Author(s): Helmi, Nanang Fakhrudin, Arief Nurrochmad, B. S. Arie Sudarmanto, Zullies Ikawati

Email(s): zullies_ikawati@ugm.ac.id

DOI: 10.5958/0974-360X.2020.00409.6   

Address: Helmi1, Nanang Fakhrudin2, Arief Nurrochmad3, B. S. Arie Sudarmanto4, Zullies Ikawati3*
1Faculty of Pharmacy, Universitas Gadjah Mada, Sekip Utara, Yogyakarta 55281, Indonesia.
2Department of Pharmaceutical Biology, Faculty of Pharmacy, Universitas Gadjah Mada, Sekip Utara, Yogyakarta 55281, Indonesia.
3Department of Pharmacology and Clinical Pharmacy, Faculty of Pharmacy, Universitas Gadjah Mada, Sekip Utara, Yogyakarta 55281, Indonesia.
4Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Universitas Gadjah Mada, Sekip Utara, Yogyakarta 55281, Indonesia.
*Corresponding Author

Published In:   Volume - 13,      Issue - 5,     Year - 2020


ABSTRACT:
Secang (Caesalpinia sappan L.) (CS) is one of the plants widely found in Indonesia and known to have a various biological activities. However, there is no scientific evidence regarding its cognitive enhancing activity through the inhibition of Phosphodisesterase-1 (PDE1). PDE1 is recently discovered as a promising molecular target for the development of cognitive enhancer agents to combat cognitive diseases. This study aimed to identify in vitro PDE1-inhibition activity of n-hexane, chloroform and ethanol extracts of CS wood and its major constituent, brazilin, with Cyclic Nucleotide Phosphodiesterase Assay Kit and in silico interaction of brazilin with PDE1 used Molecular Operating Environment (MOE) ver. 2016.01. This study demonstrates that the ethanol extract was the most active PDE1-inhibition activity compared to the other extracts with the inhibition of 52.7% at concentration of 100µg/mL. Interestingly, brazilin at concentration of 11.45µg/mL inhibited PDE1 activity (30.6%) equal to the positive control, vinpocetine (14.02 µg/mL). In conclusion, the ethanol extract of CS wood and its major constituent, brazilin, inhibited PDE1 activity and could be develop as cognitive enhancer.


Cite this article:
Helmi, Nanang Fakhrudin, Arief Nurrochmad, B. S. Arie Sudarmanto, Zullies Ikawati. In Vitro and In Silico Studies of Secang Wood (Caesalpinia sappan L.) Extracts and Brazilin as Natural Phosphodiesterase-1 (PDE1) Inhibitor for Herbal Cognitive Enhancer Development. Research J. Pharm. and Tech 2020; 13(5): 2269-2274. doi: 10.5958/0974-360X.2020.00409.6

Cite(Electronic):
Helmi, Nanang Fakhrudin, Arief Nurrochmad, B. S. Arie Sudarmanto, Zullies Ikawati. In Vitro and In Silico Studies of Secang Wood (Caesalpinia sappan L.) Extracts and Brazilin as Natural Phosphodiesterase-1 (PDE1) Inhibitor for Herbal Cognitive Enhancer Development. Research J. Pharm. and Tech 2020; 13(5): 2269-2274. doi: 10.5958/0974-360X.2020.00409.6   Available on: https://www.rjptonline.org/AbstractView.aspx?PID=2020-13-5-39


