Monoclonal Antibody to Marinobufagenin Downregulates TGFβ Profibrotic Signaling in Left Ventricle and Kidney and Reduces Tissue Remodeling in Salt-Sensitive Hypertension

J Am Heart Assoc. 2019 Oct 15;8(20):e012138. doi: 10.1161/JAHA.119.012138. Epub 2019 Oct 2.

Abstract

Background Elevated levels of an endogenous Na/K-ATPase inhibitor marinobufagenin accompany salt-sensitive hypertension and are implicated in cardiac fibrosis. Immunoneutralization of marinobufagenin reduces blood pressure in Dahl salt-sensitive (Dahl-S) rats. The effect of the anti-marinobufagenin monoclonal antibody on blood pressure, left ventricular (LV) and renal remodeling, and gene expression were investigated in hypertensive Dahl-S rats. Methods and Results Dahl-S rats were fed high NaCl (8%, HS; n=14) or low NaCl (0.1%, LS; n=14) diets for 8 weeks. Animals were administered control antibody (LS control antibody, LSC; HS control antibody, HSC; n=7 per group) or anti-marinobufagenin antibody once on week 7 of diet intervention (n=7 per group). Levels of marinobufagenin, LV, and kidney mRNAs and proteins implicated in profibrotic signaling were assessed. Systolic blood pressure was elevated (211±8 versus 133±3 mm Hg, P<0.01), marinobufagenin increased 2-fold in plasma (P<0.05) and 5-fold in urine (P<0.01), LV and kidney weights increased, and levels of LV collagen-1 rose 3.5-fold in HSC versus LSC. Anti-marinobufagenin antibody treatment decreased systolic blood pressure by 24 mm Hg (P<0.01) and reduced organ weights and level of LV collagen-1 (P<0.01) in hypertensive Dahl salt-sensitive rats with anti-marinobufagenin antibody versus HSC. The expression of genes related to transforming growth factor-β-dependent signaling was upregulated in the left ventricles and kidneys in HSC versus LSC groups and became downregulated following administration of anti-marinobufagenin antibody to hypertensive Dahl-S rats. Marinobufagenin also activated transforming growth factor-β signaling in cultured ventricular myocytes from Dahl-S rats. Conclusions Immunoneutralization of heightened marinobufagenin levels in hypertensive Dahl-S rats resulted in a downregulation of genes implicated in transforming growth factor-β pathway, which indicates that marinobufagenin is an activator of profibrotic transforming growth factor-β-dependent signaling in salt-sensitive hypertension.

Keywords: Dahl salt‐sensitive hypertension; cardiac hypertrophy; marinobufagenin; monoclonal antibody; transforming growth factor.

Publication types

  • Research Support, N.I.H., Intramural

MeSH terms

  • Animals
  • Blood Pressure / drug effects
  • Blotting, Western
  • Bufanolides / pharmacology*
  • Disease Models, Animal
  • Echocardiography
  • Enzyme Inhibitors / pharmacology
  • Gene Expression Regulation*
  • Heart Ventricles / diagnostic imaging
  • Heart Ventricles / metabolism*
  • Heart Ventricles / physiopathology
  • Hypertension / drug therapy
  • Hypertension / genetics*
  • Hypertension / physiopathology
  • Male
  • RNA / genetics
  • Rats
  • Rats, Inbred Dahl
  • Transforming Growth Factor beta / biosynthesis
  • Transforming Growth Factor beta / genetics*
  • Ventricular Remodeling / physiology*

Substances

  • Bufanolides
  • Enzyme Inhibitors
  • Transforming Growth Factor beta
  • marinobufagenin
  • RNA