Combining in silico and in vitro approaches to evaluate the acetylcholinesterase inhibitory profile of some commercially available flavonoids in the management of Alzheimer’s disease

Asokkumar, Kuppusamy; Madeswaran, Arumugam; George, Sonia

doi:10.1016/j.ijbiomac.2016.11.062

Cited by 56 publications

(25 citation statements)

References 25 publications

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“…AutoDock is one of the most frequently used molecular docking suites and has been extensively validated over the years [ 43 , 44 ]. Calculations were performed using AutoDock 4.2.1.5, which is an automated docking suite capable of performing rigid or flexible docking [ 45 ].…”

Section: Methodsmentioning

confidence: 99%

Study on the Anticoagulant or Procoagulant Activities of Type II Phenolic Acid Derivatives

Luo

Cheng

et al. 2017

Molecules

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In this study, three type II phenolic acids (caffeic acid, p-hydroxycinnamic acid, and ferulic acid) were used to synthesize a total of 18 phenolic acid derivatives. With molecular docking for molecule design and target protein (factors) screening, in combination with the confirmation of target proteins (factors) by surface plasmon resonance, and the evaluation of haemostatic and anticoagulant activities with five blood assays (plasma recalcification time, prothrombin time, activated partial thromboplastin time, fibrinogen, and thrombin time), the data indicated that caffeic acid derivatives showed certain anticoagulant or procoagulant activities and that two other series contained compounds with the best anticoagulant activities. Using Materials Studio analysis, particular functional groups that affect anticoagulant or procoagulant activities were revealed, and these conclusions can guide the discovery of compounds with better activities.

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Section: Methodsmentioning

confidence: 99%

Study on the Anticoagulant or Procoagulant Activities of Type II Phenolic Acid Derivatives

Luo

Cheng

et al. 2017

Molecules

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“…73) Myricetin inhibits Aβ production via α-secretase activation and β-secretase inhibition, 74) inhibits Aβ aggregation, 8,75) and promotes an increase in BDNF. 76) Taxifolin inhibits Aβ production via β-secretase up-regulation, 77) inhibits Aβ aggregation, 78,79) and inhibits AChE activity. 80) Although a clinical trial on a quercetin-rich onion powder was conducted, 81) it was difficult to judge the effectiveness of the powder because the scale of the trial was very small (N = 4 to 5 people).…”

Section: Discussionmentioning

confidence: 99%

The Additive Effects of Low Dose Intake of Ferulic Acid, Phosphatidylserine and Curcumin, Not Alone, Improve Cognitive Function in APPswe/PS1dE9 Transgenic Mice

Okuda

Fujita

Sugimoto

2019

Biological & Pharmaceutical Bulletin

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Alzheimer's disease (AD) is the most common form of dementia and its prevention and treatment is a worldwide issue. Many natural components considered to be effective against AD have been identified. However, almost all clinical trials of these components for AD reported inconclusive results. We thought that multiple factors such as amyloid β (Aβ) and tau progressed the pathology of AD and that a therapeutic effect would be obtained by using multiple active ingredients with different effects. Thus, in this study, we treated ferulic acid (FA), phosphatidylserine (PS) and curcumin (Cur) in combination or alone to APPswe/PS1dE9 transgenic mice and evaluated cognitive function by Y-maze test. Consequently, only the three-ingredient group exhibited a significant improvement in cognitive function compared to the control group. In addition, we determined the amounts of Aβ, brain-derived neurotrophic factor (BDNF), interleukin (IL)-1β, acetylcholine and phosphorylated tau in the mouse brains after the treatment. In the two-ingredient (FA and PS) group, a significant decrease in IL-1β and an increasing trend in acetylcholine were observed. In the Cur group, significant decreases in Aβ and phosphorylated tau and an increasing trend in BDNF were observed. In the three-ingredient group, all of them were observed. These results indicate that the intake of multiple active ingredients with different mechanisms of action for the prevention and treatment of AD.

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“…Scopoletin could have an important role in the management of many symptoms and diseases, such as convulsions, inflammation, rheumatic pains, and leprosy (17). Scopoletin has shown strong inhibition of acetylcholinesterase and thus it is a potential candidate for Alzheimer's disease treatment (18). Furthermore, scopoletin has been introduced as inhibitor of β-glucuronidase, peroxidase, acetylcholinesterase, and mono amine oxidase (19)(20)(21)(22).…”

Section: Modification Of Ldh Enzyme Can Induce Conformationalmentioning

confidence: 99%

Scopoletin and Morin Inhibit Lactate Dehydrogenase Enzyme Activity, Which Is Critical for Cancer Metabolism

Mazlaghaninia

Atri

Seyedalipour

2019

Hormozgan medical journal

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Background: Lactate dehydrogenase (LDH) is a tetrameric enzyme that catalyzes the interconversion of pyruvate to L-lactate. The importance of this enzyme is because LDH isoenzymes are involved in cancer, heart, and liver diseases. Inhibition of this enzyme can help prevent and treat different diseases. Morin is a flavonoid found in the Moraceae family and scopoletin is a coumarin found in Scopolia genus. Objectives: The aim of this study was to determine the effect of morin and scopoletin as two natural products on the activity and structure of lactate dehydrogenase enzyme. Methods: Morin and scopoletin were examined for inhibition of the activity of LDH in 100 mM sodium phosphate buffer pH 7.5, at room temperature using UV-V spectrophotometry. Fluorescence spectroscopy was used to characterize protein structural changes in the presence of morin and scopoletin. Results: Km and Vmax of LDH for pyruvate were 11.69 mM and 1.258 mM/min, respectively. The kinetic results showed that morin and scopoletin are LDH inhibitors. The Ki values of morin and scopoletin were determined as 1.78 µM and 0.8 µM, respectively, using a secondary plot. Fluorescence intensity quenching and red shift of the maximum wavelength of emission in a concentrationdependent manner showed that morin and scopoletin bind to LDH and affect its structure. Conclusions: The results suggest that morin and scopoletin bind to LDH, influence its conformation and inhibit its activity. Scopoletin showed more effective inhibition of LDH activity and it can be a promising candidate in the field of tumor metabolism inhibitors.

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Combining in silico and in vitro approaches to evaluate the acetylcholinesterase inhibitory profile of some commercially available flavonoids in the management of Alzheimer’s disease

Cited by 56 publications

References 25 publications

Study on the Anticoagulant or Procoagulant Activities of Type II Phenolic Acid Derivatives

Study on the Anticoagulant or Procoagulant Activities of Type II Phenolic Acid Derivatives

The Additive Effects of Low Dose Intake of Ferulic Acid, Phosphatidylserine and Curcumin, Not Alone, Improve Cognitive Function in APPswe/PS1dE9 Transgenic Mice

Scopoletin and Morin Inhibit Lactate Dehydrogenase Enzyme Activity, Which Is Critical for Cancer Metabolism

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