Linarin inhibits the acetylcholinesterase activity in-vitro and ex-vivo

Linarin is a flavone glycoside in the plants flos chrysanthemi indici,buddleja officinalis,cirsium setosum,mentha arvensis and buddleja davidii,and has been reported to possess analgesic,antipyretic,anti-inflammatory and neuroprotective activities. in this paper,linarin was investigated for its ache inhibitory potential both in-vitro and ex-vivo. ellman’s colorimetric method was used for the determination of ache inhibitory activity in mouse brain. in-vitro assays revealed that linarin inhibited ache activity with an ic50 of 3.801 ± 1.149 μm. ex-vivo study showed that the ache activity was significantly reduced in both the cortex and hippocampus of mice treated intraperitoneally with various doses of linarin (35,70 and 140 mg/kg). the inhibition effects produced by high dose of linarin were the same as that obtained after huperzine a treatment (0.5 mg/kg). molecular docking study revealed that both 4’-methoxyl group and 7-o-sugar moiety of linarin played important roles in ligand-receptor binding and thus they are mainly responsible for ache inhibitory activity. in view of its potent ache inhibitory activity,linarin may be a promising therapeutic agent for the treatment of some diseases associated with ache,such as glaucoma,myasthenia gravis,gastric motility and alzheimer’s disease. © 2015 by school of pharmacy shaheed beheshti university of medical sciences and health services.