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Fermentation is used not only to preserve food but also to enhance its beneficial effects on human health and achieve functional foods. This study aimed to investigate how different treatments (spontaneous fermentation or fermentation with the use of starter culture) affect phenolic content, antioxidant potential, and cholinesterase inhibitory activity in different kale cultivars: 'Halbhoner Grüner Krauser', 'Scarlet', and 'Nero di Toscana'. Chosen samples were further tested for their protective potential against the Caco-2 cell line. HPLC-MS analysis revealed that the fermentation affected the composition of polyphenolic compounds, leading to an increase in the content of rutin, kaempferol, sinapinic, and protocatechuic acids. In general, kale cultivars demonstrated various antioxidant activities, and fermentation led to an increase in total phenolic content and antioxidant activity. Fermentation boosted anti-cholinesterase activity most profoundly in 'Nero di Toscana'. Extracts of spontaneously fermented 'Scarlet' (SS) and 'Nero di Toscana' (NTS) showed cytoprotective properties, as revealed by the malondialdehyde (MDA), lactate dehydrogenase (LDH), superoxide dismutase (SOD), catalase (CAT), and glutathione (GSH) assays. Additionally, strong anti-inflammatory activity of NTS was shown by decreased release of cytokines IL-1ß and TNF-α. Collectively, the conducted studies suggest fermented kale cultivars as a potential source for functional foods.
Assuntos
Antioxidantes , Brassica , Fermentação , Fenóis , Humanos , Antioxidantes/farmacologia , Antioxidantes/química , Antioxidantes/metabolismo , Fenóis/farmacologia , Fenóis/análise , Fenóis/química , Células CACO-2 , Brassica/química , Brassica/metabolismo , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Inibidores da Colinesterase/farmacologia , Cromatografia Líquida de Alta Pressão , Polifenóis/farmacologia , Polifenóis/químicaRESUMO
Evernia prunastri is a lichen widely distributed in the Northern Hemisphere. Its biological properties still need to be discovered. Therefore, our paper focuses on studies of E. prunastri extracts, including its main metabolites evernic acid (EA) or atranorin (ATR). Phytochemical profiles using chromatographic analysis were confirmed. The antioxidant activity was evaluated using in vitro chemical tests and in vitro enzymatic cells-free tests, namely superoxide dismutase (SOD), glutathione peroxidase (GPx), glutathione reductase (GR), and catalase (CAT). The anti-inflammatory potential using cyclooxygenase-2 (COX-2) and hyaluronidase were determined. The neuroprotective potential using acetylcholinesterase, (AChE), butyrylcholinesterase (BChE), and tyrosinase (Tyr) was estimated. The hypoglycemic activity was also confirmed (α-glucosidase). Principal component analysis was performed to determine the relationship between the biological activity of extracts. The inhibitory effect of EA and ATR on COX-2 AChE, BChE, Tyr, and α-glucosidase was evaluated using molecular docking techniques and confirmed for EA and ATR (besides α-glucosidase). The penetration of EA and ATR from extracts through the blood-brain barrier was confirmed using the parallel artificial membrane permeability assay blood-brain barrier test. In conclusion, depending on chemical surroundings and the concentration, the E. prunastri extracts, EA or ATR, showed attractive pleiotropic properties, which should be further investigated.
