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The plants Bauhinia rufescens, Ocimum basilicum and Salvadora persica are well known in traditional African medicine, and particularly in traditional Chadian medicine. They are commonly used to treat infectious diseases, inflammatory diseases, fevers, gastroenteritis and other medical conditions. The aim of this study was to perform a phytochemical screening to determine the antioxidant properties of different extracts and fractions from the three plants. Ethanolic extracts and solvent fractions were prepared and analyzed for total phenolic content (TPC), total flavonoid content (TFC) and total tannin content (TTC). LC-MS and an online screening HPLC-ABTS system identified phytochemicals with antioxidant activities. DPPH and ABTS reduction methods were used to test the extracts and fractions for their antioxidant potential. The results showed that the TPC of O. basilicum was higher than that of B. rufescens, ranging from 64.70 ± 5.2 to 411.16 ± 8.11 mgGAE/g DW. B. rufescens extracts and fractions, on the other hand, showed higher TFC, ranging from 69.5 ± 5.3 to 408.26 ± 8.42 mgQE/g DW, and higher TTC, ranging from 4.57 ± 2.45 to 62.19 ± 4.7 mgTAE/g DW. The maximum TPC, TFC and TTC in both plants were recorded in the ethyl acetate fractions. S. persica extracts and fractions showed a very low quantity of TPC, TFC and TTC. Based on LC-MS and HPLC-ABTS analysis, rosmarinic acid was identified as the major component in the extracts and all fractions of O. basilicum, and epicatechin, procyanidin B and quercetin were found in B. rufescens. S. persica did not exhibit specific substances with antioxidant activity and was therefore not considered for further assays. DPPH and ABTS results showed that ethyl acetate fractions of B. rufescens and O. basilicum have the strongest antioxidant activities. This study indicates that B. rufescens and O. basilicum are good sources of phytochemicals with antioxidant properties, suitable for medicinal use in Chadian communities. Additionally, the antioxidant-rich extracts from these plants hold significant potential for cosmetic development, enhancing skin health and protecting against oxidative-stress-induced damage. [ABSTRACT FROM AUTHOR]

Anthocyanins are bioactive compounds responsible for various physiological processes in plants and provide characteristic colors to fruits and flowers. Their biosynthetic pathway is well understood; however, the enzymatic degradation mechanism is less explored. Anthocyanase (β-glucosidase (BGL)), peroxidase (POD), and polyphenol oxidase (PPO) are enzymes involved in degrading anthocyanins in plants such as petunias, eggplants, and Sicilian oranges. The aim of this work was to investigate the physicochemical interactions between these enzymes and the identified anthocyanins (via UPLC-MS/MS) in cranberry (Vaccinium macrocarpon) through molecular docking to identify the residues likely involved in anthocyanin degradation. Three-dimensional models were constructed using the AlphaFold2 server based on consensus sequences specific to each enzyme. The models with the highest confidence scores (pLDDT) were selected, with BGL, POD, and PPO achieving scores of 87.6, 94.8, and 84.1, respectively. These models were then refined using molecular dynamics for 100 ns. Additionally, UPLC-MS/MS analysis identified various flavonoids in cranberries, including cyanidin, delphinidin, procyanidin B2 and B4, petunidin, pelargonidin, peonidin, and malvidin, providing important experimental data to support the study. Molecular docking simulations revealed the most stable interactions between anthocyanase and the anthocyanins cyanidin 3-arabinoside and cyanidin 3-glucoside, with a favorable ΔG of interaction between −9.3 and −9.2 kcal/mol. This study contributes to proposing a degradation mechanism and seeking inhibitors to prevent fruit discoloration. [ABSTRACT FROM AUTHOR]

Resistance developed by cancer cell lines to conventional chemotherapeutics has a substantial impact on cancer management. The current predicament drives the ongoing search for efficacious new drugs, that have novel molecular routes, and, most critically, can withstand drug resistance acquired by cell lines. Herbal medicines have gained increasing attention as a prolific source of effective anticancer agents, among other properties. Uapaca togoensis (Euphorbiaceae) is used to treat a wide range of ailments in folk medicine. The plant is found as one of worth bioactive sources of anticancer botanicals, with demonstrated efficacy on sensitive and recalcitrant human cancer cell lines, acting through diverse mechanisms of action. The methanolic extract from the fruits of the plant was reported as having an excellent antiproliferative effect, with arborinine reported as its most active cytotoxic constituent against multidrug-resistant (MDR) cell lines. Other promising anticancer constituents of U. togoensis are futokadsurin B, procyanidin, amentoflavone, pyrogallol, vitexin, orientin, and luteolin. Diverse modes of action have been ascribed to the crude extracts and phytoconstituents identified, the ability to induce apoptosis, block cell cycle, target metastatic cell signaling pathways, and gene expression in cancer cells. The reports potentially pave the way for new anticancer treatments based on U. togoensis. The derived phytochemicals, anticancer activities, and cytotoxic modes of action of U. togoensis are comprehensively reviewed in this chapter, with an emphasis on refractory cell lines. [ABSTRACT FROM AUTHOR]

Alcoholic liver disease (ALD) is regarded as one of the main global health problems. Accumulated evidence indicates that fruit-derived polyphenols can lower the risk of ALD, this attributed to their strong antioxidant capacities. Thinned immature kiwifruits (TIK) are the major agro-byproducts in the production of kiwifruits, which have abundantly valuable polyphenols. However, knowledge about the protective effects of polyphenol-enriched extract from TIK against ALD is still lacking, which ultimately restricts their application as value-added functional products. To promote their potential applications, phenolic compounds from TIK and their corresponding mature fruits were compared, and their protective effects against ALD were studied in the present study. The findings revealed that TIK possessed extremely high levels of total phenolics (116.39 ± 1.51 mg GAE/g DW) and total flavonoids (33.88 ± 0.59 mg RE/g DW), which were about 7.4 times and 4.8 times greater than those of their corresponding mature fruits, respectively. Furthermore, the level of major phenolic components in TIK was measured to be 29,558.19 ± 1170.58 μg/g DW, which was about 5.4 times greater than that of mature fruits. In particular, neochlorogenic acid, epicatechin, procyanidin B1, and procyanidin B2 were found as the predominant polyphenols in TIK. In addition, TIK exerted stronger in vitro antioxidant and anti-inflammatory effects than those of mature fruits, which was probably because of their higher levels of polyphenols. Most importantly, compared with mature fruits, TIK exhibited superior hepatoprotective effects on alcohol-induced liver damage in mice. The administration of polyphenol-enriched extract from TIK (YK) could increase the body weight of mice, reduce the serum levels of ALP, AST, and ALT, lower the levels of hepatic TG and TC, and diminish lipid droplet accumulation and hepatic tissue damage. In addition, the treatment of YK could also significantly restore the levels of antioxidant enzymes (e.g., SOD and CAT) in the liver and lower the levels of hepatic proinflammatory cytokines (e.g., IL-6, IL-1β, and TNF-α), indicating that YK could effectively ameliorate ALD in mice by reducing hepatic oxidative stress and hepatic inflammation. Collectively, our findings can provide sufficient evidence for the development of TIK and their extracts as high value-added functional products for the intervention of ALD. [ABSTRACT FROM AUTHOR]

Using “Lianjiu No.1”, “Yuntaihongjiu” and “Yuntaijinjiu” as research objects, the anthocyanin components and content of their leaves before and after color transformation were qualitatively and quantitatively analyzed using ultra-high performance liquid chromatographymass spectrometry technology.The results showed that a total of 14 anthocyanins were detected in leaves from three varieties, including malvidin, pelargonidin, delphinidin, peonidin, cyanidin 3-galactoside, isorhamnetin, cyanidin, cyanidin 3, 5-diglucoside, petunidin, quercetin, rutin, procyanidin B4, procyanidin B2 and kaempferol. Cyanidin 3-galactoside and rutin were the main anthocyanin components of three varieties. The cyanidin 3-galactoside was the main pigment component for the red colored leaves of “Yuntaihongjiu”; rutin was the main reason for the yellow colored leaves of “Yuntaijinjiu”. The main anthocyanins types in three varieties were rutins, cyanidins and others. After the color change of leaves, the content of cyanidins from high to low was in order of “Lianjiu No.1” > ”Yuntaihongjiu” > ”Yuntaijinjiu”. After the color change of leaves, the content of rutins from hight to low was in order of “Yuntaijinjiu” > “Lianjiu No.1” > “Yuntaihongjiu”. [ABSTRACT FROM AUTHOR]

