Search

Sigesbeckia orientalis, more commonly referred to as Herba Sigesbeckiae or Xi Xian Cao in traditional Chinese medicine and hy thiêm in traditional Vietnamese medicine, is used in China and Vietnam to treat inflammatory diseases such as arthritis, rheumatism, and joint pain. In initial investigations, the dichloromethane extract from the aerial parts of S. orientalis showed distinct inhibitory effects on the release of interleukin-8 in human neutrophils. Therefore, the purpose of the present study was the phytochemical investigation of the bioactive dichloromethane extract and the in vitro analysis of the effects of the isolated compounds on interleukin-8, interleukin-1β, tumor necrosis factor-α, and monocyte chemoattractant protein 1 release, and surface expression of adhesion molecules (CD11a, CD11b, and CD62L) in lipopolysaccharide-stimulated human neutrophils to identify the active principle(s). The separation of the bioactive dichloromethane extract using various chromatographic techniques led to the isolation of nine compounds. Their chemical structures were elucidated from nuclear magnetic resonance and mass spectrometry data. One diterpene, 17(13 → 14)-abeo-ent-3S*,13S*,16-trihydroxystrob-8(15)-ene, was identified as a new natural product. Three germacranolide sesquiterpene lactones inhibited interleukin-8 production with IC50 values between 1.6 and 6.3 µM, respectively, and tumor necrosis factor-α production with IC50 values between 0.9 and 3.3 µM, respectively. Furthermore, they significantly inhibited interleukin-1β and monocyte chemoattractant protein 1 production and diminished the effects of lipopolysaccharide on the surface expression of the adhesion molecules CD11a, CD11b, and CD62L. These findings support the traditional use of S. orientalis in the treatment of inflammatory diseases.

Carpesium divaricatum Sieb. &amp, Zucc., a traditional medicinal plant used as an inflammation-relieving remedy, is a rich source of terpenoids. At least 40 germacrane-type sesquiterpene lactones, representatives of four different structural groups, were isolated from the plant. Cytotoxicity against cancer cells in vitro is the most frequently described biological activity of the compounds. However, little is known about the selectivity of the cytotoxic effect. The anti-inflammatory activity of the germacranolides is also poorly documented. The objective of the present study was to assess the cytotoxic activity of selected C. divaricatum germacranolides-derivatives of 4,5,8,9-tetrahydroxy-3-oxo-germacran-6,12-olide towards cancer and normal cell lines (including cells of different p53 status). Moreover, to assess the anti-inflammatory effect of the compounds, the release of four proinflammatory cytokines/chemokines (IL-1β, IL-8, TNF-α and CCL2) by lipopolysaccharide-stimulated human neutrophils was measured by ELISA. The investigated sesquiterpene lactones demonstrated nonselective activity towards prostate cancer (Du145 and PC3) and normal prostate epithelial cells (PNT2) as well as against melanoma cells (A375 and HTB140) and keratinocytes (HaCaT). Cytotoxic activity against osteosarcoma cells was independent of their p53 status. In sub-cytotoxic concentrations (0.5–2.5 µM) the studied compounds significantly decreased cytokine/chemokine release by lipopolysaccharide-stimulated human leukocytes.

Different in vitro cultures of the Turkish origin medicinal plant species, Salvia viridis, were estimated in order to investigate their potential for the accumulation of phenolic compounds. Among the seventeen detected compounds, thirteen phenolic acid derivatives and four phenylethanoids were identified in extracts from shoot and/or callus cultures using the UPLC-DAD/ESI-MS method. The accumulation of the compound depended on the type of culture (callus, shoot), the medium composition and age of culture (6, 12, 18 and 24 months in in vitro conditions). Six of the seventeen detected compounds were estimated in all the analyzed samples, however, sometimes only in trace amounts. The predominant metabolite was rosmarinic acid (RA). Its content ranged between 2.4 and 11.5 mg/g dry weight (DW). The highest levels of rosmarinic acid and total phenolic compounds were found in a half-year-old shoot culture. The content of the RA was nine times higher than that in the shoots of plant grown in field conditions. The antioxidant activity of S. viridis cultures was examined by the O2− and 1-1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging test and FRAP (ferric reducing antioxidant power) assay. In addition, the antifungal and the antibacterial activities were examined against a wide spectrum of micro-organisms. All the samples showed promising antioxidant potential; however, the shoot extract had the highest antioxidant activity in all the assays. Preliminary results demonstrated that all the analyzed extracts inhibited the growth of Gram-positive and Gram-negative bacteria. The extracts also showed strong activity against Candida and Aspergillus species.

