ABSTRACT
Strategies for successful aging, including the use of food supplements, are part of the approach to support skin youthfulness. To demonstrate the efficacy of fermented bilberry extract (FBE) against skin aging and uneven complexion, a clinical trial was carried out on 66 subjects with visible "crow's feet" wrinkles, mild-to-moderate skin slackness, and uneven skin tone. The wrinkle depth, skin smoothness (Ra) and roughness (Rz), skin firmness (R0) and elasticity (R2), skin coloration (ITA°), and skin antioxidant capacity were measured before and after 28 (D28), 56 (D56), and 84 (D84) days of product use (either FBE or a placebo). These parameters were also integrated with a clinical evaluation, carried out by a dermatologist, and a self-assessment questionnaire to align the measured efficacy with the visual or perceived efficacy. At D84, the wrinkle depth had decreased by 10.6%, Ra had improved by 7.9%, Rz had decreased by 7.3%, R0 had improved by 13.3%, R2 had improved by 12.4%, and skin antioxidant capacity had increased by 20.8%. ITA° increased by 20.8% and was accompanied by a decrease in the skin's redness component by 16.8% and an increase in the lightness component by 2.2%. The variation of all the above-mentioned parameters was statistically significant between the FBE and PL groups. Our findings demonstrate the efficacy of FBE in improving skin aging and complexion evenness.
Subject(s)
Antioxidants , Plant Extracts , Skin Aging , Vaccinium myrtillus , Humans , Skin Aging/drug effects , Antioxidants/pharmacology , Plant Extracts/pharmacology , Female , Vaccinium myrtillus/chemistry , Double-Blind Method , Middle Aged , Adult , Male , Skin/drug effects , Skin Pigmentation/drug effects , Fermentation , Dietary Supplements , Aged , AnthocyaninsABSTRACT
Presbyopia is a global problem with an estimated 1.3 billion patients worldwide. In the area of functional food applications, dietary supplements or herbs, there are very few reports describing the positive effects of their use. In the available literature, there is a lack of studies in humans as well as on an animal model of extracts containing, simultaneously, compounds from the polyphenol group (in particular, anthocyanins) and iridoids, so we undertook a study of the effects of a preparation composed of these compounds on a condition of the organ of vision. Our previous experience on a rabbit model proved the positive effect of taking an oral extract of Cornus mas in stabilizing the intraocular pressure of the eye. The purpose of this study was to evaluate the effect of an orally administered ternary compound preparation on the status of physiological parameters of the ocular organ. The preparation contained an extract of the chokeberry Aronia melanocarpa, the honeysuckle berry Lonicera caerulea L., and the bilberry Vaccinium myrtillus (hereafter AKB) standardized for anthocyanins and iridoids, as bioactive compounds known from the literature. A randomized, double-blind, cross-over study lasting with a "wash-out" period of 17 weeks evaluated a group of 23 people over the age of 50, who were subjects with presbyopia and burdened by prolonged work in front of screen monitors. The group of volunteers was recruited from people who perform white-collar jobs on a daily basis. The effects of the test substances contained in the preparation on visual acuity for distance and near, sense of contrast for distance and near, intraocular pressure, and conjunctival lubrication, tested by Schirmer test, LIPCOF index and TBUT test, and visual field test were evaluated. Anthocyanins (including cyanidin 3-O-galactoside, delphinidin 3-O-arabinoside, cyanidin 3-O-glucoside, cyanidin 3-O-rutinoside, cyanidin 3-O-arabinoside) and iridoids (including loganin, sweroside, loganic acid) were identified as substances present in the extract obtained by HPLC-MS. The preliminary results showed that the composition of AKB applied orally does not change visual acuity in the first 6 weeks of administration. Only in the next cycle of the study was an improvement in near visual acuity observed in 92.3% of the patients. This may indicate potential to correct near vision in presbyopic patients. On the other hand, an improvement in conjunctival wetting was observed in the Schirmer test at the beginning of week 6 of administration in 80% of patients. This effect was weakened in subsequent weeks of conducting the experiment to 61.5%. The improvement in conjunctival hydration in the Schirmer test shows the potential beneficial effect of the AKB formulation in a group of patients with dry eye syndrome. This is the first study of a preparation based on natural, standardized extracts of chokeberry, honeysuckle berry, and bilberry. Preliminary studies show an improvement in near visual acuity and conjunctival hydration on the Schirmer test, but this needs to be confirmed in further studies.
