scholarly journals A New Insight into Meloxicam: Assessment of Antioxidant and Anti-Glycating Activity in In Vitro Studies

2020 ◽  
Vol 13 (9) ◽  
pp. 240 ◽  
Author(s):  
Cezary Pawlukianiec ◽  
Małgorzata Ewa Gryciuk ◽  
Kacper Maksymilian Mil ◽  
Małgorzata Żendzian-Piotrowska ◽  
Anna Zalewska ◽  
...  
Keyword(s):  
Protein Oxidation ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Amyloid Β ◽  
Inhibitory Effect ◽  
Oxidation Products ◽  
Protein Glycation ◽  
Antioxidant Power ◽  
Anti Inflammatory

Meloxicam is a non-steroidal anti-inflammatory drug, which has a preferential inhibitory effect to cyclooxyganase-2 (COX-2). Although the drug inhibits prostaglandin synthesis, the exact mechanism of meloxicam is still unknown. This is the first study to assess the effect of meloxicam on protein glyco-oxidation as well as antioxidant activity. For this purpose, we used an in vitro model of oxidized bovine serum albumin (BSA). Glucose, fructose, ribose, glyoxal and methylglyoxal were used as glycating agents, while chloramine T was used as an oxidant. We evaluated the antioxidant properties of albumin (2,2-di-phenyl-1-picrylhydrazyl radical scavenging capacity, total antioxidant capacity and ferric reducing antioxidant power), the intensity of protein glycation (Amadori products, advanced glycation end products) and glyco-oxidation (dityrosine, kynurenine, N-formylkynurenine, tryptophan and amyloid-β) as well as the content of protein oxidation products (advanced oxidation protein products, carbonyl groups and thiol groups). We have demonstrated that meloxicam enhances the antioxidant properties of albumin and prevents the protein oxidation and glycation under the influence of various factors such as sugars, aldehydes and oxidants. Importantly, the antioxidant and anti-glycating activity is similar to that of routinely used antioxidants such as captopril, Trolox, reduced glutathione and lipoic acid as well as protein glycation inhibitors (aminoguanidine). Pleiotropic action of meloxicam may increase the effectiveness of anti-inflammatory treatment in diseases with oxidative stress etiology.

scholarly journals Pleiotropic Properties of Valsartan: Do They Result from the Antiglycooxidant Activity? Literature Review and In Vitro Study

2021 ◽  
Vol 2021 ◽  
pp. 1-20
Author(s):  
Kacper Maksymilian Mil ◽  
Małgorzata Ewa Gryciuk ◽  
Cezary Pawlukianiec ◽  
Małgorzata Żendzian-Piotrowska ◽  
Jerzy Robert Ładny ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Protein Oxidation ◽  
Positive Impact ◽  
Amyloid Β ◽  
In Vitro Study ◽  
Oxidation Products ◽  
Protein Glycation ◽  
Protein Carbonyls ◽  
Antioxidant Power

Valsartan belongs to angiotensin II type 1 (AT1) receptor blockers (ARB) used in cardiovascular diseases like heart failure and hypertension. Except for its AT1-antagonism, another mechanism of drug action has been suggested in recent research. One of the supposed actions refers to the positive impact on redox balance and reducing protein glycation. Our study is aimed at assessing the antiglycooxidant properties of valsartan in an in vitro model of oxidized bovine serum albumin (BSA). Glucose, fructose, ribose, glyoxal (GO), methylglyoxal (MGO), and chloramine T were used as glycation or oxidation agents. Protein oxidation products (total thiols, protein carbonyls (PC), and advanced oxidation protein products (AOPP)), glycooxidation products (tryptophan, kynurenine, N-formylkynurenine, and dityrosine), glycation products (amyloid-β structure, fructosamine, and advanced glycation end products (AGE)), and albumin antioxidant activity (total antioxidant capacity (TAC), DPPH assay, and ferric reducing antioxidant power (FRAP)) were measured in each sample. In the presence of valsartan, concentrations of protein oxidation and glycation products were significantly lower comparing to control. Moreover, albumin antioxidant activity was significantly higher in those samples. The drug’s action was comparable to renowned antiglycation agents and antioxidants, e.g., aminoguanidine, metformin, Trolox, N-acetylcysteine, or alpha-lipoic acid. The conducted experiment proves that valsartan can ameliorate protein glycation and oxidation in vitro in various conditions. Available animal and clinical studies uphold this statement, but further research is needed to confirm it, as reduction of protein oxidation and glycation may prevent cardiovascular disease development.

