A novel IKK inhibitor suppresses heart failure and chronic remodeling after myocardial ischemia via MMP alteration

Expert Opin Ther Targets. 2008 Dec;12(12):1469-76. doi: 10.1517/14728220802551140.

Abstract

Objective: Amplification of inflammatory response in the non-infarct area plays an important role in the pathogenesis of ventricular remodeling after myocardial ischemia. Activation of nuclear factor-kappa B (NF-kappaB) is involved in this amplification through a positive feedback loop of pro- inflammatory cytokines. We investigated the efficacy of IKK blockade with IMD-0560, a novel inhibitor of IKK, in a rat myocardial ischemia model.

Methods/results: Left coronary artery occlusion (28 days) was carried out in Sprague-Dawley rats. Daily intraperitoneal injections of IMD-0560 (5 mg/kg) were done after the operation. Treatment with IMD-0560 significantly improved cardiac function as indicated by the preservation of fractional shortening and lower serum brain natriuretic peptide level. Histological analysis showed that IMD-0560 treatment suppressed thinning in the infarcted area compared with vehicle-treated hearts. Moreover, in situ zymography showed matrix metalloprotease-9 activity was inhibited in the infarct area.

Conclusion: We revealed that the IKK blockade is potent for the suppression of chronic ventricular remodeling after myocardial ischemia.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzamides / pharmacology*
  • Blood Pressure
  • Body Weight
  • Heart Failure / prevention & control*
  • Heart Rate
  • I-kappa B Kinase / antagonists & inhibitors*
  • Male
  • Matrix Metalloproteinases / metabolism*
  • Myocardial Infarction / complications*
  • NF-kappa B / metabolism
  • Rats
  • Rats, Sprague-Dawley
  • Ventricular Remodeling / drug effects*

Substances

  • Benzamides
  • N-(2,5-bis(trifluoromethyl)phenyl)-5-bromo-2-hydroxybenzamide
  • NF-kappa B
  • I-kappa B Kinase
  • Matrix Metalloproteinases