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Herbal teas are considered as a potential constituent of novel functional beverages consumed daily. One of the commonly used herbal teas is silver birch (Betula pendula Roth) leaf infusion, traditionally used in urinary tract diseases. In this study, the potential of birch leaf infusion as a functional beverage, emphasizing its active ingredients' bioavailability, anti-inflammatory, and antiadhesive properties concerning urinary tract health, was investigated. A complex approach was proposed, which included phytochemical screening, bioavailability, gut microbiota biotransformation, and an in vivo test for urine metabolomics assessment. The bioassays confirmed significant anti-inflammatory (interleukins IL-6 and IL-8 secretion) and anti-adhesive (Uropathogenic Escherichia coli and T24 bladder cells) activities. The high-resolution mass spectrometry metabolomics studies linked gut microbiota metabolites and the metabolites present in the urine. Several metabolites connected with phenolics' consumption were detected in the urine, e.g., glucuronides and sulfates of caffeic acid and dihydroxyphenyl-γ-valerolactones. Based on the presented results, the birch leaf should be considered useful in designing functional beverages, especially targeted to the groups at high risk of urinary diseases.
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Betula , Microbioma Gastrointestinal , Folhas de Planta , Folhas de Planta/química , Betula/química , Humanos , Microbioma Gastrointestinal/efeitos dos fármacos , Microbioma Gastrointestinal/fisiologia , Chás de Ervas , Metabolômica/métodos , Sistema Urinário/microbiologia , Sistema Urinário/metabolismo , Disponibilidade Biológica , Animais , Extratos Vegetais/farmacologia , Anti-Inflamatórios/farmacologia , Masculino , Alimento FuncionalRESUMO
OBJECTIVE: This systematic review aims to analyze the existing literature investigating respiratory functioning in people with Persistent Somatic Symptoms (PSS) compared to healthy controls, to identify patterns of respiratory disturbances by symptom or syndrome, and describe any respiratory outcomes consistent across diagnoses. METHODS: A systematic review following PRISMA guidelines was conducted. A comprehensive search was carried out across five databases (PubMed (NCBI), PsycArticles (Ovid), Web of Science (Core Collection), Embase, and Scopus) using two customised search strings for persistent somatic symptoms and objective respiratory parameters. Title/abstract screening and data extraction were carried out independently by two reviewers. The modified Newcastle-Ottawa Scale was used for quality assessment of the studies. Studies investigating baseline respiratory functioning in adult patients with PSS compared to healthy controls, using at least one objective respiratory were included. RESULTS: 18 studies met the inclusion criteria for the review, with a pooled sample size of n = 3245. Chronic pain conditions were found to be the most prevalent subset of diagnoses of interest, comprising six of the studies. 10 studies included measures of lung capacity, flow and/or volume, nine studies reported measures of ventilation, and four studies investigated respiratory muscle functioning. 13 of the included studies reported significant differences in at least one objective respiratory measure between groups (at rest). Scores on self-reported measures of dysnpea and breathlessness were higher in patients compared to healthy controls, while objective respiratory outcomes were varied. CONCLUSION: The current systematic review is consistent with previous literature suggesting more pronounced experiences of breathlessness in patients with PSS, and significant disparities between reported dyspnea and objective respiratory outcomes. Research investigating the uncoupling between subjective and objective respiratory outcomes is needed to understand the mechanisms behind breathing disturbances in PSS.
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Sintomas Inexplicáveis , Humanos , Estudos Observacionais como Assunto , Transtornos Respiratórios/fisiopatologiaRESUMO
Repetitive transcranial magnetic stimulation (rTMS) is a noninvasive technique that could improve cognitive function. It is being developed as a non-pharmacological intervention to alleviate symptoms of cognitive deterioration. We assessed the efficacy of rTMS in improving cognitive functioning among people with Mild Cognitive Impairment (MCI) in a partially-blinded, sham-controlled randomized trial. Out of 91 subjects screened, 31 participants with MCI (mean age 70.73; SD = 4.47), were randomly assigned to one of three groups: (A) Active rTMS; (B) Active rTMS with Computerized Cognitive Training RehaCom; and (C) Sham control. The study evaluated cognitive function using the DemTect, FAS, and CANTAB tests before and after the stimulation. The following treatment protocol was applied: 2000 pulses at 10 Hz, 5-s train duration, and 25-s intervals at 110% of resting MT delivered over the left Dorsolateral Prefrontal Cortex (DLPFC) five times a week for 2 weeks. After 10 sessions of high-frequency rTMS, there was an improvement in overall cognitive function and memory, assessed by the DemTect evaluation, with no serious adverse effects. Analysis of differences in time (after 10 sessions) between studied groups showed statistically significant improvement in DemTect total score (time by group interaction p = 0.026) in favor of rTMS+RehaCom. The linear regression of CANTAB Paired Associates Learning revealed significant differences in favor of rTMS+RehaCom in three subtests. Our study shows that 10 sessions of rTMS over the left DLPFC (alone as well as combined with Computerized Cognitive Training) can have a positive impact on cognitive function in people with MCI. Further research should investigate the underlying mechanism and determine the optimal parameters for rTMS, which will be important for its efficacy in clinical settings.
