scholarly journals Comparison of Phytochemicals, Antioxidant, and In Vitro Anti-Alzheimer Properties of Twenty-Seven Morus spp. Cultivated in Thailand

Molecules ◽  
2020 ◽  
Vol 25 (11) ◽  
pp. 2600 ◽  
Author(s):  
Piya Temviriyanukul ◽  
Varittha Sritalahareuthai ◽  
Kriskamol Na Jom ◽  
Butsara Jongruaysup ◽  
Somying Tabtimsri ◽  
...  
Keyword(s):  
Neurodegenerative Disorder ◽  
Antioxidant Activities ◽  
Hydrogen Atom Transfer ◽  
Key Enzymes ◽  
Beta Secretase ◽  
Fruit Samples ◽  
Morus Spp ◽  
Inhibitory Activities ◽  
Bace 1

Alzheimer’s disease (AD) is a progressive neurodegenerative disorder. To fight the disease, natural products, including mulberry, with antioxidant activities and inhibitory activities against key enzymes (acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and beta-secretase 1 (BACE-1)) are of interest. However, even in the same cultivars, mulberry trees grown in different populated locations might possess disparate amounts of phytochemical profiles, leading to dissimilar health properties, which cause problems when comparing different cultivars of mulberry. Therefore, this study aimed to comparatively investigate the phytochemicals, antioxidant activities, and inhibitory activities against AChE, BChE, and BACE-1, of twenty-seven Morus spp. cultivated in the same planting area in Thailand. The results suggested that Morus fruit samples were rich in phenolics, especially cyanidin, kuromanin, and keracyanin. Besides, the aqueous Morus fruit extracts exhibited antioxidant activities, both in single electron transfer (SET) and hydrogen atom transfer (HAT) mechanisms, while strong inhibitory activities against AD key enzymes were observed. Interestingly, among the twenty-seven Morus spp., Morus sp. code SKSM 810191 with high phytochemicals, antioxidant activities and in vitro anti-AD properties is a promising cultivar for further developed as a potential mulberry resource with health benefits against AD.

scholarly journals Design of Curcumin and Flavonoid Derivatives with Acetylcholinesterase and Beta-Secretase Inhibitory Activities Using in Silico Approaches

Molecules ◽  
2020 ◽  
Vol 25 (16) ◽  
pp. 3644 ◽  
Author(s):  
Thai-Son Tran ◽  
Minh-Tri Le ◽  
Thanh-Dao Tran ◽  
The-Huan Tran ◽  
Khac-Minh Thai
Keyword(s):  
In Silico ◽  
Quantitative Structure Activity Relationship ◽  
In Vitro Assays ◽  
Experimental Investigations ◽  
Beta Secretase ◽  
Inhibitory Activities ◽  
Main Component ◽  
In Silico Models ◽  
Bace 1

Acetylcholinesterase (AChE) and beta-secretase (BACE-1) are the two crucial enzymes involved in the pathology of Alzheimer’s disease. The former is responsible for many defects in cholinergic signaling pathway and the latter is the primary enzyme in the biosynthesis of beta-amyloid as the main component of the amyloid plaques. These both abnormalities are found in the brains of Alzheimer’s patients. In this study, in silico models were developed, including 3D-pharmacophore, 2D-QSAR (two-dimensional quantitative structure-activity relationship), and molecular docking, to screen virtually a database of compounds for AChE and BACE-1 inhibitory activities. A combinatorial library containing more than 3 million structures of curcumin and flavonoid derivatives was generated and screened for drug-likeness and enzymatic inhibitory bioactivities against AChE and BACE-1 through the validated in silico models. A total of 47 substances (two curcumins and 45 flavonoids), with remarkable predicted pIC50 values against AChE and BACE-1 ranging from 4.24–5.11 (AChE) and 4.52–10.27 (BACE-1), were designed. The in vitro assays on AChE and BACE-1 were performed and confirmed the in silico results. The study indicated that, by using in silico methods, a series of curcumin and flavonoid structures were generated with promising predicted bioactivities. This would be a helpful foundation for the experimental investigations in the future. Designed compounds which were the most feasible for chemical synthesis could be potential candidates for further research and lead optimization.

