Procyanidin B2 Research Articles

Potential of Raspberry Flower Petals as a Rich Source of Bioactive Flavan-3-ol Derivatives Revealed by Polyphenolic Profiling

Inspired by the potential functional activity of polyphenol compounds contained in raspberry (Rubus idaeus), we previously explored the effects of the cultivation environment and maturity on the polyphenolic profiles of raspberry leaves and fruits. Herein, building on our previous studies, we used high-performance liquid chromatography and liquid chromatography–mass spectrometry to profile the polyphenol compounds contained in five parts of raspberry flowers (receptacles, sepals, pistils, stamens, and petals), revealing the presence of (+)-catechin, (−)-epicatechin, procyanidin B4, procyanidin C3, sanguiin H-6, and lambertianin C in all flower parts. Petals also contained (−)-epicatechin-3,5-di-O-gallate, kaempferol-7-O-glucoside, and naringenin-7-O-glucoside as well as other flavan-3-ol derivatives efficiently scavenging free radicals and inhibiting the growth of cancer (HeLa S3) cells. Thus, raspberry flower petals were concluded to be a good source of characteristic and highly functional flavan-3-ol derivatives.

Procyanidin B2: A promising multi-functional food-derived pigment for human diseases

Natural edible pigments play a paramount part in the food industry. Procyanidin B2 (PB2), one of the most representative naturally occurring edible pigments, is usually isolated from the seeds, fruits, and leaves of lots of common plants, such as grapes, Hawthorn, black soybean, as well as blueberry, and functions as a food additive in daily life. Notably, PB2 has numerous bioactivities and possesses the potential to treat/prevent a wide range of human diseases, such as diabetes mellitus, diabetic complications, atherosclerosis, and non-alcoholic fatty liver disease, and the underlying mechanisms were partially elucidated, including mediating signaling pathways like NF-κB, MAPK, PI3K/Akt, apoptotic axis, and Nrf-2/HO-1. This paper presents a review of the natural sources, bioactivities, and the therapeutic/preventive potential of PB2 and the possible mechanisms, with the aim of promoting the development of PB2 as a functional food and providing references for its clinical application in the treatment of diseases.

Foliar Application of CaCO3-Rich Industrial Residues on 'Shiraz' Vines Improves the Composition of Phenolic Compounds in Grapes and Aged Wine.

The quality of wine grapes and wine depends on their content of phenolic compounds. Under commercial conditions, the phenolic maturity of grapes is mostly achieved by applying abscisic acid analogues. Some Ca forms represent a cost-effective alternative for these compounds. In this study, 'Shiraz' vines (veraison of 90%) were sprayed with CaCO3-rich residues from the cement industry (4.26 g of Ca per L). Fruit from treated and untreated vines was harvested 45 days after CaCO3 spraying and evaluated for quality. The fruit was vinified, and the obtained wines were bottled and stored in darkness for 15 months at 20 °C. Wines were evaluated for quality after storage. The evaluation of grape and wine quality included the content of phenolic compounds and antioxidant capacity. The treatment with CaCO3 did not affect the ripening rate of grapes. However, the treatment improved the fruit yield as well as the color development, the content of phenolic compounds, and antioxidant capacity of grapes and wine. The treatment favored especially the accumulation of malvidin-3-O-glucoside, pelargonidin-3-O-glucoside, caftaric acid, caffeic acid, trans-cinnamic acid, quercetin, catechin, epicatechin, resveratrol, and the procyanidins B1 and B2. Wine made with treated fruit was of higher quality than that of control fruit.