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Acetilcolinesterase , Butirilcolinesterase , Hidroxibenzoatos , Parmeliaceae , Ciclo-Oxigenase 2 , Simulação de Acoplamento Molecular , alfa-Glucosidases , Monofenol Mono-OxigenaseRESUMO
The aim of the study was to present the fingerprint of different Lepidium peruvianum tuber extracts showing glucosinolates-containing substances possibly playing an important role in preventinting dementia and other memory disorders. Different phenotypes of Lepidium peruvianum (Brassicaceae) tubers were analysed for their glucosinolate profile using a liquid chromatograph coupled with mass spectrometer (HPLC-ESI-QTOF-MS/MS platform). Qualitative analysis in 50% ethanolic extracts confirmed the presence of ten compounds: aliphatic, indolyl, and aromatic glucosinolates, with glucotropaeolin being the leading one, detected at levels between 0-1.57% depending on phenotype, size, processing, and collection site. The PCA analysis showed important variations in glucosinolate content between the samples and different ratios of the detected compounds. Applied in vitro activity tests confirmed inhibitory properties of extracts and single glucosinolates against acetylcholinesterase (AChE) (15.3-28.9% for the extracts and 55.95-57.60% for individual compounds) and butyrylcholinesterase (BuChE) (71.3-77.2% for the extracts and 36.2-39.9% for individual compounds). The molecular basis for the activity of glucosinolates was explained through molecular docking studies showing that the tested metabolites interacted with tryptophan and histidine residues of the enzymes, most likely blocking their active catalytic side. Based on the obtained results and described mechanism of action, it could be concluded that glucosinolates exhibit inhibitory properties against two cholinesterases present in the synaptic cleft, which indicates that selected phenotypes of L. peruvianum tubers cultivated under well-defined environmental and ecological conditions may present a valuable plant material to be considered for the development of therapeutic products with memory-stimulating properties.
Assuntos
Lepidium , Acetilcolinesterase , Butirilcolinesterase , Inibidores da Colinesterase/farmacologia , Glucosinolatos/análise , Lepidium/química , Simulação de Acoplamento Molecular , Fenótipo , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Espectrometria de Massas em TandemRESUMO
The biological activity of an in vitro digested infusion of Epilobium angustifolium (fireweed) was examined in a model system of intestinal epithelial and colon cancer tissues. The content of selected phenolic compounds in the digested aqueous extract of fireweed was determined using HPLC-ESI-QTOF-MS/MS. Biological activity was examined using the human colon adenocarcinoma cell lines HT-29 and CaCo-2 and the human colon epithelial cell line CCD 841 CoTr. Cytotoxicity was assessed by an MTT assay, a Neutral Red uptake assay, May-Grünwald-Giemsa staining, and a label-free Electric Cell-Substrate Impedance Sensing cytotoxicity assay. The effect of the infusion on the growth of selected intestinal bacteria was also examined. The extract inhibited the growth of intestinal cancer cells HT-29. This effect can be attributed to the activity of quercetin and kaempferol, which were the most abundant phenolic compounds found in the extract after in vitro digestion. The cytotoxicity of the fireweed infusion was dose-dependent. The highest decrease in proliferation (by almost 80%) compared to the control was observed in HT-29 line treated with the extract at a concentration of 250 µg/mL. The fireweed infusion did not affect the growth of beneficial intestinal bacteria, but it did significantly inhibit E. coli. The cytotoxic effect of the fireweed extract indicates that it does not lose its biological activity after in vitro digestion. It can be concluded that the fireweed infusion has the potential to be used as a supporting agent in colon cancer therapy.
