scholarly journals Carbohydrate Hydrolase-Inhibitory Activity of Juice-Based Phenolic Extracts in Correlation to Their Anthocyanin/Copigment Profile

Molecules ◽  
2020 ◽  
Vol 25 (22) ◽  
pp. 5224
Author(s):  
Kirsten Berger ◽  
Johanna Josefine Ostberg-Potthoff ◽  
Tamara Bakuradze ◽  
Peter Winterhalter ◽  
Elke Richling
Keyword(s):  
Inhibitory Activity ◽  
Phenolic Content ◽  
In Vivo Studies ◽  
Size Dependent ◽  
Inhibitory Activities ◽  
Sugar Levels ◽  
Red Grape ◽  
Phenolic Extracts

Red fruits and their juices are rich sources of polyphenols, especially anthocyanins. Some studies have shown that such polyphenols can inhibit enzymes of the carbohydrate metabolism, such as α-amylase and α-glucosidase, that indirectly regulate blood sugar levels. The presented study examined the in vitro inhibitory activity against α-amylase and α-glucosidase of various phenolic extracts prepared from direct juices, concentrates, and purees of nine different berries which differ in their anthocyanin and copigment profile. Generally, the extracts with the highest phenolic content—aronia (67.7 ± 3.2 g GAE/100 g; cyanidin 3-galactoside; chlorogenic acid), pomegranate (65.7 ± 7.9 g GAE/100 g; cyanidin 3,5-diglucoside; punicalin), and red grape (59.6 ± 2.5 g GAE/100 g; malvidin 3-glucoside; quercetin 3-glucuronide)—showed also one of the highest inhibitory activities against α-amylase (326.9 ± 75.8 μg/mL; 789.7 ± 220.9 μg/mL; 646.1 ± 81.8 μg/mL) and α-glucosidase (115.6 ± 32.5 μg/mL; 127.8 ± 20.1 μg/mL; 160.6 ± 68.4 μg/mL) and, partially, were even more potent inhibitors than acarbose (441 ± 30 μg/mL; 1439 ± 85 μg/mL). Additionally, the investigation of single anthocyanins and glycosylated flavonoids demonstrated a structure- and size-dependent inhibitory activity. In the future in vivo studies are envisaged.

Anticholinesterase Activity of Cinnamic Acids Derivatives: In Vitro, In Vivo Biological Evaluation, and Docking Study

2020 ◽  
Vol 17 (8) ◽  
pp. 965-982
Author(s):  
Shahrzad Ghafary ◽  
Hamid Nadri ◽  
Mohammad Mahdavi ◽  
Alireza Moradi ◽  
Tahmineh Akbarzadeh ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Kinetic Studies ◽  
Docking Study ◽  
Biological Evaluation ◽  
In Vivo Studies ◽  
Neuroprotective Activity ◽  
Inhibitory Activities ◽  
Ellman’S Method

Background: Acetylcholine deficiency in the hippocampus and cortex, aggregation of amyloid-beta, and beta-secretase overactivity have been introduced as the main reasons in the formation of Alzheimer’s disease. Objective: A new series of cinnamic derived acids linked to 1-benzyl-1,2,3-triazole moiety were designed, synthesized, and evaluated for their acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities. Methods: Colorimetric Ellman’s method was used for the determination of IC50% of AchE and BuChE inhibitory activity. The kinetic studies, neuroprotective activity, BACE1 inhibitory activity, evaluation of inhibitory potency on Aβ1-42 self-aggregation induced by AchE, and docking study were performed for studying the mechanism of action. Results: Some of the synthesized compounds, compound 7b-4 ((E)-3-(3,4-dimethoxyphenyl)-N-((1- (4-fluorobenzyl)-1H-1,2,3-triazole-4-yl) methyl) acrylamide) depicted the most potent acetylcholinesterase inhibitory activities ( IC50 = 5.27 μM ) and compound 7a-1 (N- ( (1- benzyl- 1H- 1, 2, 3- triazole - 4-yl) methyl) cinnamamide) demonstrated the most potent butyrylcholinesterase inhibitory activities (IC50 = 1.75 μM). Compound 7b-4 showed neuroprotective and β-secretase (BACE1) inhibitory activitiy. In vivo studies of compound 7b-4 in Scopolamine-induced dysfunction confirmed memory improvement. Conculusion: It should be noted that molecular modeling (compounds 7b-4 and 7a-1) and kinetic studies (compounds 7a-1 and 7b-4) showed that these synthesis compounds interacted simultaneously with both the catalytic site (CS) and peripheral anionic site (PAS) of AChE and BuChE.