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Many Polygonaceae taxa such as Bistorta officinalis, Persicaria amphibia, Persicaria hydropiper, Persicaria lapathifolia, Persicaria maculosa, Persicaria mitis, Polygonum aviculare occur naturally in the entire territory of Poland and are also common in other European countries. Many of these species are also utilised as medicinal plants. In this manuscript we establish the phytochemical profiles of selected taxa from the Polygonaceae focusing on phenolics. Additionally, we try to find chemophenetic markers for the species investigated. Compounds were detected and characterised based on HPLC-DAD-MS data, quantified, and furtherly analysed using multivariate analyses. Chemophenetic markers were identified also considering previous literature.
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Plantas Medicinais , Polygonaceae , Polygonum , Polygonum/química , Cromatografia Líquida de Alta Pressão , Quimiometria , Polygonaceae/química , Plantas Medicinais/química , Fenóis , Extratos Vegetais/químicaRESUMO
BACKGROUND: Clinical research in natural product-based psychopharmacology has revealed a variety of promising herbal medicines that may provide benefit in the treatment of mild mood disorders, however failed to unambiguously indicate pharmacologically active constituents. The emerging role of the microbiota-gut-brain axis opens new possibilities in the search for effective methods of treatment and prevention of mood disorders. PURPOSE: Considering the clinically proven effectiveness juxtaposed with inconsistencies regarding the indication of active principles for many medicinal plants applied in the treatment of anxiety and depression, the aim of the review is to look at their therapeutic properties from the perspective of the microbiota-gut-brain axis. METHOD: A literature-based survey was performed using Scopus, Pubmed, and Google Scholar databases. The current state of knowledge regarding Hypericum perforatum, Valeriana officinalis, Piper methysticum, Passiflora incarnata, Humulus lupulus, Melissa officinalis, Lavandula officinalis, and Rhodiola rosea in terms of their antimicrobial activity, bioavailability, clinical effectiveness in depression/anxiety and gut microbiota - natural products interaction was summarized and analyzed. RESULTS: Recent studies have provided direct and indirect evidence that herbal extracts and isolated compounds are potent modulators of gut microbiota structure. Additionally, some of the formed postbiotic metabolites exert positive effects and ameliorate depression-related behaviors in animal models of mood disorders. The review underlines the gap in research on natural products - gut microbiota interaction in the context of mood disorders. CONCLUSION: Modification of microbiota-gut-brain axis by natural products is a plausible explanation of their therapeutic properties. Future studies evaluating the effectiveness of herbal medicine and isolated compounds in treating mild mood disorders should consider the bidirectional interplay between phytoconstituents and the gut microbiota community.
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Produtos Biológicos , Plantas Medicinais , Animais , Eixo Encéfalo-Intestino , Fitoterapia/métodos , Medicina Herbária/métodosRESUMO
This work aimed to obtain hybrid composites based on photoactive metal oxide and carbon having adsorption properties. The materials, composed of titanium dioxide or zinc oxide and spherical carbon, were obtained from resorcinol-formaldehyde resin, treated in a solvothermal reactor heated with microwaves and then subjected to carbonization, were received. The functional groups of pure carbon spheres (unsaturated stretching C=C, stretching C-OH and C-H bending vibrations), CS/ZnO and CS/TiO2 samples were determined by FT-IR analysis. The characteristic bands for ZnO and TiO2 were observed below 1000 cm-1. The thermal oxidative properties are similar for TiO2- and ZnO-modified carbon spheres. We have observed that the increased carbon sphere content in nanocomposites results in starting the decomposition process at a lower temperature, therefore, nanocomposites have a broader combustion temperature range. The effect of the oxides' addition to carbon spheres on their adsorption properties was evaluated in detail by examining CO2 adsorption from the gas phase. The selectivity of CO2 over N2 at a temperature of 25 °C and pressure of 1 bar (a novelty in testing CS-based sorbents) calculated for 3.00 CS/TiO2 and 4.00 CS/ZnO was 15.09 and 16.95, respectively. These nanocomposites exhibit excellent cyclic stability checked over 10 consecutive adsorption-desorption cycles.