Musa spp. cultivars as a neutralising source against some toxic activities of Bothrops and Crotalus genus snake venoms

Accidents involving snakes from Bothrops spp. and Crotalus spp. constitute the most important cause of envenomation in Brazil and Argentina. Musa spp. (banana) have been reported to be used in popular medicine against snakebite by the members of the Canudos Settlement, located in Goiás. In this way, the aim of this work was to evaluate the antivenom effect of the Ouro (AA), Prata (AAB), Prata-anã (AAB) and Figo (ABB) cultivars against in vitro (phospholipase, coagulation and proteolytic) and in vivo (lethality and toxicity) activities caused by the venoms and toxicity (Artemia salina nauplii and Danio rerio embryos) of Musa spp. as well as the annotation of chemical compounds possibly related to these activities. From the in vitro antiophidic tests with the sap, we observed 100% inhibition of the phospholipase and coagulant activities with the cultivars Prata-anã and Figo against the venoms of B. alternatus and C. d. collineatus, B. diporus and B. pauloensis, respectively, and neutralisation of the lethality against the B. diporus venom. It was observed that the cultivars of Musa spp. did not show toxicity against Artemia salina nauplii and Danio rerio embryos. The sap analysis via HPLC-MS/MS allowed the annotation of the 13 compounds: abscisic acid, shikimic acid, citric acid, quinic acid, afzelechin, Glp-hexose, glucose, sucrose, isorhamnetin-3-O-galactoside-6-raminoside, kaempferol-3-glucoside-3-raminoside, myricetin-3-O-rutinoside, procyanidin B1 and rutin. Therefore, it can be seen that Musa spp. is a potential therapeutic agent that can act to neutralise the effects caused by snakebites.

Changes in the Fruit Quality, Phenolic Compounds, and Antioxidant Potential of Red-Fleshed Kiwifruit during Postharvest Ripening

Kiwifruit is very popular for its unique flavor and nutritional value, and for its potential health benefits, which are closely related to its richness in a variety of natural antioxidant substances, in which polyphenolics play a non-negligible role. This study investigated changes in the fruit quality, phenolic compounds, and antioxidant potential of Chinese red-fleshed kiwifruit "Hongshi No. 2" during postharvest ripening at room temperature (20 ± 1 °C). Results showed that the weight loss rate slowly increased, the firmness rapidly decreased, and the soluble solid concentration gradually increased during the postharvest ripening of red-flesh kiwifruit. In addition, the total phenolic (TPC), total flavonoid (TFC), and total proanthocyanidin (TPAC) contents gradually increased during postharvest ripening. The most abundant phenolic compounds in kiwifruit throughout postharvest ripening were catechin (CC), proanthocyanidin B1 (PB1), and proanthocyanidin B2 (PB2). Furthermore, the methanolic extracts of red-flesh kiwifruit exhibited remarkable antioxidant activities throughout postharvest ripening stages. Indeed, some phenolic compounds showed good correlations with antioxidant activities; for instance, chlorogenic acid (CHL) showed a significantly positive correlation with ferric reducing antioxidant power (FRAP), and isoquercitrin (IS) showed a significantly negative correlation with DPPH free radical scavenging ability. The findings from this study are beneficial to better understanding the quality profile of red-flesh kiwifruit "Hongshi No. 2" during postharvest ripening.

Components research on Tetrastigma hemsleyanum Diels et Gilg: Identification and effect of drying methods on the content of ten main constituents by targeting metabolomics method

Tetrastigma hemsleyanum Diels et Gilg (TH) is one of the new eight Genuine Medicinal Materials of Zhejiang. It has extensive biological activities, such as anti-inflammatory, anti-tumor and analgesic activities, etc. In this study, the chemical components of TH were systematically investigated by ultra high-performance liquid chromatography-tandem quadrupole time of flight mass spectrometry (UPLC/Q-TOF-MS). Based on the MS spectrum, 39 compounds in TH extracts including 14 flavonoids, 10 fatty acids, 5 polyphenols and phenolic acids, 4 terpenes and other compounds were detected and tentatively identified. TH samples were treated under different drying methods (vacuum freeze drying, hot air drying, natural drying, light drying and vacuum drying). Besides, the effect of different drying methods on the content of 10 main chemical constituents in TH extracts including catechin, rutin, kaempferol-3-O-rutinoside and so on was also investigated by targeting metabolomics method with ultra high-performance liquid chromatography-tandem triple quadrupole mass spectrometry (UPLC-MS/MS) assisted by multivariate statistical analysis. Large differences were observed between vacuum drying and vacuum freeze drying with remarkable content changes. The contents of rutin, proanthocyanidin B1 and catechin were the most different among the various drying methods. The systematic identification of chemical constituents is helpful for the further medicinal development and application of TH. The effects of drying methods on the content of TH components were studied, which provided experimental data for the processing, storage and quality control of TH.

