Indolalkylamines derivatives as antioxidant and neuroprotective agents in an experimental model of Parkinson's disease

Translated title of the contribution: Indolalkylamines derivatives as antioxidant and neuroprotective agents in an experimental model of Parkinson's disease

Elisenda Sanz, Manuel Romera, Lydia Belyk, J. I. Marco, Mercedes Unzeta

Research output: Contribution to journalArticleResearchpeer-review

22 Citations (Scopus)

Abstract

Background: The neuroprotective effect of N-(2-propynyl)2-(5-benzyloxy- indol)methylamine (PF 9601N), a novel MAO B inhibitor, and its metabolite FA 72 on the human neuroblastoma SHSY5Y cell line lesioned with (300 μM) dopamine was assessed and compared with that of 1-deprenyl assayed at identical experimental conditions. Material/Methods: Using this experimental model, PF 9601N showed a neuroprotective effect in a dose-dependent manner, and at a concentration of 10 μM a 20% recovery of cell viability was observed. However, the metabolite FA72 assayed under the same experimental conditions showed an increase in cell viability of nearly 50%. In the case of 1-deprenyl, a concentration of 100 μM was necessary to recover only 10% of cell viability. Results: This neuroprotective effect could be explained in terms of the antioxidant capacity of PF 9601N. In this context, the antioxidant capacities of the novel series of MAO inhibitors, PF 9601N and its analogues, were evaluated by their inhibition of the auto-oxidation of dopamine to melanin and by the dichlorofluorescein and 2-deoxyribose methods. Conclusions: All of these compounds have the basic structure of an indole ring in common, but show different substituents at different positions in it. The corresponding structure-activity relationship studies allowed us to conclude that the presence of a benzyloxy group, or a hydroxy or methoxy group, at position 5 of the indol ring enhanced these antioxidant characteristics, presenting a decreasing order of antioxidant activity of the primary > secondary > tertiary amines. The antioxidant properties of PF 9601 N would explain its neuroprotective effect observed in SHSY5Y cells lesioned with dopamine.
Translated title of the contributionIndolalkylamines derivatives as antioxidant and neuroprotective agents in an experimental model of Parkinson's disease
Original languageMultiple languages
Pages (from-to)BR477-BR484
JournalMedical Science Monitor
Volume10
Issue number12
Publication statusPublished - 1 Dec 2004

Keywords

  • Acetylenic tryptamine derivatives
  • Antioxidant
  • Free-radical scavenger
  • Monoamine oxidase
  • Monoamine oxidase inhibitors
  • Neuroprotection

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