Xanthine oxidase inhibitory activity of nicotino/isonicotinohydrazides: A systematic approach from in vitro , in silico to in vivo studies

2017 ◽  
Vol 25 (8) ◽  
pp. 2351-2371 ◽  
Author(s):  
Humaira Zafar ◽  
Muhammad Hayat ◽  
Sumayya Saied ◽  
Momin Khan ◽  
Uzma Salar ◽  
...  
Keyword(s):  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
In Silico ◽  
Systematic Approach ◽  
In Vivo Studies

scholarly journals In Vitro ACE2 and 5-LOX Enzyme Inhibition by Menthol and Three Different Mint Essential Oils

2021 ◽  
Vol 16 (11) ◽  
pp. 1934578X2110550
Author(s):  
Fatih Demirci ◽  
Ayşe Esra Karadağ ◽  
Sevde Nur Biltekin ◽  
Betül Demirci
Keyword(s):  
Essential Oils ◽  
Enzyme Inhibition ◽  
In Vivo Studies ◽  
Chemical Compositions ◽  
Mentha Arvensis ◽  
Angiotensin Converting Enzyme 2 ◽  
Potential Applications ◽  
Inhibitory Activities

Mentha arvensis L., M. citrata L., and M. spicata L. (family Lamiaceae) essential oils, and their characteristic constituent, menthol, were evaluated in vitro for angiotensin converting enzyme 2 (ACE2) and 5-lipoxygenase (5-LOX) enzyme inhibitory activity. The chemical compositions of M. arvensis, M. citrata, and M. spicata essential oils were analysed both by GC-FID, and GC/MS; 82.0%, 38.1%, and 0.4% menthol were identified, respectively. M. spicata essential oil contained 88.2% carvone as its major component. The enzyme inhibitory activities of the essential oils were evaluated using a fluorometric multiplate based enzyme inhibition kit; the ACE2 inhibitions produced by M. arvensis, M. citrata, and M. spicata essential oils were 33%, 22%, and 73%, while the 5-LOX inhibitions were 84%, 79%, and 70%, respectively. In addition, menthol also showed remarkable ACE2 inhibition of 99.8%, whereas the 5-LOX inhibition was 79.9%. As a result, menthol and the three different mint essential oils may have antiviral potential applications against coronaviruses due to their ACE2 enzyme inhibition and anti-inflammatory features. However, further in vivo studies are needed to confirm the safety and efficacy.

scholarly journals In Vitro and In Vivo Studies on Quercus acuta Thunb. (Fagaceae) Extract: Active Constituents, Serum Uric Acid Suppression, and Xanthine Oxidase Inhibitory Activity

2017 ◽  
Vol 2017 ◽  
pp. 1-9 ◽  
Author(s):  
In-Soo Yoon ◽  
Dae-Hun Park ◽  
Min-Suk Bae ◽  
Deuk-Sil Oh ◽  
Nan-Hui Kwon ◽  
...  
Keyword(s):  
South Korea ◽  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
In Vivo Studies ◽  
Gas Chromatography Mass Spectrometry ◽  
Similar Extent ◽  
Active Constituents ◽  
Quercus Acuta

Quercus acuta Thunb. (Fagaceae) (QA) is cultivated as a dietary and ornamental plant in China, Japan, South Korea, and Taiwan. It has been widely used as the main ingredient of acorn tofu, a traditional food in China and South Korea. The aim of this study was to determine in vitro and in vivo xanthine oxidase (XO) inhibitory and antihyperuricemic activities of an ethyl acetate extract of QA leaf (QALE) and identify its active phytochemicals using gas chromatography-mass spectrometry (GC-MS) and liquid chromatography (LC) systems. The QALE was found to possess potent in vitro antioxidant and XO inhibitory activities. In vivo study using hyperuricemic mice induced with potassium oxonate demonstrated that the QALE could inhibit hepatic XO activity at a relatively low oral dose (50 mg/kg) and significantly alleviate hyperuricemia to a similar extent as allopurinol. Several active compounds including vitamin E known to possess XO inhibitory activity were identified from the QALE. To the best of our knowledge, this is the first study that reports the active constituents and antihyperuricemic effect of QA, suggesting that it is feasible to use QALE as a food therapy or alternative medicine for alleviating hyperuricemia and gout.

scholarly journals Recent Advances on the Anti-inflammatory and Anti-oxidant properties of Red Grape Polyphenols: In Vitro and in Vivo Studies

2019 ◽  
Author(s):  
Thea Magrone ◽  
Manrico Magrone ◽  
Matteo Antonio Russo ◽  
Emilio Jirillo
Keyword(s):  
T Regulatory Cells ◽  
In Vivo Studies ◽  
Low Grade ◽  
Regulatory Cells ◽  
Grape Polyphenols ◽  
Anti Oxidant ◽  
Anti Inflammatory ◽  
Red Grape