Plants have been used for medical purposes since ancient times. However, a detailed analysis of their biological properties and their associated active compounds is needed to justify their therapeutic use in modern medicine. The aim of the study was to identify and quantify the phenolics present in hydromethanolic extracts of the roots and shoots of the Chinese Salvia species, Salvia bulleyana. The qualitative and quantitative analyses were carried out by ultrahigh-performance liquid chromatography with electrospray ionization mass spectrometry detection (UHPLC-PDA-ESI-MS), and high-performance liquid chromatography with photodiode array (HPLC-PDA) detection. The extracts of S. bulleyana were also screened for their antioxidant activity using ferric ion (Fe3+) reducing antioxidant power (FRAP), 1,1-diphenyl-2-picrylhydrazyl (DPPH), diammonium 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonate) cation (ABTS), superoxide radical anion (O2•–), and inhibition of lipid peroxidation assays. The S. bulleyana extracts were found to contain 38 substances, of which 36 were phenols, with a total level of 14.4 mg/g DW (dry weight) in shoots, and 23.1 mg/g DW in roots. Twenty-eight phenols were polyphenolic acids or their derivatives, the most abundant in shoots being rosmarinic acid, and in roots, salvianolic acid K followed by rosmarinic acid. The other major phenolic acids were caffeic acid, caffeoyl-threonic acids, isomers of lithospermic acid, salvianolic acid F, salvianolic acid B, and yunnaneic acid E. In addition to polyphenolic acids, nine flavonoids were detected in the shoot extract. While both extracts showed significant antioxidant activity, the shoot extract, containing both polyphenolic acids and flavonoids, demonstrated a slightly greater antioxidant potential in some of the anti-radical tests than the roots. However, the root extract proved to be slightly more effective in the lipid peroxidation inhibition test. Thus, S. bulleyana was demonstrated as a promising source of antioxidants, and worthy of further more detailed studies.

Xerolekia speciosissima (L.) Anderb., a rare plant from the north of Italy, is a member of the Inuleae-Inulinae subtribe of the Asteraceae. Despite its close taxonomic relationship with many species possessing medicinal properties, the chemical composition of the plant has remained unknown until now. A hydroalcoholic extract from the aerial parts of X. speciosissima was analyzed by HPLC-DAD-MSn, revealing the presence of caffeic acid derivatives and flavonoids. In all, 19 compounds, including commonly found chlorogenic acids and less frequently occurring butyryl and methylbutyryl conjugates of dicaffeoylquinic and tricaffeoylhexaric acids, plus two flavonoids, were tentatively identified. Chromatographic separation of a hydroalcoholic extract from the capitula of the plant led to the isolation of (+)-dehydrodiconiferyl alcohol 4-O-&beta, glucopyranoside, quercimeritrin, astragalin, isoquercitrin, 6-hydroxykaempferol-7-O-&beta, glucoside, quercetagitrin, methyl caffeate, caffeic acid, protocatechuic acid, chlorogenic acid and 1,5-dicaffeoylquinic acid. Composition of a nonpolar extract from the aerial parts of the plant was analyzed by chromatographic methods supported with 1H-NMR spectroscopy. The analysis revealed the presence of loliolide, reynosin, samtamarine, 2,3-dihydroaromaticin, 2-deoxy-4-epi-pulchellin and thymol derivatives as terpenoid constituents of the plant. One of the latter compounds&mdash, 7,10-diisobutyryloxy-8,9-epoxythymyl isobutyrate&mdash, at concentrations 0.5, 1.0 and 2.5 &mu, M, significantly reduced IL-8, IL-1&beta, and CCL2 excretion by LPS-stimulated human neutrophils.

The aim of the study was to characterize phytochemicals in an infusion of the aerial parts of tarragon (Artemisia dracunculus L.) using ultra-high-performance liquid chromatography diode array detector electrospray ionisation tandem mass spectrometry UHPLC‐DAD‐ESI‐MS/MS method, as well as an evaluation of its effects on mediators of the inflammation in an in vitro model of human neutrophils, and antimicrobial activity on selected pathogens. Flavonoids and caffeoylquinic acids were the main phenolic components of the extract of tarragon’s aerial parts. The infusion was able to inhibit reactive oxygen species (ROS), interleukin 8 (IL-8), and tumour necrosis factor α (TNF-α) production. The antimicrobial assay was performed with the use of nine strains of bacteria, both Gram-negative and Gram-positive. Three human pathogens, Staphylococcus aureus ATCC6538, Staphylococcus epidermidis ATCC14990, and Staphylococcus aureus MRSA (methicyllin-resistant Staphylococcus aureus) ATCC43300, proved to be the most sensitive to tarragon infusion. Our study demonstrated the antiinflammatory and antimicrobial properties of tarragon (Artemisia dracunculus L.), meaning the common spice may be a prospective source of health-promoting constituents.

