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The targeted compounds in this research, resveratrol analogs 1-14, were synthesized as mixtures of isomers by the Wittig reaction using heterocyclic triphenylphosphonium salts and various benzaldehydes. The planned compounds were those possessing the trans-configuration as the biologically active trans-resveratrol. The pure isomers were obtained by repeated column chromatography in various isolated yields depending on the heteroaromatic ring. It was found that butyrylcholinesterase (BChE) was more sensitive to the heteroaromatic resveratrol analogs than acetylcholinesterase (AChE), except for 6, the methylated thiophene derivative with chlorine, which showed equal inhibition toward both enzymes. Compounds 5 and 8 achieved the highest BChE inhibition with IC50 values of 22.9 and 24.8 µM, respectively. The same as with AChE and BChE, methylated thiophene subunits of resveratrol analogs showed better enzyme inhibition than unmethylated ones. Two antioxidant spectrophotometric methods, DPPH and CUPRAC, were applied to determine the antioxidant potential of new heteroaromatic resveratrol analogs. The molecular docking of these compounds was conducted to visualize the ligand-active site complexes' structure and identify the non-covalent interactions responsible for the complex's stability, which influence the inhibitory potential. As ADME properties are crucial in developing drug product formulations, they have also been addressed in this work. The potential genotoxicity is evaluated by in silico studies for all compounds synthesized.
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Antioxidantes , Butirilcolinesterase , Inibidores da Colinesterase , Simulação de Acoplamento Molecular , Resveratrol , Resveratrol/análogos & derivados , Resveratrol/química , Resveratrol/farmacologia , Resveratrol/síntese química , Inibidores da Colinesterase/farmacologia , Inibidores da Colinesterase/química , Inibidores da Colinesterase/síntese química , Antioxidantes/química , Antioxidantes/farmacologia , Antioxidantes/síntese química , Butirilcolinesterase/metabolismo , Butirilcolinesterase/química , Acetilcolinesterase/metabolismo , Acetilcolinesterase/química , Humanos , Relação Estrutura-AtividadeRESUMO
Introduction: The prevalence of age-related diseases, including obesity (a lipid metabolism disorder), increases with the increase in a dog's lifespan. Most of age-related diseases are associated with oxidative stress by excessive production of reactive oxygen species (ROS) from impaired mitochondrial functions. Safe and effective supplements with antioxidative and anti-inflammatory activities are required to prevent obesity and associated complications. Shiitake mushroom exhibit various functions including antioxidant activity. We investigated the effect of shiitake powder supplementation in healthy dogs. Methods: Shiitake powder was supplemented at a dose of 800 mg/kg body weight/day for 4 weeks. The dose was set as 0.60-0.65 mg/kg/day of eritadenine, a hypocholesterolemic factor. Results: The body weight and body condition score of the dogs did not change after shiitake supplementation. In contrast, plasma total cholesterol concentrations decreased and superoxide dismutase activity and leukocyte sirtuin1 mRNA expression increased significantly in the dogs that received the supplement. Discussion: Oral administration of shiitake powder increased antioxidative activity. The supplement may be useful in ameliorating the signs of age-related diseases, including obesity, in dogs.
