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1.
Mar Drugs ; 20(3)2022 Feb 26.
Article in English | MEDLINE | ID: mdl-35323471

ABSTRACT

In the present study, a selenium-chondroitin sulfate (SeCS) was synthesized by the sodium selenite (Na2SeO3) and ascorbic acid (Vc) redox reaction using chondroitin sulfate derived from shark cartilage as a template, and characterized by SEM, SEM-EDS, FTIR and XRD. Meanwhile, its stability was investigated at different conditions of pH and temperatures. Besides, its antioxidant activity was further determined by the DPPH and ABTS assays. The results showed the SeCS with the smallest particle size of 131.3 ± 4.4 nm and selenium content of 33.18% was obtained under the optimal condition (CS concentration of 0.1 mg/mL, mass ratio of Na2SeO3 to Vc of 1:8, the reaction time of 3 h, and the reaction temperature of 25 °C). SEM image showed the SeCS was an individual and spherical nanostructure and its structure was evidenced by FTIR and XRD. Meanwhile, SeCS remained stable at an alkaline pH and possessed good storage stability at 4 °C for 28 days. The results on scavenging free radical levels showed that SeCS exhibited significantly higher antioxidant activity than SeNPs and CS, indicating that SeCS had a potential antioxidant effect.


Subject(s)
Antioxidants/chemistry , Cartilage/chemistry , Chondroitin Sulfates/chemistry , Nanoparticles/chemistry , Selenium/chemistry , Sharks , Animals , Benzothiazoles/chemistry , Biphenyl Compounds/chemistry , Chondroitin Sulfates/isolation & purification , Drug Stability , Hydrogen-Ion Concentration , Particle Size , Picrates/chemistry , Sulfonic Acids/chemistry , Temperature
2.
Bioorg Med Chem Lett ; 59: 128567, 2022 03 01.
Article in English | MEDLINE | ID: mdl-35063634

ABSTRACT

Novel PPARδ agonists, 2-(1-piperidinyl)-1,3-benzothiazole derivatives were discovered by our proprietary docking-based virtual screening technique. Compound 1 as the initial hit was effectively modified to acquire PPARδ agonist activity, resulting in the discovery of compound 12 with high agonistic potency for PPARδ and selectivity over PPARα and PPARγ. Compound 12 also had good ADME profiles and showed in vivo efficacy as a lead.


Subject(s)
Benzothiazoles/pharmacology , Drug Discovery , PPAR delta/agonists , Benzothiazoles/chemical synthesis , Benzothiazoles/chemistry , Dose-Response Relationship, Drug , Drug Evaluation, Preclinical , Humans , Molecular Structure , PPAR alpha/agonists , PPAR gamma/agonists , Structure-Activity Relationship
3.
PLoS One ; 17(1): e0263274, 2022.
Article in English | MEDLINE | ID: mdl-35089980

ABSTRACT

Black soybeans contain several bioactive compounds and commonly consumed due to their health-related activities but rarely cultivated as edible sprouts. The present study investigated the changes that occurred during germination in two new genotypes black soybeans. Raw and germinated seeds were tested against in vitro Alzheimer's disease (AD) biomarkers, including oxidative stress, inflammatory factors and cholinesterase enzymes as well as γ-aminobutyric acid (GABA) levels. Sprouts significantly inhibited the cholinesterase enzymes and inflammatory factors (protein denaturation, proteinase and lipoxygenase) than seeds. An increase in phenolic, flavonoid and GABA (10-folds) content and antioxidant capacity (ABTS, DPPH, and FRAP) was observed in germinated seeds. However, anthocyanin content was decreased in sprouts. UHPLC-ESI-QTOF-MS2 metabolites profiling approach identified 22 compounds including amino acids, peptides, fatty acids, and polyphenols. Among identified compounds, daidzein, genistein, gallic acid, spermidine, L-asparagine, and L-lysine exhibited the highest increase after germination. The current study reveals that germination of black soybeans have promising potential to inhibit/prevent AD and can be used to develop functional foods.


Subject(s)
Alzheimer Disease/drug therapy , Germination , Glycine max/chemistry , Phytochemicals/therapeutic use , Spectrometry, Mass, Electrospray Ionization , Tandem Mass Spectrometry , Anthocyanins/analysis , Antioxidants/analysis , Benzothiazoles/chemistry , Biphenyl Compounds/chemistry , Cholinesterase Inhibitors/pharmacology , Cholinesterase Inhibitors/therapeutic use , Chromatography, High Pressure Liquid , Flavonoids/analysis , Fluorescence Recovery After Photobleaching , Metabolome , Phenols , Picrates/chemistry , Plant Extracts/chemistry , Principal Component Analysis , Sulfonic Acids/chemistry , gamma-Aminobutyric Acid/analysis
4.
Molecules ; 26(23)2021 Nov 29.
Article in English | MEDLINE | ID: mdl-34885820

ABSTRACT

Sophora flavescens is a regularly used traditional Chinese medicine. In an attempt to discover adequate active agents, the isoprenoid flavonoids from S. flavescens were further investigated. In this work, two new compounds (1-2, kurarinol A-B) together with 26 known ones (3-28) were isolated and elucidated on the basis of extensive NMR, UV and MS analyses. Furthermore, the antioxidant activity of all constituents was assessed through ABTS, PTIO and DPPH methodologies and also were evaluated for cytotoxic activity by three tumor cell lines (HepG2, A549 and MCF7) and one human normal cell line (LO2 cells). As a result, a multitude of components revealed significant inhibitory activity. In particular, compound 1-2 (kurarinol A-B), two new flavanonols derivatives, exhibited the most potent ABTS inhibitory activity with IC50 of 1.21 µg/mL and 1.81 µg/mL, respectively. Meanwhile, the new compound 1 demonstrated remarkable cytotoxicity against three cancer cells lines with IC50 values ranging from 7.50-10.55 µM but showed little effect on the normal cell. The two new isoprenoid flavonoids could be promising antioxidant and anti-tumor nature agents.