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Antineoplásicos Fitogênicos/química , Epilobium/química , Extratos Vegetais/química , Polifenóis/química , Antineoplásicos Fitogênicos/farmacologia , Células CACO-2 , Proliferação de Células/efeitos dos fármacos , Células HT29 , Humanos , Neoplasias/tratamento farmacológico , Extratos Vegetais/farmacologia , Polifenóis/farmacologiaRESUMO
This work aims to assess the recently established anti-inflammatory and antioxidant potential of melatonin of plant origin extracted from the plant matrix as a phytomelatonin complex (PHT-MLT), and compare its activity with synthetic melatonin (SNT-MLT) when used on its own or with vitamin C. For this purpose, a COX-2 enzyme inhibitory activity test, an antiradical activity in vitro and on cell lines assays, was performed on both PHT-MLT and SNT-MLT products. COX-2 inhibitory activity of PHT-MLT was found to be ca. 6.5 times stronger than that of SNT-MLT (43.3% and 6.7% enzyme inhibition, equivalent to the activity of acetylsalicylic acid in conc. 30.3 ± 0.2 and 12.0 ± 0.3 mg/mL, respectively). Higher antiradical potential and COX-2 inhibitory properties of PHT-MLT could be explained by the presence of additional naturally occurring constituents in alfalfa, chlorella, and rice, which were clearly visible on the HPLC-ESI-QTOF-MS fingerprint. The antiradical properties of PHT-MLT determined in the DPPH test (IC50 of 21.6 ± 1 mg of powder/mL) were found to originate from the presence of other metabolites in the 50% EtOH extract while SNT-MLT was found to be inactive under the applied testing conditions. However, the antioxidant studies on HaCaT keratinocytes stimulated with H2O2 revealed a noticeable activity in all samples. The presence of PHT-MLT (12.5, 25 and 50 µg/mL) and vitamin C (12.5, 25 and 50 µg/mL) in the H2O2-pretreated HaCaT keratinocytes protected the cells from generating reactive oxygen species. This observation confirms that MLT-containing samples affect the intracellular production of enzymes and neutralize the free radicals. Presented results indicated that MLT-containing products in combination with Vitamin C dosage are worth to be considered as a preventive alternative in the therapy of various diseases in the etiopathogenesis, of which radical and inflammatory mechanisms play an important role.
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Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Ciclo-Oxigenase 2/metabolismo , Queratinócitos/citologia , Melatonina/farmacologia , Anti-Inflamatórios/síntese química , Anti-Inflamatórios/química , Antioxidantes/síntese química , Antioxidantes/química , Ácido Ascórbico/farmacologia , Linhagem Celular , Regulação para Baixo , Sinergismo Farmacológico , Radicais Livres/metabolismo , Regulação da Expressão Gênica/efeitos dos fármacos , Humanos , Peróxido de Hidrogênio/efeitos adversos , Queratinócitos/efeitos dos fármacos , Queratinócitos/metabolismo , Melatonina/síntese química , Melatonina/química , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologiaRESUMO
Alzheimer's disease (AD) is a progressive neurodegenerative disease characterized, among others by abnormal levels of acetyl- and butyrylcholinesterase in the brain. In this study, 47 types of Polish honeys were examined (using colorimetric method) as a source of acetyl- and butyrylcholinesterase inhibitors. The highest potential for AChE inhibition was observed in the case of buckwheat honey (39.51% inhibition), while multi-floral honey showed the highest capacity for BChE inhibition (39.76%). Our study revealed that honeys can be a rich source of cholinesterase inhibitors and therefore may play a role in AD treatment.
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Doença de Alzheimer , Mel , Doenças Neurodegenerativas , Acetilcolinesterase , Inibidores da Colinesterase , HumanosRESUMO
In people with metabolic syndrome, obesity and diseases of the cardiovascular system are more often observed. At the basis of the pathogenesis of the metabolic syndrome, chronic inflammation plays a significant role. One of the markers of this process is C-reactive protein (CRP) - one of the indicators of the acute phase of inflammation. The role of other biochemical parameters in obesity has been less well understood. AIM: The aim of the study is to assess the correlation of selected factors of inflammation in obese people and the relevant anthropometric parameters. MATERIALS AND METHODS: 263 patients participated in the study. In all subjects anthropometric measurements (body weight, waist/hip ratio and body mass index) were performed and selected biochemical parameters related to MS were determined. The obtained data were analyzed with the division into three degrees of obesity, taking into account gender and place of residence. RESULTS: The mean C-reactive protein (CRP) concentration was 5,32 ± 14 mg/dl; in women, the highest concentration in 2° of obesity (5mg/dL) and in men in 1-potency (8,41mg/dL). A statistically significant difference in the level of leukocytes between 1° and 3° of obesity in the study group was obtained (p = 0,02). In 3° of obesity in both sexes the highest concentration of monocytes was demonstrated. Positive correlations between leukocyte levels and individual parameters were demonstrated: triglyceride levels (r = 0,134); and the BMI value (r = 0,155); a waist (r = 0,147); and the level of PLT (r = 0,381) and RBC (r = 0,187). CONCLUSIONS: The consequence of obesity is the continuous production of inflammatory factors causing destruction of the body's own tissues. In the present study, CRP values were shown to slightly exceed (p<0,05) above the accepted norm, while the remaining analyzed indicators were within diagnostic standards (in their upper ranges).
