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Lookup NU author(s): Dr Ed Okello,
Emeritus Professor Chris SealORCiD
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The alkaloid piperine from the spice family Piperaceae has been reported to possess poly-pharmacological activities including anti-depressant and cognitive enhancing effects. It has been suggested that its neurocognitive benefits may be via its activity on the cholinergic system, particularly on the enzyme acetylcholinesterase (AChE), a pharmacological target for neurodegenerative disease such as Alzheimer’s disease (AD). The paucity of information on the potential mechanism of inhibition of acetylcholinesterase and butyrylcholinesterase (BuChE), also a primary target for drug development for the treatment of AD, prompted this in vitro investigation. Dose-dependent inhibition of AChE and BuChE by piperine was determined using a modified classic colorimetric method of Ellman. Kinetics of inhibition was determined by Lineweaver-Burk methods. Piperine inhibited both AChE and BuChE in a concentration dependent manner with IC50 values of 0.12 mM and 0.067mM, respectively. Piperine exhibited a higher selectivity towards BuChE with a BuChE/AChE ratio of 0.56mM. Kinetic values for AChE classify piperine as a competitive inhibitor whereas the values for BuChE classify it as a mixed inhibitor. Compared to galanthamine (a mixed competitive non-competitive AChEinhibitor, IC50 of 1.068 nmol/ml under similar assay conditions) we conclude that although the AChE inhibition by piperine is not as potent as that of galanthamine, in addition to its known antioxidant and anti-inflammatory activities, piperine could provide a novel poly-pharmacological lead of potential benefit for the symptomatic treatment of AD and therefore warrants further investigation.
Author(s): Okello EJ, Coleman A, Seal CJ
Publication type: Article
Publication status: Published
Journal: International Journal of Pharmaceutical Sciences and Research
Print publication date: 01/09/2015
Online publication date: 01/09/2015
Acceptance date: 22/08/2015
ISSN (print): 2320-5148
ISSN (electronic): 0975-8232
Publisher: Society of Pharmaceutical Sciences and Research
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