AbstractProcyanidins (PCs) have emerged as agents with potential antimicrobial and antibiofilm activities, although their mechanisms of action and structure–activity relationships remain poorly understood. This review assessed the potential mechanisms of action and applications of these compounds to explore these aspects. Studies on the antimicrobial properties of PCs suggest that they are involved in osmotic imbalance, DNA interactions and metabolic disruption. Although less studied, their antibiofilm activities include antiadhesive effects and the modulation of mobility and quorum sensing. However, most research has used uncharacterized plant extracts for in vitro assays, limiting the understanding of the structure–activity relationships of PCs and their in vivo mechanisms. Clinical trials on the antimicrobial and antibiofilm properties of PCs have not clarified these issues due to nonstandardized methodologies, inadequate chemical characterization, and the limited number of studies, preventing a consensus and evaluation of the in vivo effects. Additionally, patent analysis revealed that technological developments in the antimicrobial and antibiofilm uses of PCs are concentrated in health care and dental care, but new biotechnological uses are emerging. Therefore, while PCs are promising antimicrobial and antibiofilm compounds, further research into their chemical structures and mechanisms of action is crucial for evidence-based applications in biotechnology and health care. [ABSTRACT FROM AUTHOR]

The peel represents a significant portion of the araticum fruit (about 40%), which becomes waste after its consumption or processing. Previous studies have shown that the araticum peel is rich in phenolic compounds; however, little is known about the ideal conditions for recovering these compounds. Therefore, response surface methodology, using a central composite rotatable design, was employed to optimize the extraction process to maximize the total phenolic compounds (TPCs) and enhance the Trolox equivalent antioxidant capacity (TEAC) from araticum peel. The variables optimized were ethanol concentration (EC; 20–80%, v/v), extraction time (ET; 5–45 min), and solid–solvent ratio (SSR; 10–100 mg/mL). Additionally, condensed tannins, antioxidant capacity against synthetic free radicals (TEAC and FRAP) and reactive oxygen species (ROS), and the phenolic compounds profile, were evaluated. Optimum extraction conditions were 50% (v/v) ethanol concentration, 5 min of extraction time, and 10 mg/mL solid–solvent ratio. Under these conditions, experimental TPCs and TEAC values were 70.16 mg GAE/g dw and 667.22 µmol TE/g dw, respectively, comparable with predicted models (68.47 mg GAE/g dw for TPCs and 677.04 µmol TE/g dw for TEAC). A high condensed tannins content (76.49 mg CE/g dw) was also observed and 12 phenolic compounds were identified, predominantly flavonoids (97.77%), including procyanidin B2, epicatechin, and catechin as the major compounds. Moreover, a potent antioxidant activity was observed against synthetic free radicals and ROS, especially in scavenging peroxyl and hydroxyl radicals. From this study, we obtained the ideal conditions for recovering phenolic compounds from araticum peel using a simple, fast, sustainable, and effective method, offering a promising opportunity for the management of this plant byproduct. [ABSTRACT FROM AUTHOR]

Discarded unripe kiwifruits (DUKs) are regarded as the major agro-byproducts in the production of kiwifruits, which have abundantly valuable secondary metabolites. Nevertheless, owing to the limited knowledge about the differences in phytochemicals and bioactivity between DUKs and mature kiwifruits, the utilization of DUKs in the food industry remains scarce. Hence, to promote their food applications, the phenolic compounds and bioactivity of discarded unripe, mature, and overripe fruits from three red-fleshed kiwifruit cultivars were studied and compared. The results revealed that the levels of total phenolics, total flavonoids, and total procyanidins in kiwifruits varied significantly by maturity stage. In addition, our findings demonstrated that DUKs possessed much higher contents of valuable phenolic compounds (e.g., chlorogenic acid (CHA), neochlorogenic acid (NCHA), gallic acid (GA), protocatechuic acid (PA), procyanidin B1 (ProcB1), procyanidin B2 (ProcB2), procyanidin C1 (ProcC1), quercetin 3-O-glucoside (QueG), and quercetin 3-O-rhamnoside (QueR)) than mature and overripe kiwifruits. Furthermore, DUKs exerted much stronger in vitro antioxidant capacity, inhibitory effects on α-glucosidase, and anti-inflammatory activity than mature and overripe kiwifruits, which were mainly attributed to their higher contents of total polyphenols and individual phenolic components, such as GA, CHA, NCHA, PA, ProcB1, ProcB2, ProcC1, and QueR. Overall, these findings provide sufficient evidence for the development and utilization of DUKs in the food/functional food industry. [ABSTRACT FROM AUTHOR]

Green deep eutectic solvents (DESs) are widely used to extract bioactive components from plant biomass; however, hydrophilic DES and bioactive component isolation methods have not been developed. In this study, we synthesized hydrophilic DES (CL‐CA‐DES) using citric acid and choline chloride. We combined this with environmentally friendly anion‐ and cation‐exchange resin column chromatographic isolation methods. This approach extracted and isolated four polyphenolic compounds (catechins, epicatechins, procyanidin B1, and procyanidin B2) from raspberry root and efficiently recovered the hydrophilic DES. CL‐CA‐DES extracted significantly higher contents of catechin and procyanidin B2 from raspberry root compared to other solvents. It also extracted substantially higher contents of epicatechin compared to butyl alcohol, 70% ethanol, and water, but there was no significant difference when compared with acetone and ethyl acetate. Additionally, CL‐CA‐DES extracted significantly higher contents of procyanidin B1 compared to butyl alcohol, water, and ethyl acetate, with no significant difference when compared with 70% ethanol and acetone. The isolation efficiency of the bioactive components in the raspberry root extract by anion‐ and cation‐exchange resin column chromatography was higher than that of the organic solvent extraction and precipitation generation methods, and the method was effective in recovering CL‐CA‐DES with a recovery rate higher than 60%. In conclusion, this study developed a new method for the efficient recovery of hydrophilic CL‐CA‐DES, which can be used for isolating polyphenolic compounds from raspberry root. [ABSTRACT FROM AUTHOR]

Objective: The aim of this study was to assess the ability of polyphenolic extracts from different kiwifruit genotypes to affect tyrosinase enzyme activity and determine potential relationships between tyrosinase inhibition and polyphenolic composition. To date, research on the tyrosinase inhibitory bioactivity of kiwifruit have focused on a single A. chinensis cultivar. Given the numerous genotypes of kiwifruit commercially grown have varying compositions, and a variety of polyphenolic compounds present within each of these cultivars, the full potential of the tyrosinase inhibitory of kiwifruit has not been fully evaluated. Methods: The polyphenolic composition of ethanol extracts from the cortical flesh of 10 kiwifruit genotypes was characterized using high-resolution accurate mass liquid chromatography mass spectrometry. The tyrosinase activity of each extract was measured spectrophotometrically in vitro. Multivariate analysis was subsequently conducted to identify kiwifruit compounds that may correlate with tyrosinase enzyme inhibition. Results: The kiwifruit extracts displayed a broad range of tyrosinase inhibitory activity with some extracts having minimal or no inhibitory effect while the most potent extract showed 33.54 ± 1.59% inhibition (P < 0.01) at a dose of 125 µg/mL. Multivariate analysis of polyphenolic and tyrosinase inhibition data identified that polymeric procyanidins likely explain the tyrosinase inhibitory ability and the differences between genotypes. This was confirmed by the high relative concentrations of these procyanidins in extracts that exhibited tyrosinase inhibitory properties, while being absent or at low concentrations in extracts that did not. Conclusion: Our findings demonstrate that some polyphenol kiwifruit extracts inhibit tyrosinase activity. The variability in the tyrosinase inhibitory activity of polyphenol extracts from 10 kiwifruit genotypes is attributed to the differences in the relative concentrations of polymeric procyanidins in these extracts. These results highlight that the tyrosinase inhibitory properties of kiwifruit genotypes could be examined further to support the development of kiwifruit-based cosmetic products. [ABSTRACT FROM AUTHOR]

Copyright of Science & Technology of Food Industry is the property of Science & Technology of Food Industry Editorial Office and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

In grape (Vitis vinifera L.) cultivation, high temperatures (HTs) usually reduce the accumulation of anthocyanins. In order to elucidate the regulatory mechanism of anthocyanin biosynthesis under high-temperature environments, we investigated the effects of HT stress at veraison (5% coloring of grape ears) on fruit coloration and anthocyanin biosynthesis in 'Summer Black' (XH) and 'Flame seedless' (FL) grapevines. Compared to the control group (35 °C), the total anthocyanin content of XH and FL grapes subjected to a high-temperature (HT) treatment group (40 °C) decreased significantly as the HT treatment continued, but showed an upward trend with fruit development. However, the concentration of procyanidins increased significantly following HT treatment but decreased with fruit development. Nonetheless, FL grapes showed some resistance to the HT condition, producing anthocyanin content at ripeness comparable to the control group, demonstrating a greater adaptability to HT conditions than XH grapes. Based on the CIRG index, at stage S4, the fruit of FL was classified as dark red, while XH was classified as blue-black in the control group. Anthocyanin-targeted metabonomics identified eight different types of anthocyanins accumulating in the peels of XH and FL grapes during ripening, including cyanidins, delphinidins, malvidins, pelargonidins, peonidins, petunidins, procyanidins, and flavonoids. Malvidins were the most abundant in the two grape varieties, with malvidin-3-O-glucoside being more sensitive to high temperatures. HT treatment also down-regulated the expression of structural genes and regulators involved in the anthocyanin synthesis pathways. We used the WGCNA method to identify two modules that were significantly correlated with total anthocyanin and procyanidin contents. Among them, MYBCS1, bHLH137, WRKY65, WRKY75, MYB113-like, bZIP44, and GST3 were predicted to be involved in grape anthocyanin biosynthesis. In conclusion, this study conducted in-depth research on the HT inhibition of the biosynthesis of anthocyanins in XH and FL grapes, for reference. [ABSTRACT FROM AUTHOR]