Assuntos
Proteína C-Reativa/análise , Inflamação/sangue , Síndrome Metabólica/sangue , Obesidade/sangue , Adolescente , Adulto , Idoso , Idoso de 80 Anos ou mais , Antropometria , Biomarcadores/sangue , Índice de Massa Corporal , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Relação Cintura-Quadril , Adulto JovemRESUMO
This paper explores the ability of Lactobacillus helveticus strains to release sequences of short biologically active peptides (containing 2-10 amino acid residues) from casein. The proteolytic enzymes of the tested strains exhibit different patterns of cleavage of CN fractions. The modification of κ-casein (κ-CN) with pyrrolidone carboxylic acid inhibits the proteolytic activity of strains L. helveticus 141 and the reference strain (DSMZ 20075), while the modification with phosphothreonine inhibits enzymes of all the tested bacteria. The peptide sequencing analysis indicated that the examined strains produced functional peptides very efficiently. κ-CN proved to be the main source of short peptides released by bacterial enzymes, and the hydrolysis of κ-CN yielded eighty-two bioactive peptides. The hydrolysis of αS2-casein, αS1-casein, and ß-casein yielded six, two, and one short-chain bioactive peptides, respectively. The isolated bioactive peptides exhibited antioxidative, opioid, stimulating, hypotensive, immunomodulating, antibacterial, and antithrombotic activities. A vast majority of the isolated bioactive peptides caused inhibition of the angiotensin-converting enzyme and dipeptidyl peptidase IV. The role of hydrolysis products as neuropeptides is also pointed out. The highest number of cleavage sites in κ-casein and functional activities of short-chain peptides were obtained in hydrolyzates produced by L. helveticus strain T105.
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BACKGROUND: The cholinesterase theory stands as the most popular worldwide therapy for Alzheimer's disease (AD). Given the absence of a cure for AD, a plant-based diet has been repeatedly shown as positive in the prevention of AD, including exploring ready-made products in stores and the development of new functional foods. GOAL: This study compared the anti-acetyl- and butyrylcholinesterase activity of thirty-two Polish market soups and five newly formulated soups intended to be functional. Additionally, the research aimed to assess the significance of animal content, distinguishing between vegan and vegetarian options, in cholinesterase inhibition. MATERIALS AND METHODS: The anticholinesterase activity was investigated using a spectrophotometric method, and the inhibitory activity was expressed as % inhibition of the enzyme. The study categorized soups into three groups based on ingredients: those containing animal-derived components, vegetarian soups and vegan soups. RESULTS: Soups exhibited varying levels of activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), indicating differences in their compositions. Composition appeared to be the primary factor influencing anticholinesterase activity, as soups within each group showed significant variability in activity levels. While some commercial soups demonstrated notable anticholinesterase activity, they did not surpass the effectiveness of the optimized soups developed in the laboratory. Certain ingredients were associated with higher anticholinesterase activity, such as coconut, potato, onion, garlic, parsley and various spices and herbs. CONCLUSIONS: Vegetarian and vegan soups exhibited comparable or even superior anticholinesterase activity compared to animal-derived soups, highlighting the importance of plant-based ingredients. The study underscores the need for further research to explore the mechanisms underlying the anticholinesterase activity of soups, including the impact of ingredient combinations and processing methods.