scholarly journals Chemical Composition, In Vitro and In Silico Antioxidant Potential of Melissa officinalis subsp. officinalis Essential Oil

Antioxidants ◽  
2021 ◽  
Vol 10 (7) ◽  
pp. 1081
Author(s):  
Matilda Rădulescu ◽  
Călin Jianu ◽  
Alexandra Teodora Lukinich-Gruia ◽  
Marius Mioc ◽  
Alexandra Mioc ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Chemical Composition ◽  
Essential Oil ◽  
In Silico ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Inhibitory Effect ◽  
Melissa Officinalis ◽  
Β Carotene

The investigation aimed to study the in vitro and in silico antioxidant properties of Melissa officinalis subsp. officinalis essential oil (MOEO). The chemical composition of MOEO was determined using GC–MS analysis. Among 36 compounds identified in MOEO, the main were beta-cubebene (27.66%), beta-caryophyllene (27.41%), alpha-cadinene (4.72%), caryophyllene oxide (4.09%), and alpha-cadinol (4.07%), respectively. In vitro antioxidant properties of MOEO have been studied in 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) free-radical scavenging, and inhibition of β-carotene bleaching assays. The half-maximal inhibitory concentration (IC50) for the radical scavenging abilities of ABTS and DPPH were 1.225 ± 0.011 μg/mL and 14.015 ± 0.027 μg/mL, respectively, demonstrating good antioxidant activity. Moreover, MOEO exhibited a strong inhibitory effect (94.031 ± 0.082%) in the β-carotene bleaching assay by neutralizing hydroperoxides, responsible for the oxidation of highly unsaturated β-carotene. Furthermore, molecular docking showed that the MOEO components could exert an in vitro antioxidant activity through xanthine oxidoreductase inhibition. The most active structures are minor MOEO components (approximately 6%), among which the highest affinity for the target protein belongs to carvacrol.

scholarly journals Inhibitory Effect of Antidesma bunius Fruit Extract on Carbohydrate Digestive Enzymes Activity and Protein Glycation In Vitro

Antioxidants ◽  
2020 ◽  
Vol 10 (1) ◽  
pp. 32
Author(s):  
Pattamaporn Aksornchu ◽  
Netima Chamnansilpa ◽  
Sirichai Adisakwattana ◽  
Thavaree Thilavech ◽  
Charoonsri Choosak ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Radical Scavenging Activity ◽  
Digestive Enzyme ◽  
Radical Scavenging ◽  
Protein Glycation ◽  
Trolox Equivalent Antioxidant Capacity ◽  
Fruit Extract ◽  
Antioxidant Power ◽  
Ic50 Values