Pomace is a by-product resulting from the pressing of fruits and vegetables into juices, and it is typically treated as waste. Interestingly, pomace contains minimal amounts of protein and fat but is characterized by its high polyphenol and dietary fiber contents, which may have health benefits for human physiology. Therefore, they are a potentially attractive raw material for the food industry, but to our knowledge, no smoothies with their addition have been prepared and described so far. Consequently, products derived from apple juice, incorporating different doses of fresh (6% and 12%) and dried (3% and 6%) black or red currant pomace, were formulated, and their physical properties, chemical composition, bioactive compound content, and health-promoting potential (in vitro antioxidant and antidiabetic activity) were evaluated. Additionally, the products underwent sensory assessment by consumers. The fortified beverages exhibited different physical characteristics and chemical compositions than apple juice. All smoothies were characterized by higher concentrations of anthocyanins, flavonols, and procyanidin polymers compared to the base product. Moreover, 75% of them exhibited a significantly elevated phenolic acid content as well as a higher concentration of flavan-3-ols. The majority of fresh smoothies exhibited significantly higher in vitro antioxidant capacities and increased in vitro α-amylase and α-glucosidase inhibitory effects compared to the base product. The highest ABTS activity was recorded in the variant with 6% dried black currant pomace. In turn, the smoothie with 3% dried red currant pomace had the most effective FRAP effect and, together with the product containing 12% fresh black currant pomace, ORAC antioxidant activity and α-glucosidase inhibition also. The introduction of 6% dried red currant pomace led to the creation of a beverage that most effectively inhibited α-glucosidase. The study showed that the application of various types of pomace, mainly that of black currant, into apple juice enables the development of new functional products with sensory attributes that are favorably evaluated by consumers. [ABSTRACT FROM AUTHOR]

Hawthorn seeds are a by-product of fruit processing and due to the scale of processing of this raw material, they can be an important source of bioactive compounds. This work is the first report on the phenolic composition of hawthorn seeds and their antioxidant, anti-inflammatory, antidiabetic, antiobesity and anticancer activities. In the isolated phenolic fraction of six seed species, 23 phenolic compounds were identified using the UPLC-ESI-TQD-MS/MS method, the key ones of which included the B-type procyanidin dimer. The seeds of the tested species showed high antioxidant activity (mainly by scavenging O2•− and OH• radicals), anti-inflammatory (mainly through LOX inhibition), anti-diabetic, anti-obesity and anti-cancer, with the highest activity against colon cancer cells (Dld-1 line), showing no activity against healthy colon epithelial cells (CCD841CoN). This activity was significantly dependent on the analyzed hawthorn species and, according to PCA analysis, on the content of flavan-3-ols. These discoveries provided the theoretical basis for the possibility of industrial use of hawthorn seeds. [ABSTRACT FROM AUTHOR]

Background: Neolamarckia cadamba (Rubiaceae) is a well-recognized medicinal plant with recorded therapeutical attributes. However, a thorough assessment of active compounds in its fruits is lacking, limiting their use and valorization in pharmacological industries. Methods: Thus, this study investigated variations in the fruits' secondary metabolite (SM) profiles, as well as antioxidant activities in aqueous (WA) and ethanol (ET) extracts. Results: Liquid chromatography–electrospray ionization tandem mass spectrometry identified 541 SMs, of which 14 and 1 (di-O-glucosylquinic acid) were specifically detected in ET and WA, respectively. Phenolic acids (36.97%), flavonoids (28.10%), terpenoids (12.20%), and alkaloids (9.98%) were the dominant SMs. The SM profiles of the fruits in WA and ET were quite different. We revealed 198 differentially extracted (DE) metabolites between WA and ET, including 62 flavonoids, 57 phenolic acids, 45 terpenoids, 14 alkaloids, etc. Most DE flavones (36 out of 40), terpenoids (45 out of 45), and alkaloids (12 out of 14) had higher content in ET. Catechin and its derivatives, procyanidins, and tannins had higher content in WA. ABTS and DPPH assays showed that the antioxidant activity of ET was significantly higher than that of WA. Conclusions: Our findings will facilitate the efficient extraction and evaluation of specific active compounds in N. cadamba. [ABSTRACT FROM AUTHOR]

The Japanese plum tree (Prunus salicina Lindl.) is mainly cultivated in temperate areas of China and some European countries. Certain amounts of wood (from pruning works) are generated every year from this crop of worldwide commercial significance. The main objective of this work was to value this agricultural woody residue, for which the chemical composition of pruning wood extracts from six Japanese plum cultivars was investigated, and the antiproliferative activity of extracts and pure phenolics present in those extracts was measured. For the chemical characterization, total phenolic content and DPPH radical-scavenging assays and HPLC‒DAD/ESI‒MS analyses were performed, with the procyanidin (−)-ent-epicatechin-(2α→O→7,4α→8)-epicatechin (5) and the propelargonidin (+)-epiafzelechin-(2β→O→7,4β→8)-epicatechin (7) being the major components of the wood extracts. Some quantitative differences were found among plum cultivars, and the content of proanthocyanidins ranged from 1.50 (cv. 'Fortune') to 4.44 (cv. 'Showtime') mg/g of dry wood. Regarding the antitumoral activity, eight wood extracts and four phenolic compounds were evaluated in MCF-7 cells after 48 h of induction, showing the wood extract from cv. 'Songold' and (‒)-annphenone (3), the best antiproliferative activity (IC50: 424 μg/mL and 405 μg/mL, respectively). [ABSTRACT FROM AUTHOR]

Some tannin-rich plants such as Combretum mucronatum and Phyllanthus urinaria are widely used in Africa for the control of parasitic nematodes in both humans and livestock. Tannins have been recognized as an alternative source of anthelmintic therapies, and hence, recent studies have focused on both the hydrolyzable and condensed tannins. These groups of compounds, however, have poor oral bioavailability and are metabolized by gut microbiota into lower molecular weight compounds. The role of these metabolites in the anthelmintic activities of tannins has not been explored yet. This study investigated the effects of fecal metabolism on the anthelmintic potential of procyanidin C1 (PC1) and geraniin and the tannin-enriched extracts of C. mucronatum (CML) and P. urinaria (PUH), which contain these compounds, respectively. Metabolites were formed by anaerobic fermentation of the test compounds and extracts in a fresh human fecal suspension for 0 h, 4 h, and 24 h. Lyophilized samples were tested in vitro against hookworm larvae and whipworm (Trichuris trichiura) larvae obtained from naturally infected human populations in Pru West District, Bono East Region, Ghana, and against the wildtype strain of Caenorhabditis elegans (L4). Both extracts and compounds in the undegraded state exhibited concentrationdependent inhibition of the three nematodes. Their activity, however, significantly decreased upon fecal metabolism. Without fermentation, the proanthocyanidin-rich CML extract was lethal against hookworm L3 (LC50 = 343.5 µg/mL, 95% confidence interval (CI) = 267.5-445.4), T. trichiura L1 (LC50 = 230.1 µg/mL, CI = 198.9-271.2), and C. elegans (LC50 = 1468.1 µg/mL, CI = 990.3-1946.5). PUH, from which the ellagitannin geraniin was isolated, exhibited anthelmintic effects in the unfermented form with LC50 of 300.8 µg/mL (CI = 245.1-374.8) against hookworm L3 and LC50 of 331.6 µg/mL (CI = 290.3-382.5) against T. trichiura L1, but it showed no significant activity against C. elegans L4 larvae at the tested concentrations. Similarly, both compounds, procyanidin C1 and geraniin, lost their activity when metabolized in fecal matter. The activity of geraniin at a concentration of 170 µg/mL against C. elegans significantly declined from 30.4% ± 1.8% to 14.5% ± 1.5% when metabolized for 4 h, whereas that of PC1 decreased from 32.4% ± 2.3% to 8.9% ± 0.9% with similar treatment. There was no significant difference between the anthelmintic actions of metabolites from the structurally different tannin groups. The outcome of this study revealed that the intact bulky structure of tannins (hydrolyzable or condensed) may be required for their anthelmintic action. The fermented products from the gut may not directly contribute toward the inhibition of the larvae of soil-transmitted helminths. [ABSTRACT FROM AUTHOR]

The interactions between phenolic compounds and dietary fibers have generally received considerable attention because these interactions have a variety of applications, for example, in the production of functional foods, in the pharmaceutical industry, or in the production of films used as packaging materials for food. The aim of this study was to investigate the interactions between two flavan-3-ols: procyanidin B1 and procyanidin B2, and dietary fiber β-glucan. The adsorption process was studied at different temperatures (25, 37 and 45 °C) and different pH values (1.5, 5.5 and 10.0). The adsorption capacity of β-glucan for procyanidins (qe) ranged from 44-489 mg g-1, depending on temperature and pH, and was generally higher for procyanidin B2. At the temperatures tested, the lowest qe values for both procyanidins were obtained at 37 °C, while at the pH values used, the lowest qe values were obtained at pH 5.5. The experimental data were fitted by Langmuir, Freundlich, Dubinin-Radushkevich, Temkin, and Hill isotherms. Analysis of the fit of the applied isotherms led to the conclusion that the adsorption process studied was physical in nature in the range of applied temperatures and pH values. The process was spontaneous and exothermic for both procyanidins. [ABSTRACT FROM AUTHOR]