Subject(s)
Lonicera , Photinia , Presbyopia , Vaccinium myrtillus , Animals , Humans , Rabbits , Presbyopia/drug therapy , Anthocyanins , Cross-Over Studies , Visual Acuity , Conjunctiva , IridoidsABSTRACT
Herbivory can be reduced by the production of defense compounds (secondary metabolites), but generally defenses are costly, and growth is prioritized over defense. While defense compounds may deter herbivory, nutrients may promote it. In a field study in boreal forest in Norway, we investigated how simulated herbivory affected concentrations of phenolics (generally a defense) and the carbon/nitrogen (C/N) ratio in annual shoots of bilberry (Vaccinium myrtillus), a deciduous clonal dwarf shrub whose vegetative and generative parts provide forage for many boreal forest animals. We measured concentrations of total tannins, individual phenolics, nitrogen and carbon following several types and intensities of herbivory. We identified 22 phenolics: 15 flavonoids, 1 hydroquinone and 6 phenolic acids. After high levels of herbivory, the total tannin concentration and the concentration of these 22 phenolics together (called total phenolic concentration) were significantly lower in bilberry annual shoots than in the control (natural herbivory at low to intermediate levels). Low-intensive herbivory, including severe defoliation, gave no significantly different total tannin or total phenolic concentration compared with the control. Many individual phenolics followed this pattern, while phenolic acids (deterring insect herbivory) showed little response to the treatments: their concentrations were maintained after both low-intensive and severe herbivory. Contrary to our predictions, we found no significant difference in C/N ratio between treatments. Neither the Carbon:Nutrient Balance hypothesis nor the Optimal Defense hypotheses, theories predicting plant resource allocation to secondary compounds, can be used to predict changes in phenolic concentrations (including total tannin concentration) in bilberry annual shoots after herbivory: in this situation, carbon is primarily used for other functions (e.g., maintenance, growth, reproduction) than defense.
Subject(s)
Hydroxybenzoates , Vaccinium myrtillus , Animals , Herbivory , Tannins , Phenols , Carbon , NitrogenABSTRACT
The aim of the present study was to evaluate microwave-assisted (MAE) and pressurized liquid extraction (PLE) for the recovery of polyphenols from blackcurrant and bilberry leaves and the preservation of their antioxidant activity. The extractions were carried out varying the solvent/solid (SS) ratio, temperature and time. During MAE, increasing the SS ratio increased the polyphenol concentration in the extracts from blackcurrant and bilberry leaves, while increasing the temperature had a positive effect only on bilberry polyphenols. During PLE, only a temperature increase was a determining factor for the isolation of blackcurrant leave polyphenols. Based on polyphenol recovery, optimal extraction parameters were established resulting in a yield of 62.10 and 56.06 mg/g dw in the blackcurrant and bilberry MAE extracts and 78.90 and 70.55 mg/g dw in the PLE extracts. The optimized extracts were profiled by UPLC ESI MS2, and their antioxidant capacity was evaluated through FRAP, DPPH, ABTS and ORAC assays. The characterization of the extracts by UPLC ESI MS2 confirmed flavonols as the predominant compounds in both blackcurrant and bilberry leaves, while flavan-3-ols and procyanidins were the main compounds responsible for high antioxidant capacity as confirmed by the ABTS and ORAC assays. Due to the extract composition and antioxidant capacity, PLE proved to be a technique of choice for the production of blackcurrant and bilberry leave extracts with high potential for use as value-added ingredients in the food and nutraceutical industry.
Subject(s)
Benzothiazoles , Polyphenols , Sulfonic Acids , Vaccinium myrtillus , Polyphenols/chemistry , Antioxidants/chemistry , Microwaves , Solvents/chemistry , Plant Extracts/chemistryABSTRACT
Seven new polyketides including three chromone derivatives (1-3) and four linear ones incorporating a tetrahydrofuran ring (4-7), along with three known compounds (8-10), were obtained from the fermentation of an endophytic fungus (Chaetomium sp. UJN-EF006) isolated from the leaves of Vaccinium bracteatum. The structures of these fungal metabolites have been elucidated by spectroscopic means including MS, NMR and electronic circular dichroism. A preliminary anti-inflammatory screening with the lipopolysaccharide (LPS) induced RAW264.7â cell model revealed moderate NO production inhibitory activity for compounds 1 and 4. In addition, the expression of three LPS-induced inflammatory factors IL-6, iNOS and COX-2 was also blocked by 1 and 4.
