Abstract
Parkinson’s disease is a common neurodegenerative disorder. In this study, the monoamine oxidase inhibitory activity and potential anti-parkinsonian effects of 8-propyl-6H-[1,3]dioxolo[4,5-g]chromen-6-one (FCS303), a new synthetic coumarin, were evaluated. To do this, we used the reserpine model of Parkinson’s disease, an assay of levodopa/carbidopa potentiation, the catalepsy model of haloperidol, and an in vitro assay against monoamine oxidase (MAO) activity. Additionally, lipid peroxidation and protein carbonyl group quantification was performed in mice brain homogenates previously treated with haloperidol. FCS303 inhibited monoamine oxidase B (MAO-B) with an IC50 of 5.46 ± 0.36 µM; however, there was no effect on monoamine oxidase A (MAO-A). The oral administration of FCS303 led to a significant reversal of hypokinesia in the reserpine model (at 24 h, doses of 100 and 200 mg/kg) and in the levodopa/carbidopa potentiation assay (at 2 and 24 h, dose of 200 mg/kg). In addition, FCS303 (100 mg/kg) showed anti-cataleptic activity against haloperidol. FCS303 (50 mg/kg) significantly decreased lipid peroxidation and protein carbonyl quantification. These results suggest that FCS303 could present anti-parkinsonian activity related to MAO-B inhibitory activity.
Highlights
The World Health Organization (WHO) has estimated that four million people worldwide suffer from Parkinson’s disease (PD) (Philippens, 2008)
We evaluated the monoamine oxidase (MAO) inhibitory activity and potential anti-parkinsonian effects of 8-propyl6H-[1,3]dioxolo[4,5-g]chromen-6-one (FCS303), a new coumarin whose spectroscopic data is described below
Substitutions at position 3 and/or 4 of the coumarin nucleus contribute to the modulation of the inhibitory activity of Monoamine oxidase B (MAO-B) and the A/B selectivity (Gnerre et al, 2000)
Summary
The World Health Organization (WHO) has estimated that four million people worldwide suffer from Parkinson’s disease (PD) (Philippens, 2008). PD is a neurodegenerative disease that is characterized by a loss of dopaminergic neurons of the substantia nigra and basal ganglia This leads to alteration in the control and coordination of movement. Selegiline and rasagiline are selective MAO-B inhibitors that continue to be valuable adjunct therapies to L-DOPA for PD (Gershanik, 2015). These agents are very useful in the treatment of disease symptoms in early stage and improve the response to L-dopa in late stage of the disease (Finberg, 2014). One study evaluated 1,2-Benzopyrone (obtained from Hygrophila tyttha Leonard species) and found that coumarin was responsible, at least in part, for the anxiolytic, anticonvulsant, and sedative effects described for this species (Ariza et al, 2007). We evaluated the MAO inhibitory activity and potential anti-parkinsonian effects of 8-propyl6H-[1,3]dioxolo[4,5-g]chromen-6-one (FCS303), a new coumarin whose spectroscopic data is described below
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