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This study aimed to improve the conventional procedure of alginate isolation from the brown seaweed (Laminaria digitata L.) biomass and investigate the possibility of further valorization of the ethanolic fraction representing the byproduct after the degreasing and depigmentation of biomass. The acid treatment of biomass supported by ultrasound was modeled and optimized regarding the alginate yield using a response surface methodology based on the Box-Behnken design. A treatment time of 30 min, a liquid-to-solid ratio of 30 mL/g, and a treatment temperature of 47 °C were proposed as optimal conditions under which the alginate yield related to the mass of dry biomass was 30.9%. The use of ultrasonic radiation significantly reduced the time required for the acid treatment of biomass by about 4 to 24 times compared to other available conventional procedures. The isolated alginate had an M/G ratio of 1.08, which indicates a greater presence of M-blocks in its structure and the possibility of forming a soft and elastic hydrogel with its use. The chemical composition of the ethanolic fraction including total antioxidant content (293 mg gallic acid equivalent/g dry weight), total flavonoid content (14.9 mg rutin equivalent/g dry weight), contents of macroelements (the highest content of sodium, 106.59 mg/g dry weight), and microelement content (the highest content of boron, 198.84 mg/g dry weight) was determined, and the identification of bioactive compounds was carried out. The results of ultra high-performance liquid chromatography-electrospray ionization-tandem mass spectrometry analysis confirmed the presence of 48 compounds, of which 41 compounds were identified as sugar alcohol, phenolic compounds, and lipids. According to the 2,2-diphenyl-1-picrylhydrazyl assay, the radical scavenging activity of the ethanolic fraction (the half-maximal inhibitory concentration of 42.84 ± 0.81 µg/mL) indicated its strong activity, which was almost the same as in the case of the positive control, synthetic antioxidant butylhydroxytoluene (the half-maximal inhibitory concentration of 36.61 ± 0.79 µg/mL). Gram-positive bacteria (Staphylococcus aureus, Enterococcus faecalis, and Bacillus cereus) were more sensitive to the ethanolic fraction compared to Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa, and Shigella sonnei). The obtained results indicated the possibility of the further use of the ethanolic fraction as a fertilizer for plant growth in different species and antifouling agents, applicable in aquaculture.
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Alginatos , Antioxidantes , Etanol , Laminaria , Alga Marinha , Alginatos/química , Laminaria/química , Antioxidantes/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Etanol/química , Alga Marinha/química , Biomassa , Flavonoides/química , Flavonoides/isolamento & purificação , Algas ComestíveisRESUMO
Lonicera macranthoides, the main source of traditional Chinese medicine Lonicerae Flos, is extensively cultivated in Southwest China. However, the quality of L. macranthoides produced in this region significantly varies due to its wide distribution and various cultivation breeds. Herein, 50 Lonicerae Flos samples derived from different breeds of L. macranthoides cultivated in Southwest China were collected for quality evaluation. Six organic acids and three saponin compounds were quantitatively analyzed using HPLC. Furthermore, the antioxidant activity of a portion of samples was conducted with 2,2'-Azinobis-(3-ethylbenzthiazoline-6-sulphonate) (ABTS) and 1,1-diphenyl-2-picryl-hydrazyl (DPPH) radical scavenging experiments. According to the quantitative results, all samples met the quality standards outlined in the Chinese Pharmacopoeia. The samples from Guizhou, whether derived from unopened or open wild-type breeds, exhibited high quality, while the wild-type samples showed relatively significant fluctuation in quality. The samples from Chongqing and Hunan demonstrated similar quality, whereas those from Sichuan exhibited relatively lower quality. These samples demonstrated significant abilities in clearing ABTS and DPPH radicals. The relationship between HPLC chromatograms and antioxidant activity, as elucidated by multivariate analysis, indicated that chlorogenic acid, isochlorogenic acid A, isochlorogenic acid B, and isochlorogenic acid C are active components and can serve as Q-markers for quality evaluation.