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Porophyllum ruderale subsp. ruderale is a food product used for seasoning in Central and Southern America. The present research aimed to investigate the chemical composition of an extract prepared from aerial parts of P. ruderale using UHPLC-DAD-MS/MS, to isolate and identify major natural products present in the extract, and to furtherly investigate their anti-inflammatory activity in vitro. Twenty-five compounds were detected and characterized using UV-Vis and MS data. All characterized compounds were quantified. Ten major phenolics were isolated and identified by NMR. One previously undescribed natural product was isolated and established as 1-O-(4-hydroxy-3,5-dimethoxy)benzoyl-6-O-galloyl-ß-d-glucose (12). Anti-inflammatory activity was evaluated based on the influence of the extract and isolated compounds on the TLR4-dependent secretion of IL-8 and TNF-α by human primary neutrophils in vitro. Phenolic acids, and caffeic acid derivatives in particular, contributed to the extract's bioactivity.
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Coriandrum , Fenóis , Anti-Inflamatórios/farmacologia , Bolívia , Humanos , Fenóis/isolamento & purificação , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Espectrometria de Massas em TandemRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Phaseaoli pericarpium (bean pods) is a pharmacopeial plant material traditionally used as a diuretic and antidiabetic agents. Diuretic activity of pod extracts was reported first in 1608. Since then Phaseoli pericarpium tea figures in many textbooks as medicinal plant material used by patients. AIM OF THE STUDY: Despite the traditional use of extracts from Phaseolium vulgaris pericarp, limited information is available on bioactivity, chemical composition, and bioavailability of such preparations. The following study aimed to investigate the phytochemical composition, the in vitro permeability of selected extract's constituents over the Caco-2 permeation system, and potential antivirulence activity against uropathogenic Escherichia coli of a hydroalcoholic Phaseoli pericarpium extract (PPX) in vitro to support its traditional use as a remedy used in urinary tract infections. MATERIAL AND METHODS: The chemical composition of the extract PPX [ethanol:water 7:3 (v/v)] investigated by using UHPLC-DAD-MSn and subsequent dereplication. The permeability of compounds present in PPX was evaluated using the Caco-2 monolayer permeation system. The influence of PPX on uropathogenic E. coli (UPEC) strain NU14 proliferation and against the bacterial adhesion to T24 epithelial cells was determined by turbidimetric assay and flow cytometry, respectively. The influence of the extract on the mitochondrial activity of T24 host cells was monitored by MTT assay. RESULTS: LC-MSn investigation and dereplication, indicated PPX extract to be dominated by a variety of flavonoids, with rutin as a major compound, and soyasaponin derivatives. Rutin, selected soyasaponins and fatty acids were shown to permeate the Caco-2 monolayer system, indicating potential bioavailability following oral intake. The extract did not influence the viability of T24 cells after 1.5h incubation at 2 mg/mL and UPEC. PPX significantly reduced the bacterial adhesion of UPEC to human bladder cells in a concentration-dependent manner (0.5-2 mg/mL). Detailed investigations by different incubation protocols indicated that PPX seems to interact with T24 cells, which subsequently leads to reduced recognition and adhesion of UPEC to the host cell membrane. CONCLUSIONS: PPX is characterised by the presence of flavonoids (e.g. rutin) and saponins, from which selected compounds might be bioavailable after oral application, as indicated by the Caco-2 permeation experiments. Rutin and some saponins can be considered as potentially bioavailable after the oral intake. The concentration-dependent inhibition of bacterial adhesion of UPEC to T24 cells justifies the traditional use of Phaseoli pericarpium in the prevention and treatment of urinary tract infections.