Anthelmintic resistance in gastrointestinal nematodes produces substantial challenges to agriculture, and new strategies for nematode control in livestock animals are called for. Natural compounds, including tannins, with proven anthelmintic activity could be a functional option as structurally diverse complementary compounds to be used alongside commercial anthelmintics. However, the dual use of two anthelmintic components requires an understanding of the pharmacological effects of the combination, while information concerning the interactions between plant-based polyphenols and commercial anthelmintics is scarce. We studied the direct interactions of proanthocyanidins (PAs, syn. condensed tannins) and a commercial anthelmintic thiabendazole, as a model substance of benzimidazoles, by isothermal titration calorimetry (ITC). Our results show evidence of a direct interaction of an exothermic nature with observed enthalpy changes ranging from 0 to −30 kJ/mol. The strength of the interaction between PAs and thiabendazole is mediated by structural characteristics of the PAs with the strongest positive correlation originating from the presence of galloyl groups and the increased degree of polymerization. [ABSTRACT FROM AUTHOR]

Copyright of Science & Technology of Food Industry is the property of Science & Technology of Food Industry Editorial Office and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

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The Eleutherine bulbosa bulb has been reported as a potent antioxidant in food. This work aims to extract the E. bulbosa bulb for use as an antioxidative agent in cosmetics. Water, 95% ethanol (EtOH), and propylene glycol (PG), which are normally used in cosmetic formulation, were employed as green and sustainable extraction solvents. EtOH and PG displayed better candidacy to extract active components from E. bulbosa bulbs than using water, and the mixture of EtOH and PG (EtOH/PG) resulted in the extract with higher bioactive compounds and biological activities compared with using EtOH or PG. The total phenolic content of the EtOH/PG extract was 87.60 ± 2.00 mgGAE/mL which was about an 18–23% increase from when using single EtOH or PG (70.91 ± 2.30, 74.05 ± 0.67 mgGAE/mL). UHPLC-ESI-QTOF-MS/MS analysis showed that the E. bulbosa bulb extracted in EtOH/PG was composed of naphthalenes, naphthoquinones, anthraquinones, myricetin, quercetin, epicatechin, catechin, epigallocatechin, and their derivatives. The ethanolic crude extract exhibited anti-elastase and anti-collagenase activity with the IC50 of 7.76 ± 0.35 and 0.53 ± 0.23 mg/mL, respectively, and was non-cytotoxic to human dermal fibroblast cells at 0.0001–1 mg/mL. The emulsion cream containing 2%(w/w) E. bulbosa bulb concentrated extract was found cosmetically stable after a one-month stability test under 4 °C, ambient temperature (30–35 °C), 45 °C, fluorescent light, and daylight. However, exposure to sunlight during daytime caused changes in the emulsion's color with ΔE* of 3.85 ± 0.08, and at 45 °C caused the 12% decrease in DPPH activity of emulsion. The finding of this work heightens the antioxidative and safety potentials of the E. bulbosa bulb in cosmetic preparations. [ABSTRACT FROM AUTHOR]

Starch is the main source of energy for the human body. Natural products such as procyanidin (PC) and protocatechuic acid (PCA) can reduce postp'ran'dial blood sugar by controlling the digestion of starch. The inhibition effects of PC and PCA on α-amylase and α-glucosidase were studied using inhibition rate determination, Lineweaver-Burk double reciprocal diagram, ultraviolet spectroscopy, fluorescence quenching, equivalent mapping, and Fourier transform infrared spectroscopy. The results showed that the IC50 values of PC for α-amylase and α-glucosidase inhibition were 0.0524 and 0.0106 mg/mL, respectively, and those of PCA were 1.9426 and 1.0667 mg/mL respectively, which showed that PCA had better inhibition ability. The Lineweaver-Burk double reciprocal diagram showed that the inhibition of PC and PCA on α-amylase was a mixed inhibition, and the inhibition on α-glucosidase was non-competitive inhibition and competitive inhibition, respectively. The Binding of PC and PCA with α-amylase and α-glucosidase mainly depended on hydrophobic and hydrogen bonds, and further altered the enzyme structure by changing the microenvironment of amino acid residues. The inhibitory effects on α-glucosidase were the best when the ratio of PC and PCA was 1:21, and the inhibitory effects on α-amylase were optimal at 1:37. When the ratio of PC and PCA was 1:21, CI was less than 1, which showed a synergistic inhibitory effect on α-glucosidase. When the compounding ratio was 1:37, CI was less than 1, which showed a synergistic inhibitory effect on α-amylase. This study revealed the inhibitory mechanism of the combined use of PC and PCA on starch-digesting enzymes and would provide a theoretical basis for the development of natural hypoglycemic dietary supplements as health food excipients or drugs.

Diabetes mellitus is a metabolic disease due to the malfunctioning of B cells of the pancreas. For a very long time, various herbal remedies have been utilized to prevent diabetes. To compare the hypoglycemic impact of an allopathic medication called Metformin, which has a dosage of 650mg/kg BW, with the hypoglycemic effect of a herbal extract (a 2:1 combination of cinnamon and fenugreek) at 200mg/kg BW, this study was designed. Fenugreek and cinnamon contain bioactive ingredients called procyanidin and 4-hydroxy isoleucine, which have anti-diabetic properties. There were four groups of mice. The first group received no treatment; the second group received no treatment; a third group received herbal extract treatment; and the fourth group received metformin treatment. Swiss Albino received a single intraperitoneal injection of alloxan monohydrate at 200mg/kg BW. Group III (the treated group) received 200mg/kg of herbal extract for 14 days. Additionally, treated group IV received metformin for 14 days at a 650mg/kg dose. After treating groups III and IV with an herbal extract and metformin, the bilirubin level gradually and dramatically (P<0.05) decreased from the elevated level in the +ve control group. Similarly, serum levels of alkaline phosphate (ALP), alanine aminotransferase (ALT), and aspartate aminotransferase (AST) increased dramatically (P<0.05) in alloxan-induced diabetic mice due to liver injury. Their level was dramatically (P<0.05) reduced after the extract and metformin were administered, coming very near to the -ve control group. This decrease demonstrated the potency of metformin and herbal extract. However, metformin worked better than herbal extract. The liver portion displayed a considerable degree of damage in the diabetic group. Following treatment, the liver section's typical architecture was noted. The trial results indicate that the herbal extract has hypoglycemic properties but to a lesser extent than the allopathic medication metformin. [ABSTRACT FROM AUTHOR]

(1) Background: Salix species occurring in Finland have not been well studied for their antimicrobial potential, despite their frequent use for lung and stomach problems in traditional medicine. Thus, twig extracts of three species of Salix that are found naturally in Finland and one cultivated species were screened for their antimicrobial properties against human pathogenic bacteria. S. starkeana and S. x pendulina were screened for antibacterial effects for the first time. (2) Methods: An agar diffusion and a microplate method were used for the screenings. Time-kill effects were measured using a plate-count and a microplate method. A DPPH-method using a qualitative TLC-analysis was used to detect antioxidant compounds in antimicrobial extracts. Metabolites from a S. myrsinifolia extract showing good antibacterial effects were identified using UPLC/QTOF-MS. (3) Results: A methanol extract of S. starkeana was particularly active against B. cereus (MIC 625 µg/mL), and a methanol extract of S. myrsinifolia showed good activity against S. aureus and B. cereus (MIC 1250 µg/mL) and showed bactericidal effects during a 24 h incubation of B. cereus. Moreover, a decoction of S. myrsinifolia resulted in good growth inhibition against P. aeruginosa. Our UPLC/QTOF-MS results indicated that proanthocyanidins (PAs), and especially the dimer procyanidin B1 (m/z 577) and other procyanidin derivatives, including highly polymerized proanthocyanidins, were abundant in S. myrsinifolia methanol extracts. Procyanidin B1 and its monomer catechin, as well as taxifolin and p-hydroxycinnamic acid, all present in S. myrsinifolia twigs, effectively inhibited B. cereus (MIC 250 µg/mL). (4) Conclusions: This study indicates that Finnish Salix species contain an abundance of antibacterial condensed tannins, phenolic acids and other polyphenols that deserve further research for the antibacterial mechanisms of action. [ABSTRACT FROM AUTHOR]