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Antioxidantes , Lonicera , Cromatografia Líquida de Alta Pressão/métodos , Lonicera/química , Antioxidantes/química , Antioxidantes/farmacologia , Antioxidantes/análise , China , Picratos/química , Picratos/antagonistas & inibidores , Compostos de Bifenilo/antagonistas & inibidores , Compostos de Bifenilo/química , Ácidos Sulfônicos/química , Ácidos Sulfônicos/antagonistas & inibidores , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/normas , Controle de Qualidade , Benzotiazóis/química , Saponinas/química , Saponinas/análise , Extratos VegetaisRESUMO
Previously, we have shown that pyrogallol alleviated nasal symptoms and suppressed IL-9 gene up-regulation in allergy model rats by inhibiting calcineurin/NFAT signaling. As pyrogallol has antioxidative activity, it may be responsible for inhibiting calcineurin/NFAT signaling-mediated IL-9 gene expression. However, the relationship between antioxidative activity and suppression of IL-9 gene expression has not been elucidated yet. Here, we conducted the structure-activity relationship studies of pyrogallol and its structurally related compounds to understand the mechanism of IL-9 gene suppression by pyrogallol. 2, 2-Diphenyl-1-picrylhydrazyl radical scavenging assay showed that the antioxidative activity of catechol, resorcinol, phloroglucinol, and gallic acid is 60.1%, 10.4%, 18.8%, and 113.5% of pyrogallol, respectively. Catechol, resorcinol, and phloroglucinol did not suppress NFAT dephosphorylation. Gallic acid suppressed dephosphorylation of NFAT. Gallic acid also suppressed ionomycin-induced up-regulation of IL-9 gene expression with the IC50 value of 82.6 µM. However, catechol, resorcinol and phloroglucinol showed no suppressive activity. In addition, using gallic acid-immobilized beads, we isolated and identified Poly(U)-binding-splicing factor 60 (PUF60) as a pyrogallol binding protein. These results suggest that the antioxidative activity of pyrogallol is not likely to be the mechanism of IL-9 gene suppression. Data also suggest that PUF60 is one of its target molecules responsible for the suppression of calcineurin/NFAT signaling by pyrogallol.
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Antioxidantes , Calcineurina , Fatores de Transcrição NFATC , Pirogalol , Transdução de Sinais , Pirogalol/farmacologia , Calcineurina/metabolismo , Transdução de Sinais/efeitos dos fármacos , Fatores de Transcrição NFATC/metabolismo , Relação Estrutura-Atividade , Antioxidantes/farmacologia , Humanos , Ácido Gálico/farmacologia , Expressão Gênica/efeitos dos fármacos , Animais , Fosforilação/efeitos dos fármacos , Regulação para Cima/efeitos dos fármacos , RatosRESUMO
Edible bird's nest (EBN) is made up of sialylated-mucin glycoprotein with various health benefits due to its high antioxidative activity. However, as a macromolecule with distinct charged sialic acid and amino acids, fractions with different charges would have varied physicochemical properties and antioxidant activity, which have not been studied. Therefore, this study aimed to fractionate and purify the enzymatic hydrolysed of cleaned EBN (EBNhc) and EBN by-product (EBNhbyp) through anion exchange chromatography (AEC), and determine their molecular weights, physicochemical properties, and antioxidative activities. Overall, 26 fractionates were collected from enzymatic hydrolysate by AEC, which were classified into 5 fractions. It was found that the positively charged fraction of EBNhc (CF 1) and EBNhbyp (DF 1) showed the significantly highest (p < 0.05) soluble protein contents (22.86 and 18.40 mg/g), total peptide contents (511.13 and 800.47 mg/g) and ferric reducing antioxidant power (17.44 and 6.96 mg/g) among the fractionates. In conclusion, a positively charged fraction (CF 1 and DF 1) showed more desired physicochemical properties and antioxidative activities. This research suggests the potential of AEC fractionation as a technology to purify EBN and produce positively charged EBN fractionates with antioxidative potential that could be applied as food components to provide health benefits.
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Antioxidantes , Aves , Glicoproteínas , Animais , Cromatografia por Troca Iônica/métodos , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Glicoproteínas/química , Glicoproteínas/isolamento & purificação , Hidrólise , Peso Molecular , Ácido N-Acetilneuramínico/química , Fracionamento Químico/métodosRESUMO
Pectin, a natural polysaccharide, holds versatile applications in food and pharmaceuticals. However, there is a need for further exploration into extracting novel functional fractions and characterizing them thoroughly. In this study, a sequential extraction approach was used to obtain three distinct lemon pectin (LP) fractions from lemon peels (Citrus Eureka): LP extracted with sodium acetate (LP-SA), LP extracted with ethylenediaminetetraacetic acid (LP-EDTA), and LP extracted with sodium carbonate and sodium borohydride (LP-SS). Comprehensive analysis revealed low methyl-esterification in all fractions. LP-SA and LP-SS displayed characteristics of rhamnogalacturonan-I type pectin, while LP-EDTA mainly consisted of homogalacturonan pectin. Notably, LP-SA formed self-aggregated particles with rough surfaces, LP-EDTA showed interlocking linear structures with smooth planes, and LP-SS exhibited branch chain structures with smooth surfaces. Bioactivity analysis indicated that LP-SA had significant apparent viscosity and ABTS radical scavenging activity, while both LP-EDTA and LP-SS showed excellent thermal stability according to thermogravimetric analysis (TGA). Furthermore, LP-SS exhibited remarkable gel-forming ability and significant hydroxyl free radicals scavenging activity. In conclusion, this study presents a novel method for extracting various lemon pectin fractions with unique structural and bioactive properties, contributing insights for advanced applications in the food and pharmaceutical sectors.