Subject(s)
Antioxidants/pharmacology , Flavonoids/pharmacology , Sophora/chemistry , Terpenes/pharmacology , Benzothiazoles/chemistry , Carbon-13 Magnetic Resonance Spectroscopy , Cell Death/drug effects , Cell Line, Tumor , Cyclic N-Oxides/chemistry , Flavonoids/chemistry , Free Radical Scavengers/chemistry , Humans , Imidazoles/chemistry , Proton Magnetic Resonance Spectroscopy , Sulfonic Acids/chemistry , Terpenes/chemistry
5.
Sci Rep ; 11(1): 20316, 2021 10 13.
Article in English | MEDLINE | ID: mdl-34645930

ABSTRACT

Acacia senegal (AS) gum (Gum Arabic) is a natural emulsifier exudate from the branches and trunk of Acacia trees and it is recognized by the Food and Drug Administration (FDA) agency as a secure dietary fiber. The present research evaluated the systemic oxidative and necroinflammatory stress induced by CCl4 administration and the alleviating effect of AS gum aqueous extract (ASE, 7.5 g/Kg b.w.). The results demonstrated the presence of certain phenolic compounds in ASE, as well as its in vitro potent scavenging ability against ABTS (2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid), NO, and lipid peroxide radicals. Also, the outcomes revealed an improvement in the CCl4-induced liver, lung, brain, and spleen toxicity by reducing the levels of ROS, lipid peroxidation, NO, and the gene expression of NF-κB and its relevant ROS-mediated inflammatory genes. In contrast, the total antioxidant capacity (TAC), as well as the enzymatic and non-enzymatic antioxidants, were significantly upregulated in these organs after the treatment with ASE. These results were confirmed by improving the morphological features of each organ. Therefore, ASE can ameliorate the systemic toxicity caused by CCl4 via regulation of the ROS/NF-κB signaling pathway in the rat organs, which is owed to its phytochemical composition.


Subject(s)
Acacia/metabolism , Carbon Tetrachloride/chemistry , Gum Arabic/chemistry , NF-kappa B/metabolism , Animals , Antioxidants/chemistry , Benzothiazoles/chemistry , Body Weight , Brain/pathology , Chromatography, Liquid , In Vitro Techniques , Lipid Peroxidation , Liver/metabolism , Male , Organ Size , Oxidation-Reduction , Oxidative Stress , Phenol , Plant Extracts/pharmacology , Rats , Reactive Oxygen Species , Signal Transduction , Sulfonic Acids/chemistry , Thiobarbituric Acid Reactive Substances , Transforming Growth Factor beta/metabolism
6.
Biomed Res Int ; 2021: 5125681, 2021.
Article in English | MEDLINE | ID: mdl-34631882

ABSTRACT

Studies on green biosynthesis of newly engineered nanoparticles for their prominent medicinal applications are being the torch-bearing concerns of the state-of-the-art research strategies. In this concern, we have engineered the biosynthesized Luffa acutangula silver nanoparticles of flavonoid O-glycosides in the anisotropic form isolated from aqueous leave extracts of Luffa acutangula, a popular traditional and ayurvedic plant in south-east Asian countries. These were structurally confirmed by Ultraviolet-visible (UV-Vis), Fourier transform infrared spectroscopy accessed with attenuated total reflection (FTIR-ATR) spectral analyses followed by the scanning electron microscopic (SEM) and the X-ray diffraction (XRD) crystallographic studies and found them with the face-centered cubic (fcc) structure. Medicinally, we have explored their significant antioxidant (DPPH and ABTS assays), antibacterial (disc diffusion assay on E. coli, S. aureus, B. subtilis, S. fecilis, and S. boydii), and anticancer (MTT assay on MCF-7, MDA-MB-231, U87, and DBTRG cell lines) potentialities which augmented the present investigation. The molecular docking analysis of title compounds against 3NM8 (DPPH) and 1DNU (ABTS) proteins for antioxidant activity; 5FGK (Gram-Positive Bacteria) and 1AB4 (Gram-Negative Bacteria) proteins for antibacterial activity; and 4GBD (MCF-7), 5FI2 (MDA-MB-231), 1D5R (U87), and 5TIJ (DBTRG) proteins for anticancer activity has affirmed the promising ligand-protein binding interactions among the hydroxy groups of the title compounds and aspartic acid of the concerned enzymatic proteins. The binding energy varying from -9.1645 to -7.7955 for Cosmosioside (1, Apigenin-7-glucoside) and from -9.2690 to -7.8306 for Cynaroside (2, Luteolin-7-glucoside) implies the isolated compounds as potential bioactive compounds. In addition, the performed studies like QSAR, ADMET, bioactivity properties, drug scores, and toxicity risks confirmed them as potential drug candidates and aspartic acid receptor antagonists. This research auxiliary augmented the existing array of phytological nanomedicines with new drug candidates that are credible with multiple bioactivities.