For the first time, to optimize the creation of new neuroprotective agents based on bioflavonoids, we applied information technologies; these include docking analysis to calculate the binding of candidate molecules to the pharmacological target protein transthyretin as well as a program of virtual screening of NO scavengers. As a result of this approach, the substance catechin was isolated from candidate molecules—quercetin, catechin, Epicatechin gallate, Epicatechin, Procyanidin B1, Procyanidin B2, Procyanidin B3, and Catechin-3-gallate—according to docking analysis. As a result of virtual screening, catechin was identified as a potential NO scavenger (55.15% prediction). The results of the prediction were confirmed by in vitro experiments. Course administration of catechin to animals with experimental multiple sclerosis (MS) against the background of methylprednisolone administration completely eliminated lethal cases, reduced the number of diseased animals by 20% as well as prevented the development of severe neurological symptoms by 20% (compared to the methylprednisolone group) and by 60% compared to the control group. Course administration of catechin with methylprednisolone leads to a decrease in the neurodegradation markers in the cytosol of rats, with EAE: NSE by 37% and S-100 by 54.8%. The combined administration of methylprednisolone significantly exceeds the combination of methylprednisolone with the reference drug mexidol by the degree of NSE reduction. The obtained results indicate a significant neuroprotective effect of ocular combinations of methylprednisolone and catechin. The above-mentioned confirms the correctness of the bioflavonoid selection with the help of a virtual screening program. [ABSTRACT FROM AUTHOR]

Aronia melanocarpa (Michaux) Elliot (chokeberry) is a natural medicinal plant with a rich content of phenolic compounds such as procyanidins, anthocyanins, and phenolic acids. Chokeberry fruits are gaining worldwide popularity due to the strong bioactivities of their phenolic constituents, such as antioxidant, anti-inflammatory, anticancer, and liver-protective effects. In the present study, total phenolic, flavonoid, and anthocyanin contents of chokeberry juice were determined via the Folin-Ciocalteu method, a spectrophotometric method based on AlCl3 complexation, and pH differential method, respectively. Anthocyanin content was determined as 1.14% (equivalent to cyanidin-3-glucoside), while phenolic and flavonoid contents were measured as 5060.87 and 331.03 mg per 100 g of freeze-dried juice (equivalent to gallic acid and quercetin), respectively. The hepatoprotective effects of chokeberry fruit juice were evaluated using a zebrafish in vivo model for acetaminophen (APAP)-induced liver injury. Zebrafish is an emerging in vivo liver injury model that enables hepatoprotective bioactivity screening of samples on live organisms. The APAP-induced liver injury model was established by treating zebrafish larvae with 5 mM APAP from 2 days post fertilization (dpf) to 5 dpf. The hepatoprotective effect of chokeberry was evaluated via exposure to 1, 10, and 100 µg/mL of fruit juice. While chokeberry fruit juice did not cause any toxicity up to 100 µg/mL, it successfully reduced the injury induced by APAP when applied at 1 µg/mL concentration. To our knowledge, this is the first report evaluating the hepatoprotective effects of chokeberry using zebrafish in vivo liver injury model. [ABSTRACT FROM AUTHOR]

Periodontal breakdown in periodontitis is exacerbated by pro-inflammatory responses of periodontal stromal cells such as periodontal ligament fibroblasts (PDLFs). Procyanidin B2 (PB2) is a ligand of the peroxisome proliferator-activated receptor (PPARγ). Herein, we investigated the expression of PPARγ isoforms in PDLFs and periodontal tissue, and examined the effects of PB2 on PPARγ isoform-dependent antiinflammatory responses. PPARγ isoforms were examined by PCR. PPARγ isoform-dependent inflammatory functions and anti-inflammatory effects of PB2 in PDLFs were evaluated based on IL-6 expression. Co-immunoprecipitation analysis of fixed chromatin-tethered protein (CoIPfctp) was conducted to investigate the association of each PPARγ isoform with the NF-κB-transcriptional complex. The effects of PB2 on periodontitis progression were evaluated using a ligature-induced murine periodontitis model. Three isoforms of PPARγ were expressed in PDLFs and periodontal tissues, consisting of the main full-length isoform (PPARγ) and two dominant negative isoforms that lack the ligand binding domain, namely the ubiquitously-expressed isoform (PPARγ-UBI) and unknown isoform (PPARγ-PDL). PPARγ and PPARγ-UBI were predominantly expressed. CoIP-fctp revealed that PPARγ-UBI was selectively associated with NF-κB p65, a key transcriptional factor of IL-6 expression. PB2 suppressed LPS-induced-IL-6 expression exacerbated by the over-expression of PPARγ-UBI. In the murine periodontitis model, topical application of PB2 significantly mitigated alveolar bone loss. These results suggest that the anti-inflammatory effects of PB2 in periodontal tissues/cells are distinct, and these effects arise from the inhibition of PPARγ-UBI; hence, the application of PB2 and modification of the splicing event in three PPARγ isoforms have therapeutic potential for preventing periodontitis. [ABSTRACT FROM AUTHOR]

Tannin was extracted from different subspecies of Acacia nilotica, Acacia nilotica nilotica (Ann), Acacia nilotica tomentosa (Ant) and Acacia nilotica adansonii (Ana). The aim was to elucidate their structure and evaluate their reactivity as bioadhesives in the wood industry. The extracts were prepared by hot water extraction (90°C temperature). Their gel time with paraformaldehyde was used at first to compare their reactivity. The tannin contents and the percentage of total polyphenolic materials in different solutions of the extracts spray dried powder were determined by the hide powder method. Concentrated solutions (47%) were tested by both MALDI ToF, CNMR. The thermomechanical analysis (TMA) was performed to evaluate their modulus of elasticity (MOE) at different pHs. The gel times of all the three tannin extracts showed that their reactivity and it was comparable to other known procyanidin/prodelphinidin tannin extract types. Ana, Ann and Ant showed highest percent of total polyphenolic materials at 70%, 64%, and 57%, respectively. The 13CNMR spectra showed that the three subspecies of condensed tannins were mainly constituted of procyanidins (PC) and prodelphinidins (PD) in slightly different ratios. Ann (56.5% PC and 43.4% PD), Ant (57%PC and 43% PD) and Ana (58% PC and 42% PD). MALDI–TOF spectra showed the presence of flavonoid monomers, and oligomers some of which linked to short carbohydrates monomers or dimers. TMA revealed that the three types of tannins had high MOE at their initial pH (5). [ABSTRACT FROM AUTHOR]

Background : Torch ginger (Etlingera elatior) is an edible flower whose inflorescence is utlized for culinary purposes to enchance the taste of traditional dishes containing polyphenols and antioxidant compounds. However, investigation on the phytochemical profile and antioxidant activity of torch ginger inflorescence extract following simulated gastrointesinal digestion is still limited. Objective: This study aims to determine the phytochemical profile and evaluate the antioxidant activity of the inflorescence extract after in vitro simulated digestion. Methods: Torch ginger inflorescence (TGI) was extracted by ultrasound-assisted extraction with different solvents (water, 50%, and 80% aqueous ethanol). Total phenolics content (TPC), total flavonoid content (TFC), and antioxidant activity were determined by ORAC, DPPH, FRAP, and metal ion (Fe2+) chelating activity. The solvent extraction that gave the highest value of TPC, TFC, and antioxidant activities was used for an in vitro digestion and identification of phytochemicals profile by LC-ESI-QTOF-MS/MS. Furthermore, the TPC, TFC, and antioxidant capacities of digested TGI extract were compared to those of undigested extract. Results: TGI contained 90.24% moisture. The 80% aqueous ethanol extract exhibited the highest antioxidant capacity, with an ORAC value of 1,156.61 ± 11.55 mM TE/g extract, DPPH radical scavenging capacity of 1,087.68 ± 14.37 mM TE/g extract, FRAP value of 799.30 ± 1.45 mM TE/g extract, and Fe2+ chelating capacity of 42.32 ± 3.48% /mg extract. The 39 phytochemicals were identified for 9 flavonoids and 5 phenolic acids. The putative bioactive compounds for antioxidant, anticancer, anti-inflammatory, and anticholesterol were detected in TGIE, such as catechin, 2-hydroxycinnamic acid, astragalin, chlorogenic acid, coumarin, and procyanidin B2. After passing through an in vitro simulated mouth, gastric, and intestinal digestion, the TGI extract exhibited higher values of TPC, TFC, and antioxidative capacities than the undigested extract. Conclusion: This study reviewed the phytochemical components presented in the 80% aqueous ethanol TGIE. The expressed antioxidant capacity was increased when the TGIE passed through the in vitro simulated digestion, which could potentially represent a promising source of endogenous antioxidants in food and nutraceutical applications. [ABSTRACT FROM AUTHOR]

The fruit juice industry generates a significant amount of waste, with a strong impact on the environment and the economy. Therefore, researchers have been focusing on the characterization of resources considered as food waste. This work provides information about the lipophilic and polar metabolites of pear pomace flours (PPFs) as a tool that can shed more light on the bioactive potential of this residue. Using UPLC-PDA, UPLC-FLR, and GC-MS, the study identified and quantified PPF's polar and non-polar metabolites. Essential, conditional, and non-essential amino acids were found, with asparagine being the most abundant. Isoprenoids, including lutein, zeaxanthin, and carotene isomers, ranged from 10.8 to 22.9 mg/100 g dw. Total flavonoids and phenolic compounds were 520.5–636.4 mg/100 g dw and 536.9–660.1 mg/100 g dw, respectively. Tocotrienols and tocopherols were identified, with concentrations of 173.1–347.0 mg/100 g dw and 468.7–913.4 mg/100 g dw. Fatty acids were the major non-polar compounds. All fractions significantly reduced matrix metalloproteinase-9 (MMP-9) activity. Although PPF had lower antioxidant potential (3–6 mmol Trolox/100 g dw), it inhibited AChE and BuChE by 23–30% compared to physostigmine salicylate. These findings suggest that pear pomace waste can be repurposed into functional products with valuable bioactive properties by re-introducing it in the food chain. [ABSTRACT FROM AUTHOR]

