
  • Glomerular Filtration Rate / drug effects
  • Glucosides / administration & dosage*
  • Glycogen Synthase Kinase 3 beta / antagonists & inhibitors
  • Indoles / therapeutic use*
  • Kidney / drug effects
  • Metformin / administration & dosage*
  • Mice
  • Oximes / therapeutic use*
  • Podocytes / drug effects
  • Ramipril / administration & dosage*

Substances

  • 6-bromoindirubin-3'-oxime
  • Benzhydryl Compounds
  • Glucosides
  • Indoles
  • Oximes
  • Metformin
  • Glycogen Synthase Kinase 3 beta
  • empagliflozin
  • Ramipril