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Antioxidantes , Citrus , Pectinas , Pectinas/química , Pectinas/isolamento & purificação , Citrus/química , Antioxidantes/química , Antioxidantes/farmacologia , Antioxidantes/isolamento & purificação , Fenômenos Químicos , Viscosidade , Frutas/química , Extratos Vegetais/química , Extratos Vegetais/farmacologiaRESUMO
This work presents the design, synthesis and biological activity of novel N-substituted benzimidazole carboxamides bearing either a variable number of methoxy and/or hydroxy groups. The targeted carboxamides were designed to investigate the influence of the number of methoxy and/or hydroxy groups, the type of substituent placed on the N atom of the benzimidazole core and the type of substituent placed on the benzimidazole core on biological activity. The most promising derivatives with pronounced antiproliferative activity proved to be N-methyl-substituted derivatives with hydroxyl and methoxy groups at the phenyl ring and cyano groups on the benzimidazole nuclei with selective activity against the MCF-7 cell line (IC50 = 3.1 µM). In addition, the cyano-substituted derivatives 10 and 11 showed strong antiproliferative activity against the tested cells (IC50 = 1.2-5.3 µM). Several tested compounds showed significantly improved antioxidative activity in all three methods compared to standard BHT. In addition, the antioxidative activity of 9, 10, 32 and 36 in the cells generally confirmed their antioxidant ability demonstrated in vitro. However, their antiproliferative activity was not related to their ability to inhibit oxidative stress nor to their ability to induce it. Compound 8 with two hydroxy and one methoxy group on the phenyl ring showed the strongest antibacterial activity against the Gram-positive strain E. faecalis (MIC = 8 µM).
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Antineoplásicos , Antioxidantes , Benzimidazóis , Proliferação de Células , Desenho de Fármacos , Benzimidazóis/química , Benzimidazóis/farmacologia , Benzimidazóis/síntese química , Humanos , Proliferação de Células/efeitos dos fármacos , Antineoplásicos/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Células MCF-7 , Antioxidantes/farmacologia , Antioxidantes/síntese química , Antioxidantes/química , Relação Estrutura-Atividade , Antibacterianos/farmacologia , Antibacterianos/síntese química , Antibacterianos/química , Amidas/química , Amidas/farmacologia , Amidas/síntese química , Estrutura Molecular , Testes de Sensibilidade Microbiana , Estresse Oxidativo/efeitos dos fármacosRESUMO
The chemical composition of berries and berry pomaces is diverse, containing polyphenolic components that may have both antibacterial and antioxidative properties. In the present study, in vitro antibacterial effect of the extracts of chokeberry, blackcurrant, and rowan berries and berry pomaces against L. monocytogenes, S. aureus, E. coli, and C. jejuni was studied. In addition, the polyphenolic profile and antioxidant activity of these extracts were investigated. The polyphenolic profiles in the aqueous and 30% ethanolic extracts were determined chromatographically by HPLC-MS, and the total polyphenol content was estimated spectrophotometrically by HPLC-DAD-UV. The minimal inhibition concentrations (MICs) of the extracts against tested bacteria were determined by the broth microdilution method. The content of total polyphenols was highest and good antioxidative properties of the extracts were determined for chokeberry and blackcurrant berries and their pomaces. The highest proportions of total quercetin derivatives and anthocyanins were found in the extracts of chokeberry berry/pomace and blackcurrant berry/pomace, respectively. The sensitivity of tested microbes to the extracts of berries and berry pomaces was as follows: S. aureus > L. monocytogenes > E. coli and C. jejuni. In vitro antibacterial activity of tested extracts depended on the extraction solvent, mainly for the ethanolic extracts. Findings suggest that chokeberry and blackcurrant berries and their pomaces can be used as a good source of polyphenols with antioxidative properties, and they also have antibacterial activity against some foodborne pathogenic bacteria. It is important that the valuable compounds are extracted from juice press residues before their disposal.
