Stability assessment of a new antithrombotic small peptide, Arg-Gly-Asp-Trp-Arg (RGDWR), and its derivative

Biotechnol Lett. 2017 Aug;39(8):1183-1190. doi: 10.1007/s10529-017-2346-x. Epub 2017 May 11.

Abstract

Objective: To assess the stabilities of Arg-Gly-Asp-Trp-Arg (RGDWR, designated as RWR), a new patented antithrombotic small peptide, and its derivative with ω-aminocaprylic acid on its N-terminus (ωRWR).

Results: RWR in rat plasma was decreased by between 32 and 48% after 4 h incubation on ice, indicating its instability in plasma. In contrast, ωRWR in plasma remained at 96-107%. Concentration changes were within 6.2% for ωRWR after storage in various conditions. ωRWR is therefore stable in rat plasma, as well as under different storage methods. Furthermore, ω-aminocaprylic acid added onto the RWR peptide did not affect its antiplatelet aggregation activity.

Conclusions: A novel small peptide, ωRWR, has been developed with a good stability for possible antithrombotic use.

Keywords: Aminocaprylated peptide; Antithrombotic peptide; Embolism; Peptide derivative; Peptide stability; RGD motif.

MeSH terms

  • Animals
  • Caprylates / chemistry
  • Female
  • Fibrinolytic Agents / chemistry*
  • Fibrinolytic Agents / pharmacology
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Oligopeptides / chemistry*
  • Oligopeptides / pharmacology
  • Platelet Aggregation / drug effects
  • Protein Stability
  • Rabbits
  • Rats
  • Rats, Sprague-Dawley

Substances

  • Caprylates
  • Fibrinolytic Agents
  • Oligopeptides
  • omega-aminocaprylic acid