Therapeutic efficacy of the polymyxin-like peptide ranalexin in an experimental model of endotoxemia

J Surg Res. 2001 Oct;100(2):183-8. doi: 10.1006/jsre.2001.6235.

Abstract

Background: A rat model was used to investigate the efficacy of a polycationic peptide, the polymyxin-like ranalexin, in the prevention of lethality in a rat model of septic shock. The effect of ranalexin was compared with those of polymyxin B and imipenem.

Methods: Adult male Wistar rats (weight range: 250-300 g) were used for all the experiments. The study included five groups: an uninfected control group C(0), an untreated control group C(1), and three drug-treated groups that received 1 mg/kg ranalexin (group 2), 20 mg/kg imipenem (group 3), and 3 mg/kg polymyxin B (group 4). Rats, with the exception of the uninfected control group (C(0)), were given an intraperitoneal injection of 2 x 10(10) colony-forming units of Escherichia coli. Each group included 15 animals. Bacterial growth in abdominal exudate and plasma; endotoxin and tumor necrosis factor alpha (TNF-alpha) concentrations in plasma, and mortality were evaluated.

Results: Results were evaluated 48 h after inoculation. Ranalexin, imipenem, and polymyxin B significantly reduced the lethality (survival was 93.3, 80.0, and 93.3%, respectively) and the growth of E. coli both in abdominal fluid and plasma compared with saline treatment. Ranalexin showed higher antimicrobial activity than polymyxin B and imipenem and, at the same time, exhibited an antiendotoxin activity similar to that of polymyxin B (< or =0.015 EU/mL). Finally, ranalexin and polymyxin B significantly reduced plasma TNF-alpha levels (< or =4 pg/mL).

Conclusion: Monodose ranalexin treatment prevents bacterial growth, endotoxemia, and mortality in rats with septic shock.

MeSH terms

  • Animals
  • Anti-Bacterial Agents / pharmacology
  • Anti-Infective Agents / pharmacology*
  • Disease Models, Animal
  • Endotoxemia / drug therapy*
  • Endotoxemia / mortality
  • Escherichia coli Infections / drug therapy
  • Escherichia coli Infections / mortality
  • Imipenem / pharmacology
  • Male
  • Peptides, Cyclic / pharmacology*
  • Polymyxin B / pharmacology
  • Polymyxins
  • Rats
  • Survival Rate
  • Thienamycins / pharmacology
  • Tumor Necrosis Factor-alpha / metabolism

Substances

  • Anti-Bacterial Agents
  • Anti-Infective Agents
  • Peptides, Cyclic
  • Polymyxins
  • Thienamycins
  • Tumor Necrosis Factor-alpha
  • ranalexin
  • Imipenem
  • Polymyxin B