Author(s): Safiya Sultana T, Sivakumar M

Email(s): sashatasneem98@gmail.com

DOI: 10.52711/0974-360X.2021.00609   

Address: Safiya Sultana T*, Sivakumar M
Department of Pharmacology, Sri Ramachandra Institute of Higher Education and Research, Porur, Chennai – 600116.
*Corresponding Author

Published In:   Volume - 14,      Issue - 7,     Year - 2021


ABSTRACT:
Objective: To use virtual screening analysis to screen out the phytoconstituents of Syzygium aromaticum against multiple targets of AD and determine its anti-oxidant and inflammatory inhibitory property. Methods: The compounds listed out from Syzygium aromaticum were subjected to virtual screening based on their drug likeness property and bioactivity scores. The molecular docking simulation such as HEX 8.0, PyRx, MVD along with Auto Dock 4.2 were employed to determine the potential candidate for providing activity against multiple targets of AD. The toxicity estimation was also carried out using TEST software. The potential candidate was further evaluated using DPPH, FRAT, Albumin denaturation and Proteinase inhibition method. Results: Only eight phytoconstituents were selected for virtual screening as they possessed drug likeness property and better bioactivity score for inhibition of kinases, proteases and enzymes. The docking results from various tools predicted that Oleanolic acid can be considered as potential constituents for multi-target action against AD. Toxicity estimation was in range. It also exhibited anti-oxidant and inflammatory inhibition providing its evidence for anti-AD activity. Conclusion: Taken together, these virtual screening results and in-vitro assays suggest that Oleanolic acid has multi target action against AD, which can be proved further with in-vivo studies.


Cite this article:
Safiya Sultana T, Sivakumar M. Clove Constituents as new leads for the Design and development of Multi-targeted Anti-Alzheimer activity. Research Journal of Pharmacy and Technology. 2021; 14(7):3515-2. doi: 10.52711/0974-360X.2021.00609

Cite(Electronic):
Safiya Sultana T, Sivakumar M. Clove Constituents as new leads for the Design and development of Multi-targeted Anti-Alzheimer activity. Research Journal of Pharmacy and Technology. 2021; 14(7):3515-2. doi: 10.52711/0974-360X.2021.00609   Available on: https://rjptonline.org/AbstractView.aspx?PID=2021-14-7-6


