Evaluation of berberine nanoparticles as a strategy to modulate acetylcholinesterase activity

[Display omitted] •Intense search for natural-based reversible inhibitors for cholinesterases.•Reversible action of berberine (pure and nanoparticles) on AChE enzyme was evaluated.•Results corroborated by docking simulation and kinetic modeling.•Berberine nanoparticles are safe according to Allium c...

Full description

Saved in:

Bibliographic Details
Published in:	Food research international Vol. 173; p. 113295
Main Authors:	Leimann, Fernanda Vitória, de Souza, Luma Borges, de Oliveira, Byanca Pereira Moreira, Rossi, Bruna Franzon, da Silva, Patrícia Sabino, Shiraishi, Carlos Seiti Hurtado, Kaplum, Vanessa, Abreu, Rui Miguel, Pereira, Carla, Barros, Lillian, Peron, Ana Paula, Ineu, Rafael Porto, Oechsler, Bruno Francisco, Sayer, Claudia, de Araújo, Pedro Henrique Hermes, Gonçalves, Odinei Hess
Format:	Journal Article
Language:	English
Published:	Elsevier Ltd 01-11-2023 Elsevier
Subjects:	AChE Berberis vulgaris Bioactive Encapsulation Kinetic Solid dispersion Encapsulation AChE Solid dispersion Berberis vulgaris Kinetic Bioactive
Online Access:	Get full text
Tags:	Add Tag No Tags, Be the first to tag this record!

Description
Summary:	[Display omitted] •Intense search for natural-based reversible inhibitors for cholinesterases.•Reversible action of berberine (pure and nanoparticles) on AChE enzyme was evaluated.•Results corroborated by docking simulation and kinetic modeling.•Berberine nanoparticles are safe according to Allium cepa model and in vitro assays. Researchers have concentrated efforts in the search for natural-based reversible inhibitors for cholinesterase enzymes as they may play a key role in the treatment of degenerative diseases. Diverse plant alkaloids can inhibit the action of acetylcholinesterase and, among them, berberine is a promising bioactive. However, berberine has poor water solubility and low bioavailability, which makes it difficult to use in treatment. The solid dispersion technique can improve the water affinity of hydrophobic substances, but berberine solid dispersions have not been extensively studied. Safety testing is also essential to ensure that the berberine-loaded solid dispersions are safe for use. This study investigated the effectiveness of berberine-loaded solid dispersions (SD) as inhibitors of acetylcholinesterase enzyme (AChE). Docking simulation was used to investigate the influence of berberine on AChE, and in vitro assays were conducted to confirm the enzymatic kinetics of AChE in the presence of berberine. Berberine SD also showed improved cytotoxic effects on tumoral cells when dispersed in aqueous media. In vivo assays using Allium cepa were implemented, and no cytotoxicity/genotoxicity was found for the berberine solid dispersion. These results suggest that berberine SD could be a significant step towards safe nanostructures for use in the treatment of neurodegenerative diseases.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0963-9969 1873-7145
DOI:	10.1016/j.foodres.2023.113295