Acetylcholinesterase inhibition by medicinal plants: A Review

Navi Ranjan*, Manorma Kumari


Acetylcholinesterase (AChE), the predominant cholinesterase in the brain, hydrolyzes ACh to choline and acetate, thereby terminating the effect of this neurotransmitter at cholinergic synapses. Therefore, AChE is the target of cholinesterase inhibitors used for addressing the cholinergic deficit in Alzheimer’s disease (AD) patients. Despite decades of research and advances in our understanding of its aetiology and pathogenesis, current pharmacotherapeutic options for AD are still very limited and represent an area of need that is currently unmet. The leading AD therapeutics involves AChE inhibitors, resulting in increased acetylcholine concentrations in the synaptic cleft and enhanced cholinergic transmission. Compounds showing an AChE inhibitory effect are also used for the treatment of senile dementia, myastenia gravis, Parkinson’s disease and ataxia. Taking into account that the inhibition of AChE has been one of the most used strategies for treating AD and that existing drugs are effective only against mild to moderate type of disease while presenting considerable side effects, the search for new sources of effective and selective anti acetylcholinesterase agents with fewer side effects is imperative. Various plants and phytochemical substances have demonstrated AChE inhibitory activity and thus could be beneficial in the treatment of neurodegenerative disorders such as AD.


Alzheimer’s disease (AD); Acetylcholine (ACh); Acetylcholinesterase (AChE); Medicinal Plants.

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Birks J. Cholinesterase inhibitors for Alzheimer's disease. Cochrane Database Syst Rev. 1. (2006):CD005593

Birks J, J Grimley Evans, V Iakovidou, M Tsolaki, FE Holt. Rivastigmine for Alzheimer's disease. Cochrane Database Syst Rev 2. (2009):CD001191.

Prvulovic D, H Hampel, J Pantel. Galantamine for Alzheimer's disease. Expert Opin Drug Metab Toxicol. 6. 3 (2010): 345-354.

Stryer L. Biochemistry. 4th ed., WH Freeman: San Francisco, CA, (1995): 1017.

Howes MJR, NSL Perry, PJ Houghton. Plants with traditional uses and activities, relevant to the management of Alzheimer’s disease and other cognitive disorders. Phytother Res. 7 (2003): 1-18.

Anonymous. Compendium of Pharmaceuticals and Specialties, 25th ed. Canadian Pharmacists Association, Toronto, Canada. (2000).

Brenner GM. Pharmacology. W.B. Saunders Company, Philadelphia. (2000).

Rahman AU, MI Choudhary. Bioactive natural products as a potential source of new pharmacophores a theory of memory. Pure Appl. Chem. 73 (2001): 555–560.

Oh MH, PJ Houghton, WK Whang, JH Cho. Screening of Korean herbal medicines used to improve cognitive function for anti-cholinesterase activity. Phyto-medicine 11(2004): 544–548.

Schulz V. Ginkgo extract or cholinesterase inhibitors in patients with dementia: what clinical trial and guidelines fail to consider. Phytomedicine .10(2003): 74–79.

Melzer D. New drug treatment for Alzheimer’s diseases: lessons for healthcare policy. BMJ 316 (1998): 762–764.

Houghton PJ, Y Ren, MJ Howes. Acetylcholinesterase inhibitors from plants and fungi. Nat. Prod. Rep. 23 (2006): 181-199.

Williams P, A Sorribas, MJ Howes. Natural Products as a source of Alzheimer’s drugs leads. Nat. Prod. Rep. 28 (2011): 48-77.

Mukherjee PK, V Kumar, M Mal, PJ Houghton. Acetylcholinesterase inhibitors from plants. Phytomedicine 14 (2007): 289-300.

Orhan G, I Orhan, N Subutay-Oztekin, F Ak, B Sener. Contemporary anticholinesterase pharmaceuticals of natural origin and their synthetic analogues for the treatment of Alzheimer's disease. Recent. Pat. CNS Drug. Discov. 4 (2009): 43-51.

Ingkaninan K, D Best, VD Heijden, AJP Hofte, B Karabatak, H Irth, UR Tjaden, VD Greef, R Verpoorte. High-performance liquid chromato-graphy with on-line coupled UV, mass spectrometric and biochemical detection for identification of acetylcholines-terase inhibitors from natural products. J. Chromatogr. A 872 (2000): 61–73.

Ingkaninan K, P Temkitthawon, K Chuenchom, T Yuyaem, W Thongnoi. Screening for acetylcholinesterase inhibitory activity in plants used in Thai traditional rejuvenating and neurotonic remedies. J. Ethnopharmacol. 89 (2003): 261–264.

Adsersen A, B Gauguin, L Gudiksen, AK Jager. Screening of plants used in Danish folk medicine to treat memory dysfunction for acetylcholinesterase inhibitory activity. J. Ethnopharmacol. 104 (2006): 418-422.

Perry NSL, PJ Houghton, AE Theolad, P Jenner, EK Perry. In vitro inhibition of human erythrocyte acetylcholinesterase by Sal via lavandulaefolia essential oil and constituent terpenes. J. Pharm. Pharmacol. 52 (2000): 895-902.

Howes MJ, PJ Houghton. Plants used in Chinese and Indian traditional medicine for improvement of memory and cognitive function. Pharmacol. Biochem. Behav. 75 (2003): 513-527.

Mukherjee PK, V Kumar, M Mal, PJ Houghton. Acetylcholinesterase inhibitors from plants. Phytomedicine 14 (2007a): 289-300.