Antidesma bunius (L.) spreng (Mamao) is widely distributed in Northeastern Thailand. Antidesma bunius has been reported to contain anthocyanins, which possess antioxidant and antihypertensive actions. However, the antidiabetic and antiglycation activity of Antidesma bunius fruit extract has not yet been reported. In this study, we investigated the inhibitory activity of anthocyanin-enriched fraction of Antidesma bunius fruit extract (ABE) against pancreatic α-amylase, intestinal α-glucosidase (maltase and sucrase), protein glycation, as well as antioxidant activity. A liquid chromatography-tandem mass spectrometry (LC-MS/MS) chromatogram revealed that ABE contained phytochemical compounds such as cyanidin-3-glucoside, delphinidin-3-glucoside, ellagic acid, and myricetin-3-galactoside. ABE inhibited intestinal maltase and sucrase activity with the IC50 values of 0.76 ± 0.02 mg/mL and 1.33 ± 0.03 mg/mL, respectively. Furthermore, ABE (0.25 mg/mL) reduced the formation of fluorescent AGEs and the level of Nε-carboxymethyllysine (Nε-CML) in fructose and glucose-induced protein glycation during four weeks of incubation. During the glycation process, the protein carbonyl and β-amyloid cross structure were decreased by ABE (0.25 mg/mL). In addition, ABE exhibited antioxidant activity through DPPH radical scavenging activity and Trolox equivalent antioxidant capacity (TEAC) with the IC50 values 15.84 ± 0.06 µg/mL and 166.1 ± 2.40 µg/mL, respectively. Meanwhile, ferric reducing antioxidant power (FRAP) showed an EC50 value of 182.22 ± 0.64 µg/mL. The findings suggest that ABE may be a promising agent for inhibiting carbohydrate digestive enzyme activity, reducing monosaccharide-induced protein glycation, and antioxidant activity.

scholarly journals In vitro inhibitory potentials of ethanolic extract of Moringa oleifera flower against enzymes activities linked to diabetes

2021 ◽  
Vol 10 (4) ◽  
pp. 408-414
Author(s):  
Oluwaseun Ruth Olasehinde ◽  
Olakunle Bamikole Afolabi ◽  
Benjamin Olusola Omiyale ◽  
Oyindamola Adeniyi Olaoye
Keyword(s):  
Free Radical ◽  
Moringa Oleifera ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Ethanolic Extract ◽  
Antidiabetic Activity ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Antioxidant Power

Introduction: Diabetes mellitus (DM) has been recognized as the seventh leading cause of global mortality; however, researchers seek alternative means to manage the menace. The current study sought to investigate antioxidant potentials, α-amylase, and α-glucosidase inhibitory activities of ethanolic extract of Moringa oleifera flower in vitro. Methods: Antioxidant properties of the extract were appraised by assessing its inhibition against 1,1-diphenyl-2-picrylhydrazyl (DPPH), hydroxyl (OH•), and hydrogen peroxide (H2O2) free radicals, as well as ferric reducing antioxidant power (FRAP), the antidiabetic activity was evaluated by α-amylase and α-glucosidase inhibition.Results: In this study, ethanolic extract of M. oleifera flower demonstrated a significant (P < 0.05) inhibition against DPPH free radical (43.57–83.56%) in a concentration-dependent manner, while FRAP (101.76 ± 1.63 mg/100 g), OH• scavenging ability (71.62 ± 0.95 mg/100 g), and H2O2 free radical scavenging capacity (15.33 ± 1.20 mg/100 g) were also observed. In the same manner, ethanolic extract of M. oleifera flower revealed a significant (P < 0.05) inhibition against α-amylase (IC50= 37.63 mg/mL) and α-glucosidase activities (IC50= 38.30 mg/mL) in the presence of their respective substrates in a concentration-dependent manner in comparison with acarbose. Conclusion: Ethanoic extract of M. oleifera flower could be useful as an alternative phytotherapy in the management of DM, having shown a strong antioxidative capacity and substantial inhibition against the activities of key enzymes involved in carbohydrate hydrolysis in vitro.

scholarly journals Antioxidant and Anti-Inflammatory Activities of Six Flavonoids from Smilax glabra Roxb

Molecules ◽  
2020 ◽  
Vol 25 (22) ◽  
pp. 5295
Author(s):  
Xinyu Zhao ◽  
Ruyi Chen ◽  
Yueyue Shi ◽  
Xiaoxi Zhang ◽  
Chongmei Tian ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Raw264.7 Cells ◽  
Enzyme Linked Immunosorbent Assay ◽  
Preparative Hplc ◽  
Antioxidant Power ◽  
Ferric Reducing Antioxidant Power ◽  
Anti Inflammatory