Pyracantha is a genus of wild perennial shrubs native in an area extending from Southwest Europe to Southeast Asia, and it is used in traditional medicine for the diuretic, cardiac, and tonic properties of its fruits, which can also be cooked to make jellies, jams, and sauces. This work aims to study and compare the antioxidant activity and the phenolic and anthocyanin composition of three varieties of Pyracantha coccinea: Red Column (PCR), Orange Glow (PCO), and Soleil d'Or (PCS), and one of Pyracantha angustifolia: Orange glow (PAO), collected from the spontaneous flora of the Mediterranean region (Southern Italy). Two different extraction processes were tested using methanol and an aqueous methanol solution (80% MeOH) to evaluate the polyphenolic content and antioxidant activity of freeze-dried berries. The highest total phenolic content was found in PCR and PAO berries (174.21 ± 0.149 and 168.01 ± 0.691 mg of gallic acid equivalent per gram of dry matter, respectively) extracted with an aqueous methanol solution (80% MeOH). Polyphenolic extracts analyzed by HPLC-DAD-ESI/MS confirmed the presence of rutin, quercetin hexose, neoeriocitrin, procyanidin B, and resveratrol. Moreover, the total antioxidant activity of the berries' extracts was measured by comparing two different spectrophotometric methods (ABTS and DPPH), showing that the varieties with the highest total phenolic content, PCR and PAO, also had the highest scavenging activity. Finally, a suitable extraction process was chosen for the evaluation of the anthocyanins' composition of all frozen berries, and in all MS spectra of Pyracantha varieties, two ionic species at 449 m/z attributable to two cyanidin derivatives were found. [ABSTRACT FROM AUTHOR]

Polyphenols from agro-food waste represent a valuable source of bioactive molecules that can be recovered to be used for their functional properties. Another option is to use them as starting material to generate molecules with new and better properties through semi-synthesis. A proanthocyanidin-rich (PACs) extract from avocado peels was used to prepare several semi-synthetic derivatives of epicatechin by acid cleavage in the presence of phenol and thiol nucleophiles. The adducts formed by this reaction were successfully purified using one-step centrifugal partition chromatography (CPC) and identified by chromatographic and spectroscopic methods. The nine derivatives showed a concentration-dependent free radical scavenging activity in the DPPH assay. All compounds were also tested against a panel of pathogenic bacterial strains formed by Listeria monocytogenes (ATCC 7644 and 19115), Staphylococcus aureus (ATCC 9144), Escherichia coli (ATCC 11775 and 25922), and Salmonella enterica (ATCC 13076). In addition, adducts were tested against two no-pathogenic strains, Limosilactobacillus fermentum UCO-979C and Lacticaseibacillus rhamnosus UCO-25A. Overall, thiol-derived adducts displayed antimicrobial properties and, in some specific cases, inhibited biofilm formation, particularly in Listeria monocytogenes (ATCC 7644). Interestingly, phenolic adducts were inactive against all the strains and could not inhibit its biofilm formation. Moreover, depending on the structure, in specific cases, biofilm formation was strongly promoted. These findings contribute to demonstrating that CPC is a powerful tool to isolate new semi-synthetic molecules using avocado peels as starting material for PACc extraction. These compounds represent new lead molecules with antioxidant and antimicrobial activity. [ABSTRACT FROM AUTHOR]

Pigmented rice grains are important resources for health and nutritional perspectives. Thus, a thorough dissection of the variation of nutrients and bioactive metabolites in different colored rice is of global interest. This study applied LC–MS-based widely targeted metabolite profiling and unraveled the variability of metabolites and nutraceuticals in long grain/non-glutinous black (BR), red (RR), green (GR), and white rice (WR) grains. We identified and classified 1292 metabolites, including five flavonoid compounds specific to BR. The metabolite profiles of the four rice grains showed significant variation, with 275–543 differentially accumulated metabolites identified. Flavonoid (flavone, flavonol, and anthocyanin) and cofactor biosynthesis were the most differentially regulated pathways among the four rice types. Most bioactive flavonoids, anthocyanidins (glycosylated cyanidins and peonidins), phenolic acids, and lignans had the highest relative content in BR, followed by RR. Most alkaloids, amino acids and derivatives, lipids, and vitamins (B6, B3, B1, nicotinamide, and isonicotinic acid) had higher relative contents in GR than others. Procyanidins (B1, B2, and B3) had the highest relative content in RR. In addition, we identified 25 potential discriminatory biomarkers, including fagomine, which could be used to authenticate GR. Our results show that BR and RR are important materials for medicinal use, while GR is an excellent source of nutrients (amino acids and vitamins) and bioactive alkaloids. Moreover, they provide data resources for the science-based use of different colored rice varieties in diverse industries. [ABSTRACT FROM AUTHOR]

A whole-grain highland barley (WHB) diet has been recognized to exhibit the potential for alleviating hyperlipidemia, which is mainly characterized by lipids accumulation in the serum and liver. Previously, procyanidin B1 (PB) and coumaric acid (CA) from WHB were found to alleviate serum lipid accumulation in impaired glucose tolerance mice, while the effect on modulating the hepatic lipid metabolism remains unknown. In this study, the results showed the supplementation of PB and CA activated the expression of peroxisome proliferator-activated receptor α (PPARα) and the target genes of cholesterol 7-α hydroxylase (CYP7A1) and carnitine palmitoyl transferase I (Cpt1) in the liver cells of high-fat-diet (HFD)-induced diabetic C57BL/6J mice, resulting in decreases in the serum total cholesterol (TC), triglyceride (TG), and low-density lipoprotein (LDL-C) contents, and an increase in the high-density lipoprotein (HDL-C) content. High-throughput sequencing of 16S rRNA indicated that supplementation with PB and CA ameliorated the gut microbiota dysbiosis, which was associated with a reduction in the relative abundance of Ruminococcaceae and an increase in the relative abundance of Lactobacillus, Desulfovibrio, and Akkermansia. Spearman's correlation analysis revealed that these genera were closely related to obesity-related indices. In summary, the activation of PPARα expression by PB and CA from WHB was important for the alleviation of hyperlipidemia and the structural adjustment of the gut microbiota. [ABSTRACT FROM AUTHOR]

Sabia parviflora (SP, "xiao hua qing feng teng" in Chinese) was recorded as an important ethnic medicine to be used for treating viral hepatitis. The antiviral activity of four SP extracts and potent antiviral compounds evaluated with cathepsin L protease (Cat L PR) and HIV-1 protease (HIV-1 PR). UPLC-HRMS was used for identifying the bioactive components. In addition, the possible inhibitory mechanism of the identified compounds on viral protease was further discussed by molecular docking. As a result, four extracts of SP exhibited inhibitory activity of HIV-1 PR and Cat L PR with IC50 range from 0.015 to 0.80 mg/mL. Meanwhile, six compounds inhibited HIV-1 PR with IC50 range from 0.032 to 0.80 mg/mL. Moreover, procyanidin B2 had good affinity for HIV-1 PR and CatL PR protein, respectively. These findings suggest S. parviflora leaves can be used for treating HIV and procyanidin B2 may play a role in antiviral protease. [ABSTRACT FROM AUTHOR]

Crataegus monogyna (C. monogyna) is a prominent plant used in Moroccan traditional medicine. This study investigated the phenolic composition and the anti-inflammatory, the hepatoprotective, and the anticancer activities of a hydroethanolic extract of C. monogyna leaves and stems. Ultra-high-performance liquid chromatography identified the phenolic profile. The in vitro anticancer activity was evaluated using the MTT assay on HL-60 and K-562 myeloleukemia cells and liver (Huh-7) cell lines. The anti-inflammatory effect was assessed in vivo using carrageenan-induced paw edema in rats. The hepatoprotective effect at 300 and 1000 mg/kg doses against the acetaminophen-induced hepatotoxicity on rats was studied for seven days. Additionally, molecular docking simulations were performed to evaluate the extract's inhibitory potential against key targets: lipoxygenase, cytochrome P450, tyrosine kinase, and TRADD. The extract exhibited significant cytotoxic activity against K-562 and HL-60 cells, but not against lung cancer cells (Huh-7 line). The 1000 mg/kg dose demonstrated the most potent anti-inflammatory effect, inhibiting edema by 99.10% after 6 h. C. monogyna extract displayed promising hepatoprotective properties. Procyanidin (−7.27 kcal/mol), quercetin (−8.102 kcal/mol), and catechin (−9.037 kcal/mol) were identified as the most active molecules against lipoxygenase, cytochrome P450, and tyrosine kinase, respectively. These findings highlight the untapped potential of C. monogyna for further exploration in treating liver damage, inflammation, and leukemia. [ABSTRACT FROM AUTHOR]