In this review, special emphasis will be placed on red grape polyphenols for their anti-oxidant and anti-inflammatory activities. Therefore, their capacity to inhibit major pathways responsible for activation of oxidative systems and expression and release of pro-inflammatory cytokines and chemokines will be discussed. Furthermore, regulation of immune cells by polyphenols will be illustrated with special reference to the activation of T regulatory cells which support a tolerogenic pathway at intestinal level. Furthermore, the effects of red grape polyphenols will be analyzed in obesity, as a low grade systemic inflammation. Also, possible modifications of inflammatory bowel disease biomarkers and clinical course have been studied upon polyphenol administration, either in animal models or in clinical trials. Moreover, the ability of polyphenols to cross the blood-brain barrier has been exploited to investigate their neuroprotective properties. In cancer, polyphenols seem to exert several beneficial effects, even if conflicting data are reported about their influence on T regulatory cells. Finally, the effects of polyphenols have been evaluated in experimental models of allergy and autoimmune diseases. Conclusively, red grape polyphenols are endowed with a great anti-oxidant and anti-inflammatory potential but some issues, such as polyphenol bioavailability, activity of metabolites and interaction with microbiota, deserve deeper studies.

scholarly journals Recent Advances on the Anti-Inflammatory and Antioxidant Properties of Red Grape Polyphenols: In Vitro and In Vivo Studies

Antioxidants ◽  
2019 ◽  
Vol 9 (1) ◽  
pp. 35 ◽  
Author(s):  
Thea Magrone ◽  
Manrico Magrone ◽  
Matteo Antonio Russo ◽  
Emilio Jirillo
Keyword(s):  
T Regulatory Cells ◽  
Antioxidant Properties ◽  
In Vivo Studies ◽  
Low Grade ◽  
Regulatory Cells ◽  
Grape Polyphenols ◽  
Anti Inflammatory ◽  
Red Grape

In this review, special emphasis will be placed on red grape polyphenols for their antioxidant and anti-inflammatory activities. Therefore, their capacity to inhibit major pathways responsible for activation of oxidative systems and expression and release of proinflammatory cytokines and chemokines will be discussed. Furthermore, regulation of immune cells by polyphenols will be illustrated with special reference to the activation of T regulatory cells which support a tolerogenic pathway at intestinal level. Additionally, the effects of red grape polyphenols will be analyzed in obesity, as a low-grade systemic inflammation. Also, possible modifications of inflammatory bowel disease biomarkers and clinical course have been studied upon polyphenol administration, either in animal models or in clinical trials. Moreover, the ability of polyphenols to cross the blood–brain barrier has been exploited to investigate their neuroprotective properties. In cancer, polyphenols seem to exert several beneficial effects, even if conflicting data are reported about their influence on T regulatory cells. Finally, the effects of polyphenols have been evaluated in experimental models of allergy and autoimmune diseases. Conclusively, red grape polyphenols are endowed with a great antioxidant and anti-inflammatory potential but some issues, such as polyphenol bioavailability, activity of metabolites, and interaction with microbiota, deserve deeper studies.

scholarly journals Biphenylalkoxyamine Derivatives–Histamine H3 Receptor Ligands with Butyrylcholinesterase Inhibitory Activity

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3580
Author(s):  
Dorota Łażewska ◽  
Paula Zaręba ◽  
Justyna Godyń ◽  
Agata Doroz-Płonka ◽  
Annika Frank ◽  
...  
Keyword(s):  
Neurodegenerative Diseases ◽  
Inhibitory Activity ◽  
Symptomatic Treatment ◽  
In Vivo Studies ◽  
Avoidance Task ◽  
Receptor Ligands ◽  
Mao B ◽  
Histamine H3

Neurodegenerative diseases, e.g., Alzheimer’s disease (AD), are a key health problem in the aging population. The lack of effective therapy and diagnostics does not help to improve this situation. It is thought that ligands influencing multiple but interconnected targets can contribute to a desired pharmacological effect in these complex illnesses. Histamine H3 receptors (H3Rs) play an important role in the brain, influencing the release of important neurotransmitters, such as acetylcholine. Compounds blocking their activity can increase the level of these neurotransmitters. Cholinesterases (acetyl- and butyrylcholinesterase) are responsible for the hydrolysis of acetylcholine and inactivation of the neurotransmitter. Increased activity of these enzymes, especially butyrylcholinesterase (BuChE), is observed in neurodegenerative diseases. Currently, cholinesterase inhibitors: donepezil, rivastigmine and galantamine are used in the symptomatic treatment of AD. Thus, compounds simultaneously blocking H3R and inhibiting cholinesterases could be a promising treatment for AD. Herein, we describe the BuChE inhibitory activity of H3R ligands. Most of these compounds show high affinity for human H3R (Ki < 150 nM) and submicromolar inhibition of BuChE (IC50 < 1 µM). Among all the tested compounds, 19 (E153, 1-(5-([1,1′-biphenyl]-4-yloxy)pentyl)azepane) exhibited the most promising in vitro affinity for human H3R, with a Ki value of 33.9 nM, and for equine serum BuChE, with an IC50 of 590 nM. Moreover, 19 (E153) showed inhibitory activity towards human MAO B with an IC50 of 243 nM. Furthermore, in vivo studies using the Passive Avoidance Task showed that compound 19 (E153) effectively alleviated memory deficits caused by scopolamine. Taken together, these findings suggest that compound 19 can be a lead structure for developing new anti-AD agents.