Subject(s)
Anti-Bacterial Agents/pharmacology , Antineoplastic Agents/pharmacology , Antioxidants/pharmacology , Green Chemistry Technology , Luffa/chemistry , Metal Nanoparticles/chemistry , Plant Extracts/pharmacology , Silver/pharmacology , Bacteria/drug effects , Benzothiazoles/chemistry , Biphenyl Compounds/chemistry , Cell Death/drug effects , Cell Line, Tumor , Color , Humans , Ligands , Metal Nanoparticles/ultrastructure , Microbial Sensitivity Tests , Molecular Docking Simulation , Picrates/chemistry , Plant Extracts/chemistry , Plant Leaves/chemistry , Quantitative Structure-Activity Relationship , Spectrophotometry, Ultraviolet , Spectroscopy, Fourier Transform Infrared , Sulfonic Acids/chemistry , Toxicity Tests , X-Ray Diffraction
7.
Int J Biol Macromol ; 186: 365-376, 2021 Sep 01.
Article in English | MEDLINE | ID: mdl-34246681

ABSTRACT

Chitosan - tea tree essential oil (TTEO) films were obtained as a new biodegradable material. Malic acid or lactic acid solvents were evaluated to obtain easy-removing films. The microstructure by SEM and FT-IR, the thermal properties by TGA/DSC, the mechanical properties, the water vapor permeability, the antioxidant (DPPH• and ABTS•+) activity and the optical properties of the formulated films were evaluated. A complete dissolution of the film in water was obtained. The elongation to break was higher in the films with malic acid (145.88-317.33%), comparing with those with lactic acid (25.54-44.08%). Chitosan film obtained in malic acid with TTEO showed the highest antioxidant activity. The colour and transparency of the samples did not suffer significant variations by TTEO addition. Films showed good UV-barrier properties, with a slightly improvement by TTEO addition. The films obtained showed a great potential for food packaging applications.


Subject(s)
Antioxidants/pharmacology , Chitosan/chemistry , Food Packaging , Tea Tree Oil/pharmacology , Antioxidants/chemistry , Benzothiazoles/chemistry , Biphenyl Compounds/chemistry , Color , Elastic Modulus , Lactic Acid/chemistry , Malates/chemistry , Picrates/chemistry , Solubility , Solvents/chemistry , Sulfonic Acids/chemistry , Surface Properties , Tea Tree Oil/chemistry , Tensile Strength , Water/chemistry
8.
Molecules ; 26(11)2021 May 27.
Article in English | MEDLINE | ID: mdl-34072026

ABSTRACT

Pineapple is consumed on a large scale around the world due to its appreciated sensorial characteristics. The industry of minimally processed pineapple produces enormous quantities of by-products (30-50%) which are generally undervalued. The end-of-life of pineapple by-products (PBP) can be replaced by reuse and renewal flows in an integrated process to promote economic growth by reducing consumption of natural resources and diminishing food waste. In our study, pineapple shell (PS) and pineapple core (PC), vacuum-packed separately, were subjected to moderate hydrostatic pressure (225 MPa, 8.5 min) (MHP) as abiotic stress to increase bromelain activity and antioxidant capacity. Pressurized and raw PBP were lyophilized to produce a stable powder. The dehydrated samples were characterized by the following methodologies: chemical and physical characterization, total phenolic compounds (TPC), antioxidant capacity, bromelain activity, microbiology, and mycotoxins. Results demonstrated that PBP are naturally rich in carbohydrates (66-88%), insoluble (16-28%) and soluble (2-4%) fiber, and minerals (4-5%). MHP was demonstrated to be beneficial in improving TPC (2-4%), antioxidant activity (2-6%), and bromelain activity (6-32%) without affecting the nutritional value. Furthermore, microbial and mycotoxical analysis demonstrated that powdered PC is a safe by-product. PS application is possible but requires previous decontamination to reduce the microbiological load.


Subject(s)
Ananas/chemistry , Ananas/physiology , Antioxidants/chemistry , Functional Food/analysis , Benzothiazoles/chemistry , Biphenyl Compounds/chemistry , Bromelains/analysis , Carbohydrates/chemistry , Chemistry Techniques, Analytical , Color , Dietary Fiber , Food Packaging , Food Preservation , Freeze Drying , Fruit/chemistry , Mycotoxins/chemistry , Nutritive Value , Phenol/chemistry , Picrates/chemistry , Powders , Pressure , Sulfonic Acids/chemistry , Water/chemistry
9.
Molecules ; 26(9)2021 May 10.
Article in English | MEDLINE | ID: mdl-34068613

