•Antioxidant and anti-inflammatory activities of quercetin derivatives were studied.•Quercetin metabolites present in systemic circulation have potent biopotential.•Derivatization quercetin resulted ...in decrease of antioxidant activity.•Derivatization of quercetin does not significantly defines anti-inflammatory potential.•Metabolites should be included in defining biopotential of quercetin-rich diet.
Quercetin is hardly bioavailable and largely transformed to different metabolites. Although little is known about their biological activities, these metabolites are crucial for explanation of health benefits associated with quercetin dietary intake. In this study, the antioxidant and anti-inflammatory activities of six quercetin derivatives (quercetin-3-O-glucuronide, tamarixetin, isorhamnetin, isorhamnetin-3-O-glucoside, quercetin-3,4′-di-O-glucoside, quercetin-3,5,7,3′,4′-pentamethylether) were compared with the activity of common onion extract as the main source of dietary quercetin and standards (butylated hydroxytoluene and aspirin). The quercetin derivatives demonstrated notable bioactivities, similar to standards and onion. Derivatization of quercetin hydroxyl groups resulted in decrease of antioxidant potency. However, the number of quercetin free hydroxyl groups was not in direct correlation with its potential to inhibit inflammatory mediators production. To conclude, quercetin derivatives present in systemic circulation after consumption of quercetin may act as potent antioxidant and anti-inflammatory agents and can contribute to overall biological activity of quercetin-rich diet.
Ten novel symmetric 3,5-bis(arylidene)-4-piperidone derivatives (BAPs, 1–10) and fourteen dissymmetric BAPs (11–24) were synthesized and evaluated the cytotoxicity. All of the compounds have been ...screened for their anti-inflammatory activity characterized by evaluating their inhibitory effects on LPS-induced IL-6, TNF-α secretion. Among them, BAP 23 exhibits both the highest anti-inflammatory and anti-cancer properties. Western blot analysis showed that BAP 23 markedly reduced the levels of Bcl-2 but increased the levels of cleaved caspase-3and Bax. Moreover, BAP 23 prominently inhibited LPS-induced activation of NF-κB in RAW264.7 cells as well as TNF-α-induced activation of NF-κB in HepG2 cells by blocking phosphorylation of inhibitor IκBα and p65. Consistent with these results, we found that BAP 23 prevented the nuclear translocation of NF-κB induced by LPS or TNF-α. BAP 23 could reasonably bind to the active site of Bcl-2 protein and p65 which is proved by molecular docking modes. These data indicate that BAP 23 is a more potent inhibitor of NF-κB activity which exhibites both anti-inflammatory and anticancer activities.
Twenty four novel symmetric or dissymmetric 3,5-bis(arylidene)-4-piperidone derivatives (BAPs) were synthesized. Their cytotoxicity and anti-inflammatory activity were evaluated and BAP 23 could inhibit NF-κB activation both in inflammation and cancer. Display omitted
•Novel symmetric or dissymmetric 3,5-bis(arylidene)-4-piperidones (BAPs) (1–24) were generated and characterized.•23 exhibits both highest anti-inflammatory and anti-cancer properties, and lower cytotoxicity.•23 can promote cell apoptosis by up-regulating cleaved Caspase-3, BAX expression and down-regulating Bcl-2expression.•23 inhibited activation of NF-κB in RAW264.7 cells and HepG2 cells by blocking phosphorylation of inhibitor IκBα and p65.
The aim of this study was to determine the effect of heat treatment of edible insects on antioxidant and anti‐inflammatory activities of peptide fractions from hydrolysates obtained by in vitro ...gastrointestinal digestion thereof. Identification of bioactive peptides from the edible insects and their chemical synthesis were carried out as well. The highest antiradical activity against ABTS•+ and DPPH• was noted for the peptide fraction from the Gryllodes sigillatus protein preparation (EC50 value 2.75 and 6.91 μg mL−1, respectively). This fraction exhibited the strongest LOX and COX‐2 inhibitory activity (IC50 value 0.13 and 0.26 μg mL−1, respectively). The peptide fraction from the Tenebrio molitor protein preparation showed the highest Fe2+ chelating ability (EC50 value 2.21 μg mL−1) and the highest reducing power (0.198). The heat treatment process has a positive effect on the antioxidant and anti‐inflammatory properties of peptides. All identified and synthesised peptides from insect protein showed antioxidant and anti‐inflammatory activity.
The methodology of the study for the antioxidant and anti‐inflammatory activities of peptides obtained from edible insects proteins after in vitro digestion. Identified peptides in peptide fractions obtained after hydrolysis.
