Ameliorative effect of phosphodiesterase 4 and 5 inhibitors in deoxycorticosterone acetate-salt hypertensive uni-nephrectomized KKAy mice

FASEB J. 2020 Nov;34(11):14997-15014. doi: 10.1096/fj.202001084R. Epub 2020 Sep 16.

Abstract

Diabetic nephropathy (DN) is a leading cause of end-stage renal disease (ESRD). Hypertension increases kidney stress, which deteriorates function, and leads to peripheral renal vascular resistance. Long-term hypoperfusion promotes interstitial fibrosis and glomerular sclerosis, resulting in nephrosclerosis. Although hypertension and DN are frequent ESRD complications, relevant animal models remain unavailable. We generated a deoxycorticosterone acetate (DOCA)-salt hypertensive uni-nephrectomized (UNx) KKAy mouse model demonstrating hypertension, hyperglycemia, cardiac hypertrophy, kidney failure, increased urinary albumin creatinine ratio (UACR), and increased renal PDE4D and cardiac PDE5A mRNA levels. We hypothesized that the novel PDE4 selective inhibitor, compound A, and PDE5 inhibitor, sildenafil, exhibit nephroprotective, and cardioprotective effects in this new model. Compound A, sildenafil, and the angiotensin II receptor blocker, irbesartan, significantly reduced ventricular hypertrophy and pleural effusion volume. Meanwhile, compound A and sildenafil significantly suppressed the UACR, urinary kidney injury molecule-1, and monocyte chemoattractant protein-1 levels, as well as that of renal pro-fibrotic marker mRNAs, including collagen 1A1, fibronectin, and transforming growth factor-beta (TGF-β). Moreover, compound A significantly suppressed TGF-β-induced pro-fibrotic mRNA expression in vitro in all major kidney lesions, including within the glomerular mesangial region, podocytes, and epithelial region. Hence, PDE4 and PDE5 inhibitors may be promising treatments, in combination with irbesartan, for DN with hypertension as they demonstrate complementary mechanisms.

Keywords: deoxycorticosterone acetate-salt hypertensive KKAy mouse; diabetic nephropathy; hypertension; phosphodiesterase 4; phosphodiesterase 5; uni-nephrectomy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetates / pharmacology
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Cardiomegaly / chemically induced
  • Cardiomegaly / drug therapy*
  • Cardiomegaly / enzymology
  • Cardiomegaly / pathology
  • Cyclic Nucleotide Phosphodiesterases, Type 4 / chemistry
  • Cyclic Nucleotide Phosphodiesterases, Type 5 / chemistry
  • Desoxycorticosterone / toxicity*
  • Female
  • Hyperglycemia / chemically induced
  • Hyperglycemia / drug therapy*
  • Hyperglycemia / enzymology
  • Hyperglycemia / pathology
  • Hypertension / chemically induced
  • Hypertension / drug therapy*
  • Hypertension / enzymology
  • Hypertension / pathology
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Mineralocorticoids / toxicity
  • Phosphodiesterase 5 Inhibitors / pharmacology*
  • Renal Insufficiency / chemically induced
  • Renal Insufficiency / drug therapy*
  • Renal Insufficiency / enzymology
  • Renal Insufficiency / pathology
  • Sildenafil Citrate / pharmacology*
  • Sodium Chloride / toxicity
  • Tyramine / analogs & derivatives
  • Tyramine / pharmacology

Substances

  • 2-(4-acetoxyphenyl)-2-chloro-N-methylethylamine
  • Acetates
  • Anti-Inflammatory Agents, Non-Steroidal
  • Mineralocorticoids
  • Phosphodiesterase 5 Inhibitors
  • Desoxycorticosterone
  • Sodium Chloride
  • Sildenafil Citrate
  • Cyclic Nucleotide Phosphodiesterases, Type 4
  • PDE4D protein, mouse
  • Cyclic Nucleotide Phosphodiesterases, Type 5
  • Pde5a protein, mouse
  • Tyramine