Fenofibrate Attenuates Malignant Hypertension by Suppression of the Renin-angiotensin System: A Study in Cyp1a1-Ren-2 Transgenic Rats

Am J Med Sci. 2016 Dec;352(6):618-630. doi: 10.1016/j.amjms.2016.09.008. Epub 2016 Sep 27.

Abstract

Background: Malignant hypertension is a life-threatening condition, and its pathophysiology is still poorly understood. The present study was designed to evaluate the role of interaction of the renin-angiotensin system with 20-hydroxyeicosatetraenoic acid (20-HETE), a product of cytochrome P450 (CYP)-dependent ω-hydroxylase pathway, in the pathophysiology of angiotensin II (ANG II)-dependent malignant hypertension in Cyp1a1-Ren-2 transgenic rats.

Methods: Malignant hypertension was induced by 12 days׳ dietary administration of 0.3 % indole-3-carbinol (I3C), a natural xenobiotic that activates a mouse renin gene. We hypothesized that chronic administration of fenofibrate, 190mg/kg body weight, a lipid-lowering drug, should increase renal production of 20-HETE, a tubular transport inhibitor; an expected increase in sodium excretion would oppose the development of ANG II-dependent malignant hypertension. Blood pressure was monitored by radiotelemetry, and at the end of the experiment rats were prepared for renal functional studies to evaluate in vivo the pressure-natriuresis relationship in response to stepwise reductions in renal arterial pressure (RAP).

Results: In I3C-induced rats, the treatment with fenofibrate significantly attenuated hypertension and improved the slope of the pressure-natriuresis relationship. Although fenofibrate treatment increased kidney gene and protein expression of CYP4A1, a major isoform responsible for 20-HETE formation, it did not increase renal 20-HETE concentration. On the contrary, fenofibrate treatment significantly suppressed renin gene expression, plasma renin activity and plasma and kidney ANG II levels.

Conclusions: Fenofibrate treatment significantly attenuated the course of malignant hypertension in I3C-induced CYP1a1-Ren-2 transgenic rats, and the mechanism responsible for antihypertensive action was fenofibrate-induced suppression of renin-angiotensin system activity.

Keywords: 20-hydroxyeicosatetraenoic acid; Cytochrome P450 metabolites; Malignant hypertension; Renin-angiotensin system.

MeSH terms

  • Animals
  • Blood Pressure
  • Cytochrome P-450 CYP1A1 / genetics
  • Cytochrome P-450 CYP4A / metabolism
  • Fenofibrate / pharmacology
  • Fenofibrate / therapeutic use*
  • Glomerular Filtration Rate / drug effects
  • Homeostasis / drug effects
  • Hydroxyeicosatetraenoic Acids / metabolism
  • Hypertension, Malignant / chemically induced
  • Hypertension, Malignant / drug therapy*
  • Indoles
  • Kidney / metabolism
  • Male
  • Natriuresis / drug effects*
  • Rats, Transgenic
  • Renal Circulation / drug effects
  • Renin / genetics
  • Renin-Angiotensin System / drug effects*
  • Transcriptional Activation

Substances

  • Hydroxyeicosatetraenoic Acids
  • Indoles
  • Ren2 protein, rat
  • indole-3-carbinol
  • Cytochrome P-450 CYP1A1
  • Cytochrome P-450 CYP4A
  • Renin
  • Fenofibrate