This study aimed to isolate, prepare and identify the main flavonoids from a standardized Smilax glabra flavonoids extract (SGF) using preparative HPLC, MS, 1H NMR and 13C NMR, determine the contents of these flavonoids using UPLC, then compare their pharmacological activities in vitro. We obtained six flavonoids from SGF: astilbin (18.10%), neoastilbin (11.04%), isoastilbin (5.03%), neoisoastilbin (4.09%), engeletin (2.58%) and (−)-epicatechin (1.77%). The antioxidant activity of six flavonoids were evaluated by determining the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical and 2,2′-Azinobis (3-ethylbenzothiazoline-6-sulphonic acid) diammonium salt (ABTS+) radical scavenging activity and ferric reducing antioxidant power (FRAP). In addition, the anti-inflammatory activity of six flavonoids were evaluated by determining the production of cytokines (IL-1β, IL-6), nitric oxide (NO) using enzyme linked immunosorbent assay and the NF-κB p65 expression using Western blotting in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. The results showed that (−)-epicatechin, astilbin, neoastilbin, isoastilbin and neoisoastilbin had strong antioxidant activities, not only in DPPH and ABTS+ radicals scavenging capacities, but in FRAP system. Furthermore, all the six flavonoids could significantly inhibit the secretion of IL-1β, IL-6, NO (p < 0.01) and the protein expression of NF-κB p-p65 (p < 0.01) in LPS-stimulated RAW264.7 cells. This study preliminarily verified the antioxidant and anti-inflammatory activities of six flavonoids in S. glabra.

scholarly journals Concept of Polycystic Ovarian Syndrome: Perspectives of Ayurveda and Modern Science

2017 ◽  
Vol 9 (10) ◽  
Author(s):  
Patel M G. ◽  
Prajapati D. P.
Keyword(s):  
Antioxidant Activity ◽  
Fluorescence Intensity ◽  
Radical Scavenging ◽  
Modern Science ◽  
Protein Carbonyl ◽  
Protein Glycation ◽  
Trolox Equivalent Antioxidant Capacity ◽  
Antioxidant Power ◽  
Nitric Oxide Radical

Non enzymatic glycation is a chain reaction between reducing sugars and the free amino groups of proteins, involved in severity of diabetes and diabetic complications. Litchi chinensis used as consumed fruit and as a drug to treat certain diseases. In this study the antioxidative effects of L.chinensis and also its effect against protein oxidation and advanced glycation end products. The antioxidant potential of aqueous fruit pericarp extract of L.chinensis (APLC) was evaluated in vitro using a model of fructose-mediated protein glycation. The antioxidant activity of APLC conducted for superoxide, hydroxyl, hydrogen peroxide, nitric oxide radical scavenging activities and also demonstrated antioxidant activity with Fe+2 chelating activity, ferric reducing antioxidant power (FRAP) and Trolox equivalent antioxidant capacity (TEAC) were applied. Fructose (100mM) increased fluorescence intensity of glycated bovine serum albumin (BSA) in terms of total AGEs during 21 days of exposure. Moreover, fructose caused more protein carbonyl (PCO) formation in native BSA. The APLC prevents oxidative protein damages including effect on PCO formation which are believed to form under the glycoxidation process. The APLC at different concentrations (25-250µg/ml) has significantly decreased the formation of AGEs in term of the fluorescence intensity of glycated BSA.

scholarly journals In Vitro Antioxidant Activities of Methanolic Extracts of Caesalpinia volkensii Harms., Vernonia lasiopus O. Hoffm., and Acacia hockii De Wild