Subject(s)
Chaetomium , Polyketides , Vaccinium myrtillus , Chaetomium/chemistry , Polyketides/chemistry , Lipopolysaccharides/pharmacology , Molecular StructureABSTRACT
Exercise-induced muscle damage is common in athletes and recreational exercisers and can lead to muscle soreness, weakness, and impaired muscle function. The precise mechanisms are unclear but oxidative stress and inflammation are thought to play a role. (Poly)phenols are substances abundant in Vaccinium berries that have been suggested to possess antioxidant and anti-inflammatory effects that could help improve exercise performance and/or recovery from exercise. The objective of this systematic review was to evaluate the benefits of Vaccinium berry supplementation on exercise performance and recovery, as well as on exercise-induced oxidative and inflammatory biomarkers in healthy individuals. A comprehensive search was conducted in PubMed, ProQuest Medline, Web of Science, Cochrane Library, and Scopus. Studies were included if the participants were healthy individuals who were supplemented with any Vaccinium berry or Vaccinium berry-based products in comparison to a control group. Of the 13 articles included in this review, no significant differences in the exercise performance were found and only one study reported benefits for markers of recovery. Interleukins and c-reactive protein were the most frequently reported biomarkers, but there was limited evidence that Vaccinium berry supplementation impacted them post-exercise. Most studies were of high quality and showed a low risk of bias. Vaccinium berry supplementation is not effective in modulating markers of exercise-induced inflammation and oxidative distress in healthy individuals; nevertheless, more studies are required to evaluate their effects on exercise performance and recovery in this population.
Subject(s)
Blueberry Plants , Vaccinium macrocarpon , Vaccinium myrtillus , Vaccinium , Humans , Antioxidants/pharmacology , Biomarkers , Dietary Supplements , Fruit , Inflammation/drug therapy , Oxidative StressABSTRACT
Since Tang dynasty in China, the fresh leaves of Vaccinium bracteatum (VBL) have been applied as natural pigment to produce black rice. However, detailed information on its biosynthetic mechanism still remained unclear. Following rice dyeing capacity assay, vaccinoside, one of iridoid glycosides, was identified as the key active compound. Increased methodical research demonstrated vaccinoside as a distinct bifunctional precursor, which could be catalyzed by polyphenol oxidase or ß-glucosidase independently, followed by reaction with 15 amino acids to give blue pigments (VBPs; λmax 581-590 nm) of different hues. Two synthetic pathways of VBPs were proposed, using multiple techniques such as HPLC, HPSEC, UV-Vis spectrum and colorimeter as analysis tools. Black rice was interpreted to be prepared by cooking, using vaccinoside, intrinsic enzymes from fresh VBL and rice protein in combination. These findings promote the understanding of VBP formation mechanisms and provide an efficient method of producing novel Vaccinium blue pigments.
Subject(s)
Vaccinium myrtillus , Vaccinium , Vaccinium/chemistry , Vaccinium myrtillus/chemistry , Plant Extracts/chemistry , Iridoid Glycosides , ChinaABSTRACT
Vaccinium uliginosum L. (commonly known as bog bilberry) and Vaccinium myrtillus L. (commonly known as bilberry) are species of the genus Vaccinium (family Ericaceae). The red-purple-blue coloration of blueberries is attributed largely to the anthocyanins found in bilberries. Anthocyanins, known for their potent biological activity as antioxidants, have a significant involvement in the prophylaxis of cancer or other diseases, including those of metabolic origin. Bilberry is the most important economically wild berry in Northern Europe, and it is also extensively used in juice and food production. A review of the latest literature was performed to assess the composition and biological activity of V. uliginosum and V. myrtillus. Clinical studies confirm the benefits of V. uliginosum and V. myrtillus supplementation as part of a healthy diet. Because of their antioxidant, anti-inflammatory, anti-cancer, and apoptosis-reducing activity, both bog bilberries and bilberries can be used interchangeably as a dietary supplement with anti-free radical actions in the prevention of cancer diseases and cataracts, or as a component of sunscreen preparations.