ABSTRACT

Nowadays, natural dyes are expected by the cosmetic and food industries. In contrast to synthetic dyes, colorants derived from natural sources are more environmentally friendly and safer for human health. In this work, plant extracts from Gomphrena globasa L., Clitoria ternatea L., Carthamus tinctorius L., Punica granatum L. and Papaver rhoeas L. as the natural and functional dyes for the cosmetics industry were assessed. Cytotoxicity on keratinocyte and fibroblast cell lines was determined as well as antioxidant and anti-aging properties by determining their ability to inhibit the activity of collagenase and elastase enzymes. In addition, the composition of the extracts was determined. The obtained extracts were also applied in face cream formulation and color analyses were performed. It has been shown that the obtained extracts were characterized by no cytotoxicity and a high antioxidant potential. The extracts also show strong ability to inhibit the activity of collagenase and moderate ability to inhibit elastase and provide effective and long-lasting hydration after their application on the skin. Application analyses showed that the extracts of P. rhoeas L., C. ternatea L. and C. tinctorius L. can be used as effective cosmetic dyes that allow for attainment of an intense and stable color during the storage of the product. The extracts of P. granatum L. and G. globasa L., despite their beneficial effects as active ingredients, did not work effectively as cosmetic dyes, because cosmetic emulsions with these extracts did not differ significantly in color from emulsions without the extract.


Subject(s)
Antioxidants/pharmacology , Coloring Agents/pharmacology , Cosmetics/pharmacology , Cytoprotection , Desiccation , Flowers/chemistry , Plant Extracts/pharmacology , Benzothiazoles/chemistry , Biphenyl Compounds/chemistry , Cell Death/drug effects , Collagenases/metabolism , Color , Cytoprotection/drug effects , HaCaT Cells , Humans , Kinetics , Matrix Metalloproteinase Inhibitors/pharmacology , Oxazines/metabolism , Pancreatic Elastase/antagonists & inhibitors , Pancreatic Elastase/metabolism , Picrates/chemistry , Plants/chemistry , Skin Cream/pharmacology , Sulfonic Acids/chemistry , Ultraviolet Rays , Water Loss, Insensible/drug effects , Xanthenes/metabolism
10.
Molecules ; 26(10)2021 May 14.
Article in English | MEDLINE | ID: mdl-34068909

ABSTRACT

Due to the health-promoting properties of elderberry fruits, which result from their rich chemical composition, this raw material is widely used in herbal medicine and the food industry. The aim of the study was to demonstrate the antibacterial activity of the elderberry fruit extracts. The research showed that the content of phenolic acids and flavonoids in the extracts determined their antibacterial activity. The research showed that the content of phenolic acids and flavonoids in the extracts determined their antibacterial activity. The following phenolic acids were predominant: chlorogenic acid, sinapic acid, and t-cinnamic acid. Their average content was, respectively, 139.09, 72.84, 51.29 mg/g extract. Rutin and quercetin (their average content was 1105.39 and 306.6 mg/g extract, respectively) were the dominant flavonoids. The research showed that the elderberry polyphenol extracts exhibited activity against selected strains of bacteria within the concentration range of 0.5-0.05%. The following bacteria were the most sensitive to the extracts: Micrococcus luteus, Proteus mirabilis, Pseudomonas fragii, and Escherichia coli. Of the compounds under analysis, apigenin, kaempferol and ferulic, protocatechuic, and p-coumarin acids had the greatest influence on the high antibacterial activity of elderberry extracts. The results of the microbiological and chemical analyses of the composition of the extracts were analyzed statistically to indicate the bioactive compounds of the greatest antimicrobial significance.


Subject(s)
Anti-Infective Agents/pharmacology , Antioxidants/pharmacology , Plant Extracts/pharmacology , Sambucus nigra/chemistry , Bacteria/drug effects , Benzothiazoles/chemistry , Carboxylic Acids/analysis , Flavonoids/analysis , Microbial Sensitivity Tests , Pigments, Biological/analysis , Polyphenols/analysis , Sulfonic Acids/chemistry
11.
Int J Biol Macromol ; 181: 631-643, 2021 Jun 30.
Article in English | MEDLINE | ID: mdl-33798582

ABSTRACT

Sodium bicarbonate medium ultrasound pre-treatment can enhance the freeze-drying process of blueberries, but the quality of dried products cannot meet the actual production needs. To yield higher quality products, chitosan coating was applied in blueberry sodium bicarbonate medium ultrasound pre-treatment enhanced freeze-drying process. The improvement effect of different chitosan coating methodologies on the procedure of blueberry freeze-drying, enhanced by ultrasound pre-treatment in sodium bicarbonate medium, was investigated. These include: chitosan solution soaking alone (CH-A), chitosan medium ultrasound treatment (US-CH), first sodium bicarbonate medium ultrasound treatment then chitosan solution soaking (US-NaHCO3 + CH) and first sodium bicarbonate soaking followed by chitosan medium ultrasound treatment (NaHCO3 + US-CH). While the treatments that presoaking in sodium bicarbonate solution (NaHCO3-A), water medium ultrasound treatment (US-W) and sodium bicarbonate medium ultrasound treatment (US-NaHCO3) were used as the control groups. Results demonstrated that ultrasound treatment and sodium bicarbonate soaking have positive effect on improving the freeze-drying characteristics of blueberries, while chitosan coating has a negative effect. Chitosan coating has a significant effect on strengthening limit effect of blueberry skin on juice overflow and weakening moisture absorption capacity of dried blueberry. US-NaHCO3 + CH pretreatment yielded the best results for blueberry freeze-drying.