2020 ◽  
Vol 2020 ◽  
pp. 1-10
Author(s):  
Beatrice Muthoni Guchu ◽  
Alex King’ori Machocho ◽  
Stephen Kiruthi Mwihia ◽  
Mathew Piero Ngugi
Keyword(s):  
Oxidative Stress ◽  
Therapeutic Potential ◽  
Antioxidant Activities ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Antioxidant Power ◽  
Chain Reactions ◽  
Methanolic Extracts ◽  
Ferric Reducing Antioxidant Power

Oxidative stress is the result of the disparity between pro-oxidants and antioxidants in an organism, and it is important in the pathogenesis of several degenerative disorders, such as arthritis, Alzheimer’s, cancer, and cardiovascular diseases. Free radicals can damage biomolecules, such as nucleic acids, lipids, proteins, polyunsaturated fatty acids, and carbohydrates, and the DNA leading to mutations. The use of antioxidants is effective in delaying the oxidation of biomolecules. Antioxidants are complexes found in the food that can retard or deter oxidation by preventing the initiation and propagation of oxidizing chain reactions. Medicinal plants have been used for centuries by man to manage diseases and have a host of antioxidant complexes. Traditionally, Caesalpinia volkensii, Vernonia lasiopus, and Acacia hockii have folkloric remedies against associated oxidative stress-mediated complications. However, the upsurge in its use has not been accompanied by scientific validations to support these claims. In this study, in vitro antioxidant activity of Caesalpinia volkensii, Vernonia lasiopus, and Acacia hockii collected from Embu County (Kenya) were determined by radical scavenging activities of 1,1-diphenyl-2-picrylhydrazyl (DPPH) and hydroxyl radical in addition to ferric reducing antioxidant power analyzed against that of L-ascorbic acid as the standard. The obtained results revealed remarkable antioxidant activities of the studied plant extracts as evidenced by the low IC50 and EC50 values. These antioxidant activities could be due to the presence of antioxidants phytochemicals such as flavonoids, phenols, terpenoids, and saponins among others. Therefore, the therapeutic potential of this plant could be due to their antioxidant properties. This study recommends bioassay of the extracts against oxidative stress-related disorders for development of phytomedicine with antioxidant properties.

scholarly journals IN VITRO ANTIOXIDANT ACTIVITY, IN VIVO ANTIPYRETIC AND ANTI-INFLAMMATORY ACTIVITIES OF PARONYCHIA CAPITATA L.

2017 ◽  
Vol 10 (3) ◽  
pp. 177
Author(s):  
Soumia Bouzidi ◽  
Benkiki Naima ◽  
Allaoua Zina
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Butanol Extract ◽  
Antipyretic Activity ◽  
Male Wistar Rats ◽  
Anti Inflammatory ◽  
In Vitro Antioxidant Activity

ABSTRACTObjective: The aim of this study is to evaluate the in vitro antioxidant activity of Paronychia capitata various extracts, acute toxicity, the in vivoantipyretic and anti-inflammatory activities of the n-butanol extract.Methods: The antioxidant properties were tested using 2,2-diphenyl 1-picrylhydrazyl radical scavenging and β-carotene linoleic acid system, thetotal phenolic and flavonoid contents were determined. Furthermore, anti-inflammatory activity and antipyretic activity of the n-butanol extractwere assessed on male Wistar rats at the dose levels 250, 500 mg/kg body weight, using the egg albumin-induced edema, and brewer’s yeast-inducedpyrexia method, respectively.Results: The n-butanol extract of P. capitata had considerably the highest antiradical activity with inhibitory concentration 50 value of 8.667 μg/ml.Conclusion: The experimental data demonstrated that n-butanol extract of P. capitata possess significantly remarkable anti-inflammatory andantipyretic activities compared to the standard drugs.Keywords: Caryophyllaceae, Flavonoid, Inflammation, Fever, Paronychia capitata.

scholarly journals Inhibitory Effects of Novel 7-Substituted 6-iodo-3-O-Flavonol Glycosides against Cholinesterases and β-secretase Activities, and Evaluation for Potential Antioxidant Properties