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Aderência Bacteriana/efeitos dos fármacos , Phaseolus , Extratos Vegetais/farmacologia , Escherichia coli Uropatogênica/efeitos dos fármacos , Linhagem Celular , Células Epiteliais/metabolismo , Etanol/química , Flavonoides/análise , Flavonoides/farmacologia , Humanos , Permeabilidade/efeitos dos fármacos , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Saponinas/análise , Saponinas/farmacologia , Sementes/química , Solventes/química , Escherichia coli Uropatogênica/fisiologia , Água/químicaRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Solidago virgaurea L. (also known as European goldenrod) is a pharmacopoeial plant material popularly used by patients in the form of an infusion. It was traditionally used in Europe and North America for the treatment of urinary tract conditions. It is also reported as a topical agent for skin disorders. AIM OF THE STUDY: Gut microbiota metabolism plays a crucial role in the bioavailability of natural products contained in plant extracts taken orally. The aim of the current study was to establish the biotransformation of compounds contained in an infusion from goldenrod using human and piglet fecal microbiota in vitro. The permeability of unmetabolized natural products and gut microbiota metabolites was evaluated using a Caco-2 cell model. Preliminary anti-inflammatory assays of raw extract using human neutrophils were also established. MATERIAL AND METHODS: An infusion was prepared from Solidaginis virgaureae herba commercially available on the market. The characterization of the raw extract was performed by UHPLC-DAD-MS method. The infusion was incubated with human or swine fecal samples in anaerobic conditions. Metabolism products were analyzed and identified by UHPLC-DAD-MS technique. The permeability of the natural products contained in the raw infusion and after metabolism was checked by UHPLC method. The influence of raw extracts on proinflammatory functions of human neutrophils after LPS stimulation was established by flow cytometry and ELISA. RESULTS: The experiments showed that goldenrod infusion contains mainly caffeoylquinic acid derivatives, flavonoids, and some phenylpropanoids. Natural products present in the extract were transformed by human and swine microbiota to smaller molecules mainly phenylpropanoid acid derivatives. The permeability assays showed that most of the parental compound present in the infusion cannot cross the gut epithelial barrier. In contrast, metabolites were able to cross the Caco-2 monolayer. Depending on the structure, different possible mechanisms of transport were observed. The infusion did not significantly influence the proinflammatory functions of human neutrophils. CONCLUSIONS: Following oral administration of goldenrod infusion, phytochemicals are prone to undergoing metabolism by gut microbiota to smaller phenylpropionic acid derivatives that can be bioavailable after crossing the gut epithelial barrier to be further metabolized and distributed. Detected metabolites should be considered as potentially active compounds responsible for the bioactivity of the raw plant material in vivo.
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Anti-Inflamatórios/metabolismo , Anti-Inflamatórios/farmacologia , Microbioma Gastrointestinal , Extratos Vegetais/metabolismo , Extratos Vegetais/farmacologia , Solidago/química , Animais , Anti-Inflamatórios/química , Biotransformação , Células CACO-2 , Permeabilidade da Membrana Celular , Europa (Continente) , Fezes/microbiologia , Humanos , Neutrófilos/efeitos dos fármacos , Neutrófilos/imunologia , Permeabilidade , Extratos Vegetais/química , SuínosRESUMO
The widely accepted strategy to justify the use of medicinal plant extracts in diseases with inflammatory background is their examination on in vitro models using immune cells. It is also a key initial step of research for active principles, which could be then isolated and tested on more advanced models, becoming new pharmacologically active lead molecules. The crucial aspect which has not been so far addressed in this context, is the presence of pyrogens in plant preparations. The aim of this study was the examination of pyrogens interference with in vitro evaluation of anti-inflammatory activity of plant extracts using human primary neutrophils model together with introduction of effective method of interfering factors elimination. The obtained results showed that chosen plant extracts contained pyrogens, which were responsible for concentration-dependent stimulation of pro-inflammatory cytokines production by human neutrophils in vitro in the same extent as LPS did. The ultrafiltration method was successfully applied for pyrogens elimination, which effectiveness was confirmed using LAL test. The determined interference of pyrogens implies the necessity of their consideration and removal when in vitro studies include direct addition of plant extracts to the cell culture, what can be obtained by ultrafiltration, which does not affect extract composition.
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Anti-Inflamatórios/química , Neutrófilos/imunologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Pirogênios/química , Animais , Anti-Inflamatórios/imunologia , Anti-Inflamatórios/farmacologia , Células Cultivadas , Humanos , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Inflamação/imunologia , Neutrófilos/efeitos dos fármacos , Neutrófilos/metabolismo , Pirogênios/isolamento & purificaçãoRESUMO
Linden trees are a source of food products called lime flowers (Tiliae flos), traditionally used in the form of infusion for the treatment of feverish colds and coughs. Lime flowers should include flowers of Tilia cordata Mill, T.x europaea L., and T. platyphyllos Scop. or a mixture of these. The aim of current research was to establish a fast, sensitive HPTLC (high-performance thin-layer chromatography) method that would allow the differentiation of material obtained from five species of lime occurring in Europe. The fingerprints for distinguishing these species were established, as well as a key for identification based on a visual evaluation of chromatograms. The results obtained were also subjected to chemometric analyses. It was shown that each species contains characteristic compounds i.e. linarin that can be used for their identification. The method developed can, in theory, be introduced for the quality control or authentication of linden flowers on the European market.