Subject(s)
Blueberry Plants , Vaccinium myrtillus , Anthocyanins/pharmacology , Functional Food , Fruit , Antioxidants/pharmacology , Plant Extracts/pharmacologyABSTRACT
The purpose of this study was to investigate the differences between the phenolics compositions of bilberry and blueberry liqueurs, to determine whether these are comparable. Both bilberry and blueberry liqueurs have the same name on the market, however they differ in phenolic composition and content. A total of 43 compounds were identified, 36 in the bilberry liqueur, and 21 in the blueberry liqueur. High performance liquid chromatography coupled with mass spectrometry (HPLC-MS) was used to identify and quantify these compounds, where they were fragmented to the MS4 fragments. Anthocyanins were the major phenolics group detected in the bilberry liqueurs, but only the second most abundant phenolics group in the blueberry liqueurs. The most abundant phenolics group in the blueberry liqueurs was hydroxycinnamic acids. The lowest content of individual phenolic compounds was for blueberry liqueur made from whole fruit. This study will provide valuable data to consumers in their choice of a more expensive bilberry liqueur or a cheaper blueberry liqueur.
Subject(s)
Blueberry Plants , Vaccinium myrtillus , Chromatography, High Pressure Liquid , Vaccinium myrtillus/chemistry , Blueberry Plants/chemistry , Anthocyanins/analysis , Phenols/analysis , Mass SpectrometryABSTRACT
(1) Background: The study aimed to investigate the impact of gold nanoparticles capped with Cornus sanguinea (NPCS) and mixed with a fruit extract (Vaccinum myrtillus L.-VL) on human hepatic stellate cells (LX-2) exposed to TGF-ß. (2) Methods: NPCS were characterized by UV-Vis, transmission electron microscopy (TEM), zeta potential measurement, X-ray diffraction (XRD) and energy dispersive spectroscopy (EDX). The cytotoxic effects of VL, NPCS and of the hybrid compounds obtained by mixing the two components in variable proportions (NPCS-VL) were assessed. LDH activity, MDA levels, secretion of inflammation markers, the expression of fibrogenesis markers and collagen I synthesis were estimated after treating the cells with a mixture of 25:25 µg/mL NPCS and VL. (3) Results: TEM analysis showed that NPCS had spherical morphology and homogenous distribution, while their formation and elemental composition were confirmed by XRD and EDX analysis. TGF-ß increased cell membrane damage as well as secretion of IL-1ß, IL-1α and TLR4. It also amplified the expression of α-SMA and type III collagen and induced collagen I deposition. NPCS administration reduced the inflammation caused by TGF-ß and downregulated α-SMA expression. VL diminished LDH activity and the secretion of proinflammatory cytokines. The NPCS-VL mixture maintained IL-1ß, IL-1α, TLR4 and LDH at low levels after TGF-ß exposure, but it enhanced collagen III expression. (4) Conclusions: The mixture of NPCS and VL improved cell membrane damage and inflammation triggered by TGF-ß and mitigated collagen I deposition, but it increased the expression of collagen III, suggestive of a fibrogenetic effect of the hybrid material.
Subject(s)
Cornus , Metal Nanoparticles , Vaccinium myrtillus , Humans , Hepatic Stellate Cells , Transforming Growth Factor beta , Gold/pharmacology , Toll-Like Receptor 4 , Metal Nanoparticles/toxicity , Oxidative Stress , Collagen Type IABSTRACT
Despite its small share of total forest biomass, ground vegetation plays an important role in biogeochemical cycles, being able to modify carbon (C) and nutrients fluxes. Global climate warming may affect plant nutrient uptake and the carbon:nitrogen:phosphorus (C:N:P) stoichiometry, the release of nutrients from the soil and soil organic matter, as well as significantly influence the tree stand nutrient supply. In this context, the response of Norway spruce (Picea abies (L.) H.Karst) stands' ground vegetation to warming is uncertain. An open-top chamber soil-warming simulation, lasting two growing seasons, was conducted in a spruce forest. At the end of each of the two growing seasons, before leaf senescence, European blueberry (Vaccinium myrtillus L.) aboveground biomass (leaves and stems) and mineral topsoil samples were collected from the plots. The C, N, P, micronutrient, and macronutrient concentrations were estimated in the samples. Warming caused significant decreases in C, N, and P in the soil. Warming also decreased the C:P and N:P stoichiometric ratios in the soil and increased the C:P ratio in plant stems. Significant increase in foliar C and decrease in foliar P in warmed plots were observed. The most evident effect was reduction of N and P in the soil, which directly affected the plant C:P and soil N:P stoichiometry. Our results show that warming has caused a significant decrease in the content of some nutrients in the aboveground plant tissues of blueberries. Given that N is a limiting factor of ecosystems productivity, its reduction in the soil caused by warming may be a serious threat to proper nutrient uptake and cause disruption of biogeochemical cycles. The decrease in nutrient content in aboveground tissues due to warming can result in disruptions to physiological processes.
