Polymer complex of WR 2721. Synthesis and radioprotective efficiency

Eur J Pharm Sci. 2014 Dec 18:65:9-14. doi: 10.1016/j.ejps.2014.08.006. Epub 2014 Aug 23.

Abstract

Polymer complex constructed from WR 2721 and poly(hydroxyoxyethylene phosphate) was synthesized. The structure of complex formed was elucidated by (1)H-, (13)C, (31)P NMR and FT-IR spectroscopy. The radioprotector was immobilized via ionic bonds. Radioprotective efficacy was evaluated by clonal survival of stem cells in crypts of mouse small intestine, and incidence and latency of the acute radiation induced bone marrow syndrome. Protection factors were assessed for WR 2721 and for the polymer complex. Protection factors for the polymer complex ranged from 2.6 for intestinal stem cell survival to 1.35 for 30 day survival (LD50) following whole body radiation exposure. In all cases, the polymer complex was a significantly better radiation protector than the parent compound.

Keywords: Poly(hydroxyoxyethylene phosphate); Polymer complex; Protection factor; Radioprotector; WR 2721.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amifostine / chemical synthesis*
  • Amifostine / pharmacology*
  • Animals
  • Cell Survival / drug effects
  • Intestine, Small / drug effects
  • Magnetic Resonance Spectroscopy / methods
  • Male
  • Mice
  • Mice, Inbred C3H
  • Polymers / chemical synthesis*
  • Polymers / pharmacology*
  • Radiation-Protective Agents / chemical synthesis*
  • Radiation-Protective Agents / pharmacology*
  • Spectroscopy, Fourier Transform Infrared / methods
  • Stem Cells / drug effects

Substances

  • Polymers
  • Radiation-Protective Agents
  • Amifostine