REFERENCES:
1.    Froestl, W., Muhs, A. and Pfeifer, A. Cognitive Enhancers (Nootropics). Part 1: Drugs Interacting with Receptors. J. Alzheimers Dis. 2012; 32: 793–887.
2.    Tabassum, N., Rasool, S., Malik, Z. A. and Ahmad, F. Natural Cognitive Enhancers. J. Pharm.  Res. 2012; 8.
3.    Vasudev Pai, C. S Shreedhara, Chandrashekar K. S, Aravinda Pai, Venkatesh Kamath. Cognitive Enhancement and Neuroprotective Effects of Ancient Ayurvedic Medicinal Plant Celastrus Paniculatus: An Overview. Research J. Pharm. and Tech 2016; 9(8):1295-1298.
4.    Rohan R.Vakhariya, Swati S.Talokar, V. R. Salunkhe, C.S. Magdum. Cognitive Disorders and its Herbal Remedies. Res. J. Pharmacognosy and Phytochem. 2017; 9(1): 42-46.
5.    Monirul Islam, Ramanjaneyulu. J, Veeresh Babu. D, Mohibul Hoque, Narayana Swamy V.B. Studies on Memory Enhancing Property of Bravobol- A Polyherbal Formulation in Experimentally Induced Alzheimers Disease in Experimental Animals. Asian J. Res. Pharm. Sci. 5(2): 2015; 103-110.
6.    Conti, M. and Richter, W. Phosphodiesterases and Cyclic Nucleotide Signaling In The CNS. in Cyclic-Nucleotide Phosphodiesterases In The Central Nervous System. John Wiley and Sons, Inc. 2014; eds. Brandon, N. J. and West, A. R.: pp. 1-46.
7.    Wu, Y., Li, Z., Huang, Y.-Y., Wu, D. and Luo, H.-B. Novel Phosphodiesterase Inhibitors for Cognitive Improvement in Alzheimer’s Disease: Miniperspective. J. Med. Chem. 2018; 61: 5467–5483.
8.    DS Patel, IS Anand, PA Bhatt. Physiological Activity of Phosphodiesterase. Research J. Pharmacology and Pharmacodynamics. 2011; 3(5): 223-233.
9.    Blokland, A., Menniti, F. S. and Prickaerts, J. PDE Inhibition and cognition enhancement. Expert Opin. Ther. Pat. 2012; 22: 349–354.
10.    Froestl, W., Muhs, A. and Pfeifer, A. Cognitive Enhancers (Nootropics). Part 2: Drugs Interacting with Enzymes. Update 2014. J. Alzheimers Dis. 2014; 42: 1–68.
11.    Omori, K. and Kotera, J. Overview of PDEs and Their Regulation. Circ. Res. 2007; 100: 309–327.
12.    Rahimi, R., Ghiasi, S., Azimi, H., Fakhari, S. and Abdollahi, M. A review of the herbal phosphodiesterase inhibitors; Future perspective of new drugs. Cytokine. 2010; 49: 123–129.
13.    Bairagi G.B., Kabra A.O., Mandade R.J. Sexual Dysfunction in Men with Diabetes Mellitus. Research J. Pharm. and Tech. 4(5): May 2011; Page 677-684.
14.    Bender, A. T. Cyclic Nucleotide Phosphodiesterases: Molecular Regulation to Clinical Use. Pharmacol. Rev. 2006; 58: 488–520.
15.    Boswell-Smith, V., Spina, D. and Page, C. P. Phosphodiesterase inhibitors: Phosphodiesterase inhibitors. Brit. J. Pharmacol. 2009; 147: S252–S257.
16.    Kulbe, P. Vinpocetine : a step towards memory enhancement. Int. J. Pharma Res. Dev., 2013; 2: 99-108.
17.    Medina, A. E. Therapeutic Utility of Phosphodiesterase Type I Inhibitors in Neurological Conditions. Front. Neurosci. 2011; 5.
18.    Ogunrin, A. Effect of Vinpocetinee (CognitolTM) on Cognitive Performances of a Nigerian Population. Ann Med Health Sci Res. 2014; 4: 654–661.
19.    Szatmari, S. Z. and Whitehouse, P. J. Vinpocetinee for cognitive impairment and dementia. Cochrane Database Syst Rev. 2003.
20.    Payal Patil, Mukesh Patil, Dipak D Patil. Development and Validation of RP-HPLC Method for Simultaneous Estimation of Piracetam and Vinpocetine. Asian J. Pharm. Ana. 2018; 8(2):103-108.
21.    Hamzah, H., Hertiani, T., Pratiwi, S. U. T. and Nuryastuti, T. The Inhibition Activity of Tannin on the Formation of Mono-Species and Polymicrobial Biofilm Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, and Candida albicans. Trad.Med.J. 2019;(24):110–118.
22.    Nirmal, N. P., Rajput, M. S., Prasad, R. G. S. V. and Ahmad, M. Brazilin from Caesalpinia sappan heartwood and its pharmacological activities: A review. Asian Pac. J. Trop. Med. 2015; 8: 421–430.
23.    Pawar, C. R. Phytochemical and pharmacological aspects of Caesalpinia sappan. J. Pharm. Res. 2008; 8.
24.    Rina, O. Stabilities natural colorant of Sappan wood (Caesalpinia sappan. L) for food and beverages in various pH, temperature, and matrices of food. Int. J. ChemTech Res. 2017; 6.
25.    K. Mekala, R. Radha. A Review on Sappan Wood - A Therapeutic Dye Yielding Tree. Res. J. Pharmacognosy and Phytochem. 2015; 7(4): 227-231.
26.    Iffath Badsha, Valli Nachiyar C. Elucidation of Antibacterial effects of Spices as Drinking Water Additives. Research J. Pharm. and Tech 2017; 10(11): 3795-3797.
27.    Jennifer F, Thomas AK, Fernandes R, Subrhamanyam EVS. Anti-inflammatory activity of Ethanolic Extract of the Roots of the Plant Caesalpinia sappan Linn. Research J. Pharm. and Tech. 3(1): Jan.-Mar. 2010; Page 99-101.
