Rutin Attenuates Carfilzomib-Induced Cardiotoxicity Through Inhibition of NF-κB, Hypertrophic Gene Expression and Oxidative Stress

Cardiovasc Toxicol. 2017 Jan;17(1):58-66. doi: 10.1007/s12012-015-9356-5.

Abstract

Carfilzomib is a proteasome inhibitor, commonly used in multiple myeloma, but its clinical use may be limited due to cardiotoxicity. This study was aimed to evaluate the influence of rutin in carfilzomib-induced cardiotoxicity in rats. Wistar albino male rats weighing 200-250 g (approximately 10 weeks old) were taken for this study. Animals were divided into four groups of six animals each. Group 1 served as normal control (NC), received normal saline; group 2 animals received carfilzomib (dissolved in 1 % DMSO) alone; group 3 animals received rutin (20 mg/kg) + carfilzomib; and group 4 animals received rutin (40 mg/kg) + carfilzomib. Hematological changes, biochemical changes, oxidative stress, hypertrophic gene expression, apoptotic gene expression, NFκB and IκB-α protein expression and histopathological evaluation were done to confirm the finding of carfilzomib-induced cardiotoxicity. Treatment with rutin decreased the carfilzomib-induced changes in cardiac enzymes such as lactate dehydrogenase, creatine kinase (CK) and CK-MB. For the assessment of cardiotoxicity, we further evaluated cardiac hypertrophic gene and apoptotic gene expression such as α-MHC, β-MHC and BNP and NF-κB and p53 gene expression, respectively, using RT-PCR. Western blot analysis showed that rutin treatment prevented the activation of NF-κB by increasing the expression of IκB-α. Rutin also attenuated the effects of carfilzomib on oxidant-antioxidant including malondialdehyde and reduced glutathione. Histopathological study clearly confirmed that rutin attenuated carfilzomib-induced cardiotoxicity in rats.

Keywords: Apoptosis; Cardiotoxicity; Carfilzomib; Natriuretic peptide; Nuclear factor-kappa B; Oxidative stress; Rutin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antioxidants / pharmacology*
  • Cardiomegaly / chemically induced
  • Cardiomegaly / genetics
  • Cardiomegaly / metabolism
  • Cardiomegaly / prevention & control*
  • Cardiotoxicity
  • Cytoprotection
  • Disease Models, Animal
  • Gene Expression Regulation / drug effects*
  • Male
  • Myocardium / metabolism*
  • Myocardium / pathology
  • NF-kappa B / genetics
  • NF-kappa B / metabolism*
  • Oligopeptides*
  • Oxidative Stress / drug effects*
  • RNA, Messenger / genetics
  • RNA, Messenger / metabolism
  • Rats, Wistar
  • Rutin / pharmacology*
  • Signal Transduction / drug effects

Substances

  • Antioxidants
  • NF-kappa B
  • Oligopeptides
  • RNA, Messenger
  • Rutin
  • carfilzomib