Inhibitory effect of ursolic acid purified from Origanum majorana L on the acetylcholinesterase

We screened 139 herbal spices in search of the acetylcholinesterase (AChE) inhibitor from natural resources. AChE inhibitors, which enhance cholinergic transmission by reducing the enzymatic degradation of acetylcholine, are the only source of compound currently approved for the treatment of Alzheim...

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Bibliographic Details
Published in:Molecules and cells 2001-04, Vol.11 (2), p.137-143
Main Authors: Chung, Y K, Heo, H J, Kim, E K, Kim, H K, Huh, T L, Lim, Y, Kim, S K, Shin, D H
Format: Article
Language:English
Subjects:
Acetylcholinesterase - metabolism
Alzheimer Disease - drug therapy
Animals
Cholinesterase Inhibitors - isolation & purification
Cholinesterase Inhibitors - pharmacology
Cholinesterase Inhibitors - therapeutic use
Chromatography
Humans
Lamiaceae - chemistry
Molecular Structure
PC12 Cells
Phytotherapy
Plant Extracts - chemistry
Plant Extracts - pharmacology
Plants, Medicinal
Rats
Tacrine - pharmacology
Triterpenes - isolation & purification
Triterpenes - pharmacology
Triterpenes - therapeutic use
Ursolic Acid
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Summary:We screened 139 herbal spices in search of the acetylcholinesterase (AChE) inhibitor from natural resources. AChE inhibitors, which enhance cholinergic transmission by reducing the enzymatic degradation of acetylcholine, are the only source of compound currently approved for the treatment of Alzheimer's Disease (AD). Among these herbs, edible plants and spices, the ethanol extract from Origanum majorana L. showed the highest inhibitory effect on AChE in vitro. By sequential fractionation of Origanum majorana L. the active component was finally identified as ursolic acid (3 beta-Hydroxyurs-12-en-28-oic acid). The ursolic acid of Origanum majorana L. inhibited AChE activity in a dose-dependent and competitive/non-competitive type. The Ki value (representing the affinity of the enzyme and inhibitor) of Origanum majorana L. ursolic acid was 6 pM, and that of tacrine was 0.4 nM. The concentration required for 50% enzyme inhibition of the active component (IC50 value) was 7.5 nM, and that of tacrine was 1 nM. This study demonstrated that the ursolic acid of Origanum majorana L. appeared to be a potent AChE inhibitor in Alzheimer's Disease.
ISSN:1016-8478
DOI:10.1016/S1016-8478(23)17016-6