Erdosteine affects eicosanoid production in COPD

Int J Clin Pharmacol Ther. 2011 Jan;49(1):41-5. doi: 10.5414/cpp49041.

Abstract

Oxidant-antioxidant imbalance and lipid peroxidation are known to activate the 5-LO pathway with increased expression of inflammatory eicosanoids. Erdosteine has recently shown important anti-oxidant properties, including the ability to reduce 8-isoprostane in COPD patients.

Aim: To assess the effects of erdosteine (E) on eicosanoids, and to compare the time-course of effect with that of E anti-oxidant activity.

Methods: 12 moderate COPD patients (9 males, 60 - 78 y) randomly received E 300 mg b.i.d. or placebo (P) for 10 days in a double-blind, controlled design. Blood ROS (Fort/Units); serum LTB4 and urine LTE4 (pg/ml) were measured at baseline and after 1, 3, 5 and 10 days of treatment. Analysis of covariance (ANCOVA) was performed.

Results: In COPD patients, both LTB4 and LTE4 dropped significantly during the 10-day treatment with E: s-LTB4 from 136.0 ± 35.4 SD to 54.5 ± 31.2 SD; u-LTE4 from 267.0 ± 91.5 SD to 84.0 ± 64.7 SD, p < 0.001 vs. p from Days 5 and 3, respectively. Moreover, a significant decrease of blood ROS was confirmed in patients using E. FEV1 values slightly increased during erdosteine treatment, whereas a trend to decrease was observed in the placebo group, with a significant difference in favor of erdosteine after 10 days of treatment (p = 0.0088).

Conclusions: 1) The scavenging and anti-inflammatory effects of Erdosteine were both confirmed; 2) erdosteine proved to affect eicosanoids significantly; 3) this novel effect underlines the important anti-inflammatory potentialities of the drug in COPD; 4) further investigation is needed in order to assess the capability of Erdosteine in controlling ongoing inflammation in chronic respiratory diseases.

Publication types

  • Randomized Controlled Trial

MeSH terms

  • Aged
  • Antioxidants / pharmacology*
  • Double-Blind Method
  • Eicosanoids / biosynthesis*
  • Female
  • Forced Expiratory Volume / drug effects
  • Humans
  • Leukotriene B4 / blood
  • Leukotriene E4 / urine
  • Male
  • Middle Aged
  • Pulmonary Disease, Chronic Obstructive / metabolism*
  • Reactive Oxygen Species / metabolism
  • Thioglycolates / pharmacology*
  • Thiophenes / pharmacology*

Substances

  • Antioxidants
  • Eicosanoids
  • Reactive Oxygen Species
  • Thioglycolates
  • Thiophenes
  • Leukotriene B4
  • Leukotriene E4
  • erdosteine