Inhibition of acetylcholinesterase activity and β-amyloid oligomer formation by 6-bromotryptamine A, a multi-target anti-Alzheimer's molecule.

Inhibition of acetylcholinesterase activity and β-amyloid oligomer formation by 6-bromotryptamine A, a multi-target anti-Alzheimer's molecule. Oncol Lett. 2020 Feb;19(2):1593-1601 Authors: Jin X, Wang M, Shentu J, Huang C, Bai Y, Pan H, Zhang D, Yuan Z, Zhang H, Xiao X, Wu X, Ding L, Wang Q, He S, Cui W Abstract Alzheimer's disease (AD) is a neurodegenerative disorder characterized by learning and memory impairments. Recent studies have suggested that AD can be induced by multiple factors, such as cholinergic system dysfunction and β-amyloid (Aβ) neurotoxicity. It was reported that 6-bromo-N-propionyltryptamine could treat neurological diseases, including AD. In the present study, 6-bromotryptamine A, a derivative of 6-bromo-N-propionyltryptamine, was synthesized by the condensation of 2-(6-bromo-1H-indol-3-yl)ethan-1-amine and 2-(4-bromophenyl)acetic acid, and was used as a potential anti-AD molecule. Furthermore, scopolamine can induce impairments of learning and memory, and was widely used to establish AD animal models. The results demonstrated that 6-bromotryptamine A significantly prevented scopolamine-induced short-term cognitive impairments, as revealed by various behavioral tests in mice. Furthermore, an acetylcholinesterase (AChE) activity assay revealed that 6-bromotryptamine A directly inhibited AChE activity. Notably, it was observed that 6-bromotryptamine A blocked the formation of Aβ oligomer, as evaluated by the do...
Source: Oncology Letters - Category: Cancer & Oncology Tags: Oncol Lett Source Type: research