Introduction In European traditional medicine, common ash leaf infusion is recommended by European Medicines Agency to treat minor articular pain and to increase the amount of urine for flushing minor urinary complaints. However, a comprehensive ultra‐high‐performance liquid chromatography diode array detector electrospray ionisation tandem mass spectrometry (UHPLC‐DAD‐ESI‐MS/MS) analysis of this pharmacopeial plant material has never been performed. Moreover, the number of biological and pharmacological investigations proving the usefulness of this plant material in recommended traditional uses is surprisingly small. Objective Phytochemical profiling of ash leaf samples from different commercial and natural sources and the determination of the in vitro effects on inflammatory mediators in a model of human neutrophils. Methods Ash leaf samples were characterised by total hydroxycinnamic acid content and by high‐performance thin layer chromatography (HPTLC), UHPLC‐DAD‐ESI‐MS/MS methods. The effects of leaf infusions on reactive oxygen species (ROS), tumor necrosis factor (TNF‐α), interleukin 8 (IL‐8), interleukin 1β (IL‐1β), and monocyte chemoattractant protein 1 (MCP‐1) production by neutrophils were measured using luminol‐dependent chemiluminescence and enzyme‐linked immunosorbent assay (ELISA). Results In ash leaf samples 64 compounds were identified or partly identified together with four unknown compounds. The major compounds detected belong to different structural groups, including phenolic acid derivatives, phenylethanoids, flavonoids, iridoids, secoiridoids and lignans. The major compounds detected in ash samples were chlorogenic acid, quercetin‐3‐O‐rutinoside, verbascoside, oleuropein and ligstroside. However, one sample contained coumarin derivatives. This finding suggested adulteration with other Fraxinus species and/or plant parts. All infusions were able to inhibit ROS, cytokine and chemokine production. Conclusions The performed phytochemical and biological analyses contribute to the knowledge about this pharmacopeial plant material and supports its traditional use to treat minor inflammatory complaints.

Aim of the study: Taking into account that overactivated leukocytes are an important factor in the development of many chronic diseases, we investigated the activity of phytochemically characterized (HPLC-DAD-MSn) extracts from forsythia leaves and flowers on the pro- and anti-inflammatory functions of leukocytes (effects on IL-1β, IL-8, TNF-α, and TGFβ release) and their adherence to endothelial cells. Using bio-guided fractionation, we isolated the active compounds and determined their biological activity, and we included the positive control quercetin.Methods: The effect on IL-1β, TNF-α, IL-8, and TGF-α production by leukocytes was measured by enzyme-linked immunosorbent assay (ELISA). The surface expression of adhesion molecules was analyzed with flow cytometry, and the neutrophil attachment to the endothelial cells was assessed fluorimetrically. The effects on p38MAPK, ERK1/2 and JNK phosphorylation were determined using western blots.Results: Leaf extracts had the effect of decreasing TNF-α production in neutrophils and monocyte/macrophage cells. The bio-guided fractionation led to the isolation of the following lignan aglycones: (+)-pinoresinol, (+)-epipinoresinol, (−)-matairesinol, (+)-phillygenin, and (−)-arctigenin. Only phillygenin was able to stimulate the anti-inflammatory function of macrophages by inducing TGF-β release and IL-10 receptor surface expression. Arctigenin, phillygenin, and a metabolite produced by the gut microbiota, enterolactone, decreased TNF-α and IL-1β production and neutrophil adhesion to endothelial cells, probably by attenuating the p38 and ERK kinase pathways.Conclusion: Forsythia x intermedia is a valuable source of active lignans, which may be potential candidates for treating inflammatory diseases that are associated with the excessive production of cytokines such as TNF-α and IL-1β.

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The aim of this article is to briefly present progress in the development of the potent adenosine receptor (AR) antagonists with high selectivity for either A1, A2A, or A2B ARs. The structural requirements for each AR subtype were discussed as well as their potential therapeutic use. In the search for new AR antagonists, series of imidazo-, pyrimido-, and diazepino-purindione derivatives as well as oxazolo-, oxazino-, and oxazepino-purindiones were designed, synthesized, and preliminarily evaluated in pharmacological studies. Oxygen-containing tricyclic derivatives were shown to be moderately potent AR antagonists exhibiting selectivity either for A1 or A2A ARs. Tricyclic purindiones with nitrogen in the third ring were generally more A2A AR selective. The compounds tested in vivo according to the Antiepileptic Drug Development Program of the National Institutes of Health (USA) were generally active as anticonvulsants in chemically induced seizures.