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Commercial lactic acid bacteria strains and indigenous Chinese acetic acid bacterium were co-cultivated bi- and tri-culturally in Junzao jujube puree for the first time to investigate their effects on physicochemical properties and quality attributes. Lactic-acetic acid bacteria co-fermentation was performed at 37 °C for 48 h during the anaerobic fermentation phase and at 30 °C for 144 h during aerobic fermentation. FTIR results showed that predominant wave numbers at 1716-1724 cm-1 and 2922-3307 cm-1 exhibited discernible alterations in the lactic-acetic acid co-fermented jujube purees compared to the control sample. Pearson correlation analysis showed that the flavonoid and flavonol contents were responsible for the enhanced 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) and 2,2-diphenyl-1-picrylhydrazyl scavenging activities of the fermented jujube purees. Consequently, fermented jujube puree from tricultures of Lactobacillus casei, Lactobacillus plantarum, and Acetobacter pasteurianus gave the best results, with the highest phenolics, flavonoid, and flavonol contents and the most improved antioxidative properties and color. Overall, lactic-acetic acid bacteria co-culture holds significant promise in valorizing Junzao jujube purees for functional ingredient development, paving the way for further research into similar interactions with different food matrices or microbial strains.
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This study compared the proliferation and differentiation potential of bone marrow-derived mesenchymal stem cells (BMSCs) derived from infants with polydactyly and adults with basal joint arthritis. The proliferation rate of adult and infant BMSCs was determined by the cell number changes and doubling times. The γH2AX immunofluorescence staining, age-related gene expression, senescence-associated ß-galactosidase (SA-ß-gal) staining were analyzed to determine the senescence state of adult and infant BMSCs. The expression levels of superoxide dismutases (SODs) and genes associated with various types of differentiation were measured using Real-Time Quantitative Polymerase Chain Reaction (RT-qPCR). Differentiation levels were evaluated through histochemical and immunohistochemical staining. The results showed that infant BMSCs had a significantly higher increase in cell numbers and faster doubling times compared with adult BMSCs. Infant BMSCs at late stages exhibited reduced γH2AX expression and SA-ß-gal staining, indicating lower levels of senescence. The expression levels of senescence-related genes (p16, p21, and p53) in infant BMSCs were also lower than in adult BMSCs. In addition, infant BMSCs demonstrated higher antioxidative ability with elevated expression of SOD1, SOD2, and SOD3 compared with adult BMSCs. In terms of differentiation potential, infant BMSCs outperformed adult BMSCs in chondrogenesis, as indicated by higher expression levels of chondrogenic genes (SOX9, COL2, and COL10) and positive immunohistochemical staining. Moreover, differentiated cells derived from infant BMSCs exhibited significantly higher expression levels of osteogenic, tenogenic, hepatogenic, and neurogenic genes compared with those derived from adult BMSCs. Histochemical and immunofluorescence staining confirmed these findings. However, adult BMSCs showed lower adipogenic differentiation potential compared with infant BMSCs. Overall, infant BMSCs demonstrated superior characteristics, including higher proliferation rates, enhanced antioxidative activity, and greater differentiation potential into various lineages. They also exhibited reduced cellular senescence. These findings, within the context of cellular differentiation, suggest potential implications for the use of allogeneic BMSC transplantation, emphasizing the need for further in vivo investigation.