Subject(s)
Blueberry Plants , Picea , Vaccinium myrtillus , Ecosystem , Nutrients , Carbon , NorwayABSTRACT
Polyphenolic extracts from natural sources have received great interest due to their beneficial properties for human health. A method to reduce their variability is to use the design of experiments which allows a limited number of experiments to be performed while exploring the experimental space. Firstly, a 23-full factorial model was used to investigate the polyphenols extraction from wild bilberry leaves. Spectrophotometric data (the content of polyphenols, flavonoids, chlorophyll and radical scavenger activity) and extraction yield were used as responses, and six statistical models were determined depending on the two numerical factors (temperature and alcohol % of ethanol-water mixture) being significant (p < 0.05) in all cases. Numerical optimisation performed by Design Expert 13 software correlates well with the chemical profile determined by high-performance liquid chromatography and the amount of the polyphenol. Afterwards, under the optimised conditions, an extract was prepared in three extraction steps for which composition, chemical stability and antimicrobial properties were evaluated. The antimicrobial potential of the extract was compared with that of the standard compounds (rutin and chlorogenic acid), and the results supported a synergistic effect of the extract components.
Subject(s)
Anti-Infective Agents , Vaccinium myrtillus , Humans , Polyphenols/chemistry , Vaccinium myrtillus/chemistry , Antioxidants/chemistry , Flavonoids/chemistry , Plant Extracts/chemistry , Anti-Infective Agents/pharmacology , Anti-Infective Agents/analysis , Chromatography, High Pressure Liquid/methods , Ethanol/chemistry , Plant Leaves/chemistryABSTRACT
Recently, consumer preferences for bilberries have increased markedly. This fact is probably related to their natural constituents, such as phenolic compounds including anthocyanins and tannins, as well as the vitamins and minerals they contain. Phenolic compounds are known for their numerous beneficial effects on human health. Moreover, bilberry fruits have been shown to inhibit the activity of carbohydrate hydrolyzing enzymes, which can significantly decrease the postprandial increase in blood glucose levels. Thus, the aim of the present study is to investigate the inhibitory effect of Vaccinium myrtillus L. extracts on key enzyme α-amylase, linked to type 2 diabetes. No data have been published on the inhibitory properties of Vaccinium myrtillus L. fruits growing wild in Bulgaria against carbohydrate enzymes. Bilberry extracts were analyzed for total polyphenols, total anthocyanin content, antioxidant activity and their inhibitory properties against α-amylase. The contents of flavonols, anthocyanins and stilbenes were determined by HPLC analysis. The identified flavonols in the analyzed bilberry extracts were mainly represented by quercetin derivatives as rutinoside. The predominant anthocyanins for both aqueous and organic solvents were delphinidin-3-galactoside and malvidin-3-glucoside. The results revealed that bilberry extracts are effective inhibitors of α-amylase, with IC50 values from 20.8 to 194.8 µg GAE/mL. All the samples proved to have antioxidant activity measured by three different in vitro assays (FRAP, CUPRAC and DPPH). The inhibitory properties of V. myrtillus L. extracts may provide a new direction in the development and research of new pharmaceuticals for the suppression of postprandial hyperglycemia in diabetic patients.