•An acidic polysaccharide was isolated from the lignified okra.•The structural characterization of the lignified okra was analyzed and identified.•AP1-b possessed immune-enhancing activities on ...RAW264.7 macrophages.•AP1-b showed stronger in vitro anti-inflammatory activity via nuclear factor kappa-B signaling pathway.
The polysaccharide (AP1-b) of molecular weight 6.59 × 105 Da was isolated from lignified okra (Abelmoschus esculentus (L.) Moench) by hot-water extraction, 40 % ethanol precipitation and purified by DEAE Cellulose chromatography, respectively. The structure and anti-inflammatory activity of AP1-b were investigated. AP1-b was composed of galactose, rhamnose, gluctose, arabinose and galacturonic acid in a molar ratio of 1.98:1.00:0.15:0.32:0.29. The structural features showed that the AP1-b consisted of →2)-α-d-Rhap-(1→, →4)-β-d-Galp-(1→, →4)-α-d-GalpA-(1→, →6)-β-d-Galp-(1→, β-d-Glcp-(1→ and α-l-Araf-(1→. AP1-b could observably improve the inflammatory injury of LPS-induced RAW 264.7 cells by inhibiting the secretion of NO and decreasing the levels of pro-inflammatory factors (IL-1β, iNOS and TNF-α). AP1-b also inhibited the phosphorylation levels of IκB and p65 proteins, manifesting the anti-inflammatory activity of AP1-b may associated with inhibition of NF-κB signaling pathway. Therefore, AP1-b had potential value in treating inflammatory injury.
Microbial fermentation is often used to improve the functionality of plant-based food materials. Herein, we investigated changes in the physicochemical and functional properties of cabbage during ...yeast fermentation to develop new products using fermented cabbage. Among the 8 types of food-grade yeast, both Saccharomyces cerevisiae and Saccharomyces boulardii fermented 10% cabbage powder solution (w/w) the most effectively, leaving no soluble sugars after 12 h of fermentation. In addition, the yeast fermentation of cabbage resulted in functionally positive outcomes in terms of sulforaphane content, antioxidant properties, and anti-inflammatory activity. Specifically, the yeast-fermented cabbages contained about 500% more sulforaphane. The soluble fraction (5 μg/ml) of yeast-fermented cabbage had no cytotoxicity in murine RAW 264.7 cells, and the radicalscavenging capacity was equivalent to 1 μg/ml of ascorbic acid. Moreover, cabbage fermented with S. boulardii significantly suppressed both lipopolysaccharides (LPS)-induced nitric oxide production and LPS-induced reactive oxygen species production in RAW 264.7 cells, suggesting a potential antiinflammatory effect. These results support the idea that yeast fermentation is promising for developing functionally improved cabbage products.
In this study, β-1,3-xylanase (Xyl3088) was designed and prepared by constructing the expression vector plasmid and expressing and purifying the fusion protein. β-1,3-xylo-oligosaccharides were ...obtained through the specific enzymatic degradation of β-1, 3-xylan from Caulerpa lentillifera. The enzymolysis conditions were established and optimized as follows: Tris-HCl solution 0.05 mol/L, temperature of 37 °C, enzyme amount of 250 μL, and enzymolysis time of 24 h. The oligosaccharides' compositions and structural characterization were identified by thin-layer chromatography (TLC), ion chromatography (IC) and liquid chromatography electrospray ionization tandem mass spectrometry (LC-ESI-MS). The IC50 values for scavenging 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2-azino-bis-3-ethyl-benzothiazoline-p-sulfonic acid (ABTS+), and superoxide anion radical (•O2−) were 13.108, 1.258, and 65.926 mg/mL for β-1,3-xylo-oligosaccharides, respectively, and 27.588, 373.048, and 269.12 mg/mL for β-1,4-xylo-oligosaccharides, respectively. Compared with β-1,4-xylo-oligosaccharides, β-1,3-xylo-oligosaccharides had substantial antioxidant activity and their antioxidant effects were concentration dependent. β-1,3-xylo-oligosaccharides also possessed a stronger anti-inflammatory effect on RAW 264.7 cells stimulated by lipopolysaccharide (LPS) than β-1,4-xylo-oligosaccharides. At a working concentration of 100 μg/mL, β-1,3-xylo-oligosaccharides inhibited the release of NO and affected the expression of IL-1β, TNF-α, and other proteins secreted by cells, effectively promoting the release of pro-inflammatory mediators by immune cells in response to external stimuli and achieving anti-inflammatory effects. Therefore, β-1,3-xylo-oligosaccharides are valuable products in food and pharmaceutical industries.
