8-Propyl-6H-[1,3]dioxolo[4,5-g]chromen-6-one: A new coumarin with monoamine oxidase B inhibitory activity and possible anti-parkinsonian effects
Document title: 8-Propyl-6H-[1,3]dioxolo[4,5-g]chromen-6-one: A new coumarin with monoamine oxidase B inhibitory activity and possible anti-parkinsonian effects
Journal: Brazilian Journal of Pharmaceutical Sciences
Database: PERIÓDICA
System number: 000451483
ISSN: 1984-8250
Authors: 1
1
2
3
1
Institutions: 1Universidad Nacional de Colombia, Facultad de Ciencias, Bogotá. Colombia
2Universidad de Salamanca, Escuela de Farmacia, Salamanca. España
3Universidad de Santiago de Compostela, Centro de Investigación en Medicina Molecular y Enfermedades Crónicas, Santiago de Compostela, La Coruña. España
Year:
Volumen: 56
Country: Brasil
Language: Inglés
Document type: Artículo
Approach: Experimental, aplicado
English 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
Disciplines: Química,
Medicina
Keyword: Química farmacéutica,
Neurología,
Enfermedad de Parkinson,
Cumarinas,
Monoamino oxidasa B,
Reserpina,
Levodopa,
Carbidopa,
Actividad biológica
Keyword: Medicinal chemistry,
Neurology,
Parkinson disease,
Coumarins,
Monoamine oxidase B,
Biological activity,
Reserpine,
Levodopa,
Carbidopa
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