Subject(s)
Diabetes Mellitus, Type 2 , Salivary alpha-Amylases , Vaccinium myrtillus , Humans , Vaccinium myrtillus/chemistry , Anthocyanins/chemistry , Antioxidants/pharmacology , Antioxidants/analysis , Salivary alpha-Amylases/analysis , Phenols/chemistry , Plant Extracts/chemistry , Fruit/chemistryABSTRACT
BACKGROUND: Herbal medicinal products containing Vaccinium myrtillus L. (bilberry) fruits and fruit extracts are widely available in the market. Although bilberry leaves and stems are considered as bio-waste, they contain much higher levels of phenolic compounds than fruits. The study aimed to investigate the antimicrobial and anticancer potential of aerial part extracts from Vaccinium myrtillus L. (V. myrtillus, VM) plants harvested at high altitudes in Armenian landscape and characterize the bioactive phytochemicals. MATERIAL AND METHODS: For evaluation of antioxidant properties, chemical-based tests (total phenolic and flavonoid content, and antiradical activity in 2,2'-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) tests) and cellular antioxidant activity (CAA) assay were applied. Genotoxicity and anticancer properties of the extract alone and in combination with fluorouracil were explored in human cancer and normal cell lines. Antibacterial properties of V. myrtillus extract alone and in combination with antibiotics, as well as their effect on proton-flux rate through cell membrane were explored on bacterial strains. The characterization of active phytochemicals was done using Liquid Chromatography-Quadrupole-Orbitrap High-Resolution Mass Spectrometry (LC-Q-Orbitrap HRMS). RESULTS: The V. myrtillus aerial part extract demonstrated promising antioxidant properties in all tests. The selective cytotoxic activity was documented against various cancer cell lines (human colon adenocarcinoma (HT29), human breast cancer (MCF-7) and human cervical carcinoma (HeLa)), while it did not inhibit the growth of tested human normal primary renal mixed epithelial cells (HREC) even at 10-fold higher concentrations. The extract did not have genotoxic properties in comet assay making it a potential source for the development of anticancer preparations. The investigated extract did not directly inhibit the growth of Escherichia coli (E. coli) and Salmonella typhimurium (S. typhimurium) strains at up to 1 mg/mL concentration. However, V. myrtillus extract enhanced the kanamycin intake and increased its efficiency against E. coli strain. The phytochemical characterization of the extract showed the presence of different groups of phenolics. CONCLUSIONS: Based on obtained data, we suggest the aerial parts of the V. myrtillus plant as an alternative source of bioactive natural products for food supplements, nutraceuticals, functional foods and medicine.
Subject(s)
Adenocarcinoma , Colonic Neoplasms , Vaccinium myrtillus , Humans , Vaccinium myrtillus/chemistry , Vaccinium myrtillus/metabolism , Antioxidants/pharmacology , Antioxidants/chemistry , Antioxidants/metabolism , Anti-Bacterial Agents/pharmacology , Escherichia coli , Phenols/analysis , Phenols/chemistry , Phenols/metabolism , Phytochemicals/pharmacology , Phytochemicals/chemistry , Phytochemicals/metabolism , Plant Extracts/pharmacologyABSTRACT
We estimated climate niche shifts and threat levels under various climate change scenarios for Vaccinium myrtillus L. and V. vitis-idaea L. We developed the MaxEnt species distribution models, and predicted future climatic optima for climate change scenarios for 2041-2060 and 2061-2080. The precipitation of the warmest quarter was the most important factor shaping the climatic niches of the studied species. We predicted the largest shifts in climate niches from the present to the 2040-2060 period, with the most pessimistic scenario predicting significant range losses for both species, mainly in Western Europe. Under the most optimistic SSP126 scenario, both species will lose 39 % of their climatic niche for both periods. In the worst-case scenario (SSP585) for 2061-2080, climatic niche contraction will cover 47 % and 39 % of the current climatic niche for V. myrtillus and V. vitis-idaea, respectively. The predicted changes in species distribution could have far-reaching consequences for temperate and boreal forests due to their crucial biocenotic role in forest ecosystems, high potential for carbon sequestration, and prevention of soil erosion. Furthermore, the changes would likely affect the economic potential regarding fruit production and culturally relevant uses of different parts of the plants, mainly fruits.
