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

ABSTRACT: 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 ±

SUBMITTER: Lee J 

PROVIDER: S-EPMC6410325 | biostudies-literature | 2019 Feb

REPOSITORIES: biostudies-literature