REFERENCE:
1.    Perry EK, Perry RH, Blessed G, Tomlinson BE. Changes in brain cholinesterases in senile dementia of Alzheimer type. Neuropathology and Applied Neurobiology. 1978;4(4): 273-7.
2.    Rombouts SA, Barkhof F, Van Meel CS, Scheltens P. Alterations in brain activation during cholinergic enhancement with rivastigmine in Alzheimer’s disease. Journal of Neurology, Neurosurgery and Psychiatry. 2002 1;73(6): 665-71.
3.    US department of Health and Human Service, Public Health Services, National Institute on Aging. Alzheimer’s disease Genetics: Fact Sheet. Silver Spring, MD: Alzheimer’s Disease Education and Referral Center; 1999. NIH Publication 99-4664.
4.    Ciro A, Park J, Burkhard G, Yan N, Geula C. Biochemical differentiation of cholinesterases from normal and Alzheimer's disease cortex. Current Alzheimer Research. 2012 Jan 1;9(1):138-43.
5.    Caputo CB, Salama AL. The amyloid proteins of Alzheimer’s disease as potential target for drug therapy. Neurobiol Aging 1989; 10: 451-461.
6.    Liddell M, Willams J, Bayer A, et al. Conformation of association between the e4 allele of apolipoprotein E and Alzheimer’s disease. J Med Genet 31: 197-200, 1994.
7.    Reddy CH, Reddy G, Mahto MK, Kunala P, Kanth RC. Insilico Design and Discovery of Some Novel Ache Inhibitors for Treatment of Alzheimer's Disorder. Research Journal of Pharmacy and Technology. 2012;5(3): 424-7.
8.    Dalai MK, Bhadra S, Chaudhary SK, Bandyopadhyay A, Mukherjee PK. Anti-cholinesterase activity of the standardized extract of Syzygium aromaticum L. Pharmacognosy Magazine. 2014 Apr;10(Suppl 2): S276
9.    Geun Kim H, Sook Oh M. Herbal medicines for the prevention and treatment of Alzheimer's disease. Current Pharmaceutical Design. 2012 Jan 1;18(1): 57-75.
10.    Kassab RB, Bauomy AA. The neuroprotective efficiency of the aqueous extract of clove (Syzygium‎ aromaticum) in aluninium induced neurotoxicity. Int J Pharm Pharm Sci. 2014;6(5): 503-8.
11.    Keerti Shrivastava, Sherendra Sahu, Skand K. Mishra, Kantishree De. In vitro Antimicrobial Activity and Phytochemical Screening of Syzygium aromaticum. Asian J. Res. Pharm. Sci. 4(1): Jan.-Mar. 2014; Page 12-15.
12.    Patil P, Thakur A, Sharma A, Flora SJ. Natural products and their derivatives as multifunctional ligands against Alzheimer's disease. Drug Development Research. 2019 Aug 20.
13.    Hassan M, Shahzadi S, Seo SY, Alashwal H, Zaki N, Moustafa AA. Molecular docking and dynamic simulation of AZD3293 and solanezumab effects against BACE1 to treat Alzheimer's disease. Frontiers in Computational Neuroscience. 2018 Jun 1; 12:34.
14.    Hassan ST, Švajdlenka E. Biological evaluation and molecular docking of protocatechuic acid from Hibiscus sabdariffa L. as a potent urease inhibitor by an ESI-MS based method. Molecules. 2017 Oct;22(10): 1696.
15.    Srikanth J, Kavimani S, Reddy CU. In silico Docking Study of Active Constituents Identified in Morinda citrifolia Linn as Enzyme targets of Alzheimer's Disease. In Proceedings of the International Conference on Bioinformatics and Computational Biology (BIOCOMP) 2012 (p. 159). The Steering Committee of The World Congress in Computer Science, Computer Engineering and Applied Computing (World Comp).
16.    K. Hemalatha, K. Girija. Evaluation of Drug Candidature of some Benzimidazole Derivatives as Biotin Carboxylase Inhibitors: Molecular docking and Insilico studies. Asian J. Res. Pharm. Sci. 6(1): Jan.-Mar., 2016; Page 15-20.
17.    Mathew A. Docking studies on anticancer drugs for breast cancer using Hex.
18.    Kumar RS, Basha SN, Nallasivan PK, Solomon WD, Venkatnarayanan R. Computer Aided Docking Studies on Antiviral Drugs for Bird Flu. Asian J Research Chem. 2010; 3(2): 370-3.
19.    Fereidoonnezhad M, Mostoufi A, Zali S, Eskandari M, Afshar D, Aliyan F. Molecular Docking and PLIF Studies of Novel Tacrine-Naphtoquinone Hybrids Based on Multi-Target-Directed Ligand Approach for Alzheimer’s Disease. Jundishapur Journal of Natural Pharmaceutical Products. 2018; 13(2).
20.    K. Hemalatha, Joseph Selvin, K. Girija. Synthesis, In silico Molecular Docking Study and Anti-bacterial Evaluation of some Novel 4-Anilino Quinazolines. Asian J. Pharm. Res. 2018; 8(3): 125-132.
21.    Blois MS. Antioxidant determinations by the use of a stable free radical. Nature 1958;181: 1199–200.
22.    Ch. Madhu, J. Swapna, K. Neelima, Monic V. Shah. A Comparative Evaluation of the Antioxidant Activity of Some Medicinal Plants Popularly Used in India. Asian J. Res. Pharm. Sci. 2(3): July-Sept. 2012; 98-100.
23.    Gülçin İ, Bursal E, Şehitoğlu HM, Bilsel M, Gören AC. Polyphenol contents and antioxidant activity of lyophilized aqueous extract of propolis from Erzurum, Turkey. Food Chem Toxicol 2010;48(8–9): 2227−2238.
24.    Ghanshyam B. Jadhav, Ravindranath B. Saudagar. Free radical Scavenging and Antioxidant Activity of Punica granatum Linn. Asian J. Res. Pharm. Sci. 4(2): April-June 2014; 51-54.
25.    Sakat S, Juvekar AR, Gambhire MN. In vitro antioxidant and anti-inflammatory activity of methanol extract of Oxalis corniculata Linn. International Journal of Pharma and Pharmacological Sciences 2010; 2(1): 146-155.
26.    Oyedepo OO and Femurewa AJ. Anti-protease and membrane stabilizing activities of extracts of Fagra zanthoxiloides, Olax subscorpioides and Tetrapleura tetraptera. Int J of Pharmacong 1995; 33: 65‐69.
27.    Perry EK, Pickering AT, Wang WW, Houghton PJ, Perry NSL. Medicinal plants and Alzheimer's disease: from ethnobotany to phytotherapy. J Pharm Pharmacol 1999; 51(5): 527-534
28.    Roberson MR, Harrell LE. Cholinergic activity and amyloid precursor protein metabolism. Brain Res Rev 1997; 25(1): 50-69.
29.    Scarpini E, Scheltens P, Feldman H. Treatment of Alzheimer's disease; current status and new perspectives. Lancet Neurol 2003; 2(9): 539-547.
30.    Holmes C, Wilkinson D. Molecular biology of Alzheimer's disease. Adv Psychiatr Treat 2000; 6(3): 193-200.
31.    Sravani M, Lakshmi PS, Reddy KA, Deepthi NN, Kantheti US. Insilico Analysis and Docking of Tacrine and Donepezil Derivatives Targeting Histamine-N-Methyltransferase and Acetyl Cholinesterase Protein Respectively for Alzheimer's Disease. Research Journal of Pharmacy and Technology. 2013;6(1): 86-9.
32.    Schulz V. Ginkgo extract or cholinesterase inhibitors in patients with dementia: what clinical trial and guidelines fail to consider. Phytomedicine. 2003; 10(4): 74-79.
33.    Jayasurya SS, Keerthi K, Rambabu M, Jayanthi S. Identification of ZAP-70 Inhibitor from Macroalgae through Docking and Molecular Dynamics Studies. Research J Pharm and Tech. 2017;10(12): 4162-6.
34.    Shankari B, Rambabu M, Jayanthi S. Claudin-7 Inhibitors for Colon Cancer: A Computational Approach. Research J Pharm and Techn. 2018;11(8): 3415-8.
35.    Osawa T. Novel natural antioxidants for utilization in food and biological systems, in Postharvest Biochemistry of Plant Food Materials in the Tropics, ed. by Uritani, I., Garcia, V. V. and Mendoza, E. M., Japan Scientific Societies Press, Tokyo, 1994; pp. 241–251.
36.    Mueller M, Hobiger S, Jungbauer A. Anti-inflammatory activity of extracts from fruits, herbs and spices. Food Chem 2010; 122:987–96.

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