scholarly journals Typhonium trilobatum Demonstrates Both Antioxidant and Acetylcholinesterase Inhibitory Activities In vitro

2019 ◽  
Vol 22 (1) ◽  
pp. 92-98
Author(s):  
Simin Shabnam Lopa ◽  
Md Kamrul Hasan ◽  
Md Salim Ahammed ◽  
KM Monirul Islam ◽  
AHM Khurshid Alam ◽  
...  
Keyword(s):  
Petroleum Ether ◽  
Neurodegenerative Disorder ◽  
Antioxidant Activities ◽  
Petroleum Ether Extract ◽  
Folk Medicine ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Ether Extract ◽  
Inhibitory Activities

Alzheimer’s disease (AD) is a progressive neurodegenerative disorder of the elderly people. Cholinergic dysfunction and oxidative stress have been found to be related with the development of the disease. Typhonium trilobatum L. Scott has been used traditionally in folk medicine as a central nervous system stimulant. In this study, we have investigated the various extracts of T. trilobatum for acetylcholinesterase and antioxidant activities in vitro. All the tested extracts exhibited inhibition against acetylcholinesterase. Petroleum ether extract exhibited the highest inhibition with an IC50 of 255.26 g/ml. Likewise all the extracts were found to possess antioxidant activity. In reducing power assay, petroleum ether extract showed the highest reducing power with an absorbance of 0.874 at 0.1 mg/ml concentration and in DPPH radical scavenging assay, chloroform extract exhibited the highest scavenging activity with an IC50 of 619.54 µg/ml. Phytochemical analyses of the four extracts revealed that the ethyl acetate extract contained the highest amount of flavonoids and petroleum ether had the highest amount of phenolics. These results suggest that T. trilobatum has both antioxidant and cholinesterase inhibitory activities, which may be useful in reducing the risk of AD. Bangladesh Pharmaceutical Journal 22(1): 92-98, 2019

Acetylcholinesterase Inhibitory Potential and Antioxidant Activities of Five Cultivars of Rosa Damascena Mill. From Isparta, Turkey

2020 ◽  
Vol 18 (4) ◽  
pp. 354-359
Author(s):  
Shirin Tarbiat ◽  
Azize Simay Türütoğlu ◽  
Merve Ekingen
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Free Radical ◽  
Neurodegenerative Disorder ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Acetylcholinesterase Activity ◽  
Rosa Damascena ◽  
Free Radical Damage

Alzheimer's disease is a neurodegenerative disorder characterized by memory loss and impairment of language. Alzheimer's disease is strongly associated with oxidative stress and impairment in the cholinergic pathway, which results in decreased levels of acetylcholine in certain areas of the brain. Hence, inhibition of acetylcholinesterase activity has been recognized as an acceptable treatment against Alzheimer's disease. Nature provides an array of bioactive compounds, which may protect against free radical damage and inhibit acetylcholinesterase activity. This study compares the in vitro antioxidant and anticholinesterase activities of hydroalcoholic extracts of five cultivars of Rosa Damascena Mill. petals (R. damascena 'Bulgarica', R. damascena 'Faik', R. damascena 'Iranica', R. damascena 'Complex-635' and R. damascena 'Complex-637') from Isparta, Turkey. The antioxidant activities of the hydroalcoholic extracts were tested for ferric ion reduction and DPPH radical scavenging activities. The anti-acetylcholinesterase activity was also evaluated. All rose cultivars showed a high potency for scavenging free radical and inhibiting acetylcholinesterase activity. There was a significant correlation between antioxidant and acetylcholinesterase inhibitory activity. Among cultivars, Complex-635 showed the highest inhibitory effect with an IC50 value of 3.92 µg/mL. Our results suggest that all these extracts may have the potential to treat Alzheimer's disease with Complex-635 showing more promise.

