Uptake and metabolism of the novel peptide angiotensin-(1-12) by neonatal cardiac myocytes

PLoS One. 2011 Jan 10;6(1):e15759. doi: 10.1371/journal.pone.0015759.

Abstract

Background: Angiotensin-(1-12) [Ang-(1-12)] functions as an endogenous substrate for the productions of Ang II and Ang-(1-7) by a non-renin dependent mechanism. This study evaluated whether Ang-(1-12) is incorporated by neonatal cardiac myocytes and the enzymatic pathways of ¹²⁵I-Ang-(1-12) metabolism in the cardiac myocyte medium from WKY and SHR rats.

Methodology/principal findings: The degradation of ¹²⁵I-Ang-(1-12) (1 nmol/L) in the cultured medium of these cardiac myocytes was evaluated in the presence and absence of inhibitors for angiotensin converting enzymes 1 and 2, neprilysin and chymase. In both strains uptake of ¹²⁵I-Ang-(1-12) by myocytes occurred in a time-dependent fashion. Uptake of intact Ang-(1-12) was significantly greater in cardiac myocytes of SHR as compared to WKY. In the absence of renin angiotensin system (RAS) enzymes inhibitors the hydrolysis of labeled Ang-(1-12) and the subsequent generation of smaller Ang peptides from Ang-(1-12) was significantly greater in SHR compared to WKY controls. ¹²⁵I-Ang-(1-12) degradation into smaller Ang peptides fragments was significantly inhibited (90% in WKY and 71% in SHR) in the presence of all RAS enzymes inhibitors. Further analysis of peptide fractions generated through the incubation of Ang-(1-12) in the myocyte medium demonstrated a predominant hydrolytic effect of angiotensin converting enzyme and neprilysin in WKY and an additional role for chymase in SHR.

Conclusions/significance: These studies demonstrate that neonatal myocytes sequester angiotensin-(1-12) and revealed the enzymes involved in the conversion of the dodecapeptide substrate to biologically active angiotensin peptides.

Publication types

  • Comparative Study
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Angiotensinogen
  • Angiotensins / metabolism*
  • Angiotensins / pharmacokinetics
  • Animals
  • Animals, Newborn
  • Hydrolysis
  • Iodine Radioisotopes
  • Metabolic Networks and Pathways
  • Myocytes, Cardiac / metabolism*
  • Peptide Fragments / metabolism*
  • Peptide Fragments / pharmacokinetics
  • Rats
  • Rats, Inbred SHR
  • Rats, Inbred WKY
  • Substrate Specificity

Substances

  • Angiotensins
  • Iodine Radioisotopes
  • Peptide Fragments
  • proangiotensin-12, rat
  • Angiotensinogen