Effect of scopoletin on monoamine oxidases and brain amines

Neurochemistry International
Mahua BasuNibha Mishra

Abstract

Naturally, occurring compounds with MAO inhibitory property may provide promising lead molecules against neurodegenerative disorders. We report MAO inhibitory activity of a naturally occurring coumarin (validated chemical scaffold as MAO inhibitors), scopoletin. It selectively (and reversibly) inhibits human (Ki = 20.7 μM) and mouse (Ki = 22 μM) MAO-B, ∼3.5 times more selective towards MAO-B than MAO-A. Docking studies revealed its molecular recognition and explained the selectivity mechanism towards MAO isoforms. Scopoletin occupied the hydrophobic aromatic pockets showing favorable interactions for MAO-B; experimental Ki agreed with the predicted Ki. In vivo, scopoletin (80 mg/kg, i.p.) treatment significantly increases dopamine level and decreases its metabolite DOPAC in striatum. Overall, scopoletin is a partially selective MAO-B inhibitor that increases brain dopamine level.

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Citations

Sep 19, 2017·Phytotherapy Research : PTR·Ra-Yeong ChoiMi-Kyung Lee
May 8, 2020·Oxidative Medicine and Cellular Longevity·Emad H M HassaneinAyman M Mahmoud
May 16, 2021·International Journal of Biological Macromolecules·Ankita R RaneSinjan Choudhary

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