Burn Defect and Phenol Prediction for Flavoured Californian-Style Black Olives Using Digital Sensors

Californian-style black olives can undergo different chemical changes during the sterilization process that can affect their sensory and phenol characteristics. Thus, these olives were stuffed with flavoured hydrocolloids and submitted to different thermal sterilization treatments to assess sensory categories. The triangular test indicated that the panellists were able to discriminate between samples from different categories according to their aromas with more than 85% success. The results indicated that the negative aroma detected by tasters was related to burn defects. The highest level of defects was found in standard olives, while the lowest was identified in the extra category. Furthermore, olives submitted to the lowest thermal sterilization treatment (extra) presented significantly higher phenol profile content, such as for hydroxytyrosol, tyrosol, oleuropein and procyanidin B1. The electronic nose (E-nose) discriminated between samples from different categories according to the specific aroma (PC1 = 82.1% and PC2 = 15.1%). The PLS-DA classified the samples with 90.9% accuracy. Furthermore, the volatile organic compounds responsible for this discrimination were creosol, copaene, benzaldehyde and diallyl disulphide. Finally, the models established by the PLS analysis indicated that the E-nose could predict olives according to their aroma and total phenol profile (RCV2 values were 0.89 and 0.92, respectively). Thus, this device could be used at the industrial level to discriminate between olives with different sensory aromas to determine those with the highest quality.

Effects of grape seed-derived proanthocyanidin B2 pretreatment on oxidative stress, endoplasmic reticulum stress and apoptosis of renal tubular epithelial cells in renal ischemia–reperfusion injury model of mice

PurposeTo investigate the effect of grape seed-derived proanthocyanidin B2 (GSPB2) pretreatment on acute renal ischemia–reperfusion injury model of mice.Methods50 mice were divided into 5 groups: Sham group: mice were treated with right nephrectomy. GSPB2 group: GSPB2 was injected intraperitoneally 45 min before right nephrectomy. IRI group: right kidney was resected and the left renal arteriovenous vessel was blocked for 45 min. GSPB2 + IRI group: GSPB2 was intraperitoneally injected 45 min before IRI established. GSPB2 + BRU + IRI group: GSPB2 and brusatol (BRU) were injected intraperitoneally 45 min before IRI established. Creatinine and urea nitrogen of mice were detected, and the kidney morphology and pathological changes of each group were detected by HE staining, PAS staining and transmission electron microscopy. Expressions of Nrf2, HO-1, GRP78, CHOP, and cleaved-caspase3 were detected by immunofluorescence staining and western blotting.ResultsMorphology and mitochondrial damages of kidney in GSPB2 + IRI group were significantly alleviated than those in IRI group. Expression levels of Nrf2 and HO-1 were significantly higher in GSPB2 + IRI group than those in IRI group. Expression levels of GRP78, CHOP and cleaved-caspase3 were significantly lower in GSPB2 + IRI group than those in IRI group. However, compared to GSPB2 + IRI group, protective effects of GSPB2 pretreatment were weakened in GSPB2 + BRU + IRI group.ConclusionsGSPB2 pretreatment could alleviate oxidative stress damage and reduce apoptosis of renal tubular epithelial cells, which might be related to activating the antioxidant system, up-regulating the expression of Nrf2 and HO-1, inhibiting the expressions of GRP78, CHOP and cleaved-caspase3. However, the protective effect could be reversed by brusatol.