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Artrite , Células-Tronco Mesenquimais , Polidactilia , Adulto , Criança , Humanos , Medula Óssea , Proliferação de Células , Diferenciação Celular , Osteogênese/genética , Células Cultivadas , Células da Medula Óssea , Artrite/metabolismo , Polidactilia/metabolismoRESUMO
New analogs of the well-known bioactive trihydroxy-stilbene resveratrol were synthesized to investigate their potential biological activity. The focus was on assessing their ability to inhibit cholinesterase enzymes (ChEs) and their antioxidative properties, which were thoroughly examined. New resveratrol analogs were synthesized through Wittig or McMurry reaction in moderate-to-good yields. In all synthetic pathways, mixtures of cis- and trans-isomers were obtained, then separated by chromatography, and trans-isomers were isolated as targeted structures. The stilbene derivatives underwent evaluation for antioxidant activity (AOA) using DPPH and CUPRAC assay, and their potential to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) was also measured. The biological tests have shown that the same compounds exhibited significant antioxidative and butyrylcholinesterase inhibitory potential, as evidenced by lower IC50 values compared to the established standards, trans-resveratrol, and galantamine, respectively. Additionally, molecular docking of the selected synthesized potential inhibitors to the enzyme's active site was performed, followed by assessing the complex stability using molecular dynamics simulation lasting 100 ns. Lastly, the new compounds underwent examination to determine their potential mutagenicity.
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Acetilcolinesterase , Butirilcolinesterase , Butirilcolinesterase/metabolismo , Acetilcolinesterase/metabolismo , Inibidores da Colinesterase/química , Resveratrol/farmacologia , Simulação de Acoplamento Molecular , Relação Estrutura-Atividade , Antioxidantes/farmacologiaRESUMO
Dual-sweeping-frequency ultrasound (DSFU) was utilized in the preparation of polypeptides from housefly (Musca domestica) larvae protein (HLP). Results indicated that ultrasonication (20 ± 2/28 ± 2 kHz, 42 W/L, 25 min) significantly increased peptide yield and DPPH scavenging capacity by 8.25 % and 14.83 %, respectively. Solubility, foaming and emulsification properties of polypeptides were improved by 19.89 %, 33.33 % and 38.74 % over the control; along with notable reduction in particle size and increase in zeta potential. Tertiary structural changes of the sonicated hydrolysates were illustrated by UV and fluorescence spectra. FTIR showed that ultrasonication increased α-helix, ß-turn, and random coil by 38.23 %, 46.35 % and 16.36 %, respectively, but decreased ß-sheet by 48.03 %, indicating partial unfolding in HLP hydrolysate conformation and reduction in intermolecular interactions. The research results demonstrated that dual-sweeping-frequency ultrasonication has a great prospect in industry application for the purpose of improving enzymolysis efficiency and product quality for housefly larvae protein hydrolysates production.
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Antioxidantes , Moscas Domésticas , Animais , Antioxidantes/química , Hidrolisados de Proteína/química , Hidrólise , Larva/química , Peptídeos/metabolismoRESUMO
Selenium nanoparticles (SeNPs) represent novel selenium (Se) formulation characterized by improved biocompatibility and a wider therapeutic range in comparison to inorganic Se. The aim of this work was to investigate the possibilities of functionalization of SeNPs with olive pomace extract (OPE), rich in health-promoting polyphenols, and to obtain innovative forms of nutraceuticals. Cytotoxic and antioxidative activities of four types of SeNPs (polyvinylpyrrolidone stabilized (PVP SeNPs), polysorbate stabilized (PS SeNPs), polyvinylpyrrolidone stabilized and functionalized using OPE (f PVP SeNPs) and polysorbate stabilized and functionalized using OPE (f PS SeNPs) were investigated. SeNPs showed lower toxicity on human hepatocellular carcinoma (HepG2) and human colorectal adenocarcinoma (Caco2) cells compared to selenite. Functionalization with polyphenols significantly improved their direct antiradical (f PVP SeNPs: 24.4 ± 1.84 and f PS SeNPs: 30.9 ± 2.47 mg TE/mmol Se) and reducing properties (f PVP SeNPs: 50 ± 3.16 and f PS SeNPs: 53.6 ± 3.22 mg GAE/mmol) compared to non-functionalized SeNPs. The significant impact of tested SeNPs on intracellular antioxidative mechanisms has been observed and it was dependent on both cell type and physico-chemical properties of SeNPs, indicating the complexity of involved mechanisms.
