PMID:
ACS Omega. 2019 Jul 31 ;4(7):12259-12270. Epub 2019 Jul 17. PMID: 31460342
Abstract Title:
Anti-Alzheimer's Disease Activity of Bromophenols from a Red Alga,(Harvey) Yamada.
Abstract:
(Harvey) Yamada is a red alga with a myriad of bromophenols accompanied by a diverse array of biological activities. The main purpose of the present study was to characterize the anti-Alzheimer's disease activity of bromophenols fromvia inhibition of cholinesterases (AChE and BChE),β-site amyloid precursor protein cleaving enzyme 1 (BACE1), and glycogen synthase kinase-3β (GSK-3β). The results of enzyme inhibition assays demonstrated 2,3,6-tribromo-4,5-dihydroxybenzyl alcohol (), 2,3,6-tribromo-4,5-dihydroxybenzyl methyl ether (), and bis-(2,3,6-tribromo-4,5-dihydroxybenzyl) ether () as potent inhibitors of aforementioned enzymes. Among the tested bromophenols,showed multifold higher inhibition of all of the tested enzymes. Enzyme kinetics revealed different modes of inhibition, and in silico molecular docking simulation demonstrated the importance of the 7-OH group and bromine number for H-bond and halogen-bond interactions, respectively. Similarly,-at 20μM concentration showed more than 50% inhibition of self-induced Aβaggregation. These results suggest that bromophenols from, especially highly brominated (), may represent a novel class of anti-Alzheimer's disease drugs.
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