Development of an Analytical Workflow to Support the Establishment of Monographs in African Pharmacopoeias - Combretum mucronatum Leaves as Example.

Herbal medicines are invaluable in African medicine, but quality and safety are not documented in many cases. Besides controlled farming, validated quality control methods are needed to ensure identity, purity, and content. Analytical specifications within modern monographs are needed for consistent batch quality. Combretum mucronatum leaves are widely used in West Africa, but state-of-the-art quality control methods and specifications are non-existent. The aim of the following study was the development of ICH-validated chromatographic protocols for identity, purity, content assay, and analytical specifications for consideration into pharmacopoeial monographs. UPLC-ESI-Q-TOF-MS/MS was used for untargeted phytochemical information on composition. Optimisation of extraction was based on phytochemical profiling. HPTLC was used for differentiation of C. mucronatum from other Combretum species and UPLC for simultaneous determination of 7 marker compounds. C. mucronatum batch analyses (n = 49) investigated the influence of harvest time and geographical origin. Pesticides screening from a 349-compound panel were carried out. 30 compounds, identified by LC-MS, were used for characterization of the plant material. Orietin, isoorientin, vitexin and isovitexin were used as specific marker compounds for qualitative and quantitative HPTLC purposes, while UPLC quantified additionally epicatechin, procyanidins B2 and C1. Influence of harvest time and geographic origin on the content of marker compounds was observed. Differences in the metabolite profiles of C. mucronatum compared to related Combretum species were established for quality control purposes. Contamination with high amoounts of chlorpyrifos, and folpet (sum of folpet and phtalimide, expressed as folpet) were also observed.The study provides analytical protocols, analytical specifications and a drafted monograph for consideration for African pharmacopoeias, and reveals potential challenges in the quality of C. mucronatum.

Investigating the induction of polyphenol biosynthesis in the cultured Cycolocarya paliurus cells and the stimulatory mechanism of co-induction with 5-aminolevulinic acid and salicylic acid.

Background: Plant cell culture technology is a potential way to produce polyphenols, however, this way is still trapped in the dilemma of low content and yield. Elicitation is regarded as one of the most effective ways to improve the output of the secondary metabolites, and therefore has attracted extensive attention. Methods: Five elicitors including 5-aminolevulinic acid (5-ALA), salicylic acid (SA), methyl jasmonate (MeJA), sodium nitroprusside (SNP) and Rhizopus Oryzae Elicitor (ROE) were used to improve the content and yield of polyphenols in the cultured Cyclocarya paliurus (C. paliurus) cells, and a co-induction technology of 5-ALA and SA was developed as a result. Meanwhile, the integrated analysis of transcriptome and metabolome was adopted to interpret the stimulation mechanism of co-induction with 5-ALA and SA. Results: Under the co-induction of 50 μM 5-ALA and SA, the content and yield of total polyphenols of the cultured cells reached 8.0 mg/g and 147.12 mg/L, respectively. The yields of cyanidin-3-O-galactoside, procyanidin B1 and catechin reached 28.83, 4.33 and 2.88 times that of the control group, respectively. It was found that expressions of TFs such as CpERF105, CpMYB10 and CpWRKY28 increased significantly, while CpMYB44 and CpTGA2 decreased. These great changes might further make the expression of CpF3'H (flavonoid 3'-monooxygenase), CpFLS (flavonol synthase), CpLAR (leucoanthocyanidin reductase), CpANS (anthocyanidin synthase) and Cp4CL (4-coumarate coenzyme A ligase) increase while CpANR (anthocyanidin reductase) and CpF3'5'H (flavonoid 3', 5'-hydroxylase) reduce, ultimately enhancing the polyphenols accumulation Conclusion: The co-induction of 5-ALA and SA can significantly promote polyphenol biosynthesis in the cultured C. paliurus cells by regulating the expression of key transcription factors and structural genes associated with polyphenol synthesis, and thus has a promising application.