Aim of the study: The aim of the present study was to investigate the effects of phytochemically characterized extracts connected with the traditional use (infusions and ethanolic extracts) of different parts of Syringa vulgaris (common lilac) on the pro-inflammatory functions of neutrophils. Active compounds were isolated from the most promising extract(s) using bioassay-guided fractionation, and their activity and molecular mechanisms of action were determined.Methods: The extracts were characterized using a HPLC-DAD- MSn method. The effects on ROS, MMP-9, TNF-α, IL-8, and MCP-1 production by neutrophils were measured using luminol-dependent chemiluminescence and enzyme-linked immunosorbent assay (ELISA) methods. The effects on p38MAPK, ERK1/2, JNK phosphorylation, and NF-kB p65 translocation were determined using western blots.Results: The major compounds detected in the extracts and infusions belong to structural groups, including caffeic acid derivatives, flavonoids, and iridoids. All extracts and infusions were able to significantly reduce ROS and IL-8 production. Bioassay-guided fractionation led to the isolation of the following secoiridoids: 2″-epiframeroside, oleonuezhenide, oleuropein, ligstroside, neooleuropein, hydroxyframoside, and framoside. Neooleuropein appeared to be the most active compound in the inhibition of cytokine production by attenuating the MAP kinase pathways.Conclusion: The present study demonstrated that common lilac, which is a traditionally used medicinal plant in Europe, is a valuable source of active compounds, especially neooleuropein.

Carpesium divaricatum Sieb. & Zucc. has a long history of use as both a medicinal and a food plant. However, except for terpenoids, its chemical constituents have remained poorly investigated. The composition of hydroalcoholic extract from aerial parts of C. divaricatum was analyzed by HPLC-DAD-MSn, revealing the presence of numerous caffeic acid derivatives that were formerly unknown constituents of the plant. In all, 17 compounds, including commonly found chlorogenic acids and rarely occurring butyryl and methylbutyryl tricaffeoylhexaric acids, were tentatively identified. Fractionation of lipophilic extract from cultivated shoots led to the isolation of 12-oxo-phytodienoic acid (12-OPDA), which is a newly identified constituent of the plant. The compound, at concentrations of 0.5, 1.0, and 2.5 μM, significantly reduced IL-8, IL-1β, TNFα, and CCL2 excretion by lipopolysaccharide (LPS)-stimulated human neutrophils. Reactive oxygen species (ROS) production induced by f-MLP was also significantly diminished in the neutrophils pretreated by 12-OPDA. The newly identified constituents of the plant seem to be partly responsible for its pharmacological activity and elevate the value of C. divaricatum as a potential functional food.

Cold‐pressed rapeseed oil is among the most popular virgin oils. Different processing methods yield oils varying in chemical composition and oxidative stability. The experiment aimed at identifying the differences (mostly in volatiles) between rapeseed oil obtained from peeled seeds (RO) and oils obtained by three pre‐treatment methods: pressing whole seeds (WSO), flakes (FO) and roasted flakes (RFO). Volatiles were analysed using GCxGC‐ToFMS and data were processed using statistical multivariate analysis. Fatty acid composition was determined using GC‐FID. The oils’ oxidative stability was measured using peroxide value. Free fatty acids’ value, absorbance at 236 and 238 nm and chlorophyll content were also determined. Also, a sensory panel evaluation was performed. PCA was found to be effective tool for differentiating the oils on the basis of their volatile compounds. RO was most similar to WSO from the second pressing. Fatty acid composition analysis yielded differences between the experimental oils and RO. RO had the highest PV, p‐AV and Totox values. WSO from the first pressing (WSO1) had the highest oxidative stability. Sensory analysis found that WSO1 was most similar to RO. Both oils had an intense cabbage‐like and fruity odour. The study showed that the results of volatile compounds’ analysis differs from those of sensory analysis in oils comparison. Practical applications: The results demonstrate that the rapeseed oil obtained from whole seeds may have a volatile compounds composition that is similar to that of rapeseed oil obtained from peeled seeds. PCA makes it possible to differentiate between samples varying in pre‐treatment method as well as between samples subjected to the same pre‐treatment method, but obtained from a second pressing. Sensory panel performed by trained panellists may demonstrate which oils are most desirable when rated for selected attributes. The results of sensory panel may differ from those of volatile compound analysis performed with GCxGC‐ToFMS. In the current study, the volatile compounds in cold‐pressed rapeseeds oil obtained from peeled seeds with those in rapeseed oils obtained from seeds prepared with various pre‐treatment methods are compared. The obtained results are compared with those of sensory evaluation. The study shows that the results obtained by means of statistical analysis based on volatile compounds do not always correlate with those of sensory panel evaluation in oils comparison.

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