Inhibitory activities of Cystoseira crinita sulfated polysaccharide on key enzymes related to diabetes and hypertension: in vitro and animal study

2016 ◽  
Vol 123 (1) ◽  
pp. 31-42 ◽  
Author(s):  
Amel Ben Gara ◽  
Rihab Ben Abdallah Kolsi ◽  
Neila Jardak ◽  
Rim Chaaben ◽  
Abdelfattah El-Feki ◽  
...  
Keyword(s):  
Animal Study ◽  
Sulfated Polysaccharide ◽  
Key Enzymes ◽  
Inhibitory Activities

scholarly journals Chemical Composition, Antioxidant and Enzyme Inhibitory Properties of Different Extracts Obtained from Spent Coffee Ground and Coffee Silverskin

Foods ◽  
2020 ◽  
Vol 9 (6) ◽  
pp. 713 ◽  
Author(s):  
Gokhan Zengin ◽  
Kouadio Ibrahime Sinan ◽  
Mohamad Fawzi Mahomoodally ◽  
Simone Angeloni ◽  
Ahmed M. Mustafa ◽  
...  
Keyword(s):  
Bioactive Compounds ◽  
Antioxidant Activities ◽  
Coffee Silverskin ◽  
Methanolic Extracts ◽  
Waste Production ◽  
Starting Point ◽  
Spent Coffee Ground ◽  
Coffee Ground ◽  
Inhibitory Activities

In a world where an eco-friendlier approach is becoming more and more necessary, it is essential to reduce waste production and to reuse residues of the company’s supply chain. Coffee silverskin (CS) and spent coffee ground (SCG), two by-products of coffee production, are important sources of bioactive compounds and, for this, some authors have proposed their reuse in the nutraceutical, food, and cosmetic sector. However, their potential enzyme inhibitory properties have been poorly investigated. Hence, the objective of the current work was to study the enzymatic inhibitory activities against acetylcholinesterase, butyrylcholinesterase, α-amylase, α-glucosidase, and tyrosinase of different extracts of CS and SCG. Before these in vitro bioassays, the phytochemical composition of each extract was investigated via colorimetric assays and HPLC-MS/MS analysis. In addition, the antioxidant activities were evaluated by different chemical approaches. SCG extracts contained a higher content of bioactive compounds, notably the SCG EtOH:H2O extract was the richest in caffeine and possessed the highest antioxidant activities. The hydroalcoholic and methanolic extracts were shown to be the most active against all tested enzymes, while the water extracts displayed lower activity. Our results showed a weak correlation between bioactive compounds and enzyme inhibitory effects, proving inhibitory activities likely due to non-phenolic molecules such as alkaloids and terpenoids. Obtained findings could be a starting point to develop novel nutraceuticals from CS and SCG.

scholarly journals Chemical and Cellular Antioxidant Activities of In Vitro Digesta of Tilapia Protein and Its Hydrolysates

Foods ◽  
2020 ◽  
Vol 9 (6) ◽  
pp. 833
Author(s):  
Xiaogang Zhang ◽  
Parinya Noisa ◽  
Jirawat Yongsawatdigul
Keyword(s):  
Structural Modification ◽  
Physiological Condition ◽  
Antioxidant Activities ◽  
Protein Hydrolysate ◽  
Principal Component ◽  
Hydrogen Atom Transfer ◽  
Trolox Equivalent Antioxidant Capacity ◽  
Degree Of Hydrolysis ◽  
Trolox Equivalent

Production of protein hydrolysate as nutraceuticals is typically based on the activity of the hydrolysate, which might not yield the optimal activity under physiological condition due to structural modification of peptides upon gastrointestinal (GI) digestion. This study systematically compared the chemical and cellular antioxidant activities of the in vitro digesta of tilapia protein and its hydrolysates prepared with various degree of hydrolysis (DH) by Alcalase. The enzymes used in the in vitro GI digestion analysis significantly contributed to the peptide content, Trolox equivalent antioxidant capacity (TEAC), and oxygen radical absorbance capacity (ORAC). Proteins and all hydrolysates were slightly digested by pepsin but hydrolyzed extensively by pancreatin. Both hydrolysate and digesta predominantly scavenged free radicals via hydrogen atom transfer (HAT). The antioxidant activities of the hydrolysates increased with the increasing DH up to 16 h of hydrolysis. However, the digesta of 10-h hydrolysate displayed the highest chemical and HepG2 cellular antioxidant activities, while the protein digesta displayed the lowest. Principal component analysis (PCA) showed that the TEAC of the digesta was positively correlated with the cellular antioxidant activity (CAA). Therefore, the production of protein hydrolysate should be optimized based on the activity of the hydrolysate digesta rather than that of hydrolysates.