De Caires S, V Steenkamp. Use of Yokukansan (TJ-54) in the Treatment of Neurological Disorders: A Review. Phytother. Res. (2010) Doi: 10.1002/ptr.3146.

Heinrich M, HL Teoh. Galanthamine from snowdrop-the development of a modern drug against Alzheimer’s disease from local Caucasian knowledge. J. Ethnopharmacol. 92 (2004): 688-697.

Singh R, N Singh, BS Saini, HS Rao. In vitro antioxidant activity of pet ether extract of black pepper. Indian J Pharmacol .40. 4 (2008):147-51.

Chonpathompikunlert P, J Wattanathorn, S Muchimapura. Piperine, the main alkaloid of Thai black pepper, protects against neurodegeneration and cognitive impairment in animal model of cognitive deficit like condition of Alzheimer's disease. Food Chem Toxicol. 48.3 (2010):798-802.

De M, AK De, R Mukhopadhay, AB Banerjee, M Micro. Antimicrobial activity of Cuminum cyminum L. Ars Pharmaceutica .44 (2005):257-69.

Koppula S, DK Choi. Cuminum cyminum extract attenuates scopolamine-induced memory loss and stress- induced urinary biochemical changes in rats: a noninvasive biochemical approach. Pharm biol .49.7 (2011):702-8.

Sharma R, R Gupta. Cyperus rotundus extract inhibits acetylcholinesterase activity from animal and plants as well as inhibits germination and seedling growth in wheat and tomato. Life Sci. 80.24-25 (2007): 2389-2392.

Das A, G Shanker, C Nath, R Pal, S Singh, H Singh. A comparative study in rodents of standardized extracts of Bacopa monniera and Ginkgo biloba: anticholinesterase and cognitive enhancing activities. Pharmacol Biochem Behav 73.4 (2002): 893-900.

Pachauri SD, S Tota, K Khandelwal, PR Verma, C Nath, K Hanif et al. Protective effect of fruits of Morinda citrifolia L. on scopolamine induced memory impairment in mice: a behavioral, biochemical and cerebral blood flow study. J Ethnopharmacol 139.1 (2012): 34-41.

Muralidharan P, VR Kumar, G Balamurugan. Protective effect of Morinda citrifolia fruits on β-amyloid induced cognitive dysfunction in mice: an experimental and biochemical study. Phytother Res 24.2(2010): 252-258.

Hanumanthachar J, P Milind. Pharmacological Evidences for the Antiamnesic Effects of Desmodium gangeticum in mice. Iranian Journal of Pharmaceutical Research. 6.3 (2007):199-207.

Rastogi S, MM Pandey, AKS Rawat. An ethnomedicinal, phytochemical and pharmacological profile of Desmodium gangeticum (L.) DC. and Desmodium adscendens (Sw.) DC. Journal of Ethnopharmacology. 136 (2011): 283-296.

Kumar S, CJ Seal, EJ Okello. Kinetics of acetylcholinesterase inhibition by an aqueous extract of Withania somnifera roots. Intrenational journal of pharmaceutical sciences and research. 2 .5 (2011): 1188-1192.

Borhade P, A Tankar, S Joshi, K Khandelwal. Pharmacological Review on Ficus racemosa linn. International Journal of Pharmaceutical Research and Bio –Science 1 .6 (2012): 51-66.

Dugoua JJ, D Seely, D Perri, K Cooley, T Forelli. From type 2 diabetes to antioxidant activity: a systematic review of the safety and efficacy of common and cassia cinnamon bark. Can J Physiol Pharmaco .85 (2007):837–847.

Peterson DW, RC George, F Scaramozzino, NE La Pointe, RA Anderson, DJ Graves, J Lew. Cinnamon extract inhibits tau aggregation associated with Alzheimer's disease in vitro. J Alzheimers Dis. 17.3 (2009):583-97.

Frydman-Marom A, A Levin, D Farfara, T Benromano, R Scherzer-Attali, S Peled Orally administered cinnamon extract reduces β-amyloid oligomerization and corrects cognitive impairment in AD animal models. PLoS One 6.1(2011): e16564.

Shobana S, KA Naidu. Antioxidant activity of selected India spices. Prostaglandin Leukotri Essent Fat Acids. 62.2 (2000):107–10.

Halder S, AK Mehta, R Kar, M Mustafa, PK Mediratta, KK Sharma. Clove oil reverses learning and memory deficits in scopolamine treated mice. Planta Med. 77.8 (2011):830-4.

Akinrimisi EO, AL Akinwande. Effect of aqueous extract of Eugenia caryophyllus on brain acetylcholinesterase in rats. West Afr J Pharmacol Drug Res. 2.2(1975):127-31.

Bores GM, FP Huger, W Petko, AE Mutlib, F Camacho, DK Rush et al., Pharmacological evaluation of novel Alzheimer’s disease therapeutics: Acetylcholinesterase inhibitors related to galanthamine. J Pharmacol Exp Ther. 277 (1996):728-38.

lkay O, O Gurdal and S Bilge. An update on plant-originated treatment for Alzheimer’s disease. Ethnomedicine: A Source of Complementary Therapeutics Available from: [Last accessed on 2011 Jul 25]. (2010): 245-65.

Lannert H, S Hoyer. Intracerebroventricular administration of streptozotocin causes long-term diminutions in learning and memory abilities and in cerebral energy metabolism in adult rats. Behav Neurosci. 112 (1998):1199-208.


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