Subject(s)
Blueberry Plants/chemistry , Chitosan/chemistry , Freeze Drying , Sodium Bicarbonate/chemistry , Ultrasonics , Adsorption , Anthocyanins/analysis , Antioxidants/analysis , Benzothiazoles/chemistry , Biphenyl Compounds/chemistry , Free Radical Scavengers/chemistry , Hardness , Kinetics , Magnetic Resonance Spectroscopy , Models, Theoretical , Picrates/chemistry , Sulfonic Acids/chemistry , Temperature , Time Factors , Water
12.
Molecules ; 26(7)2021 Mar 28.
Article in English | MEDLINE | ID: mdl-33800622

ABSTRACT

Croton hirtus L'Hér methanol extract was studied by NMR and two different LC-DAD-MSn using electrospray (ESI) and atmospheric pressure chemical ionization (APCI) sources to obtain a quali-quantitative fingerprint. Forty different phytochemicals were identified, and twenty of them were quantified, whereas the main constituents were dihydro α ionol-O-[arabinosil(1-6) glucoside] (133 mg/g), dihydro ß ionol-O-[arabinosil(1-6) glucoside] (80 mg/g), ß-sitosterol (49 mg/g), and isorhamnetin-3-O-rutinoside (26 mg/g). C. hirtus was extracted with different solvents-namely, water, methanol, dichloromethane, and ethyl acetate-and the extracts were assayed using different in vitro tests. The methanolic extracts presented the highest 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline)-6-sulfonic acid (ABTS), and ferric reducing antioxidant power (FRAP) values. All the tested extracts exhibited inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with a higher activity observed for dichloromethane (AChE: 5.03 and BChE: 16.41 mgGALAE/g), while the methanolic extract showed highest impact against tyrosinase (49.83 mgKAE/g). Taken together, these findings suggest C. hirtus as a novel source of bioactive phytochemicals with potential for commercial development.


Subject(s)
Antioxidants/chemistry , Cholinesterase Inhibitors/chemistry , Croton/chemistry , Glucosides/chemistry , Phytochemicals/chemistry , Phytosterols/chemistry , Terpenes/chemistry , Acetates/chemistry , Acetylcholinesterase/chemistry , Acetylcholinesterase/metabolism , Antioxidants/classification , Antioxidants/isolation & purification , Benzothiazoles/antagonists & inhibitors , Benzothiazoles/chemistry , Biphenyl Compounds/antagonists & inhibitors , Biphenyl Compounds/chemistry , Butyrylcholinesterase/chemistry , Butyrylcholinesterase/metabolism , Cholinesterase Inhibitors/isolation & purification , Croton/metabolism , Glucosides/classification , Glucosides/isolation & purification , Humans , Methanol/chemistry , Methylene Chloride/chemistry , Phytochemicals/classification , Phytochemicals/isolation & purification , Phytosterols/classification , Phytosterols/isolation & purification , Picrates/antagonists & inhibitors , Picrates/chemistry , Plant Extracts/chemistry , Solvents/chemistry , Structure-Activity Relationship , Sulfonic Acids/antagonists & inhibitors , Sulfonic Acids/chemistry , Terpenes/classification , Terpenes/isolation & purification , Water/chemistry
13.
Molecules ; 26(7)2021 Mar 28.
Article in English | MEDLINE | ID: mdl-33800652

ABSTRACT

In Thailand, people in the highland communities whose occupational exposure to pesticides used the root of Litsea martabanica as a detoxifying agent. However, the scientific data to support the traditional use of this plant are insufficient. This study aimed to evaluate the antioxidant activity and anti-pesticide potential of L. martabanica root extract. Antioxidant properties were investigated by 2,2'-diphenyl-1-picrylhydrazyl (DPPH) assay, superoxide radicals scavenging assay, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assay, ferric reducing antioxidant power (FRAP), and total phenolic content determination. In all assays, L. martabanica extracts and their fractions exhibited high antioxidant activities differently. The water extract is traditionally used as a detoxifying agent. Therefore, it was chosen for in vivo experiments. The rats received the extract in a way that mimics the traditional methods of tribal communities followed by chlorpyrifos for 16 days. The results showed that acetylcholinesterase activity decreases in pesticide-exposed rats. Treatment with the extract caused increasing acetylcholinesterase activity in the rats. Therefore, L. martabanica extract may potentially be used as a detoxifying agent, especially for the chlorpyrifos pesticide. The antioxidant properties of L. martabanica may provide a beneficial effect by protecting liver cells from damage caused by free radicals. Histopathology results revealed no liver cell necrosis and showed the regeneration of liver cells in the treatment group. L. martabanica extract did not cause changes in behavior, liver weight, hematological and biochemical profiles of the rats.


Subject(s)
Antidotes/pharmacology , Antioxidants/pharmacology , Chemical and Drug Induced Liver Injury/drug therapy , Chlorpyrifos/toxicity , Insecticides/toxicity , Litsea/chemistry , Acetylcholinesterase/metabolism , Alanine Transaminase/metabolism , Alkaline Phosphatase/metabolism , Animals , Antidotes/isolation & purification , Antioxidants/isolation & purification , Aspartate Aminotransferases/metabolism , Benzothiazoles/antagonists & inhibitors , Benzothiazoles/chemistry , Bilirubin/metabolism , Biphenyl Compounds/antagonists & inhibitors , Biphenyl Compounds/chemistry , Chemical and Drug Induced Liver Injury/etiology , Chemical and Drug Induced Liver Injury/metabolism , Chemical and Drug Induced Liver Injury/pathology , Chlorpyrifos/antagonists & inhibitors , Creatinine/metabolism , Insecticides/antagonists & inhibitors , Liver/drug effects , Liver/metabolism , Liver/pathology , Male , Phytotherapy/methods , Picrates/antagonists & inhibitors , Picrates/chemistry , Plant Extracts/chemistry , Plant Roots/chemistry , Rats , Rats, Sprague-Dawley , Sulfonic Acids/antagonists & inhibitors , Sulfonic Acids/chemistry
14.
Int J Mol Sci ; 22(7)2021 Mar 25.
Article in English | MEDLINE | ID: mdl-33806141

