6-Methylnitroarachidonate: a novel esterified nitroalkene that potently inhibits platelet aggregation and exerts cGMP-mediated vascular relaxation

Free Radic Biol Med. 2011 Feb 1;50(3):411-8. doi: 10.1016/j.freeradbiomed.2010.11.031. Epub 2010 Dec 8.

Abstract

Nitro-fatty acids represent endogenously occurring products of oxidant-induced nitration reactions. We have previously synthesized a mixture of four isomers of nitroarachidonic acid, a novel anti-inflammatory signaling mediator. In this study, we synthesized and chemically and biologically characterized for the first time an esterified nitroalkene derived from the nitration of methylarachidonate (AAMet): 6-methylnitroarachidonate (6-AAMetNO(2)). Synthesis was performed by reacting AAMet with sodium nitrite under acidic conditions. Analysis by mass spectrometry (positive-ion ESI-MS) showed an [M+H](+) ion of m/z 364, characteristic of AAMetNO(2). Fragmentation of this ion yielded a daughter ion at m/z 317, corresponding to the neutral loss of the nitro group ([M+H-HNO(2)](+)). Furthermore, IR signal at 1378 cm(-1) and NMR data confirmed the structure of a 6-nitro-positional isomer. This novel esterified nitroalkene was capable of promoting vascular protective actions including: (a) the induction of vasorelaxation via endothelium-independent mechanisms, associated with an increase in smooth muscle cell cGMP levels, and (b) a potent dose-dependent inhibition of human platelet aggregation. We postulate that 6-AAMetNO(2) could be a potential drug for the prevention of vascular and inflammatory diseases, and the presence of the methyl group may increase its pharmacological potential.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Aorta, Thoracic / drug effects
  • Aorta, Thoracic / physiology
  • Arachidonic Acids / chemical synthesis*
  • Arachidonic Acids / chemistry
  • Arachidonic Acids / pharmacology*
  • Cyclic GMP / metabolism*
  • Endothelium, Vascular / drug effects
  • Endothelium, Vascular / physiology
  • Humans
  • In Vitro Techniques
  • Male
  • Muscle, Smooth, Vascular / drug effects
  • Muscle, Smooth, Vascular / physiology
  • Nitric Oxide / metabolism
  • Nitric Oxide Donors / chemical synthesis
  • Nitric Oxide Donors / chemistry
  • Nitric Oxide Donors / pharmacology
  • Platelet Aggregation Inhibitors / chemical synthesis*
  • Platelet Aggregation Inhibitors / chemistry
  • Platelet Aggregation Inhibitors / pharmacology
  • Rats
  • Rats, Inbred WKY
  • Vasodilation / drug effects
  • Vasodilator Agents / chemical synthesis*
  • Vasodilator Agents / chemistry
  • Vasodilator Agents / pharmacology

Substances

  • Arachidonic Acids
  • Nitric Oxide Donors
  • Platelet Aggregation Inhibitors
  • Vasodilator Agents
  • methyl 6-nitroarachidonate
  • Nitric Oxide
  • Cyclic GMP