scholarly journals IN VITRO ANTI-DIABETIC AND ANTI-OXIDANT ACTIVITIES OF ETHANOL EXTRACT OF TINOSPORA SINENSIS

2017 ◽  
Vol 9 (2) ◽  
pp. 42 ◽  
Author(s):  
Anindita Banerjee ◽  
Bithin Maji ◽  
Sandip Mukherjee ◽  
Kausik Chaudhuri ◽  
Tapan Seal
Keyword(s):  
Plant Extract ◽  
Antioxidant Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Ethanol Extract ◽  
Total Phenolic ◽  
Inhibitory Activities ◽  
Ethanol Extracts

Objective: The aim of the present study was to evaluate the alpha (α)-amylase and alpha (α)-glucosidase inhibitory activities and in vitro antioxidant activities of the 80 % aqueous ethanol extracts of Tinosporasinensis Lour (Merr.).Methods: The 80% aq. ethanol extract of the plant was prepared. The plant extract was examined for its antioxidant activity by using free radical 1,1-diphenyl-2-picryl hydrazyl (DPPH) scavenging method, ABTS radical scavenging ability, reducing power capacity, estimation of total phenolic content, flavonoid content and flavonol content. Different concentrations (2, 4, 8,10and 15 μg/ml) of the extract was subjected to α-amylase inhibitory and α-glucosidase inhibitory activities and IC50were calculated.Results: The study revealed that the different concentrations of the plant extract possessed a very good amount of total phenolics, flavonoid and flavonol and exhibited potent radical scavenging activity using DPPH and ABTS as a substrate. The ethanol extracts exhibited significant α-amylase and α-glucosidase inhibitory activities with an IC50 value1.093µg and 1.04µg dry extract respectively and well compared with standard acarbose drug.Conclusion: Thus, it could be concluded that due to the presence of antioxidant components the plant extracts could be used for the treatment of hyperglycemia, diabetes and the related condition of oxidative stress. This knowledge will be useful in finding more potent components from the natural resources for the clinical development of antidiabetic therapeutics.

scholarly journals Synthesis, In Silico and In Vitro Evaluation of Some Flavone Derivatives for Acetylcholinesterase and BACE-1 Inhibitory Activity

Molecules ◽  
2020 ◽  
Vol 25 (18) ◽  
pp. 4064
Author(s):  
Thai-Son Tran ◽  
Thanh-Dao Tran ◽  
The-Huan Tran ◽  
Thanh-Tan Mai ◽  
Ngoc-Le Nguyen ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Inhibitory Activity ◽  
Biological Effects ◽  
Novel Therapies ◽  
Dual Action ◽  
Flavone Derivatives ◽  
Inhibitory Activities ◽  
High Yields ◽  
Bace 1

Acetylcholinesterase (AChE) and β-secretase (BACE-1) have become attractive therapeutic targets for Alzheimer’s disease (AD). Flavones are flavonoid derivatives with various bioactive effects, including AChE and BACE-1 inhibition. In the present work, a series of 14 flavone derivatives was synthesized in relatively high yields (35–85%). Six of the synthetic flavones (B4, B5, B6, B8, D6 and D7) had completely new structures. The AChE and BACE-1 inhibitory activities were tested, giving pIC50 3.47–4.59 (AChE) and 4.15–5.80 (BACE-1). Three compounds (B3, D5 and D6) exhibited the highest biological effects on both AChE and BACE-1. A molecular docking investigation was conducted to explain the experimental results. These molecules could be employed for further studies to discover new structures with dual action on both AChE and BACE-1 that could serve as novel therapies for AD.

Sign in / Sign up

Export Citation Format

Share Document