Functional effects of glucose transporters in human ventricular myocardium

Eur J Heart Fail. 2010 Feb;12(2):106-13. doi: 10.1093/eurjhf/hfp191.

Abstract

Aims: Insulin-dependent positive inotropic effects (PIE) are partially Ca(2+) independent. This mechanism is potentially glucose dependent. In contrast to most animal species, human myocardium expresses high levels of sodium-glucose-transporter-1 (SGLT-1) mRNA besides the common glucose-transporters-1 and -4 (GLUT1, GLUT4).

Methods and results: We used ventricular myocardium from 61 end-stage failing human hearts (ischaemic cardiomyopathy, ICM and dilated cardiomyopathy, DCM) and 13 non-failing donor hearts. The effect of insulin on isometric twitch force was examined with or without blocking of PI3-kinase, GLUT4-translocation, or SGLT-1. Substrate-dependent (glucose vs. pyruvate vs. palmitoyl-carnitine) effects were tested in atrial myocardium. mRNA expression of glucose transporters was analysed. Insulin increased developed force by 122 + or - 7.4, 121.7 + or - 2.5, and 134.1 + or - 5.7% in non-failing, DCM, and ICM (P < 0.05 vs. DCM), respectively. Positive inotropic effect was partially blunted by inhibition of PI-3-kinase, GLUT4, or SGLT1. Combined inhibition of PI3-kinase and glucose-transport completely abolished PIE. Positive inotropic effect was significantly stronger in glucose-containing solution compared with pyruvate or palmitoyl-carnitine containing. mRNA expression showed only a tendency towards elevated GLUT4-expression in ICM.

Conclusions: Positive inotropic effect of insulin is pronounced in ICM, but underlying mechanisms are unaltered. The Ca(2+)-independent PIE of insulin is mediated via glucose-transporters. Together with the Ca(2+)-dependent PI-3-kinase mediated pathway, it is responsible for the entire PIE. Substrate-dependency affirms a glucose-dependent part of the PIE.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aged
  • Carbonates / pharmacology
  • Cardiomyopathy, Dilated / physiopathology
  • Dose-Response Relationship, Drug
  • Female
  • Gene Expression Regulation
  • Glucose Transporter Type 1 / genetics
  • Glucose Transporter Type 1 / metabolism*
  • Glucose Transporter Type 4 / genetics
  • Glucose Transporter Type 4 / metabolism*
  • Glucosides / pharmacology
  • Heart Failure / physiopathology*
  • Heart Ventricles
  • Humans
  • In Vitro Techniques
  • Inhibitory Concentration 50
  • Insulin / pharmacology
  • Male
  • Middle Aged
  • Myocardial Contraction / drug effects
  • Myocardial Contraction / physiology*
  • Myocardial Ischemia / physiopathology
  • Myocardium / metabolism*
  • Phosphoinositide-3 Kinase Inhibitors
  • RNA, Messenger / metabolism
  • Sodium-Glucose Transporter 1 / antagonists & inhibitors
  • Sodium-Glucose Transporter 1 / genetics
  • Sodium-Glucose Transporter 1 / metabolism*
  • Sodium-Glucose Transporter 2 / genetics
  • Sodium-Glucose Transporter 2 / metabolism
  • Sodium-Glucose Transporter 2 Inhibitors

Substances

  • Carbonates
  • Glucose Transporter Type 1
  • Glucose Transporter Type 4
  • Glucosides
  • Insulin
  • Phosphoinositide-3 Kinase Inhibitors
  • RNA, Messenger
  • Sodium-Glucose Transporter 1
  • Sodium-Glucose Transporter 2
  • Sodium-Glucose Transporter 2 Inhibitors
  • T 1095