scholarly journals Evaluation of Various Starchy Foods: A Systematic Review and Meta-Analysis on Chemical Properties Affecting the Glycemic Index Values Based on In Vitro and In Vivo Experiments

Foods ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 364
Author(s):  
Frendy Ahmad Afandi ◽  
Christofora Hanny Wijaya ◽  
Didah Nur Faridah ◽  
Nugraha Edhi Suyatma ◽  
Anuraga Jayanegara
Keyword(s):  
Phenolic Content ◽  
Meta Analysis ◽  
Chemical Properties ◽  
In Vivo Studies ◽  
Starchy Food ◽  
Crop Type ◽  
Red Kidney Bean ◽  
Starchy Foods

The chemical properties that serve as major determinants for the glycemic index (GI) of starchy food and recommended low-GI, carbohydrate-based foods have remained enigmatic. This present work performed a systematic assessment of linkages between chemical properties of foods and GI, and selected low-GI starchy foods. The data were sourced from literature published in various scientific journals. In total, 57 relevant studies and 936 data points were integrated into a database. Both in vitro and in vivo studies on GI values were included. The database was subsequently subjected to a meta-analysis. Meta-analysis from in vitro studies revealed that the two significant factors responsible for the GI of starchy foods were resistant starch and phenolic content (respectively, standardized mean difference (SMD): −2.52, 95% confidence interval (95%CI): −3.29 to −1.75, p (p-value) < 0.001; SMD: −0.72, 95%CI: −1.26 to −0.17, p = 0.005), while the lowest-GI crop type was legumes. Subgroup analysis restricted to the crop species with significant low GI found two crops, i.e., sorghum (SMD: −0.69, 95%CI: −2.33 to 0.96, p < 0.001) and red kidney bean (SMD: −0.39, 95%CI: −2.37 to 1.59, p = 0.001). Meta-analysis from in vivo studies revealed that the two significant factors responsible for the GI of starchy foods were flavonoid and phenolic content (respectively, SMD: −0.67, 95%CI: −0.87 to −0.47, p < 0.001; SMD: −0.63, 95%CI: −1.15 to −0.11, p = 0.009), while the lowest-GI crop type was fruit (banana). In conclusion, resistant starch and phenolic content may have a desirable impact on the GI of starchy food, while sorghum and red kidney bean are found to have low GI.

scholarly journals Utilizing the Combination of Binding Kinetics and Micro-Pharmacokinetics Link in Vitro α-Glucosidase Inhibition to in Vivo Target Occupancy

Biomolecules ◽  
2019 ◽  
Vol 9 (9) ◽  
pp. 493
Author(s):  
Wang ◽  
Ji ◽  
Li ◽  
Wang ◽  
Gong ◽  
...  
Keyword(s):  
Simulation Model ◽  
Rate Constants ◽  
Inhibitory Activity ◽  
Time Course ◽  
Dynamic Change ◽  
Binding Kinetics ◽  
In Vivo Studies ◽  
Epicatechin Gallate

Many compounds with good inhibitory activity (i.e., high affinity) within in vitro experiments failed in vivo studies due to a lack of efficacy from limited target occupancy (TO) in the drug discovery process. Recently, it was found that rate constants of the formation and dissociation of the binary drug-target complex, rather than affinity, often govern in vivo efficacy. Therefore, the binding kinetics (BK) properties of compound-target interaction are emerging as a pivotal parameter. However, it is obvious that BK rate constants of the compound against target would not be directly linked to the in vivo TO unless the compound concentration in the target vicinity at any time point (TPK) can be evaluated. Here, we developed a novel simulation model to quantitate the dynamic change of target engagement over time in rat with a combined use of BK and TPK features of Epicatechin gallate (ECG) and epigallocatechin gallate (EGCG) on the basis of α-glucosidase (AGH). Analysis of the results displayed that the percent of maximum AGH occupancies by the ECG were varied significantly from 48.9 to 95.3% and by the EGCG slightly from 96 to 99.8%; that the time course of above 70% engagement by ECG spanned a range from 0 to 0.64 h and by EGCG a range of 1.5 to 8.9 h in four different intestinal segments of the rat. It was clearly analyzed how each parameter in the simulation model effected on the in vivo the AGH engagement by ECG and EGCG. Our results provide a novel approach for assessing the potential inhibitory activity of the compounds against AGH.

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