Influence of nanoencapsulated lutein on acetylcholinesterase activity: In vitro determination, kinetic parameters, and in silico docking simulations

Abstract

A B S T R A C TLutein is a bioactive found in dark leafy vegetables that may be used as a nutraceutical agent in foodstuff and an inhibitor of key enzymes of the human body such as those involved in the cholinergic system. However, its high hydrophobicity leads to low bioavailability and must be overcome if lutein is to be added in foods. The objective of this study was to evaluate the influence of nanoencapsulated lutein in the activity of the acetylcholinesterase enzyme. The in vitro study was carried out using water in order to evaluate the impact of encapsulation on the hydrophilicity of lutein. In vitro assays showed that lutein, both free and nanoencapsulated, presented a mixedtype inhibition behavior, and encapsulated lutein was able to inhibit acetylcholinesterase activity even in an aqueous medium. Inhibition was also showed by the in silico docking results which show that lutein interacted with the pocket region of the enzyme. that the damage to the cholinergic system is closely related to brain dysfunctions such as affective disorders, depression, schizophrenia and https://doi.

Chemometric evaluation of enzymatic hydrolysis in the production of fish protein hydrolysates with acetylcholinesterase inhibitory activity

“…The structure of AChE enzyme from Mus musculus was used for having tertiary structure similar to that of AChE enzyme from Electrophorus electricus and identity of 60.065 %. Similar studies available in the literature also report the use of rat structure in simulations (Grella Miranda et al, 2020).…”

“…There has been an effort in the last decades to find compounds from natural sources that could act as acetylcholinesterase (AChE) inhibitors. The main reason is that there is evidence that the damage to the cholinergic system is closely related to brain dysfunctions such as Parkinson's disease (Ventura et al, 2010;Grella Miranda et al, 2020;Prasasty et al, 2018). This relationship is recognized for Alzheimer's disease (AD), in which the loss of cholinergic function contributes to the decrease in cognitive activity associated with AD (Tan et al, 2018).…”

Neuroligin-mediated neurodevelopmental defects are induced by mitochondrial dysfunction and prevented by lutein in C. elegans

“…Chronic exposure to lutein in the diseased worms could thus activate NLG-1-regulated compensatory mechanisms that rescue their paralysis defects. Interestingly, NLG-1 contains an extracellular cholinesterase-like domain that forms the interaction with the neurexin domain [84], and lutein was shown to have acetylcholinesterase (AChE) inhibitory activity [85][86][87]. Whether lutein neuroprotection in this disease model is mediated by direct inhibition of synaptic AChE and/or NLG-1 activity (in turn suppressing compensatory nlg-1 overexpression), is an attractive possibility that require further investigation.…”

“…Lutein can be naturally ingested either through the diet (dark leave vegetables) or as a dietary supplement or as an ingredient in nutraceutical foods. However, due to its highly hydrophobic nature different strategies are being developed to improve its bioavailability [72, 78, 79], which can therefore offer more effective therapeutic strategies. Finally, besides lutein, our suppressor screen identified few other compounds that partially rescued the developmental arrest of CI deficient animals and it will be interesting to assess them alone or in combination with lutein in the different neuronal assays.…”

Synthesis of New 3-Arylcoumarins Bearing N-Benzyl Triazole Moiety: Dual Lipoxygenase and Butyrylcholinesterase Inhibitors With Anti-Amyloid Aggregation and Neuroprotective Properties Against Alzheimer’s Disease

“…The cost of the treatment is also estimated about 2 trillion USD by 2030 ( Dong et al, 2019 ; Kazmi et al, 2019 ; Oukoloff et al, 2019 ; Zhao et al, 2020 ). During the last 40 years, tacrine, donepezil, rivastigmine, and galantamine were the only four cholinesterase inhibitors launched in the market ( De Simone et al, 2020 ; Miranda et al, 2020 ) for AD treatment. The high failure rate (99.6%) of the anti-AD drugs entered in clinical trials to meet the prefixed clinical endpoints from 2002 to 2012 clearly demonstrates the urgent and unmet need for the development of new anti-AD drugs with different mechanisms of action ( Das Neves et al, 2019 ).…”