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Nanopartículas , Olea , Selênio , Humanos , Antioxidantes/farmacologia , Antioxidantes/química , Selênio/química , Células CACO-2 , Polissorbatos , Povidona , Nanopartículas/químicaRESUMO
Natural flavonoids are renowned for their exceptional antioxidant properties, but their limited water solubility hampers their bioavailability. One approach to enhancing their water solubility and antioxidant activity involves the use of cyclodextrin (CD) inclusion. This study investigated the impact of CD inclusion on the three primary radical scavenging mechanisms associated with flavonoid antioxidant activity, utilizing apigenin as a representative flavonoid and employing density functional theory (DFT) calculations. Initially, the optimized geometries of CD-apigenin inclusion complexes were analyzed, revealing the formation of hydrogen bonds between CD and apigenin. In less polar environments, the inclusion complex strengthened the bond dissociation enthalpies of hydroxyl groups, thereby reducing antioxidant activity. Conversely, in polar environments, the inclusion complex had the opposite effect by lowering proton affinity. These findings align with experimental results demonstrating that CD inclusion complexation enhances flavonoid antioxidant activity in aqueous ethanol solutions.
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Although the honey produced by Lespedeza bicolor Turcz. is precious because of its medicinal value, its pharmacological mechanism is still unclear. Here, its anti-inflammatory and antioxidant functions on lipopolysaccharide (LPS)-treated murine RAW 264.7 macrophages were analyzed using targeted and non-targeted metabolomics. Results showed that twelve polyphenols were identified in L. bicolor honey using UHPLC-QQQ-MS/MS. L. bicolor honey extract could scavenge the free radicals DPPH⢠and ABTS+ and reduce Fe3+. Furthermore, pretreatment with L. bicolor honey extract significantly decreased NO production; suppressed the expression of COX-2, IL-10, TNF-α, and iNOS; and upregulated HO-1's expression in the cells with LPS application. UHPLC-Q-TOF-MS/MS-based metabolomics results revealed that L. bicolor honey extract could protect against inflammatory damage caused by LPS through the reduced activation of sphingolipid metabolism and necroptosis pathways. These findings demonstrate that L. bicolor honey possesses excellent antioxidant and anti-inflammatory activities.
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This study investigates the use of encapsulating agents for establishing a synbiotic relationship with Bacillus coagulans (TISTR 1447). Various ratios of wall materials, such as skim milk powder, maltodextrin, and cellulose acetate phthalate (represented as SMC1, SMC3, SMC5, and SMC7), were examined. In all formulations, 5% inulin was included as a prebiotic. The research assessed their impact on cell viability and bioactive properties during both the spray-drying process and in vitro gastrointestinal digestion. The results demonstrate that these encapsulating agents efficiently protect B. coagulans spores during the spray-drying process, resulting in spore viability exceeding 6 log CFU/g. Notably, SMC5 and SMC7 displayed the highest spore viability values. Moreover, SMC5 showcased the most notable antioxidant activity, encompassing DPPH, hydroxy radical, and superoxide radical scavenging, as well as significant antidiabetic effects via the inhibition of α-amylase and α-glucosidase. Furthermore, during the simulated gastrointestinal digestion, both SMC5 and SMC7 exhibited a slight reduction in spore viability over the 6 h simulation. Consequently, SMC5 was identified as the optimal condition for synbiotic production, offering protection to B. coagulans spores during microencapsulation and gastrointestinal digestion while maintaining bioactive properties post-encapsulation. Synbiotic microcapsules containing SMC5 showcased a remarkable positive impact, suggesting its potential as an advanced food delivery system and a functional ingredient for various food products.
