Mechanism of the salutary effects of flutamide on intestinal myeloperoxidase activity following trauma-hemorrhage: up-regulation of estrogen receptor-{beta}-dependent HO-1

J Leukoc Biol. 2006 Feb;79(2):277-84. doi: 10.1189/jlb.0705363. Epub 2005 Dec 5.

Abstract

Hemeoxygenase (HO)-1 induction following adverse circulatory conditions is known to be protective, and precastrated males have less intestinal damage than sham-operated males following trauma-hemorrhage (T-H). Previous studies have also shown that administration of flutamide up-regulated estrogen receptor (ER) expression in males following T-H. We hypothesized that flutamide administration in males following T-H up-regulates HO-1 via an ER-dependent pathway and protects against intestinal injury. Male Sprague-Dawley rats underwent T-H [mean blood pressure (MBP) 40 mmHg for 90 min and then resuscitation]. A single dose of flutamide (25 mg/kg body weight), with or without an ER antagonist (ICI 182,780), a HO enzyme inhibitor [chromium-mesoporphyrin (CrMP)], or vehicle, was administered subcutaneously during resuscitation. At 2 h after T-H or sham operation, intestinal myeloperoxidase (MPO) activity, intercellular adhesion molecule (ICAM)-1, cytokine-induced neutrophil chemoattractant (CINC)-1, and CINC-3 levels were measured. Intestinal ER-alpha, ER-beta, androgen receptor, and HO-1 mRNA/protein levels were also determined. Results showed that T-H increased intestinal MPO activity, ICAM-1, CINC-1, and CINC-3 levels. These parameters were improved significantly in the flutamide-treated rats subjected to T-H. Flutamide treatment increased intestinal HO-1 and ER-beta mRNA/protein levels as compared with vehicle-treated T-H rats. Administration of the ER antagonist ICI 182,780 or the HO inhibitor CrMP prevented the flutamide-induced attenuation of shock-induced intestinal damage. Thus, the salutary effects of flutamide administration on attenuation of intestinal injury following T-H are mediated via up-regulation of ER-beta-dependent HO-1 expression.

Publication types

  • Comparative Study
  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Chemokine CXCL1
  • Chemokines, CXC / metabolism
  • Enzyme Activation / drug effects
  • Enzyme Inhibitors / pharmacology
  • Estradiol / analogs & derivatives
  • Estradiol / pharmacology
  • Estrogen Receptor alpha / antagonists & inhibitors
  • Estrogen Receptor alpha / metabolism
  • Estrogen Receptor beta / antagonists & inhibitors
  • Estrogen Receptor beta / genetics
  • Estrogen Receptor beta / metabolism*
  • Flutamide / administration & dosage*
  • Flutamide / antagonists & inhibitors
  • Fulvestrant
  • Gene Expression Regulation, Enzymologic / drug effects
  • Heme Oxygenase-1 / antagonists & inhibitors
  • Heme Oxygenase-1 / genetics
  • Heme Oxygenase-1 / metabolism*
  • Hemorrhage / physiopathology*
  • Intercellular Adhesion Molecule-1 / metabolism
  • Intestines / drug effects
  • Intestines / enzymology*
  • Intestines / injuries*
  • Male
  • Mesoporphyrins / pharmacology
  • Peroxidase / drug effects
  • Peroxidase / metabolism*
  • RNA, Messenger / drug effects
  • RNA, Messenger / genetics
  • Rats
  • Rats, Sprague-Dawley
  • Up-Regulation / drug effects

Substances

  • Chemokine CXCL1
  • Chemokines, CXC
  • Cxcl1 protein, rat
  • Enzyme Inhibitors
  • Estrogen Receptor alpha
  • Estrogen Receptor beta
  • Mesoporphyrins
  • RNA, Messenger
  • chromium mesoporphyrin
  • Intercellular Adhesion Molecule-1
  • Fulvestrant
  • Estradiol
  • Flutamide
  • Peroxidase
  • Heme Oxygenase-1