28.    Balamurugan Gunasekaran, P. Muralidharan, A. Pandiselvi, P. Amutha. Preliminary Phytochemical screening and Anti oxidant activities of Ethanolic extract of Caesalpinia sappan Linn. Research J. Pharm. and Tech. 1(3): July-Sept. 2008; Page 179-181.
29.    Kaur, H., Amini, M. H., Prabhakar, D. P., Singh, A. and Suttee, D. A. Phytochemical Screening and Antimicrobial Activity of Caesalpinia sappan L. Leaves. Int. J. Pharmacogn. Phytochem. Res. 2016; 8.
30.    Parveen, A., Farooqi, M., Kyunn, W. and Arshad, M. Phytochemical Screening and Content Determination of Different Species of Genus Caesalpinia belonging to Different Origin with Antidiabetic Activity. Pharmacogn. J. 2017; 9: 743–749.
31.    Tulin, E., Loreto, M., Tulin, E. and Tulin, E. Alpha-Glucosidase Inhibitory Activity and Fractionation of Bioactive Compounds from bark Extracts of Sibucao (Caesalpinia sappan L.) In the Philippines. Pharmacogn. J. 2017; 9: 356–360.
32.    Rasheed Ahmed, KL Senthilkumar, M Rajkumar. Antidiarrhoeal Activity of Bark Extracts of Caesalpinia sappan. Linn. Research J. Pharmacology and Pharmacodynamics. 2009; 1(3):128-129.
33.    Nikaido, T. et al. Inhibitors of cyclic AMP phosphodiesterase in medicinal plants. Planta Med. 1981; 43: 18–23.
34.    Temkitthawon, P. et al. Screening for phosphodiesterase inhibitory activity of Thai medicinal plants. J Ethnopharmacol. 2008; 119: 214–217.
35.    Hesse, R. et al. Reduced cGMP levels in CSF of AD patients correlate with severity of dementia and current depression. Alzheimers. Res. Ther. 2017; 9.
36.    Oeckl, P. et al. CSF Concentrations of cAMP and cGMP Are Lower in Patients with Creutzfeldt-Jakob Disease but Not Parkinson’s Disease and Amyotrophic Lateral Sclerosis. PLoS ONE. 2012; 7.
37.    Alberini, C. M. Transcription Factors in Long-Term Memory and Synaptic Plasticity. Physiol. Rev. 2009; 89: 121–145.
38.    Keravis, T. and Lugnier, C. Cyclic nucleotide phosphodiesterase (PDE) isozymes as targets of the intracellular signalling network: benefits of PDE inhibitors in various diseases and perspectives for future therapeutic developments: PDEs: intracellular network targets for diseases. Brit. J. Pharmacol. 2012; 165: 1288–1305.
39.    Nair, A. and Vaidya, V. A. Cyclic AMP response element binding protein and brain-derived neurotrophic factor: Molecules that modulate our mood? J. Biosciences. 2006; 31: 423–434.
40.    Saavedra, A., Giralt, A., Arumí, H., Alberch, J. and Pérez-Navarro, E. Regulation of Hippocampal cGMP Levels as a Candidate to Treat Cognitive Deficits in Huntington’s Disease. PLoS ONE. 2013; 8.
41.    Radha Mahendran, Suganya Jeyabasker, Astral Francis, Sharanya Manoharan. Homology Modeling and in silico docking analysis of BDNF in the treatment of Alzheimer’s disease. Research J. Pharm. and Tech. 2017; 10(9): 2899-2906.
42.    Zainab Mir1, Rosliza2, Behroz Naeem1, Ilyas Muhammad Nadeem2, Prof. Nordin Bin Simbak, Prof. Zubaidi ALA, Prof. Tengku Mohammad Ariff, Khalili MR, Mohammad Amjad Kamal, Atif Amin Baig. Synergistic Molecular Effect of BDNF, ApoE and MTHFR in inducing Depression in Alzheimer’s Disease. Research J. Pharm. and Tech 2018; 11(10): 4317-4323.
43.    Mohamad Qulam Zaki Bin Mohamad Rasidi. Review: Dietary habits and its effect on the short and long term memory. Research J. Pharm. and Tech 2016; 9(8):1291-1294.
44.    Tae-Gon Kim, Sea-Hyun Bae, Kyung-Yoon Kim. Effects of Dual-Task Training with different Intensity of Aerobic Exercise on Cognitive Function and Neurotrophic Factors in Chronic Stroke Patients. Research J. Pharm. and Tech 2019; 12(2):693-698.
45.    Mohammad Ahmed Issa Al-Hatamleh Tengku Mohammad Ariff Omar Mahmoud Al-Shajrawi Muhammad Ilyas Nadeem Nordin Bin Simbak Ahmad Zubaidi A. Latif Atif Amin Baig. Computational Evaluation of the Promoter Region of the Brain Derived Neurotrophic Factor (BDNF) Gene; towards its Involvement in Stress-Induced Haematological Parameters Alteration in Medical Students. Research J. Pharm. and Tech 2018; 11(10): 4657-4661.
46.    Shovit Ranjan, Praveen Kumar Sharma. Association of Brain-Derived Neurotrophic factor (BDNF) gene SNP G196A with Type 2 Diabetes and Obesity: A Meta- Analysis. Research J. Pharm. and Tech 2017; 10(12): 4297-4305.

Recomonded Articles:

Research Journal of Pharmacy and Technology (RJPT) is an international, peer-reviewed, multidisciplinary journal.... Read more >>>

RNI: CHHENG00387/33/1/2008-TC                     
DOI: 10.5958/0974-360X 

1.3
2021CiteScore
 
56th percentile
Powered by  Scopus


SCImago Journal & Country Rank

Journal Policies & Information


Recent Articles




Tags


Not Available