Assuntos
Butirilcolinesterase , Inibidores da Colinesterase , Dieta Vegetariana , Acetilcolinesterase , Humanos , Veganos , Animais , Dieta Vegana , Doença de Alzheimer/tratamento farmacológico , Doença de Alzheimer/prevenção & controle , Vegetarianos , Alimento FuncionalRESUMO
BACKGROUND: As the cholinesterase theory is a prominent hypothesis underlying our current understanding of Alzheimer's disease (AD), the goal of this study was to compose functional vegan lunchtime soups with potential health benefits in the prevention of AD (in the context of cholinesterase inhibition). MATERIALS AND METHODS: The potential of 36 edible plant raw materials in terms of acetyl- and butyrylcholinesterase inhibition was investigated using a 96-well microplate reader. The most promising ingredients were combined to obtain 18 palatable vegetable soup recipes with 6 dominant flavor, appearance, and aroma variants. To shortlist candidates for in-depth analysis and potential consideration in industrial production, our team performed a sensory analysis of the soups. RESULTS: The white boletus soup exhibited the highest potential for cholinesterase inhibition, further bolstered by the inclusion of other ingredients known for their elevated capacity to inhibit both AChE and BChE. Ingredients such as blackthorn (Prunus spinosa), garlic, and white potato contributed significantly to this inhibitory effect (nearly 100% of AChE inhibition). Notably, intriguing results were also observed for asparagus soup, despite the fact that the inhibitory potential of asparagus itself is negligible compared to other raw materials. The success of the asparagus soup lies in the meticulous selection of various ingredients, each contributing to its overall effectiveness. It was observed that mushroom soups scored the highest in this respect, while the team members' response to nettle soup was the least favorable. CONCLUSION: The outcomes of our study should serve as a catalyst for further exploration of this important research domain. Our current research focuses on deeper insights into the potential of comprehensive meal options. Furthermore, the synergy/antagonism/non-interaction between respective soup ingredients as well as elements of individual soups' chemical composition is a very interesting topic currently under our intensive scientific investigation.
Assuntos
Doença de Alzheimer , Butirilcolinesterase , Inibidores da Colinesterase , Doença de Alzheimer/prevenção & controle , Inibidores da Colinesterase/farmacologia , Humanos , Butirilcolinesterase/metabolismo , Acetilcolinesterase/metabolismo , Plantas Comestíveis/químicaRESUMO
Coffee is the most consumed beverage in the world. Consumption of phenolic compounds present in coffee protects the body against oxidative stress generation, inflammatory response, and cancer development. The aim of the study was evaluation of biological activity of coffee extracts (obtained from green, as well as light and dark roasted Robusta and Arabica beans) and isolated fractions on human colon adenocarcinoma Caco-2 cells, which are used as a cellular model of intestinal barrier in bioavailability studies. Additionally, impact of coffee phenolics on oxidative stress level and anti-inflammatory activity has been studied with RAW 264.7 macrophages used in immunomodulatory research. It was demonstrated that the coffee constituents protection against oxidative stress, lipotoxicity and secretion of proinflammatory mediators is correlated with the presence of mono- and dichlorogenic acids and roasting process. It was demonstrated that coffee phytochemicals can decrease cells proliferation and bind to topoisomerase IIα being a dietary tool in cancer prevention.
RESUMO
SCOPE: Bilberry, bananas, and apples are used for smoothie production because the health-promoting activities and to prevent human diseases including neurodegenerative disorders. The smoothie is prepared to promote a promising practice for increasing the intake of fruit in the diet. METHODS AND RESULTS: The smoothie is packed into dark glass jars, pasteurized, and stored for up to 4 months at 4 or 22 °C. Then, it is analyzed for the polyphenols profile using liquid chromatography-high resolution mass spectometry (LC-HRMS) Polyphenols content and the antiinflammatory, anticholinesterase, and antioxidant activities, and the impact on catalase activity are controlled using biochemical analyses. A significant decrease in the flavanol content (p < 0.05) is investigated, while there are lower decreases or no changes in the other polyphenols content in the smoothies stored at 4 °C. The changes in the anticholinesterase and antioxidant activities of the smoothie are correlated with the total polyphenols, anthocyanins, flavonols, and tannins content. CONCLUSION: The proposed preservation of the smoothie and its storage at refrigeration temperature is adequate to maintain the smoothie's nutritional and functional effect for a 4-month shelf life. Even significant changes in the content of individual subgroups of polyphenols are not drastically reflected in the decrease of the smoothie biological activities.