Films made with blends of agar and gelatin are usually unstable in aqueous environments and susceptible to temperature, so modifying these films with the addition of compatible compounds is necessary to improve their structural stability, properties, and potential uses. This work determined the effects of adding sorghum procyanidins on the structure, molecular interactions and thermal properties of agar-glycerol-gelatin films. Films were prepared by solution cast method and characterized by Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), scanning electron microscopy (SEM), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC) and computational methods. Adding sorghum procyanidins to agar-gelatin films plasticized with glycerol produced significant modifications compared to control films. They contributed to the amorphous character and roughness of these films and the film's microstructure, reducing weight loss and enhancing thermal stability. The predominant interactions among the film components were hydrogen bonds, van der Waals, and π – π interactions. Agar-glycerol-gelatin-procyanidins films showed a rough surface Sorghum procyanidins increased the thermal stability of agar-glycerol-gelatin films π - π interactions, hydrogen bonding and van der Waals forces contributed to the binding of the film components [ABSTRACT FROM AUTHOR]

The aim of this research work was to investigate the influence of parameters such as particle size, mass/solvent ratio, temperature and spray drying on the tannin extraction process in order to develop cost-effective methods with better environmental and structural performance. The pods of Acacia nilotica ssp. tomentosa (ANT) were fractionated into three fractions, coarse fraction (C) (>2 mm), medium fraction (M) (1–2 mm), and fine fraction (F) < 1 mµ), and extracted with different water-to-pod ratios (2:1, 4:1 and 6:1) at different temperatures (30, 50 and 70 °C). The best results were scaled up using the three fractions of ANT, its bark and the bark of Acacia seyal var. seyal (ASS). Part of their extract was spray dried. The tannin content and total polyphenolic materials were evaluated using standard methods. Their adhesives were tested for their tensile strength. Tannins of ASS were characterized by 13C NMR and MALDI-TOF. The results revealed that the fine fraction (F) gave the highest percentage of tannins in both small and scaled-up experiments. The results of the tensile strength conformed to the European standard. The 13C NMR spectra of ANT and ASS showed that the bark contained condensed tannins mainly consisting of procyanidins/prodelphinidin of 70%/30% and 60%/40%, respectively. MALDI–TOF spectra confirmed the results obtained by 13C NMR and detailed the presence of flavonoid monomers and oligomers, some of which were linked to short carbohydrate monomers or dimers. [ABSTRACT FROM AUTHOR]

Pyracantha fortuneana (P. fortuneana) fruit is a wild fruit that is popular because of its delicious taste and numerous nutrients, and phenolic compounds are considered to be the main bioactive components in P. fortuneana fruits. However, the relationship between phenolic compounds and their antioxidant and tyrosinase (TYR) inhibitory activities during the ripening process is still unclear. The study compared the influence of the five developmental stages on the accumulation of phenolic compounds, antioxidant activity, and TYR inhibitory activity in the fruits of P. fortuneana. The compounds were identified by offline two‐dimensional liquid chromatography‐electrochemical detection (2D‐LC‐ECD) combined with liquid chromatography–tandem mass spectrometry, and the main active ingredients were quantified. The results showed that stage II had higher total phenolic and flavonoid content, as well as higher antioxidant and TYR inhibitory activity, but the total anthocyanin content was lowest at this stage. A total of 30 compounds were identified by 2D‐LC‐ECD. Orthogonal partial least squares discriminant analysis screened out six major potential markers, including phenolic acids, procyanidins, and flavonoids. In addition, it was found that caffeoylquinic acids, procyanidins, and flavonoids were higher in stage II than in stages I, III, IV, and V, whereas anthocyanins accumulated gradually from stages III to V. Therefore, this study suggests that the changes in antioxidant and TYR inhibitory activities of P. fortuneana during the five developmental stages may be due to the transformation of procyanidins, caffeoylquinic acids, and phenolic glycosides into other forms during the fruit maturation process. Practical Application: Differences in chemical constituents, antioxidant, and tyrosinase inhibitory activities in fruit maturity stages of P. fortuneana were elucidated to provide reference for rational harvesting and utilization of the fruits and their bioactive components. These findings are expected to provide a comprehensive assessment of the bioactive profile and guide the food industrial production. [ABSTRACT FROM AUTHOR]

[Display omitted] • HIGD1A and ZG16, lower expressed in COAD than in READ, are both associated with poor prognosis in COAD, but not in READ. • Compared with ZG16, HIGD1A showed more efficiency in suppressing tumor growth and metastasis in CRC cells. • miR-501-3p, higher expressed in COAD than in READ, promoted CRC cells proliferation, invasion, and migration through suppressing HIGD1A expression. • High leveled miR-501-3p inhibited HIGD1A expression in COAD, which promoted tumor growth and metastasis, and eventually caused poor prognosis in COAD. • Procyanidin C1 (PCC1), a kind of natural polyphenol has been verified as a potential miR-501-3p inhibitor, which modulated miR-501-3p/HIGD1A axis and inhibited tumor growth and metastasis in vivo and in vitro. Although colon (COAD) and rectal adenocarcinoma (READ) combined to refer to colorectal cancer (CRC), substantial clinical evidence urged that CRC should be treated as two different cancers due to compared with READ, COAD showed higher morbidity and worse 5-year survival. This study has tried to screen for the crucial gene that caused the worse prognosis and investigate its mechanism for mediating tumor growth and metastases in COAD. Meanwhile, the potential anti-COAD compound implicated in this mechanism was identified and testified from 1,855 food-borne chemical kits. This study aims to bring a new perspective to the development of new anti-COAD drugs and personalized medicine for patients with COAD. The survival-related hub genes in COAD and READ were screened out from The Cancer Genome Atlas (TCGA) database and the results showed that HIGD1A , lower expressed in COAD than in READ, was associated with poor prognosis in COAD patients, but not in READ. Over-expressed HIGD1A suppressed CRC cell proliferation, invasion, and migration in vitro and in vivo. Meanwhile, the different expressed microRNA profiles between COAD and READ showed that miR-501-3p was highly expressed in COAD and inhibited HIGD1A expression by targeting 3′UTR of HIGD1A. MiR-501-3p mimics promoted cell proliferation and metastasis in CRC cells. In addition, Procyanidin C1 (PCC1), a kind of natural polyphenol has been verified as a potential miR-501-3p inhibitor. In vitro and in vivo , PCC1 promoted HIGD1A expression by suppressing miR-501-3p and resulted in inhibited tumor growth and metastasis. The present study verified that miR-501-3p/HIGD1A axis mediated tumor growth and metastasis in COAD. PCC1, a flavonoid that riched in food exerts anti-COAD effects by inhibiting miR-501-3p and results in the latter losing the ability to suppress HIGD1A expression. Subsequently, unfettered HIGD1A inhibited tumor growth and metastasis in COAD. [ABSTRACT FROM AUTHOR]

The aim of this study was to find a purely natural and effective preservative that could be used in fresh-cut apples extracting proanthocyanidin (PC) components from black chokeberry (Aronia melanocarpa (Michx.) Elliott) using DESs (deep eutectic solvents). DM130 microporous resins were used in purification experiments to obtain proanthocyanidin purifiers with a higher content. To investigate the free radical scavenging ability (DPPH, ·OH, O2−, ABTS) of the resulting proanthocyanidin purifiers, experiments were conducted due to their potent antioxidant properties. The results show that the polyphenol extract from black chokeberry demonstrated an excellent antioxidant capacity, with more than 95% scavenging of DPPH, ABTS and superoxide anion at concentrations above 0.1 mg/mL. Furthermore, the antibacterial efficacy of the product was also evaluated. The results of this study on the inhibitory ability of bacteria demonstrated that PC exhibited superior inhibitory efficacy against E. coli and S. aureus, with inhibitory circles of 16 ± 0.11 mm and 18 ± 0.09 mm, respectively. Conversely, PC demonstrated no inhibitory efficacy against A. niger and Penicillium sp. Finally, the effect of PC in preserving fresh-cut apples was tested in terms of weight loss, hardness, appearance and total number of microorganisms. The results demonstrated a 26.44% reduction in weight loss and a 13.5% increase in hardness, as well as a 98% reduction in total bacterial counts in apple pieces treated with 5 mg/mL of PC in comparison to those left untreated. [ABSTRACT FROM AUTHOR]

Inflammation is a common occurrence in many medical conditions and is a natural defense mechanism of the human body. Ferroptosis, an iron-dependent form of cell death related to lipid peroxide build-up, has been found to be involved in inflammation. The anti-inflammatory effects of procyanidin, however, are not yet fully understood. Through network pharmacology and bioinformatics analysis, it was suggested that procyanidin could modulate ferroptosis and cause anti-inflammatory effects on RAW264.7 cells. This was further evidenced through molecular docking, molecular dynamics, and in vitro experiments. The results indicated that procyanidin could diminish inflammation in LPS-induced RAW264.7 cells by regulating ferroptosis via the Nrf2/HO-1/Keap-1 pathway. In conclusion, procyanidin supplementation might be an effective way to reduce inflammation by decreasing the release of inflammatory cytokines and suppressing ferroptosis. [ABSTRACT FROM AUTHOR]

