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Molecules 2018, 23(4), 719; https://doi.org/10.3390/molecules23040719

Amaryllidaceae Alkaloids as Potential Glycogen Synthase Kinase-3β Inhibitors

1
ADINACO Research Group, Department of Pharmacognosy, Faculty of Pharmacy, Charles University, 500 05 Hradec Králové, Czech Republic
2
Department of Pharmaceutical Botany, Faculty of Pharmacy, Charles University, 500 05 Hradec Králové, Czech Republic
3
Department for Life Quality Studies, University of Bologna, 47921 Rimini, Italy
*
Author to whom correspondence should be addressed.
Received: 15 February 2018 / Revised: 19 March 2018 / Accepted: 19 March 2018 / Published: 21 March 2018
(This article belongs to the Collection Bioactive Compounds)
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Abstract

Glycogen synthase kinase-3β (GSK-3β) is a multifunctional serine/threonine protein kinase that was originally identified as an enzyme involved in the control of glycogen metabolism. It plays a key role in diverse physiological processes including metabolism, the cell cycle, and gene expression by regulating a wide variety of well-known substances like glycogen synthase, tau-protein, and β-catenin. Recent studies have identified GSK-3β as a potential therapeutic target in Alzheimer´s disease, bipolar disorder, stroke, more than 15 types of cancer, and diabetes. GSK-3β is one of the most attractive targets for medicinal chemists in the discovery, design, and synthesis of new selective potent inhibitors. In the current study, twenty-eight Amaryllidaceae alkaloids of various structural types were studied for their potency to inhibit GSK-3β. Promising results have been demonstrated by alkaloids of the homolycorine-{9-O-demethylhomolycorine (IC50 = 30.00 ± 0.71 µM), masonine (IC50 = 27.81 ± 0.01 μM)}, and lycorine-types {caranine (IC50 = 30.75 ± 0.04 μM)}. View Full-Text
Keywords: Amaryllidaceae alkaloids; Alzheimer’s disease; glycogen synthase kinase-3β; masonine; caranine; 9-O-demethylhomolycorine Amaryllidaceae alkaloids; Alzheimer’s disease; glycogen synthase kinase-3β; masonine; caranine; 9-O-demethylhomolycorine
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Hulcová, D.; Breiterová, K.; Siatka, T.; Klímová, K.; Davani, L.; Šafratová, M.; Hošťálková, A.; De Simone, A.; Andrisano, V.; Cahlíková, L. Amaryllidaceae Alkaloids as Potential Glycogen Synthase Kinase-3β Inhibitors. Molecules 2018, 23, 719.

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