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Antioxidantes , Frutas , Polifenóis , Espectrometria de Massas em Tandem , Polifenóis/análise , Polifenóis/farmacologia , Frutas/química , Espectrometria de Massas em Tandem/métodos , Antioxidantes/análise , Antioxidantes/farmacologia , Cromatografia Líquida/métodos , Inibidores da Colinesterase/farmacologia , Espectrometria de Massa com Cromatografia LíquidaRESUMO
The presence of nanoparticle fractions (<100 nm, NPs) in the food additive TiO2 (E171) rises concerns about its potential harmful impact on human health. The knowledge about the interaction of TiO2 NPs with food components is limited to proteins or polyphenols. The present paper is the first to report on interactions between TiO2 NPs and high molecular pectins that form gels in boluses and are remain nearly intact during digestion until they reach the colon. Direct interactions were studied using Fourier Transform Infrared Spectroscopy while indirect ones were monitored by measuring the "absorption" of TiO2 using a 0.2 microfiltration membrane, during in vitro digestion in a model of the gastro-intestinal tract. The FT-IR spectra registered for pectin-TiO2 NPs solutions confirmed changes in band intensities at 1020, 1100, 1610, and 1740 cm-1, suggesting interactions taking place mainly via the COO- groups. Furthermore, the I(1020)/I(1100) ratio was decreased (C-O stretching vibrations), suggesting partial blocking of the skeletal vibrations caused by interactions between pectin and TiO2. The modelled in vitro digestions confirmed that the "availability" of Ti was reduced when TiO2 NPs were combined with pectin, as compared to TiO2 NPs "digested" alone.
Assuntos
Trato Gastrointestinal , Nanopartículas , Pectinas , Titânio , Titânio/química , Pectinas/química , Espectroscopia de Infravermelho com Transformada de Fourier , Trato Gastrointestinal/metabolismo , Nanopartículas/química , Digestão , Humanos , Modelos Biológicos , Aditivos Alimentares/químicaRESUMO
In the present study, the effect of the addition of quince and collagen type I and III to dessert chocolate on its functional properties was determined. The study evaluated the antioxidant potential of the tested formulations using the FRAP method and the linoleic acid oxidation test and beta-carotene bleaching test. The tested samples were also evaluated for inhibitory activity against enzymes important in preventive health (inflammation and neurodegenerative disorders) namely: AChE, BChE, GR, GPx, COX, and SOD. The addition of quince and collagen to the chocolate samples resulted in higher activity compared to the control sample, as indicated by the FRAP test. The experiment highlighted the impact of including quince fruit on the antioxidant activity of the chocolate samples. Interestingly, merely increasing the quince fruit amount did not consistently enhance antioxidant potential. Specifically, chocolate samples with a lower proportion of quince fruit (2 g/100 g) exhibited greater antioxidant activity when supplemented with collagen I. Conversely, in samples with higher quince percentages (3 g and 4 g), those enriched with collagen III showed higher antioxidant activity. Similar correlations were observed in the linoleic acid oxidation test. Notably, samples containing 3 g and 4 g of quince and type III collagen demonstrated statistically similar highest antioxidant properties. Regardless of the collagen type used, there was no observed increase in activity towards the tested enzymes for samples with the lowest percentage of quince fruit. Both collagen types exhibited the highest activity in the inhibition assay against acetylcholinesterase and butyrylcholinesterase when combined with 3 g and 4 g of quince. Overall, the experimental incorporation of both fruit and collagen enhanced the chocolates' activity. Similarly to the antioxidant activity findings, chocolates with lower quince fruit quantities showed increased activity when supplemented with collagen III, while those with higher quince content (3 g and 4 g) displayed higher activity with collagen I. Bitter chocolate by itself is an attractive food product, rich in many bioactive compounds. However, enriching it with other attractive raw materials can make its properties and taste even more attractive.