Camellia polyodonta flowers are rich sources of phenolics and less attention has been paid to their potential biological activity. This study aims to explore the crude extracts and resulting purified fractions (CPFP-I, II, III, and IV) through compositional analysis and antioxidant and hypolipidemic activities in vitro and in vivo. Among four fractions, CPFP-II contained the highest total phenolic content and flavonoid content, while CPFP-III exhibited the greatest total proanthocyanidin content. Among the 14 phenolic compounds, CPFP-II displayed the highest content of procyanidin B2, B4, and C1, whereas CPFP-III contained the highest amount of 1,2,3,6-tetragalloylglucose. The DPPH, ABTS, and FRAP assessments demonstrated a consistent trend: CPFP-II > CPFP-III > CPFP-I > CPFP-IV. In vivo experiments showed that that all four fractions significantly reduced lipid levels in hyperlipidemic C. elegans (p < 0.05), with CPFP-II exhibiting the most potent effect. Furthermore, CPFP-II effectively bound to bile acids and inhibited the enzymatic activity of pancreatic lipase in vitro. Consequently, CPFP-II should be prioritized as a promising fraction for further exploration and should provide substantial support for the feasibility of the C. polyodonta flower as a natural alternative. [ABSTRACT FROM AUTHOR]

Grapes present recognized beneficial effects on human health due to their polyphenolic composition. The grape overproduction together with the wine sales down and the world socioeconomic situation makes the wine grape valorization a promising strategy to give an added-value to this natural product. The objective of the present work was to study the influence of in vitro gastrointestinal digestion on antioxidant capacity and polyphenolic profile of skin and seed extracts of different grape varieties (Tempranillo, Graciano, Maturana tinta and Hondarrabi zuri). After in vitro gastrointestinal digestion, total phenolic content (TPC) of seed polyphenolic extracts decreased significantly for all the varieties. The highest decrease was for Tempranillo going from 108 ± 9 to 50 ± 3 mg / g dry matter (dm). This variety also showed the highest decrease of 90% in antioxidant capacity. However, for all the skin polyphenolic extracts there was an increase in TPC. The highest variation was also for Tempranillo. It varied from 10.1 ± 0.8 to 55.1 ± 0.9 mg / g dm. Among red varieties Tempranillo skin polyphenolic extract showed the lowest undigested anthocyanin content but the highest bioaccessibility index (BI) of 77%. For flavanols, flavonols and procyanidins the seed polyphenolic extracts showed a BI at the intestinal phase between 11% for (+)-epicatechin gallate to 130% procyanidin A2. The results of this study suggest that grape skin extracts and grape seed extracts are a reliable source of bioaccessible antioxidant polyphenols, to be used for the development of antioxidant supplements with specific functionalities depending on the grape variety. [ABSTRACT FROM AUTHOR]

Background: Recent studies have shown that peripheral nerve regeneration process is closely related to neuropathic pain. Toll-like receptor 4 (TLR4) signaling was involved in different types of pain and nerve regeneration. TLR4 induced the recruitment of myeloid differentiation factor-88 adaptor protein (MyD88) and NF-κB-depended transcriptional process in sensory neurons and glial cells, which produced multiple cytokines and promoted the induction and persistence of pain. Our study aimed to investigate procyanidins's effect on pain and nerve regeneration via TLR4-Myd88 signaling. Methods: Spinal nerve ligation (SNL) model was established to measure the analgesic effect of procyanidins. Anatomical measurement of peripheral nerve regeneration was measured by microscopy and growth associated protein 43 (GAP43) staining. Western blotting and/or immunofluorescent staining were utilized to detect TLR4, myeloid differentiation factor-88 adaptor protein (MyD88), ionized calcium-binding adapter molecule 1 (IBA1) and nuclear factor kappa-B-p65 (NF-κB-p65) expression, as well as the activation of astrocyte and microglia. The antagonist of TLR4 (LPS-RS-Ultra, LRU) were intrathecally administrated to assess the behavioral effects of blocking TLR4 signaling on pain and nerve regeneration. Result: Procyanidins reduced mechanical allodynia, thermal hyperalgesia and significantly suppressed the number of nerve fibers regenerated and the degree of myelination in SNL model. Compared with sham group, TLR4, MyD88, IBA1 and phosphorylation of NF-κB-p65 were upregulated in SNL rats which were reversed by procyanidins administration. Additionally, procyanidins also suppressed activation of spinal astrocytes and glial cells. Conclusion: Suppression of TLR4-MyD88 signaling contributes to the alleviation of neuropathic pain and reduction of nerve regeneration by procyanidins. [ABSTRACT FROM AUTHOR]

Background: Cereals have historically played a crucial role in the human diet, serving as a significant natural source of energy and offering various health benefits. Barley (Hordeum vulgare L.) has been given significant attention in recent years due to its exceptional nutritional value, surpassing that of other cereals. The objective of this research is to evaluate the antioxidant activity of various solvent extracts obtained from three different barley cultivars. Results: The G.136 variety's acetone extract exhibited the highest level of antioxidant activity in both the DPPH assay, with an IC50 of 55.62 µg/ml, and the FRAP assay, with 447 μM trolox/mg extract. The dominant compounds identified before in the acetone fraction were subjected to an evaluation of their docking scores, along with an assessment of ADMET (Absorption, Distribution, Metabolism, Excretion, and Toxicity) and TOPKAT (Toxicity Prediction by Komputer Assisted Technology) studies. Notably, hordatine A1, prodelphinidin B3, hordatine B1, procyanidin B2, and isovitexin 7-O-glucoside were the major compounds with the highest LipDock scores compared to trolox the reference drug with polyphenol oxidase. Conclusions: The findings indicate that the acetone extract from all three cultivars demonstrates noteworthy results, surpassing the efficacy of other solvent extracts against the antioxidant activity. [ABSTRACT FROM AUTHOR]

Schisandra henryi is an endemic species of medicinal potential known from traditional Chinese medicine. As part of this study, a complex biotechnological and phytochemical assessment was conducted on S. henryi with a focus on phenolic compounds and antioxidant profiling. The following in vitro cultures were tested: microshoot agar and callus, microshoot agitated, and suspension, along with the microshoot culture in PlantForm bioreactors. Qualitative profiling was performed by ultra-high-performance liquid chromatography with a photodiode array detector coupled with ion-trap mass spectrophotometry with electrospray ionization and then quantitative analysis by high-performance liquid chromatography with a diode array detector using standards. In the extracts, mainly the compounds from procyanidins were identified as well as phenolic acids (neochlorogenic acid, caffeic acid, protocatechuic acid) and catechin. The highest content of phenolic compounds was found for in vitro agar microshoot culture (max. total content 229.87 mg/100 g DW) and agitated culture (max. total content 22.82 mg/100 g DW). The max. TPC measured using the Folin-Ciocalteu assay was equal to 1240.51 mg GAE/100 g DW (agar microshoot culture). The extracts were evaluated for their antioxidant potential by the DPPH, FRAP, and chelate iron ion assays. The highest potential was indicated for agar microshoot culture (90% of inhibition and 59.31 nM/L TEAC, respectively). The research conducted on the polyphenol profiling and antioxidant potential of S. henryi in vitro culture extracts indicates the high therapeutic potential of this species. Key points: • Different types of S. henryi in vitro cultures were compared for the first time. • The S. henryi in vitro culture strong antioxidant potential was determined for the first time. • The polyphenol profiling of different types of S. henryi in vitro cultures was shown. [ABSTRACT FROM AUTHOR]

Cistus ladanifer L., Acacia dealbata L., and Aloysia citrodora Paláu were subject to an optimization procedure for two extraction techniques (heat-assisted extraction (HAE) and ultrasound-assisted extraction (UAE)). The extracts were then analyzed by HPLC-DAD-ESI/MS for their phenolic profile (cistus—15 compounds, acacia—21 compounds, and lemon verbena—9 compounds). The response surface methodology was applied, considering four varying factors: ethanol percentage; extraction time; temperature/power; and S/L ratio, generating two responses (the major phenolic compound, or family of compounds, and the extraction yield). For cistus, both techniques optimized the extraction yield of punicalagins, with UAE proving to be the most efficient extraction method (3.22% ethanol, 22 min, 171 W, and 35 g/L). For acacia, HAE maximized the extraction of procyanidin (74% ethanol, 86 min, 24 °C, and 50 g/L), and UAE maximized the content of myricetin (65% ethanol, 8 min, 50 W, and 50 g/L). For lemon verbena, HAE favored the extraction of martynoside (13% ethanol, 96 min, 49 °C and 17 g/L) and forsythiaside UAE (94% ethanol, 25 min, 399 W, and 29 g/L). The optimal conditions for the extraction of compounds with high added value and potential for use in pharmaceuticals and nutraceuticals were defined. [ABSTRACT FROM AUTHOR]