Chemical, biological and in silico assessment of date (P. dactylifera L.) fruits grown in Ha'il region.

Background: Dates palm (Phoenix dactylifera L.) fruits are among the most widely used fruits in the Middle East and African nations. Numerous researchers confirmed the presence of phytochemicals in P. dactylifera L. fruit and its by-products with broad-ranging biological activities. Objectives: In the present work, phytochemical and biological assessments of two different cultivars of date fruit (Shishi M1 and Majdool M2 grown in the Ha'il region of Saudi Arabia) have been carried out. Methods: Date fruits were extracted and analyzed by gas chromatography-mass spectrometry (GS-MS),liquid chromatography-mass spectrometry (LC-MS) and Fourier-transform infrared spectroscopy (FT-IR)techniques. The lyophilized methanolic extracts were analyzed for their in-vitro antiproliferative andcytotoxicity against colon cancer (HCT116) cell line. To identify the possible constituents responsible for the bioactivity, in-silico molecular docking and molecular dynamics (MD) simulation studies were carried out. Results: Both cultivars exhibited in-vitro anticancer activity (IC50 = 591.3μg/mL and 449.9μg/mL for M1 and M2, respectively) against colon cancer HCT-116 cells. The computational analysis results indicated procyanidin B2 and luteolin-7-O-rutinoside as the active constituents. Conclusion: Based on these results, we conclude that these cultivars could be a valuable source for developing health promoter phytochemicals, leading to the development of the Ha'il region, Saudi Arabia.

Effect of Antioxidant Procyanidin B2 (PCB2) on Ovine Oocyte Developmental Potential in Response to in Vitro Maturation (IVM) and Vitrification Stress

BACKGROUND: It was demonstrated that external stress, such as in vitro maturation (IVM) and vitrification process can induce significantly reduced development capacity in oocytes. Previous studies indicated that antioxidants play a pivotal part in the acquisition of adaptation in changed conditions. At present, the role of the natural potent antioxidant PCB2 in response to IVM and vitrification during ovine oocyte manipulation has not been explored. OBJECTIVE: To investigate whether PCB2 treatment could improve the developmental potential of ovine oocytes under IVM and vitrification stimuli. MATERIALS AND METHODS: The experiment was divided into two parts. Firstly, the effect of PCB2 on the development of oocytes during IVM was evaluated. Unsupplem ented and 5 μg/mL PCB2 -supplemented in the IVM solution were considered as control and experimental groups (C + 5 μg/mL PCB2). The polar body extrusion (PBE) rate, mitochondrial membrane potential (MMP), ATP, reactive oxygen species (ROS) levels and early apoptosis of oocytes were measured after IVM. Secondly, we further determine whether PCB2 could improve oocyte quality under vitrification stress. The survival rate, PBE rate and early apoptosis of oocytes were compared between fresh group, vitrified group and 5 μg/mL PCB2 -supplemented in the IVM solution after vitrification (V + 5μg/mL PCB2). RESULTS: Compared to the control group, adding PCB2 significantly increased PBE rate (79.4% vs. 62.8%, P < 0.01) and MMP level (1.9 ± 0.08 vs. 1.3 ± 0.04, P < 0.01), and decreased ROS level (47.1 ± 6.3 vs. 145.3 ± 8.9, P < 0.01). However, there was no significant difference in ATP content and early apoptosis. Compared to the fresh group, vitrification significantly reduced oocytes viability (43.0% vs. 90.8%, P < 0.01) as well as PBE rate (24.2% vs. 60.6%, P < 0.05). However, 5 μg/mL PCB2-supplemention during maturation had no effect on survival, PBE or early apoptosis in vitrified oocytes. CONCLUSION: PCB2 could effectively antagonise the oxidative stress during IVM and promote oocyte development.

