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Mar. Drugs 2019, 17(2), 91;

Dual BACE1 and Cholinesterase Inhibitory Effects of Phlorotannins from Ecklonia cava—An In Vitro and in Silico Study

Korean Bioinformation Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), 125, Gwahak-ro, Yuseong-gu, Daejeon 34141, Korea
Department of Bioinformatics, KIRBB School of Bioscience, Korea University of Sciences and Technology, 217 Gajung-ro, Yuseong-gu, Daejeon 34113, Korea
Department of Food Science and Nutrition, College of Health Sciences, Dong-A University, 37, Nakdong-daero 550 beon-gil, Saha-gu, Busan 49315, Korea
Center for Silver-Targeted Biomaterials, Brain Busan 21 Plus Program, Graduate School, Dong-A University, Nakdong-daero 550 beon-gil, Saha-gu, Busan 49315, Korea
Institute of Convergence Bio-Health, Dong-A University, Busan 49315, Korea
Author to whom correspondence should be addressed.
Received: 8 January 2019 / Revised: 24 January 2019 / Accepted: 28 January 2019 / Published: 1 February 2019
(This article belongs to the Special Issue Enzyme Inhibitor from Marine Organisms)
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Alzheimer′s disease (AD) is one of the most common neurodegenerative diseases with a multifactorial nature. β-Secretase (BACE1) and acetylcholinesterase (AChE), which are required for the production of neurotoxic β-amyloid (Aβ) and the promotion of Aβ fibril formation, respectively, are considered as prime therapeutic targets for AD. In our efforts towards the development of potent multi-target, directed agents for AD treatment, major phlorotannins such as eckol, dieckol, and 8,8′-bieckol from Ecklonia cava (E. cava) were evaluated. Based on the in vitro study, all tested compounds showed potent inhibitory effects on BACE1 and AChE. In particular, 8,8′-bieckol demonstrated the best inhibitory effect against BACE1 and AChE, with IC50 values of 1.62 ± 0.14 and 4.59 ± 0.32 µM, respectively. Overall, kinetic studies demonstrated that all the tested compounds acted as dual BACE1 and AChE inhibitors in a non-competitive or competitive fashion, respectively. In silico docking analysis exhibited that the lowest binding energies of all compounds were negative, and specifically different residues of each target enzyme interacted with hydroxyl groups of phlorotannins. The present study suggested that major phlorotannins derived from E. cava possess significant potential as drug candidates for therapeutic agents against AD. View Full-Text
Keywords: Alzheimer′s disease; BACE1; acetylcholinesterase; in silico docking; phlorotannins Alzheimer′s disease; BACE1; acetylcholinesterase; in silico docking; phlorotannins

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Lee, J.; Jun, M. Dual BACE1 and Cholinesterase Inhibitory Effects of Phlorotannins from Ecklonia cava—An In Vitro and in Silico Study. Mar. Drugs 2019, 17, 91.

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