Inflammatory diseases have a high prevalence and has become of great interest due to the increase in life expectancy and the costs to the health care system worldwide. Chronic diseases require ...long-term treatment frequently using corticosteroids and non-steroidal anti-inflammatory drugs, which are associated with diverse side effects and risk of toxicity. Betulinic acid, a lupane-type pentacyclic triterpene, is a potential lead compound for the development of new anti-inflammatory treatments, and a large number of derivatives have been produced and tested. The potential of betulinic acid and its derivatives has been shown in a number of pre-clinical studies using different experimental models. Moreover, several molecular mechanisms of action have also been described. Here we reviewed the potential use of betulinic acid as a promissory lead compound with anti-inflammatory activity and the perspectives for its use in the treatment of inflammatory conditions.
Active edible films were prepared consisting of tea polyphenols incorporated within thin calcium alginate gels. These films were prepared by plating an alginate solution, air drying (50 °C), and then ...cross-linking with calcium. In this study, the effects of tea polyphenol incorporation (1–5% w/w) on the physicochemical, morphological, and antioxidant properties of the films were evaluated. The tensile strength, breaking strain, and water vapor permeability of the films increased as the tea polyphenol level increased, whereas the optical transmittance as measured by UV–visible spectrometer decreased. Fourier transform infrared spectroscopy indicated that various types of intermolecular interactions occurred between the alginate and tea polyphenols. Scanning electron microscopy showed that the films had smooth surfaces with dense internal structures. The antioxidant capacity of the films, as determined by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzthiozoline-6)-sulphonic acid (ABTS) radical analysis, and the anti-inflammatory properties were enhanced by incorporating tea polyphenols into them. Overall, this study showed that the functional properties of active edible films can be enhanced by introducing tea polyphenols, which may lead to new applications of these films for food packaging applications.
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•Active edible films were prepared consisting of tea polyphenols incorporated into thin alginate gels.•The alginate-polyphenol films had better mechanical and physical properties.•The antioxidant and anti-inflammatory properties were enhanced by incorporating tea polyphenols.•The functional properties of active edible films can be enhanced by introducing tea polyphenols.
Cinnamic acids are aromatic acids primarily found in plants and plant-derived food. Phenolic cinnamic acids, with one or more hydroxyl groups in the aromatic ring, often contribute to the biological ...activities attributed to these compounds. The presence of hydroxyl groups and a carboxyl group makes cinnamic acids very hydrophilic, preventing them from crossing biological membranes and exerting their biological activities. To alleviate this condition, a panel of synthetic modifications have been made leading to a diverse set of phenolic cinnamic structures. In this review, an overview of the natural phenolic cinnamic acid derivatives and their plant sources (more than 200) is described. The synthetic approaches to obtain the referred derivatives (more than 200) namely esters and amides are reviewed. Further, their anti-inflammatory activity (more than 70 compounds) is scrutinized. Finally, future directions will be indicated to translate the research on phenolic cinnamic derivatives into potentially effective anti-inflammatory drugs.
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•Cinnamic acid derivatives are primarily found in plants and plant-derived food•Cinnamic acid derivatives can be synthesized to improve their biological activities•Phenolic cinnamic derivatives studied were esters and amides•Natural and synthetic phenolic cinnamic derivatives show anti-inflammatory activity•Ferulic acid demonstrating promising results in a clinical study
Honeydew honey has differentiated chemical and physicochemical characteristics besides potential functional properties such as antimicrobial, anti-inflammatory and antioxidant. In this sense, the ...interest and consumption of this honey as a functional product by the food industry and consumers have increased. Honeydew honeys usually present dark color, a lower content of monosaccharides and higher values of pH, acidity, electric conductivity, proteins, minerals, phenolic compounds, and oligosaccharides compared to blossom honeys, which contribute to its outstanding biological activities. Consequently, contaminations and adulterations of this honey can occur and compromise the quality, safety and authenticity of honeydew honey. Thus, detailed knowledge of the composition and properties of honeydew honeys is of great importance, especially considering that honeydew honeys are still few studied and therefore underestimated. Therefore, in this review, the physicochemical characteristics, chemical and bioactive composition, functional and health-promoting properties of honeydew honey as well as contamination, adulteration and authenticity of this honey are summarized.
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•Honeydew honey (HH) has antioxidant, antimicrobial, and anti-inflammatory potential.•Benzoic, protocatechuic, p-coumaric, salicylic acids, and rutin were abundant in HH.•Proline, phenylalanine, and glutamic acid were reported as the major amino acid.•High content of melezitose, raffinose, and citric acid are commonly found in HH.•Physicochemical parameters and individual compounds have been studied for authenticity.
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