Subject(s)
Vaccinium myrtillus , Vaccinium vitis-idaea , Vitis , Ecosystem , Climate Change , EuropeABSTRACT
BACKGROUND: Vaccinium bracteatum Thunb. leaves (VBL) are used in traditional herbal medicines to treat various biological diseases. p-coumaric acid (CA), the main active component of VBL, has neuroprotective effects against corticosterone-induced damage in vitro. However, the effects of CA on immobility induced by chronic restraint stress (CRS) in a mouse model and 5-HT receptor activity have not been investigated. HYPOTHESIS/PURPOSE: We investigated the antagonistic effects of VBL, NET-D1602, and the three components of Gαs protein-coupled 5-HT receptors. Additionally, we identified the effects and mechanism of action of CA, the active component of NET-D1602, in the CRS-exposed model. METHODS: For in vitro analyses, we used 1321N1 cells stably expressing human 5-HT6 receptors and CHO-K1 expressing human 5-HT4 or 5-HT7 receptors cell lines to study the mechanism of action. For in vivo analyses, CRS-exposed mice were orally administered CA (10, 50, or 100 mg/kg) daily for 21 consecutive days. The effects of CA were analyzed by assessing behavioral changes using a forced swim test (FST), measuring levels of hypothalamic-pituitary-adrenal (HPA) axis-related hormones in ntial therapeutic effects as 5-HT6 receptor antagonists for neurodegenerative diseases and depressioserum, and acetylcholinesterase (AChE), monoamines, including 5-HT, dopamine, and norepinephrine, using enzyme-linked immunosorbent assay kits. The underlying molecular mechanisms of the serotonin transporter (SERT), monoamine oxidase A (MAO-A), and extracellular signal-regulated kinase (ERK)/protein kinase B (Akt)/mTORC1 signaling were detected using western blotting. RESULTS: CA was confirmed to be an active component in the antagonistic effects of NET-D1602 on 5-HT6 receptor activity through decreases in cAMP and ERK1/2 phosphorylation. Moreover, CRS-exposed mice treated with CA showed a significantly reduced immobility time in the FST. CA also significantly decreased corticosterone, corticotropin-releasing hormone (CRH), and adrenocorticotropic hormone (ACTH) levels. CA enhanced 5-HT, dopamine, and norepinephrine levels in the hippocampus (HC) and prefrontal cortex (PFC) but decreased MAO-A and SERT protein levels. Similarly, CA significantly upregulated the ERK, Ca2+/calmodulin-dependent protein kinase II (CaMKII), Akt/mTOR/p70S6K/S6 signaling pathways in both HC and the PFC. CONCLUSION: CA contained in NET-D1602 may play the antidepressant effects against CRS-induced depression-like mechanism and the selective antagonist effect of 5-HT6 receptor.
Subject(s)
Vaccinium myrtillus , Mice , Humans , Animals , Vaccinium myrtillus/metabolism , Serotonin/metabolism , Proto-Oncogene Proteins c-akt/metabolism , Corticosterone , Dopamine/metabolism , Acetylcholinesterase/metabolism , Receptors, Serotonin/metabolism , Antidepressive Agents/pharmacology , Hypothalamo-Hypophyseal System , Norepinephrine , Monoamine Oxidase/metabolism , Stress, Psychological/drug therapyABSTRACT
The present study aimed at exploring to explore the penoxsulam toxicity and protective effects of blueberry extract in roots of Allium cepa L. The effective concentration (EC50) of penoxsulam was determined at 20 µg/L by the root growth inhibition test as the concentration reducing the root length by 50%. The bulbs of A. cepa L. were treated with tap water, blueberry extracts (25 and 50 mg/L), penoxsulam (20 µg/L) and combination of blueberry extracts (25 and 50 mg/L) with penoxsulam (20 µg/L) for 96 h. The results revealed that penoxsulam exposure inhibited cell division, rooting percentage, growth rate, root length and weight gain in the roots of A. cepa L. In addition, it induced chromosomal anomalies such as sticky chromosome, fragment, unequal distribution of chromatin, bridge, vagrant chromosome and c-mitosis and DNA strand breaks. Further, penoxsulam treatment enhanced malondialdehyde content and SOD, CAT and GR antioxidant enzyme activities. Molecular docking results supported the up-regulation of antioxidant enzyme SOD, CAT and GR. Against all these toxicity, blueberry extracts reduced penoxsulam toxicity in a concentration-dependent manner. The highest amount of recovery for cytological, morphological and oxidative stress parameters was observed when using blueberry extract at a concentration of 50 mg/L. In addition, blueberry extracts application showed a positive correlation with weight gain, root length, mitotic index and rooting percentage whereas a negative correlation with micronucleus formation, DNA damage, chromosomal aberrations, antioxidant enzymes activities and lipid peroxidation indicating its protecting effects. As a result, it has been seen that the blueberry extract can tolerate all these toxic effects of penoxsulam depending on the concentration, and it has been understood that it is a good protective natural product against such chemical exposures.