Comparative Phenolic Profiles of Monovarietal Wines from Different Croatian Regions

The phenolic profile of wines is often used to evaluate their quality and authenticity. The phenolic composition of twenty-five commercial wines produced in different Croatian regions from eight red and nine white grape varieties was studied. A total of twenty-four polyphenols were analyzed using HPLC-DAD and classified into five groups based on their structure: phenolic acids, flavan-3-ols, anthocyanins, flavonoids, and stilbenes. The red wines contained higher concentrations of phenolic constituents than the white wines, of which gallic acid (11.8–90.3 mg/L), procyanidin B1 (13.7–63.8 mg/L), and catechin (10.5–34.5 mg/L) were the most abundant. In contrast to the white wines, great variability was observed in the red wines, with the autochthonous Plavac Mali and Babić showing the most specific phenolic profiles. The most representative phenolic components in the studied Croatian wines showed strong antioxidant activity. Gallic acid proved to be the most effective DPPH (IC50 = 0.33 µg/mL) and NO scavenger (IC50 = 12.36 µg/mL), while myricetin was the most potent inhibitor of lipid peroxidation (IC50 = 1.68 µg/mL). Our research has contributed to the characterization and varietal differentiation of Croatian wines, highlighting those rich in certain polyphenols as potential nutraceuticals.

Bioaccessibility of phenolic compounds from Brazilian grape juices using a digestion model with intestinal barrier passage

Grape juices are rich in bioactive compounds; however, for these compounds to exert their functionality, they must be bioaccessible. Thus, the present study evaluated a simulated digestion process on the main bioactive compounds of monovarietal grape juices of five Brazilian hybrid cultivars (V. vinifera x V. labrusca). Characterization of the chemical profiles in liquid chromatography (HPLC-DAD-RID), behaviour of phenolics in the stages of digestion and bioaccessibility through the INFOGEST protocol plus intestinal barrier passage were carried out. Of the 24 polyphenols identified in the grape juice samples, 11 were bioaccessible, with emphasis on the class of flavanols. Procyanidin B2 (101–426%), (+)-catechin (169–370%) and gallic acid (61–230%) stood out in all juices, showing that these compounds are key to the functionality of these drinks. Particularities were observed to differ between juices, demonstrating that factors such as the cultivar should be explored more extensively in studies on functional foods. The study also suggests that quality components such as sugars and organic acids influence the bioaccessibility of beverages.

Integration of lipidomics and metabolomics approaches for the discrimination of harvest time of green tea in spring season by using UPLC-Triple-TOF/MS coupled with chemometrics

The production season is one of the judgment standards of the green tea quality and spring tea is generally considered of higher quality. Moreover, early spring tea is usually more precious and sells for a higher price. Therefore, a multifaceted strategy that integrates lipidomics and metabolomics, based on UPLC-Triple-TOF/MS coupled with chemometrics, was developed to discriminate early spring green tea (ET) and late spring green tea (LT). Twenty-six lipids and forty-five metabolites were identified as characteristic components. As for characteristic lipids, most of glycerophospholipids and acylglycerolipids have higher contents in ET. By contrast, glycoglycerolipids, sphingolipids and hydroxypheophytin a were shown higher levels in LT samples. Most of the differential metabolites identified were more abundant in ET samples. LT samples have much higher catechin, procyanidin B2, and 3',8-dimethoxyapigenin 7-glucoside contents. Based on the integration of differential lipids and metabolites, the reconstructed orthogonal partial least squares discriminant analysis (OPLS-DA) model displayed 100% correct classification rates for harvest time discrimination of green tea samples. These results demonstrated that the integration of lipidomics and metabolomics approaches is a promising method for the discrimination of tea quality.

Extraction, identification, and starch-digestion inhibition of phenolics from Euryale ferox seed coat.