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Cromatografia em Camada Fina , Flores/química , Análise de Alimentos/métodos , Chás de Ervas/análise , Tilia/química , Controle de QualidadeRESUMO
Lythrum salicaria herb (LSH) was applied in diarrhea therapy since ancient times. Despite empirically referenced therapeutic effects, the bioactivity mechanisms and chemical constituents responsible for pharmacological activity remain not fully resolved. Taking into consideration the historical use of LSH in treatment of diarrhea in humans and farm animals, the aim of the study was to examine in vitro the influence of LSH and its C-glycosylic ellagitannins on processes associated with maintaining intestinal epithelium integrity and enteropathogenic Escherichia coli (EPEC) growth and adhesion. LSH was not only inhibiting EPEC growth in a concentration dependent manner but also its adhesion to IPEC-J2 intestinal epithelial cell monolayers. Inhibitory activity toward EPEC growth was additionally confirmed ex vivo in distal colon samples of postweaning piglets. LSH and its dominating C-glycosylic ellagitannins, castalagin (1), vescalagin (2), and salicarinins A (3) and B (4) were stimulating IPEC-J2 monolayer formation by enhancing claudin 4 production. Parallelly tested gut microbiota metabolites of LSH ellagitannins, urolithin C (5), urolithin A (6), and its glucuronides (7) were inactive. The activities of LSH and the isolated ellagitannins support its purported antidiarrheal properties and indicate potential mechanisms responsible for its beneficial influence on the intestinal epithelium.
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Aderência Bacteriana/efeitos dos fármacos , Escherichia coli Enteropatogênica/efeitos dos fármacos , Taninos Hidrolisáveis/farmacologia , Lythrum/química , Linhagem Celular , Escherichia coli Enteropatogênica/crescimento & desenvolvimento , Escherichia coli Enteropatogênica/fisiologia , Células Epiteliais/metabolismo , Microbioma Gastrointestinal/efeitos dos fármacosRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Bistort rhizome (Bistorta officinalis) is a traditionally used plant material popular in Europe and Asia in the treatment of diarrhea and as a topical agent for skin conditions. It contains tannins mostly condensed flavan-3-ol derivatives. However, the in-depth phytochemical investigation of infusions from this plant materials is still lacking. Additionally, the scientific reports supporting the traditional topical application of bistort rhizome are scarce. AIM OF THE STUDY: The major objective of the present study was to comprehensively investigate the chemical composition of infusion from subterranean parts of common bistort both using hyphenated chromatographic technique and isolation approach. Additionally, the influence of water extract on pro-inflammatory functions of human neutrophils was performed. As bacterial infections play a crucial role in the generation of skin inflammations the antimicrobial activity of the infusion and its major components was established. MATERIAL AND METHODS: The chemical composition of the infusion was established using UHPLC-DAD-MS3 method. Major compounds which could not be identified using chromatographic analysis were isolated by column chromatography and preparative HPLC. Obtained pure phytochemicals were identified by NMR analysis. The influence of the extract and compounds on the cell viability and apoptosis was evaluated by flow cytometry. The release of pro-inflammatory cytokines after LPS stimulation was established by ELISA. Finally, the antimicrobial assays were performed by establishing MIC and MBC values using several bacterial strains. RESULTS: The UHPLC analysis revealed the infusion contained mainly, galloyl glucose derivatives, procyanidins and chlorogenic acid. Several compounds were isolated and identified for the first time from the investigated plant material. It was shown that the infusion and its constituents influenced the release of proinflammatory cytokines such as IL-1ß, TNF-α and IL-8 and also affected the viability and apoptosis of healthy cells. Both extract and isolated natural products displayed antimicrobial activity against skin pathogens. CONCLUSIONS: The results obtained in the present study support that the infusions from common bistort influence key biological processes are crucial for skin conditions with the inflammatory background. The study justifies the traditional topical application of common bistort.