Molecules ◽  
2019 ◽  
Vol 24 (19) ◽  
pp. 3500 ◽  
Author(s):  
Agbo ◽  
Gildenhuys ◽  
Mphahlele
Keyword(s):  
Active Sites ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Inhibitory Effect ◽  
Flavonol Glycosides ◽  
Active Compounds ◽  
Secretase Activity ◽  
In Silico Studies ◽  
Increased Activity

A series of 7-halogeno- (X = F, Cl, Br) and 7-methoxy-substituted acetylated 6-iodo-3-O-flavonol glycosides were prepared, and evaluated for inhibitory effect in vitro against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activities. 7-Bromo-2-(4-chlorophenyl)-6-iodo-4H-chromen-4-one-3-O-2,3,4,6-O-tetraacetyl-β-d-glucopyranoside (2k) and 7-bromo-6-iodo-2-(4-methoxyphenyl)-4H-chromen-4-one-3-O-2,3,4,6-O-tetraacetyl-β-d-glucopyranoside (2l) exhibited significant inhibitory effect against AChE activity when compared to the activity of the reference standard, donepezil. Compound 2k was found to be selective against AChE and to exhibit reduced inhibitory effect against BChE activity. 6-Iodo-7-methoxy-2-(4-methoxyphenyl)-4H-chromen-4-one-3-O-2,3,4,6-O-tetraacetyl-β-d-glucopyranoside (2p) was found to exhibit increased activity against BChE, more so than the activity of donepezil. The most active compounds were also evaluated for inhibitory effect against β-secretase activity and for potential radical scavenging activities. The experimental data were complemented with molecular docking (in silico) studies of the most active compounds into the active sites of these enzymes.

scholarly journals Synthesis, In Vitro, and In Silico Analysis of the Antioxidative Activity of Dapsone Imine Derivatives

Molecules ◽  
2021 ◽  
Vol 26 (19) ◽  
pp. 5747
Author(s):  
Ricardo Guzmán-Ávila ◽  
Mayra Avelar ◽  
Edgar A. Márquez ◽  
Julio C. Rivera-Leyva ◽  
José R. Mora ◽  
...  
Keyword(s):  
Antioxidant Properties ◽  
Radical Scavenging ◽  
In Silico Analysis ◽  
Aromatic Aldehydes ◽  
Total Charge ◽  
Antibacterial Drug ◽  
Dpph Radical ◽  
Antioxidant Power ◽  
Donor Acceptor

Dapsone (DDS) is an antibacterial drug with well-known antioxidant properties. However, the antioxidant behavior of its derivatives has not been well explored. In the present work, the antioxidant activity of 10 dapsone derivatives 4-substituted was determined by an evaluation in two in vitro models (DPPH radical scavenging assay and ferric reducing antioxidant power). These imine derivatives 1–10 were obtained through condensation between DDS and the corresponding aromatic aldehydes 4-substuited. Three derivatives presented better results than DDS in the determination of DPPH (2, 9, and 10). Likewise, we have three compounds with better reducing activity than dapsone (4, 9, and 10). In order to be more insight, the redox process, a conceptual DFT analysis was carried out. Molecular descriptors such as electronic distribution, the total charge accepting/donating capacity (I/A), and the partial charge accepting/donating capacity (ω+/ω−) were calculated to analyze the relative donor-acceptor capacity through employing a donor acceptor map (DAM). The DFT calculation allowed us to establish a relationship between GAPHOMO-LUMO and DAM with the observed antioxidant effects. According to the results, we concluded that compounds 2 and 3 have the lowest Ra values, representing a good antioxidant behavior observed experimentally in DPPH radical capturing. On the other hand, derivatives 4, 9, and 10 display the best reducing capacity activity with the highest ω− and Rd values. Consequently, we propose these compounds as the best antireductants in our DDS imine derivative series.

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