ABSTRACT

The study of antioxidants and their implications in various fields, from food engineering to medicine and pharmacy, is of major interest to the scientific community. The present paper is a critical presentation of the most important tests used to determine the antioxidant activity, detection mechanism, applicability, advantages and disadvantages of these methods. Out of the tests based on the transfer of a hydrogen atom, the following were presented: the Oxygen Radical Absorption Capacity (ORAC) test, the Hydroxyl Radical Antioxidant Capacity (HORAC) test, the Total Peroxyl Radical Trapping Antioxidant Parameter (TRAP) test, and the Total Oxyradical Scavenging Capacity (TOSC) test. The tests based on the transfer of one electron include the Cupric Reducing Antioxidant Power (CUPRAC) test, the Ferric Reducing Antioxidant Power (FRAP) test, the Folin-Ciocalteu test. Mixed tests, including the transfer of both a hydrogen atom and an electron, include the 2,2'-Azinobis-(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) test, and the [2,2-di(4-tert-octylphenyl)-1-picrylhydrazyl] (DPPH) test. All these assays are based on chemical reactions and assessing the kinetics or reaching the equilibrium state relies on spectrophotometry, presupposing the occurrence of characteristic colours or the discolouration of the solutions to be analysed, which are processes monitored by specific wavelength adsorption. These assays were successfully applied in antioxidant analysis or the determination of the antioxidant capacity of complex samples. As a complementary method in such studies, one may use methods based on electrochemical (bio)sensors, requiring stages of calibration and validation. The use of chemical methods together with electrochemical methods may result in clarification of the operating mechanisms and kinetics of the processes involving several antioxidants.


Subject(s)
Antioxidants/pharmacology , Ascorbic Acid/analysis , Free Radical Scavengers/pharmacology , Hydroxyl Radical/pharmacology , Animals , Benzothiazoles/chemistry , Biological Assay/methods , Biphenyl Compounds , Electrochemical Techniques , Humans , Hydrogen/chemistry , Kinetics , Oxygen/chemistry , Phenols/analysis , Picrates , Reactive Oxygen Species/metabolism , Sulfonic Acids/chemistry , Superoxide Dismutase/metabolism
15.
Molecules ; 26(8)2021 Apr 08.
Article in English | MEDLINE | ID: mdl-33918007

ABSTRACT

A pectin/chitosan matrix-loaded curcumin film (PCCF) with a deep eutectic solvent (DES) as the solvent and plasticizer was prepared in this study. Different quantities of curcumin (identified as PCCF-0, PCCF-1, PCCF-2. PCCF-3) were loaded on the pectin/chitosan film in order to evaluate their effects on the film properties. Results showed that curcumin could interact with the pectin/chitosan matrix and form a complex three-dimensional network structure. PCCF could promote the thickness, tensile strength, thermal properties, antioxidant and antiseptic capacities, but deteriorate the light transmission and elongation at the same time. The addition of curcumin would change the color of the film, without significantly affecting the moisture content. The tensile strength of PCCF-3 reached the maximum value of 3.75 MPa, while the elongation decreased to 10%. Meanwhile, the water-resistance properties of PCCF-3 were significantly promoted by 8.6% compared with that of PCCF-0. Furthermore, PCCF showed remarkable sustained antioxidant activities in a dose-dependent manner. PCCF-3 could inhibit DPPH and ABTS free radicals by 58.66% and 29.07%, respectively. It also showed antiseptic capacity on fresh pork during storage. Therefore, curcumin addition could improve the barrier, mechanical, antioxidant and antiseptic properties of the polysaccharide-based film and PCCF has the potential to be used as a new kind of food packaging material in the food industry.


Subject(s)
Biocompatible Materials/chemistry , Chitosan/chemistry , Curcumin/pharmacology , Pectins/chemistry , Anti-Infective Agents, Local/pharmacology , Antioxidants/pharmacology , Benzothiazoles/chemistry , Biphenyl Compounds/chemistry , Food , Free Radical Scavengers/chemistry , Humidity , Picrates/chemistry , Solubility , Spectroscopy, Fourier Transform Infrared , Sulfonic Acids/chemistry , Water/chemistry , X-Ray Diffraction
16.
Molecules ; 26(7)2021 Apr 04.
Article in English | MEDLINE | ID: mdl-33916551