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Antibacterianos/farmacologia , Anti-Inflamatórios/farmacologia , Bactérias/efeitos dos fármacos , Fármacos Dermatológicos/farmacologia , Neutrófilos/efeitos dos fármacos , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Polygonum , Administração Tópica , Antibacterianos/administração & dosagem , Antibacterianos/isolamento & purificação , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/isolamento & purificação , Apoptose/efeitos dos fármacos , Bactérias/crescimento & desenvolvimento , Células Cultivadas , Citocinas/metabolismo , Fármacos Dermatológicos/administração & dosagem , Fármacos Dermatológicos/isolamento & purificação , Humanos , Mediadores da Inflamação/metabolismo , Testes de Sensibilidade Microbiana , Ativação de Neutrófilo/efeitos dos fármacos , Neutrófilos/imunologia , Neutrófilos/metabolismo , Neutrófilos/patologia , Compostos Fitoquímicos/administração & dosagem , Compostos Fitoquímicos/isolamento & purificação , Extratos Vegetais/administração & dosagem , Extratos Vegetais/isolamento & purificação , Polygonum/química , Rizoma , Solventes/química , Água/químicaRESUMO
The isolation of phenolics from aerial parts of Corispermum marschallii yielded a total of 13 compounds including nine previously undescribed patuletin and spinacetin glycosides. These were identified as patuletin 3- O-ß-d-galactopyranosyl-7- O-ß-d-glucopyranoside (1), spinacetin 3- O-ß-d-galactopyranosyl-7- O-ß-d-glucopyranoside (2), patuletin 3- O-(6â³- O-ß-d-glucopyranosyl)-ß-d-galactopyranoside (3), patuletin 3- O-(6â³- O-α-l-arabinopyranosyl)-ß-d-galactopyranoside (4), patuletin 3- O-(2â³- O-(5â´- O-α-l-arabinopyranosyl)-ß-d-apiofuranosyl)-ß-d-galactopyranoside (5), patuletin 3- O-(2â³- O-ß-d-apiofuranosyl)-ß-d-galactopyranoside (6), spinacetin 3- O-ß-d-galactopyranoside (7), patuletin 3- O-ß-d-galactopyranosyl-7- O-(6â´- O-feruloyl)-ß-d-glucopyranoside (8), and spinacetin 3- O-ß-d-galactopyranosyl-7- O-(6â´- O-feruloyl)-ß-d-glucopyranoside (9). Structure elucidation was based on UV-visible, multistage MS, and 1D and 2D NMR spectroscopy and chemical derivatization, which allowed the identification on the glycosides with two different hexose moieties occurring at different positions of the aglycones. Most of the compounds tested inhibited the production of pro-inflammatory factors such as ROS, IL-8, and TNF-α in stimulated neutrophils.
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Amaranthaceae/química , Anti-Inflamatórios não Esteroides/farmacologia , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Componentes Aéreos da Planta/química , Antioxidantes/farmacologia , Humanos , Interleucina-8/antagonistas & inibidores , Interleucina-8/biossíntese , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Neutrófilos/efeitos dos fármacos , Neutrófilos/metabolismo , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Espectrofotometria Ultravioleta , Fator de Necrose Tumoral alfa/antagonistas & inibidores , Fator de Necrose Tumoral alfa/biossínteseRESUMO
Linden flower is a wildly used plant material among patients in the treatment of common cold symptoms and mucosa inflammations. However, the structure and bioactivity of flavan-3-ol derivatives present in infusions from flowers of Tilia cordata have not been studied so far. The aim of current study was to isolate and identify main procyanidins present in the flowers of small-leaved lime and to evaluate their influence on the inflammatory response of human neutrophils ex vivo. The chemical structure of isolated compounds was established by 1D and 2D NMR experiments. The bioactivity of obtained compounds was tested in human neutrophils model. Cytotoxicity and influence of compounds on apoptosis was established by flow cytometry. The levels of produced cytokines were established by ELISA after stimulation with lipopolysaccharide (LPS). The inhibition of the production of reactive oxygen species was checked by luminol-dependent chemiluminescence method after N-formylmethionyl-leucyl-phenylalanine (f-MLP) induction. The phytochemical work resulted in the isolation of 10 compounds. Compounds were identified as oligomeric procyanidins and their precursor epicatechin. The potential anti-inflammatory activity of compounds was evaluated in the concentration range 5-20⯵M. All compounds were able to decrease the production of ROS from f-MLP-stimulated neutrophils. Most of compounds were able to inhibit the LPS-induced release of IL-8. Some trimeric and tetrameric derivatives were also able to decrease the production of MIP-1ß. Obtained results partially support the traditional usage of infusion from lime flowers in the treatment of symptoms of inflammation and irritation of mucosa in common cold, pharyngitis and tonsillitis.