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Antioxidant properties of PF9601N, a novel MAO-B inhibitor: assessment of its ability to interact with reactive nitrogen species.

Abstract
The novel MAO-B inhibitor PF9601N, its cytochrome P450-dependent metabolite FA72 and l-deprenyl were studied as potential peroxynitrite (ONOO(-)) scavengers and nitric oxide synthase (NOS) inhibitors. The scavenging activity of these compounds was evaluated by measuring the oxygen consumption through peroxynitrite-mediated oxidation of both linoleic acid and brain homogenate. FA72, PF9601N and l-deprenyl caused a concentration-dependent inhibition of ONOO(-)-induced linoleic acid oxidation with an IC(50) value of 60.2 microM, 82.8 microM and 235.8 microM, respectively. FA72 was the most potent also in inhibiting ONOO(-)-induced brain homogenate oxidation with an IC(50) value of 99.4 microM, while PF9601N and l-deprenyl resulted weaker inhibitors in the same experimental model, showing an IC(50) value of 164.8 and 112.0 microM, respectively. Furthermore, both the novel MAO-B inhibitor as well as its metabolite were able to strongly inhibit rat brain neuronal NOS (IC(50) of 183 microM and 192 microM, respectively), while l-deprenyl at the highest concentration used (3 mM), caused only a slight decrease of the enzyme activity. Moreover, inducible NOS was strongly inhibited by FA72 only. All these results suggest that PF9601N could be a promising therapeutic agent in neurodegenerative disorders such as Parkinson's disease.
AuthorsLydia Bellik, Stefania Dragoni, Federica Pessina, Elisenda Sanz, Mercedes Unzeta, Massimo Valoti
JournalActa biochimica Polonica (Acta Biochim Pol) Vol. 57 Issue 2 Pg. 235-9 ( 2010) ISSN: 1734-154X [Electronic] Poland
PMID20532254 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antioxidants
  • Indoles
  • Monoamine Oxidase Inhibitors
  • N-(2-propynyl)-2-(5-benzyloxy-indolyl) methylamine
  • Reactive Nitrogen Species
  • Monoamine Oxidase
Topics
  • Animals
  • Antioxidants (chemistry, pharmacology)
  • Brain Chemistry
  • Indoles (chemistry, pharmacology)
  • Monoamine Oxidase
  • Monoamine Oxidase Inhibitors (chemistry, pharmacology)
  • Rats
  • Reactive Nitrogen Species (chemistry)

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