scholarly journals Nature as a source of metabolites with cholinesterase-inhibitory activity: an approach to Alzheimer's disease treatment

2013 ◽  
Vol 65 (12) ◽  
pp. 1681-1700 ◽  
Author(s):  
Brígida R. Pinho ◽  
Federico Ferreres ◽  
Patrícia Valentão ◽  
Paula B. Andrade
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Inhibitory Activity ◽  
Disease Treatment ◽  
Cholinesterase Inhibitory Activity

scholarly journals Identification of Polyphenolics from Loranthus globosus as Potential Inhibitors of Cholinesterase and Oxidative Stress for Alzheimer’s Disease Treatment

2021 ◽  
Vol 2021 ◽  
pp. 1-16
Author(s):  
Netish Kumar Kundo ◽  
Md. Imran Nur Manik ◽  
Kushal Biswas ◽  
Riniara Khatun ◽  
Md. Yusuf Al-Amin ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Inhibitory Activity ◽  
Folk Medicine ◽  
Disease Treatment ◽  
Potential Source ◽  
Cholinesterase Inhibitory Activity ◽  
Potential Inhibitors ◽  
Crude Methanol Extract ◽  
And Oxidative Stress

Mistletoes are considered to be the potential medicinal herbs due to their rich traditional uses. Loranthus globosus is a Bangladeshi mango mistletoe that has been reported as folk medicine for various ailments and diseases. In an attempt to explore its effectiveness in Alzheimer’s disease (AD), we investigated the antioxidant and acetylcholinesterase inhibitory activity of L. globosus. We report that the crude methanol extract (CME) of the plant contains a good amount of polyphenolics and possesses antioxidant and cholinesterase inhibitory activity. Fractionation of CME with solvents of varying polarity revealed the highest activity and polyphenolic content in the ethylacetate fraction (EAF). Correlation analysis revealed a significant ( P < 0.05 ) association of polyphenolics with the antioxidant and cholinesterase inhibitory properties. Using column chromatography with diaion resin, the polyphenolics (EAF-PP) were isolated from the EAF that displayed the potent antioxidant and cholinesterase inhibitory activities. Kinetic analysis showed that EAF-PP exhibited a competitive type of inhibition. A total of thirty-six compounds including catechin and its different derivatives were identified in the EAF-PP by LC/MS analysis. Bioactivity-guided separation approach afforded the isolation of the two major active compounds catechin and catechin dimer from the EAF-PP. Hence, EAF-PP represents a potential source of antioxidants and cholinesterase inhibitors, which can be used in the management of AD.

Design, Synthesis and Biological Evaluation of New Cycloalkyl Fused Quinolines Tethered to Isatin Schiff Bases as Cholinesterase Inhibitors

2020 ◽  
Vol 23 ◽  
Author(s):  
Baswaraju Macha ◽  
Ravindra Kulkarni ◽  
Anil Kumar Garige ◽  
Rambabu Palabindala ◽  
Raghuramrao Akkinepally ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Schiff Bases ◽  
Active Site ◽  
Inhibitory Activity ◽  
Docking Studies ◽  
Behavioral Studies ◽  
Cholinesterase Inhibitory Activity ◽  
Butyryl Cholinesterase

Aims and Objective: Alzheimer’s disease is now a most prevalent neuro degenerative disease of central nervous system leading to dementia in elderly aged population. Numerous pathological changes have been associated in the progression of Alzheimer’s disease. One of such pathological hypothesis is declined cholinergic activity which eventually affects cognitive and memory deficits. Inhibition cholinesterases will apparently elevate acetyl choline levels which is benefactor on cognitive symptoms of the disease. This manuscript describes the new tacrine derivatives tethered to isatin Schiff bases through alkanoyl linker and screened for cholinesterase inhibitory activity. Materials and Methods: Tacrine and two more cycloalkyl ring fused quinolones were synthesized and converted to Ncycloalkyl fused quinoline chloroamides. Isatin Schiff bases were also synthesized by the reaction between isatin and substituted aromatic anilines and in subsequent reaction, isatin Schiff bases were reacted with cycloalkyl fused quinolones to afford anticipated compounds 10a-i, 11a-i and 12a-i. All the compounds have been screened for acetyl and butyryl cholinesterase inhibitory activity and in vivo behavioral studies. Binding interactions of the desired compounds have also been studied by docking them in active site of both cholinesterases. Results: Three compounds 12d, 12e and 12h with propionyl and butyroyl linker between amine and isatin Schiff base scaffold have shown potent acetyl and butyryl cholinesterase inhibitory activity. However most potent cholinesterase inhibitor was 13d with IC50 value of 0.71±0.004 and 1.08±0.02 μM against acetyl and butyryl cholinesterases respectively. The hepatotoxicity of potent compounds revealed that the tested compounds were less hepatotoxic than tacrine and also exhibited encouraging in vivo behavioral studies in test animals. Docking studies of all the molecules disclosed close hydrogen bond interactions within the binding site of both cholinesterases. Conclusion: New cycloalkyl fused quinolones tethered with alkoyl linker to isatin Schiff bases endowed significant and potent cholinesterase inhibitory activities. Few of the compounds have also exhibited lesser hepatotoxicity and all the synthesized compounds were good in behavioral studies. Molecular docking studies also indicated close interactions in active site of cholinesterases.