ABSTRACT

Vaccinium dunalianum Wight, usually processed as a traditional folk tea beverage, is widely distributed in the southwest of China. The present study aimed to investigate the antioxidant, α-glucosidase and pancreatic lipase inhibitory activities of V.dunalianum extract and isolate the bioactive components. In this study, the crude extract (CE) from the buds of V. dunalianum was prepared by the ultrasound-assisted extraction method in 70% methanol and then purified with macroporous resin D101 to obtain the purified extract (PM). Five fractions (Fr. A-E) were further obtained by MPLC column (RP-C18). Bioactivity assays revealed that Fr. B with 40% methanol and Fr. D with 80% methanol had better antioxidant with 0.48 ± 0.03 and 0.62 ± 0.01 nM Trolox equivalent (TE)/mg extract for DPPH, 0.87 ± 0.02 and 1.58 ± 0.02 nM TE/mg extract for FRAP, 14.42 ± 0.41 and 19.25 ± 0.23 nM TE/mg extract for ABTS, and enzyme inhibitory effects with IC50 values of 95.21 ± 2.21 and 74.55 ± 3.85 for α-glucosidase, and 142.53 ± 11.45 and 128.76 ± 13.85 µg/mL for pancreatic lipase. Multivariate analysis indicated that the TPC and TFC were positively related to the antioxidant activities. Further phytochemical purification led to the isolation of ten compounds (1-10). 6-O-Caffeoylarbutin (7) showed significant inhibitory effects on α-glucosidase and pancreatic lipase enzymes with values of 38.38 ± 1.84 and 97.56 ± 7.53 µg/mL, and had the highest antioxidant capacity compared to the other compounds.


Subject(s)
Antioxidants/isolation & purification , Arbutin/analogs & derivatives , Caffeic Acids/isolation & purification , Flavonoids/isolation & purification , Glycoside Hydrolase Inhibitors/isolation & purification , Lipase/chemistry , Vaccinium/chemistry , alpha-Glucosidases/chemistry , Antioxidants/chemistry , Arbutin/chemistry , Arbutin/isolation & purification , Benzothiazoles/antagonists & inhibitors , Benzothiazoles/chemistry , Biphenyl Compounds/chemistry , Caffeic Acids/chemistry , Flavonoids/chemistry , Glycoside Hydrolase Inhibitors/chemistry , Lipase/antagonists & inhibitors , Lipase/metabolism , Liquid-Liquid Extraction/methods , Methanol/chemistry , Picrates/chemistry , Plant Extracts/chemistry , Plant Leaves/chemistry , Solvents/chemistry , Sonication , Sulfonic Acids/antagonists & inhibitors , Sulfonic Acids/chemistry , alpha-Glucosidases/metabolism
17.
Molecules ; 26(4)2021 Feb 13.
Article in English | MEDLINE | ID: mdl-33668450

ABSTRACT

Greek oregano and common oregano were compared in respect of the antioxidant and antibacterial activity of the corresponding essential oils and hydroethanolic extracts in relation with their chemical profile. The chemical composition of essential oils was determined by GC-MS and GC-FID, while extracts (phenolic acids and flavonoids fractions) were analyzed by HPLC-DAD. Based on given volatiles, the investigated subspecies represented two chemotypes: a carvacrol/γ-terpinene/p-cymene type in the case of Greek oregano and a sabinyl/cymyl type rich in terpinen-4-ol in common oregano. Within non-volatile phenolic compounds, rosmarinic acid appeared to dominate in both subspecies. Lithospermic acid B, chlorogenic acid and isovitexin were present only in Greek oregano extracts. However, the total content of flavonoids was higher in common oregano extracts. The essential oil and extract of Greek oregano revealed visibly stronger antibacterial activity (expressed as MIC and MBC) than common oregano, whereas the antioxidant potential (determined by DPPH, ABTS and FRAP) of these extracts was almost equal for both subspecies. In the case of Origanum plants, the potential application of essential oils and extracts as antiseptic and antioxidant agents in the food industry should be preceded by subspecies identification followed by recognition of their chemotype concerning both terpene and phenolics composition.


Subject(s)
Anti-Bacterial Agents/pharmacology , Antioxidants/pharmacology , Ethanol/chemistry , Oils, Volatile/pharmacology , Origanum/chemistry , Plant Extracts/pharmacology , Water/chemistry , Benzothiazoles/chemistry , Biphenyl Compounds/chemistry , Chromatography, High Pressure Liquid , Flavonoids/analysis , Free Radical Scavengers/pharmacology , Microbial Sensitivity Tests , Phenols/analysis , Picrates/chemistry , Reproducibility of Results , Sulfonic Acids/chemistry
18.
Biomolecules ; 11(2)2021 02 04.
Article in English | MEDLINE | ID: mdl-33557215