Assuntos
Antioxidantes , Chocolate , Rosaceae , Chocolate/análise , Antioxidantes/farmacologia , Animais , Rosaceae/química , Colágeno , Inflamação/prevenção & controle , Frutas/química , Suínos , Oxirredução/efeitos dos fármacosRESUMO
The ability of 36 phenolic acids and their derivatives to inhibit acetyl- and butyrylcholinesterase was studied. The most efficient acetylcholine inhibitors were: carnosic acid = gentisic acid > 3-hydroxy-4-methoxycinnamic acid = ethyl ferulate = ethyl vanillate = nordihydroguaiaretic acid > ethyl 4-hydroxybenzoate = methyl ferulate. The order of effectiveness towards butyrylcholinesterase was: carnosic acid > nordihydroguaiaretic acid = ethyl ferulate > salicylic acid > gentisic acid > rosmarinic acid = caftaric acid > homogentisic acid. The inhibitory activity was dependent on the number/position of OH or/and OCH3 groups attached to a phenol ring. It can be speculated that OCH3 substitution in the phenol ring can promote a higher antibutyrylcholinesterase activity (although not statistically confirmed at p < 0.05). The presence of a CH=CH-COOH group had a highly favourable effect on the antiacetylcholinesterase activity compared with a CH2-CH2-COOH or a COOH group. Methyl and ethyl esters were more potent inhibitors than the corresponding free acids. The molecular weight of the compounds (in the range of M = 154.12 - 474 g/mol) played a minor role in this context.
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Inibidores da Colinesterase/farmacologia , Hidroxibenzoatos/farmacologia , Avaliação Pré-Clínica de MedicamentosRESUMO
Lactobacillus rhamnosus E/N is a probiotic bacterium, which synthesizes exopolysaccharides (EPS) with significant bifidogenic and antioxidant activities. The sugar composition of the EPSs produced depended on carbohydrates used as a carbon source in the growth media. Five Bifidobacterium strains were tested in vitro for their ability to utilize all the EPSs studied. The highest bifidogenic activity was revealed by EPSs obtained from Lactobacillus cultures supplemented with Gal, Lac, and Mal as the only carbon source, while significant antioxidant effects were observed in EPSs isolated from growth media enriched with galactose, lactose, and sucrose.
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Antioxidantes/metabolismo , Carboidratos/química , Carbono/metabolismo , Meios de Cultura/química , Lacticaseibacillus rhamnosus/metabolismo , Polissacarídeos Bacterianos/metabolismo , Metabolismo dos Carboidratos , Carbono/química , Lacticaseibacillus rhamnosus/classificação , Polissacarídeos Bacterianos/química , Fatores de TempoRESUMO
Despite that the applicability of Cu-based engineered nanoparticles (ENPs) as an antibacterial and antifungal agent for plant protection has been studied widely, little is known about their role in the improvement of crop yield and quality. Here, a full life study was performed to investigate the nutritional quality and bioactivity of barley grains under foliar application of nano-/microparticulate (nano-Cu, nano-CuO, micro-Cu) and ionic Cu compounds (CuSO4, CuEDTA). Hordeum vulgaris L. plants were sprayed with Cu compounds at 500 mg/L during the end of tillering and the beginning of heading. Yield, mineral composition, protein and dietary content, antioxidant (phenolic, anthocyanin, flavonoid, tannin, flavanol) content and antioxidant capacity of barley grain were evaluated. Grain yield was unaffected by all treatments. Only nano-Cu and ionic compounds enhanced Cu accumulation in grain: 2-fold increase was observed compared to the control (2.6 µg/kg). Nano-Cu also increased the dietary fiber content by 19.9 %, while no impact of the other treatments was determined. The content of phenolic compounds, the main group of antioxidants, remained unchanged after Cu supply. In general, for all Cu treatment, antiradical and reducing abilities were decreased or were at the similar level in relation to the control. On the other hand, chelating power in grain extracts was 2-4 times higher under nano-Cu/nano-CuO/micro-Cu than in the untreated sample, while the ionic compounds had no impact on the chelating indicator. Our results demonstrated that more favorable effects were triggered by nano-Cu than CuSO4 or CuEDTA on the tested indicators of barley grain, despite that both compounds resulted in similar superior Cu acquisition. It suggests that nano-Cu may be considered as an alternative agent to be used as economic and traditional fertilizers.
