IN VITRO SCREENING FOR ACETYLCHOLINESTERASE ENZYME INHIBITION POTENTIAL OF MUTHU PARPAM – THERAPEUTIC LEAD FOR ALZHEIMER’S DISEASE
Objective: Siddha system is an ancient traditional system of medicine treats many chronic ailments and neurological disorders. Muthu parpam is one of the herbo marine Siddha drugs which have the indication for neurocognitive dysfunction. The main objective of this current study was to evaluate the acetylcholine esterase (AChE) inhibition of Muthu parpam.
Methods: AChE activity was evaluated using a modified 96-well microplate assay based on Ellman’s method. Physostigmine (5, 10, 20, and 40 μg/ml) was used as the positive control.
Results: The result of this study clearly indicates that the test drug Muthu Parpam was effective in inhibiting AChE enzyme at the specified concentration dose dependently. Maximum percentage inhibition of about 71.68% was observed at 500 μg/ml when compared to that of the Physostigmine, a known AChE inhibitor with the maximum inhibition 84.87% at the concentration of 40 μg/ml.
Conclusion: Hence, this preliminary screening has proven the efficacy of Muthu parpam through AChE inhibition potential in the management of Alzheimer disease.
2. Giacobini E. Cholinergic function and Alzheimer’s disease. Int J Geriatr Psychiatry 2003;18 Suppl 1:S1-5.
3. DeKosky ST, Harbaugh RE, Schmitt FA, Bakay RA, Chui HC, Knopman DS, et al. Cortical biopsy in Alzheimer’s disease: Diagnostic accuracy and neurochemical, neuropathological, and cognitive correlations. Intraventricular bethanecol study group. Ann Neurol 1992;32:625-32.
4. Bartus RT, Dean RL, Beer B, Lippa AS. The cholinergic hypothesis of geriatric memory dysfunction. Science 1982;217:408-17.
5. Sims NR, Bowen DM, Allen SJ, Smith CC, Neary D, Thomas DJ, et al. Presynaptic cholinergic degeneration in patients with dementia. J Neurochem 1983;40:503-9.
6. Brenner GM. Pharmacology. Philadelphia, PA: WB Saunders Company; 2000.
7. Rahman AU, Choudhary MI. Bioactive natural products as a potential source of new pharmacophores a theory of memory. Pure Appl Chem 2001;73:555-60.
8. Oh MH, Houghton PJ, Whang WK, Cho JH. Screening of Korean herbal medicines used to improve cognitive function for anti-cholinesterase activity. Phytomedicine 2004;11:544-8.
9. Melzer D. New drug treatment for Alzheimer’s disease: Lessons for healthcare policy. BMJ 1998;316:762-4.
10. Schulz V. Ginkgo extract or cholinesterase inhibitors in patients with dementia: What clinical trial and guidelines fail to consider. Phytomedicine 2003;10 Suppl 4:74-9.
11. Wollen KA. Alzheimer’s disease: The pros and cons of pharmaceutical, nutritional, botanical, and stimulatory therapies, with a discussion of treatment strategies from the perspective of patients and practitioners. Altern Med Rev 2010;15:223-44.
12. Orhan I, Sener B, Choudhary MI, Khalid A. Acetylcholinesterase and butyrylcholinesterase inhibitory activity of some Turkish medicinal plants. J Ethnopharmacol 2004;91:57-60.
13. Traditional Medicine, Definition, World health Organisation; 2020. Available from: https://www.who.int/traditional-complementary-integrative-medicine/about/en.
14. Thiyagarajan R. Gunapadam Thadhu-Jeeva Vaguppu. 8th ed., Vol. 2, 3. Chennai: Directorate of Indian medicine and Homeopathy; 2013. p. 500, 501.
15. Pillai TV. Tamil-English Dictionary. Vol. 5, 6. Chennai: The Research Institute of Siddhar’s Science; 1931. p. 717.
16. Thiyagarajan R. Theran Yamaga Venbaa. 1st ed., Vol. 2. Chennai: Booma Devi Printers; 1997. p.105.
17. Ellman GL, Courtney KD, Andres V, Featherstone RM. A new and rapid colorimetric determination of acetylcholinesterase activity. Biochem Pharmacol 1961;7:88-95.
18. Thal LJ, Fuld PA, Masur DM, Sharpless NS. Oral physostigmine and lecithin improve memory in Alzheimer disease. Ann Neurol 1983;13:491-6.
19. Arens AM, Kearney T. Correction to: Adverse effects of physostigmine. J Med Toxicol 2019;15:310.
20. Ali TB, Schleret TR, Reilly BM, Chen WY, Abagyan R. Adverse effects of cholinesterase inhibitors in dementia, according to the pharmacovigilance databases of the United-States and Canada. PLoS One 2015;10:e0144337.
21. Gupta RK, Tandon VR. Antinociceptive activity of Vitex negundo Linn leaf extract Indian. J Physiol Pharmacol 2005;49:163-70.
22. Kanwal A, Mehla J, Kuncha MS, Naidu VG. Anti-amnesic activity of Vitex negundo in scopolamine induced amnesia in rats. Pharmacol Pharm 2010;1:1-8.
23. Chen QS, Chen WQ, Yang SY. Pharmacologic study of Curculigo orchioides gaertn. Zhongguo Zhong Yao Za Zhi 1989;14:618-20, 640.
24. Jiang W, Fu F, Tian J, Zhu H, Hou J. Curculigoside A attenuates experimental cerebral ischemia injury in vitro and vivo. Neuroscience 2011;192:572-9.
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