ABSTRACT

Alchornea cordifolia (Schumach. & Thonn.) Müll. Arg. is a well-known African medicinal plant traditionally used for various healing purposes. In the present study, methanolic, ethyl acetate and infusion extracts of A. cordifolia leaves were studied for their total phenolic and flavonoid contents and screened for their chemical composition. Moreover, the enzyme (acetyl- and butyryl-cholinesterases, α-amylase, α-glucosidase, and tyrosinase) inhibitory and cytotoxicity activities on HepG2: human hepatocellular carcinoma cells, B16 4A5: murine melanoma cells, and S17: murine bone marrow (normal) cells of extracts were evaluated. Finally, components-targets and docking analyzes were conducted with the aim to unravel the putative mechanisms underlying the observed bio-pharmacological effects. Interestingly, the infusion and methanolic extracts showed significantly higher total phenolic and flavonoid contents compared with the ethyl acetate extract (TPC: 120.38-213.12 mg GAE/g and TFC: 9.66-57.18 mg RE/g). Besides, the methanolic extracts followed by the infusion extracts were revealed to contain a higher number of compounds (84 and 74 compounds, respectively), while only 64 compounds were observed for the ethyl acetate extract. Gallic acid, ellagic acid, shikimic acid, rutin, quercetin, myricetin, vitexin, quercitrin, kaempferol, and naringenin were among the compounds that were commonly identified in all the studied extracts. Additionally, the methanolic and infusion extracts displayed higher antioxidant capacity than ethyl acetate extract in all assays performed. In ABTS and DPPH radical scavenging assays, the methanol extract (500.38 mg TE/g for DPPH and 900.64 mg TE/g for ABTS) exhibited the best ability, followed by the water and ethyl acetate extracts. Furthermore, the extracts exhibited differential enzyme inhibitory profiles. In particular, the methanolic and infusion extracts showed better cytotoxic selectivity activity against human hepatocellular carcinoma cells. Overall, this study demonstrated A cordifolia to be a species worthy of further investigations, given its richness in bioactive phytochemicals and wide potentialities for antioxidants and pharmacological agents.


Subject(s)
Antioxidants/chemistry , Euphorbiaceae/chemistry , Euphorbiaceae/metabolism , Molecular Docking Simulation , Phytochemicals/pharmacology , Plant Extracts/chemistry , Animals , Antioxidants/pharmacology , Benzothiazoles/chemistry , Biphenyl Compounds/chemistry , Carcinoma, Hepatocellular/drug therapy , Computational Biology , Drug Evaluation, Preclinical , Flavonoids/pharmacology , Free Radical Scavengers , Hep G2 Cells , Humans , Kaempferols , Liver Neoplasms/drug therapy , Melanoma, Experimental , Methanol/chemistry , Mice , Monophenol Monooxygenase , Phenols/chemistry , Picrates/chemistry , Plant Extracts/pharmacology , Plant Leaves/chemistry , Plants, Medicinal , Sulfonic Acids/chemistry
19.
Acta Sci Pol Technol Aliment ; 20(1): 37-46, 2021.
Article in English | MEDLINE | ID: mdl-33449518

ABSTRACT

BACKGROUND: Extracts of milk thistle, particularly from seeds, are used as a valuable source of natural antioxidants in different industries, for example pharmaceutical and cosmetic. The leaves and flowers are also known to be a source of biologically active compounds, as well as those with an antioxidant capacity. The selection of the extraction parameters, such as type and concentration of extractant, and extraction time, have an impact on the antioxidant capacity of the obtained extracts. The aim of this study was to evaluate the antioxidant activities of extracts obtained using different parts of raw material. The impact of different parameters of extraction on antioxidant capacity was also assessed. METHODS: The seeds, flowers and leaves were extracted using a Soxhlet apparatus, ultrasound and shaking. 96% (v/v) and 70% (v/v) ethanol, concentrated methanol, acetone and petroleum ether were applied as solvents. The impact of the extraction time was also evaluated. The extracts were evaluated using DPPH, ABTS, FRAP and Folin-Ciocalteu techniques. RESULTS: The obtained extracts, except for the samples in petroleum ether, showed the antioxidant capacity. Soxhlet extraction, especially that which uses ethanol, methanol and acetone, seems to be a valuable extraction method. CONCLUSIONS: To sum up, many factors could affect the antioxidant capacity and the total polyphenol content of Silybum marianum L. extracts. The solvent and an appropriately selected extraction method seem to be important factors in the effective isolation of active substances and could lead to the more effective application of this valuable plant material in different industries.


Subject(s)
Antioxidants/chemistry , Chemical Fractionation/methods , Flowers/chemistry , Plant Extracts/chemistry , Seeds/chemistry , Silybum marianum/chemistry , Benzothiazoles/chemistry , Biphenyl Compounds/chemistry , Fluorescence Recovery After Photobleaching , Picrates/chemistry , Plant Leaves/chemistry , Sulfonic Acids/chemistry
20.
Nat Prod Res ; 35(4): 570-578, 2021 Feb.
Article in English | MEDLINE | ID: mdl-30931624

ABSTRACT

Investigation of the n-butanol extract of Flos populi led to the isolation of one new phenolic glycoside, 4'-hydroxybenzyl-2-hydroxybenzoate-1'-O-ß-D-glucopyranoside (1), together with twelve known compounds, which have been determined on the basis of spectroscopic analysis including UV, IR, HR-ESI-MS and 1D/2D NMR. The antioxidant capacity of all compounds were evaluated by ABTS radical-scavenging test and ferric reducing antioxidant power (FRAP) assay. And during a screening procedure for the anti-inflammatory activities among most compounds on lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophage cells, compound 13 exhibited remarkable inhibitory effects on nitric oxide (NO), tumor necrosis factor-α (TNF-α), interleukin (IL)-6 and IL-1ß, suggesting that it might be a promising candidate as an anti-inflammatory agent.


Subject(s)
Anti-Inflammatory Agents/pharmacology , Antioxidants/pharmacology , Drugs, Chinese Herbal/chemistry , Animals , Benzothiazoles/chemistry , Lipopolysaccharides/pharmacology , Macrophages/drug effects , Macrophages/metabolism , Mice , Nitric Oxide/biosynthesis , Plant Extracts/chemistry , RAW 264.7 Cells , Sulfonic Acids/chemistry
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