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Title 

Biological evaluation and in silico docking study of γ-linolenic acid as a potential BACE1 inhibitor

Authors 

K YounJinhyuk LeeE Y YunC T HoM V KarweW S JeongM Jun

Publisher 

Journal of Functional Foods

Issue Date 

2014

Citation 

Journal of Functional Foods, vol. 10, no. 0, pp. 187-191

Keywords 

Alzheimer's diseaseβ-amyloid peptide (Aβ)β-secretase (BACE1)γ-linolenic acid

Abstract 

Sequential proteolytic cleavage of amyloid precursor protein (APP) by β-secretase (BACE1) is a crucial process in β-amyloid peptide (Aβ) generation, which further forms into neurotoxic amyloid plaques that are considered to be a pivotal hallmark in the development and progress of Alzheimer's disease (AD). Hence, the inhibition of BACE1 has emerged as a credible target for the prevention and/or treatment of AD. In this study, γ-linolenic acid (GLA) was discovered as a novel BACE1 specific inhibitor. GLA non-competitively suppressed BACE1 activity with an IC50 value of 7.6×10-5M and Ki value of 3.5×10-5M. In addition, we demonstrated the calculated docking poses of GLA to human BACE1 and revealed the interactions of GLA with the allosteric site of the enzyme bound with the OH group of CYS359. Our findings provide a novel possibility of GLA to be efficacious for the prevention of AD and provide scaffolds to explore more potent natural BACE1 inhibitors.

ISSN 

1756-4646

Link 

http://dx.doi.org/10.1016/j.jff.2014.06.005

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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