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2022-10-30

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cc-by (c) Alvarez-Berbel, Irene et al., 2022
Please use this identifier to cite or link to this item: https://hdl.handle.net/2445/192126

Three to Tango: Inhibitory Effect of Quercetin and Apigenin on Acetylcholinesterase, Amyloid-β Aggregation and Acetylcholinesterase-Amyloid Interaction

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https://doi.org/10.3390/pharmaceutics14112342

Abstract

One of the pathological hallmarks of Alzheimer's disease (AD) is the formation of amyloid-β plaques. Since acetylcholinesterase (AChE) promotes the formation of such plaques, the inhibition of this enzyme could slow down the progression of amyloid-β aggregation, hence being complementary to the palliative treatment of cholinergic decline. Anti-aggregation assays performed for apigenin and quercetin, which are polyphenolic compounds that exhibit inhibitory properties against the formation of amyloid plaques, reveal distinct inhibitory effects of these compounds on Aβ40 aggregation in the presence and absence of AChE. Furthermore, the analysis of the amyloid fibers formed in the presence of these flavonoids suggests that the Aβ40 aggregates present different quaternary structures, viz., smaller molecular assemblies are generated. In agreement with a non-competitive inhibition of AChE, molecular modeling studies indicate that these effects may be due to the binding of apigenin and quercetin at the peripheral binding site of AChE. Since apigenin and quercetin can also reduce the generation of reactive oxygen species, the data achieved suggest that multitarget catechol-type compounds may be used for the simultaneous treatment of various biological hallmarks of AD.

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Malaltia d'Alzheimer, Pèptids, Amiloïdosi

Subject (English)

Alzheimer's disease, Peptides, Amyloidosis

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Articles publicats en revistes (Nutrició, Ciències de l'Alimentació i Gastronomia)
Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)
Articles publicats en revistes (Química Inorgànica i Orgànica)

Citation

ALVAREZ-BERBEL, Irene, et al. Three to Tango: Inhibitory Effect of Quercetin and Apigenin on Acetylcholinesterase, Amyloid-β Aggregation and Acetylcholinesterase-Amyloid Interaction. Pharmaceutics. 2022. Vol. 14, num. 11, pags. 2342. ISSN 1999-4923. [consulted: 11 of June of 2026]. Available at: https://hdl.handle.net/2445/192126

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