AChE/BuChE-IN-1

AChE/BuChE-IN-1 (Compound 1), a chrysin derivative, is a selective butyrylcholinesterase (BuChE) inhibitor with an IC50 of 0.48 μM. AChE/BuChE-IN-1 inhibits acetylcholinesterase (AChE) with an IC50 of 7.16 μM. AChE/BuChE-IN-1 shows strong scavenging ·OH activities with a IC50 of 0.1674 μM. AChE/BuChE-IN-1 inhibits reactive oxygen species (ROS), Aβ1-42 aggregation (self-, Cu2+-induced, AChE-induced). AChE/BuChE-IN-1 has high BBB permeability and bioavailability and low cell toxicity. AChE/BuChE-IN-1 has the potential for Alzheimer' disease (AD) research[1].

Research Areas >> Neurological Disease

Signaling Pathways >> Neuronal Signaling >> AChE

AChE/BuChE-IN-1 (Compound 1) is mixed-type inhibitor of competitive inhibition and non-competitive inhibition that can simultaneously bind to CAS and PAS of the AChE and BuChE enzyme. AChE/BuChE-IN-1 has no significant inhibitory effect in the ·DPPH scavenging assay (IC50>500 μM)[1]. AChE/BuChE-IN-1 selectively chelates Cu2+, Fe2+, Zn2+ and Al3+ ions, while had no chelating ability to other biometals[1].

[1]. Aihong Yang, et al. A multifunctional anti-AD approach: Design, synthesis, X-ray crystal structure, biological evaluation and molecular docking of chrysin derivatives. Eur J Med Chem. 2022 Apr 5;233:114216.