Effects of structural modifications on the metal binding, anti-amyloid activity, and cholinesterase inhibitory activity of chalcones

2015 ◽  
Vol 13 (36) ◽  
pp. 9418-9426 ◽  
Author(s):  
Marina Y. Fosso ◽  
Harry LeVine 3rd ◽  
Keith D. Green ◽  
Oleg V. Tsodikov ◽  
Sylvie Garneau-Tsodikova
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Inhibitory Activity ◽  
Metal Binding ◽  
Acetylcholinesterase Activity ◽  
Structural Modifications ◽  
Chalcone Derivatives ◽  
Cholinesterase Inhibitory Activity

Twenty chalcone derivatives were synthesized and found to bind Cu2+and Zn2+ions, modulate the dissociation of Aβ aggregates, and inhibit acetylcholinesterase activity. These chalcones show promise for the development of probes and/or therapeutics for Alzheimer's disease.

Drug Design of Inhibitors of Alzheimer’s Disease (AD): POM and DFT Analyses of Cholinesterase Inhibitory Activity of β-amino di-Carbonyl Derivatives

2019 ◽  
Vol 19 (8) ◽  
pp. 688-705
Author(s):  
Taibi Ben Hadda ◽  
Abdur Rauf ◽  
Hsaine Zgou ◽  
Fatma Sezer Senol ◽  
Ilkay Erdogan Orhan ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Cholinesterase Inhibitors ◽  
Metal Accumulation ◽  
Microtiter Plate ◽  
Metal Chelation ◽  
Carbonyl Derivatives ◽  
Cholinesterase Inhibitory Activity ◽  
Inhibitory Potential

Background:Since deficit of acetylcholine has been evidenced in the Alzheimer’s disease (AD) patients, cholinesterase inhibitors are currently the most specified drug category for the remediation of AD.Method:In the present study, 16 compounds (1-16) with dicarbonyl skeletons have been synthesized and tested for their inhibitory potential in vitro against AChE and BChE using ELISA microtiter plate assays at 100 μg/mL. Since metal accumulation is related to AD, the compounds were also tested for their metal-chelation capacity.Results and Conclusion:All the investigated dicarbonyl compounds exerted none or lower than 30% inhibition against both cholinesterases, whereas compounds 2, 8 and 11 showed 37, 42, 41% of inhibition towards BChE, being the most active. The highest metal-chelation capacity was observed with compound 8 (53.58 ± 2.06%). POM and DFT analyses are in good harmonization with experimental data.

Huprine Y – tryptophan heterodimers with potential implication to Alzheimer’s disease treatment

2021 ◽  
pp. 128100
Author(s):  
Eva Mezeiova ◽  
Martina Hrabinova ◽  
Vendula Hepnarova ◽  
Daniel Jun ◽  
Jana Janockova ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Disease Treatment ◽  
Potential Implication

Computational modelling of potent β-secretase (BACE1) inhibitors towards Alzheimer's disease treatment

2021 ◽  
Vol 270 ◽  
pp. 106536
Author(s):  
Samuel C. Ugbaja ◽  
Zainab K. Sanusi ◽  
Patrick Appiah-Kubi ◽  
Monsurat M. Lawal ◽  
Hezekiel M. Kumalo
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Computational Modelling ◽  
Disease Treatment
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