Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 82, Issue -, Pages 164-171Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.05.048
Keywords
Crocin; Crocus sativus L; hMAO inhibitors; Depression; Neurodegenerative disorders; Safranal
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Funding
- Ateneo 2012 project
- Interregional Research Center for Food Safety and Health at the Magna Graecia University of Catanzaro [MIUR PON a3_00359]
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Although there are clinical trials and in vivo studies in literature regarding the anxiolytic and antidepressant activities of the components of Crocus sativus L., their effects on the human monoamine oxidases (hMAO-A and hMAO-B), enzymes which are involved in mental disorders and neurodegenerative diseases, have not yet been investigated. We have thus examined the hMAO inhibitory activities of crocin and safranal (the most important active principles in saffron) and, subsequently, designed a series of safranal derivatives to evaluate which chemical modifications confer enhanced inhibition of the hMAO isoforms. Docking simulations were performed in order to identify key molecular recognitions of these inhibitors with both isoforms of hMAO. In this regard, different mechanisms of action were revealed. This study concludes that safranal and crocin represent useful leads for the discovery of novel hMAO inhibitors for the clinical management of psychiatric and neurodegenerative disorders. (C) 2014 Elsevier Masson SAS. All rights reserved.
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