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Antioxidantes , Hordeum , Antioxidantes/farmacologia , Antioxidantes/metabolismo , Minerais/metabolismo , Grão Comestível/metabolismo , FenótipoRESUMO
The primary purpose of this work was to design and obtain a series of curcuminoid chalcone-NSAID hybrid derivatives. The ester-type hybrid compounds with ibuprofen (i), ketoprofen (ii), and naproxen (iii) were obtained in two ways, using the Claisen-Schmidt reaction and the Steglich esterification reaction. The designed molecules were successfully synthesised, and FT-IR, MS, and NMR spectroscopy confirmed their structures. Moreover, the cytotoxic effect of the sonodynamic therapy and the anti-inflammatory, antioxidant, and anticholinergic properties of some curcuminoid chalcones and curcuminoid chalcones hybrids were evaluated. The curcuminoid chalcone derivatives showed promising neuroprotective activity as sonosensitisers for sonodynamic therapy in the studied cell lines. Additionally, the stability of the ester-type hybrid compounds with promising activity was determined. The RP-HPLC method was used to observe the degradation of the tested compounds. Studies have shown that structural isomers of ester-type hybrid compounds (3ai, 3bi) are characterised by a similar susceptibility to degradation factors, i.e., they are extremely unstable in alkaline environments, very unstable in acidic environments, unstable in neutral environments, practically stable in oxidising environments, and photolabile in solutions and in the solid phase. These compounds maintain adequate stability in environment at pH 1.2 and 6.8, which may make them good candidates for developing formulations for oral administration.
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Butyrylcholinesterase (BChE) is a major enzyme from the alpha-glycoprotein family that catalyzes the hydrolysis of neurotransmitter acetylcholine (ACh), lowering the concentration of ACh in the nervous system, which could cause aggravation of Alzheimer's disease (AD). In select pathological conditions, it is beneficial to reduce the activity of this enzyme. The aim of this study was to evaluate the degree of BChE inhibition by coffee extracts fractionated into mono- and diesters of caffeic acid/caffeine, digested in vitro in the gastrointestinal tract. The bioactive compounds from coffee showed high affinity for BchE, -30.23--15.28 kJ/mol, and was the highest for the caffeine fraction from the green Arabica extract. The isolated fractions were highly effective in inhibiting BChE activity at all in vitro digestion phases. It has been shown that the fractionation of coffee extracts could be potentially used to obtain high prophylactic or even therapeutic effectiveness against AD.
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Doença de Alzheimer , Butirilcolinesterase , Humanos , Cafeína/farmacologia , Cafeína/uso terapêutico , Calorimetria , Trato Gastrointestinal , Doença de Alzheimer/tratamento farmacológico , Doença de Alzheimer/prevenção & controle , Inibidores da Colinesterase/farmacologia , Inibidores da Colinesterase/química , Simulação de Acoplamento MolecularRESUMO
Food-grade titanium dioxide (TiO2) containing a nanoparticle fraction (TiO2 NPs-nanoparticles) is widely used as a food additive (E171 in the EU). In recent years, questions concerning its effect on the gastrointestinal microbiota have been raised. In the present study, we examined interactions between bacteria and TiO2. The study involved six pathogenic/opportunistic bacterial strains and four different-sized TiO2 types: three types of food-grade E171 compounds and TiO2 NPs (21 nm). Each bacterial strain was exposed to four concentrations of TiO2 (60, 150, 300, and 600 mg/L TiO2). The differences in the growth of the analyzed strains, caused by the type and concentration of TiO2, were observed. The growth of a majority of the strains was shown to be inhibited after exposure to 300 and 600 mg/L of the food-grade E171 and TiO2 NPs.