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Cirsium japonicum DC. var. australe Kitam. has been used as an herbal remedy and often involves using the whole plant or roots. However, the bioactivities of different parts of the plant have been far less explored. This study aimed to evaluate the antioxidative ability of methanol extracts from the flowers, leaves, stems, and roots of the Cirsium plant and their possible active components against juglone-induced oxidative stress in the nematode Caenorhabditis elegans. The results showed that the highest dry weight (12.3 g per plant) was observed in leaves, which was followed by stems (8.0 g). The methanol extract yields from the flowers, leaves, and roots were all similar (13.0-13.8%), while the yield from stems was the lowest (8.6%). The analysis of the silymarin contents in the extracts indicated that the flowers, leaves, stems, and roots contained silychristin and taxifolin; however, silydianin was only found in the leaves, stems, and roots. The flower, leaf, and stem extracts, at a concentration of 10 mg/L, significantly reduced juglone-induced oxidative stress in C. elegans, which was potentially due to the presence of silychristin and taxifolin. Overall, C. japonicum DC. var. australe Kitam. contains a significant amount of silymarin and exhibits in vivo antioxidative activity, suggesting that the prospects for the plant in terms of health supplements or as a source of silymarin are promising.
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Cirsium , Silimarina , Animais , Caenorhabditis elegans , Flavonoides/farmacologia , Extratos Vegetais/farmacologia , Metanol , Estresse Oxidativo , Antioxidantes/farmacologiaRESUMO
Background & objectives: Impaired high density lipoprotein (HDL) functionality has been shown to be associated with cardiovascular disease risk. The study was aimed to identify the alterations in HDL function [antioxidative activity (AOA)] and subfraction distribution between acute coronary syndrome (ACS) and stable coronary artery disease (SCAD) individuals and analysing the accuracy of HDL parameters to discriminate between the groups. Methods: HDL subfraction distribution analysis was performed in 200 coronary artery disease patients (ACS and SCAD) and 60 control individuals using dextran sulphate, heparin and manganese chloride precipitation method. In terms of HDL function, AOA was evaluated by dihydrorhodamine-based fluorescent cell-free assay and paraoxonase (PON1) enzyme paraoxonase and arylesterase activity. Results: We found that higher AOA [odds ratio (95% confidence interval {CI})]: 0.09 (0.02-0.44), P<0.01 for SCAD; 0.008 (0.001-0.07), P<0.001 for ACS and higher PON1 activity [0.22 (0.8-0.59), P<0.01 for SCAD; 0.16 (0.06-0.4), P<0.001 for ACS] were associated with a lower odds of developing coronary artery disease (CAD). AOA of apoB-depleted serum was significantly correlated with HDL2-C/HDL3-C (HDL-cholesterol) ratio in controls (r=-0.31, P=0.01) and ACS (r=-0.18, P=0.04). It was observed that AOA and HDL subfraction distribution together could discriminate between the two groups of CAD with an accuracy of 72.8 per cent (P=0.004). Interpretation & conclusions: Impaired AOA and altered subfraction distribution of HDL may be responsible for its diminished anti-athero protective activity and can discriminate between the two groups of CAD individuals.
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Doença da Artéria Coronariana , Humanos , Lipoproteínas HDL , Arildialquilfosfatase/genética , HDL-Colesterol , AntioxidantesRESUMO
Bread was prepared using wheat flour with grape seed proanthocyanidin (GSP) (0.4%). GSP improved the textural properties of bread including hardness, cohesiviness, gumminess and chewiness. At the last stage of fermentation, GSP reinforced the gluten microstructure with increased the disulfide bonds and hydrophobic interaction and α-helix in the secondary structures. Moreover, GSP addition could increase the total phenolics and antioxidative acitivity of the bread significantly. In addition, the degree of fermentation had a strong influence on the dough forces, and the reasonable control of bread fermentation time was beneficial to improve the bread quality, which provided a reference for the bread processing industry.