Euryale ferox is an important cash crop and valuable tonic in traditional medicine. The seeds of E.ferox are rich in starch, which is hard to digest, and the digestion speed is significantly slower than that of rice starch. The goal of this study was to evaluate the effects of E.ferox seed-coat phenolics (EFCPs) on the digestion of E.ferox seed starch. EFCPs were extracted and identified by ultra-high performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry. We optimized the extraction parameters, and the final extraction yield was about 1.49%. We identified seven phenolics from the E.ferox seed-coat extracts: gallic acid, digalloylhexoside, catechin, procyanidin B2, epicatechin, ellagic acid, and epicatechin gallate. Quantitative analysis results showed that the E.ferox seed phenolics mainly distributed in the seed coat and the gallic acid, digalloylhexoside, and epicatechin gallate were three main phenolic compounds. The phenolics displayed strong inhibitory activities on α-glucosidase and α-amylase with an IC50 of 3.25 μg mL-1 and 1.36 mg mL-1 respectively. Furthermore, these phenolics could interact with starch by hydrogen bonds, which might make its starch more difficult to digest. Our investigation suggests that the EFCPs can strongly inhibit the digestion of E.ferox seed starch by inhibiting the α-amylase and α-glucosidase activities and interacting with starch by hydrogen bonds; therefore, E.ferox seeds have a promising application prospect in foods for hypoglycemia. © 2023 Society of Chemical Industry.

Genistein and Procyanidin B2 Reduce Carcinogen-Induced Reactive Oxygen Species and DNA Damage through the Activation of Nrf2/ARE Cell Signaling in Bronchial Epithelial Cells In Vitro.

Cancer is one of the leading causes of death worldwide. Chemotherapy and radiation therapy are currently providing the basis for cancer therapies, although both are associated with significant side effects. Thus, cancer prevention through dietary modifications has been receiving growing interest. The potential of selected flavonoids in reducing carcinogen-induced reactive oxygen species (ROS) and DNA damage through the activation of nuclear factor erythroid 2 p45 (NF-E2)-related factor (Nrf2)/antioxidant response element (ARE) pathway was studied in vitro. Dose-dependent effects of pre-incubated flavonoids on pro-carcinogen 4-[(acetoxymethyl)nitrosamino]-1-(3-pyridyl)-1-butanone (NNKAc)-induced ROS and DNA damage in human bronchial epithelial cells were studied in comparison to non-flavonoids. The most effective flavonoids were assessed for the activation of Nrf2/ARE pathway. Genistein, procyanidin B2 (PCB2), and quercetin significantly suppressed the NNKAc-induced ROS and DNA damage. Quercetin significantly upregulated the phosphorylated protein kinase B/Akt. PCB2 significantly upregulated the activation of Nrf2 and Akt through phosphorylation. Genistein and PCB2 significantly upregulated the phospho-Nrf2 nuclear translocation and catalase activity. In summary, genistein and PCB2 reduced the NNKAc-induced ROS and DNA damage through the activation of Nrf2. Further studies are required to understand the role of dietary flavonoids on the regulation of the Nrf2/ARE pathway in relation to carcinogenesis.

Enhanced UV-B Radiation Induced the Proanthocyanidins Accumulation in Red Rice Grain of Traditional Rice Cultivars and Increased Antioxidant Capacity in Aging Mice

Proanthocyanidins are major UV-absorbing compounds. To clarify the effect of enhanced UV-B radiation on the proanthocyanidin synthesis and antioxidant capacity of traditional rice varieties in Yuanyang terraced fields, we studied the effects of enhanced UV-B radiation (0, 2.5, 5.0, 7.5 kJ·m-2·d-1) on the rice grain morphology, proanthocyanidins content, and synthesis. The effects of UV-B radiation on the antioxidant capacity of rice were evaluated by feeding aging model mice. The results showed that UV-B radiation significantly affected the grain morphology of red rice and increased the compactness of starch grains in the starch storage cells of central endosperm. The content of proanthocyanidin B2 and C1 in the grains was significantly increased by 2.5 and 5.0 kJ·m-2·d-1 UV-B radiation. The activity of leucoanthocyanidin reductase was higher in rice treated by 5.0 kJ·m-2·d-1 than other treatments. The number of neurons in the hippocampus CA1 of mice brain fed red rice increased. After 5.0 kJ·m-2·d-1 treatment, red rice has the best antioxidant effect on aging model mice. UV-B radiation induces the synthesis of rice proanthocyanidins B2 and C1, and the antioxidant capacity of rice is related to the content of proanthocyanidins.