Subject(s)
Blueberry Plants , Vaccinium myrtillus , Antioxidants/pharmacology , Molecular Docking Simulation , Plant Roots , Onions , Chromosome Aberrations/chemically induced , Plant Extracts/pharmacology , Superoxide Dismutase/genetics , DNA DamageABSTRACT
Wild edible fruits, neglected by the development of commercial agriculture, have recently aroused as a good source of natural colorants and bioactive compounds. These novel uses could cover the recent demand for healthier foods with functional properties. Prunus avium, Fragaria vesca and Vaccinium myrtillus wild fruits were characterized by individual anthocyanin profile and color CIELAB parameters, as well as phenolic fraction. In addition, some bioactivities were evaluated. In P. avium cyanidin-O-deoxyhexosyl-pentoside was the representative anthocyanin, in F. vesca pelargonidin-3-O-glucoside and in V. myrtillus delphinidin-O-hexoside. The three wild edible fruits showed interesting antioxidant activity especially in OxHLIA assays. V. myrtillus was the fruit with the best results for the bacterial growth inhibition, while F. vesca with better fungal growth inhibition. These results evidenced the richness of these wild fruits in bioactive compounds and pigments with antioxidant capacity, therefore, their potential use as natural colorants for healthier food products design.
Subject(s)
Fragaria , Prunus avium , Vaccinium myrtillus , Anthocyanins , Antioxidants/pharmacology , FruitABSTRACT
Anthocyanins have been reported to have potential as dietary or pharmaceutical supplements in the application of cancer prevention and adjunctive treatment. However, there are few studies on the effect of anthocyanins on melanoma, which have only been performed in cell lines. The objective of this work was to investigate the anticancer effects and mechanisms of bilberry anthocyanin extract (BAE) on melanoma In Vitro and In Vivo. Moreover, a primary study was done to investigate how BAE influenced C57BL/6 mice bearing subcutaneous B16-F10 tumors treated with dacarbazine (DTIC). BAE-induced apoptosis in B16-F10 cells was associated with activation of the mitochondrial pathway induced by increased reactive oxygen species. More, In Vivo anticancer activity studies indicated that BAE attenuated melanoma growth, as identified by hematoxylin-eosin staining, Ki-67, and TUNEL assays. Further western blot results revealed higher phospho-Akt expression with the combination of BAE and DTIC, indicating no suppression of the PI3K/AKT signaling pathway. In summary, this study demonstrated the anti-melanoma activity of BAE and investigated its mechanism. Notably, it should be careful to use products enriching BAE for those melanoma patients treated with DTIC.
Subject(s)
Melanoma , Vaccinium myrtillus , Mice , Animals , Dacarbazine , Anthocyanins/pharmacology , Proto-Oncogene Proteins c-akt , Phosphatidylinositol 3-Kinases , Mice, Inbred C57BL , ApoptosisABSTRACT
Traumatic brain injury may trigger the secondary brain injury, which has the potential to be reversible and thus preventable. Anthocyanins are phylotherapeutic plants, which are reported to exhibit anti-inflammatory properties. This study aimed to evaluate the therapeutic efficiency of an anthocyanin, namely Vaccinium myrtillus, to alleviate secondary brain injury and identify possible mechanism of actions. It is hypothesized that lipid peroxidation and Na+ -K+ -ATPase activity may be involved in neuronal ischemia. Thus, brain tissue Malondialdehyde content, Na+ -K+ -ATPase content, and cleaved caspase-3 content was investigated following moderate head trauma in a rat model. Twenty-four Sprague-Dawley male rats were allocated into four groups: Control, Trauma, Solvent-Control, and Treatment. Trauma and Solvent-Control groups showed more prominent brain edema, neuronal ischemia, vascular congestion, increase in brain tissue Malondialdehyde and cleaved caspase-3 levels, and decreased Na+-K+-ATPase activity compared to the Control group. Although the Treatment group had comparable histological signs to the Trauma and Solvent-Control groups, Malondialdehyde level and Na+-K+-ATPase activity was similar to Control group, and cleaved caspase-3 levels were lower compared to Trauma and Solvent-Control groups. We conclude that anthocyanin extracts may alleviate secondary brain injury via anti-oxidative and anti-apoptotic mechanisms.