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Title 

Oleic acid and linoleic acid from Tenebrio molitor larvae inhibit BACE1 activity in vitro: molecular docking studies

Authors 

K YounE Y YunJinhyuk LeeJ Y KimJ S HwangW S JeongM Jun

Publisher 

Mary Ann Liebert

Issue Date 

2014

Citation 

Journal of Medicinal Food, vol. 17, no. 2, pp. 284-289

Keywords 

Alzheimer's diseaseb-secretase (BACE1)docking analysislinoleic acidoleic acidTenebrio molitor

Abstract 

In our ongoing research to find therapeutic compounds for Alzheimer's disease (AD) from natural resources, the inhibitory activity of the BACE1 enzyme by Tenebrio molitor larvae and its major compounds were evaluated. The T. molitor larvae extract and its fractions exhibited strong BACE1 suppression. The major components of hexane fraction possessing both high yield and strong BACE1 inhibition were determined by thin layer chromatography, gas chromatography, and nuclear magnetic resonance analysis. A remarkable composition of unsaturated long chain fatty acids, including oleic acid and linoleic acid, were identified. Oleic acid, in particular, noncompetitively attenuated BACE1 activity with a half-maximal inhibitory concentration (IC50) value of 61.31 μM and Ki value of 34.3 μM. Furthermore, the fatty acids were stably interacted with BACE1 at different allosteric sites of the enzyme bound with the OH of CYS319 and the NH3 of TYR320 for oleic acid and with the C=O group of GLN304 for linoleic acid. Here, we first revealed novel pharmacophore features of oleic acids and linoleic acid to BACE1 by in silico docking studies. The present findings would clearly suggest potential guidelines for designing novel BACE1 selective inhibitors.

ISSN 

1096-620X

Link 

http://dx.doi.org/10.1089/jmf.2013.2968

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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