Antimicrobial Potential, Antioxidant Activity, and Phenolic Content of Grape Seed Extracts from Four Grape Varieties

The aim of this study was to evaluate the total phenolic content, composition, and antioxidant and antibacterial activities of four grape seed extracts (Cabernet Sauvignon, Marselan, Pinot Noir, and Tamyanka). The total phenolic content (TPC) and flavonoid, anthocyanin, procyanidin, ascorbic acid, DPPH, and ABTS antioxidant capacities of the grape seed extracts (GSEs) were determined. The extracts showed high TPC values (79.06-111.22 mg GAE/g). The individual components in the GSEs were determined using HPLC. High contents of catechin, epicatechin, and procyanidin B1 were found in the extracts. The antimicrobial activity of the obtained GSEs against Staphylococcus aureus, Bacillus cereus, and Escherichia coli was evaluated using the agar diffusion test and a test to determine the minimum inhibitory concentration (MIC). According to the effect on the growth of pathogens, the extracts were ranked in the following order: Pinot Noir > Marselan > Cabernet Sauvignon > Tamyanka. The tested bacteria showed high sensitivity to the extracts (MIC = 0.12-0.50 mg/mL). According to the MIC values, the bacteria were in the following order: S. aureus > B. cereus > E. coli. A correlation was found between the phenolic content of the GSEs and their antibacterial potential. The obtained results show that the studied GSEs have good potential as antioxidant and antimicrobial agents.

Procyanidin B2 3,3″-di-O-gallate suppresses IFN-γ production in murine CD4+ T cells through the regulation of glutamine influx via direct interaction with ASCT2.

Excessive activation of CD4+ T cells increases cytokine production substantially and induces immune-mediated diseases. Procyanidins are polyphenols with anti-inflammatory properties. Procyanidin B2 (PCB2) gallate [specifically, PCB2 3,3''-di-O-gallate (PCB2DG)] inhibits cytokine production through the suppression of glycolysis via mammalian target of rapamycin (mTOR) in T cells. Several amino acids play critical roles in T cell activation, especially glutamine, which is important in mTOR signaling and interferon-γ (IFN-γ) production in CD4+ T cells. However, the mechanisms underlying the effects of PCB2DG, including its interaction partners, have yet to be clarified. In the present study, the mechanisms underlying the inhibitory effect of PCB2DG on IFN-γ through glutamine metabolism regulation were investigated. We found that PCB2DG treatment reduced intracellular glutamine levels in CD4+ T cells, whereas the addition of glutamine abrogated the inhibitory effects of PCB2DG on IFN-γ production. The PCB2DG-induced reduction in intracellular glutamine accumulation led to the upregulated expression of activating transcription factor 4, which was induced by the cytoprotective signaling pathway in the amino acid response. In addition, the mRNA and protein expression levels of alanine serine cysteine transporter 2 (ASCT2), a major glutamine transporter in CD4+ T cells, were not altered by PCB2DG treatment. Further analysis using a target identification strategy revealed that PCB2DG binds to ASCT2, suggesting that PCB2DG interacts directly with this major glutamine transporter to inhibit glutamine influx. Overall, this study indicates that ASCT2 is a novel target protein of a dietary polyphenol and provides new insights into the mechanism underlying the immunomodulatory effects of polyphenols.