Extracts from the roots of Ononis spinosa L. (restharrow roots) are traditionally used for the treatment of patients with urinary tract infections due to its mild diuretic activity, caused by the inhibition of renal human hyaluronidase-1 by isoflavonoids. Preliminary studies also indicated anti-inflammatory effects. The following study aimed at investigating potential anti-inflammatory effects of restharrow extracts, prepared with solvents of different polarity. A dichloromethane extract (OS1), mainly composed of isoflavonoids and triterpenes as characterized by LC-MS, showed a concentration-dependent (25–100 μg/ml) inhibition of IL-8 and TNF-α release from LPS-stimulated human neutrophils. Significant inhibition was also found for the triterpene α-onocerin and the norneolignan clitorienolactone B, isolated from OS1. Further, OS1 and both compounds significantly decreased the expression of the adhesion molecules CD11b/CD18 and conversely increased the expression of CD62L in LPS-stimulated human neutrophils. This finding corresponds to a reduced inflammatory response by the inhibition of adhesion and migration of immune cells. As all of the observed effects are potentially mediated via Toll-like receptor 4 (TLR4) signaling, TLR4 transfected HEK293 cells were incubated with OS1. LPS-induced IL-8 secretion was significantly inhibited in a concentration-dependent manner, confirming TLR4 antagonism. This inhibition, however, was in part caused by an interaction of OS1 with LPS. In addition, also an aqueous extract containing high amounts of isoflavonoid glycosides and saponins from the roots of O. spinosa showed anti-inflammatory effects by interacting with the TLR4 signaling pathway. This study rationalizes the traditional use of extracts from O. spinosa for therapy of urinary tract infections, due to its potential anti-inflammatory effects that are mediated via TLR4 receptor antagonism.

This study was to obtain stable transformed roots of Salvia bulleyana using A. rhizogenes strain A4 and then evaluate their phytochemical profile and selected the most productive clone. Our results indicated that the type of explant and medium used for bacterium and explant incubation had an influence on the frequency of hairy root formation. The best response was obtained on leaves infected with bacteria cultivated on YMB medium supplemented with acetosyringone. Of the four selected transformed root clones, after five-week cultivation in Woody Plant (WP) medium, the highest growth indexes were demonstrated for line C1: i.e. 13 for fresh and 15 for dry weight (81.4 and 8.2 g/l fresh and dry weight, respectively). The qualitative analysis of hydromethanolic extracts of hairy roots of S. bulleyana using UPLC-PDA-ESI-MS/MS method showed the presence of 10 polyphenolic compounds including predominant rosmarinic acid (RA), its derivatives (hexoside and methyl rosmarinate), caffeic acid, its derivatives and several salvianolic acids: K, E and F. Their production varied among the four root clones studied; the highest RA (39.6 mg/g dry weight) and total polyphenol (48.9 mg/g dry weight) level were found in the roots of C4 clone. These values were significantly higher than those of the roots of plants grown for several years under field conditions. The transformation of the obtained root cultures was confirmed by polymerase chain reaction using aux1, aux2, rolB, rolC and rolD primers.

Acmella oleracea (jambu) is a South American plant whose pharmacological properties include antimalarial, anesthetic, and anti-inflammatory activities. However, the compounds contributing to the anti-inflammatory effect have received little attention. In this study, the active compound spilanthol was isolated using a Green Chemistry approach and presented significant anti-inflammatory activity in a lipopolysaccharide-activated human neutrophil model. First, the aerial parts of jambu were extracted and fractionated using supercritical carbon dioxide. The spilanthol-enriched fractions obtained were then subjected to further purification by flash chromatography, yielding spilanthol with 97% purity. Use of enzyme-linked immunosorbent assay (ELISA) revealed a reduction in the release of Interleukin-8 and Tumor Necrosis Factor - alpha by leukocytes exposed to spilanthol. In conclusion, this new approach enabled spilanthol to be obtained at high purity, in a fairly rapid procedure, while the results of the in vitro anti-inflammatory activity study indicated that the compound could be a promising new therapeutic agent.

Thirteen compounds were isolated and identified from the aerial parts of Eupatorium cannabinum subsp. cannabinum comprising six caffeic acid derivatives, five flavonol glycosides and two flavone aglycones. Additionally, the first HPLC-DAD-MS method for the phytochemical screening of phenolics in the analyzed plant material was developed allowing unequivocal identification of further six constituents occurring in the raw extract including four caffeic acid derivatives and two malonylated flavonol glycosides. This report is the first comprehensive study focused on phenolic compounds in the aerial parts of E. cannabinum. The chemotaxonomic significance in respect to the genus Eupatorium is discussed.

Salvia viridis is a containing bioactive phenols plant, which has been used in Turkish medicine. The aim of the study was to establish hairy root culture of the species in order to increase the production of the compounds with pharmacological activity. Transformed roots are promising biotechnological systems that produce great amounts of secondary metabolites; this is attributed to their fast growth and their genetic and biosynthetic stability. Stable hairy root lines of S. viridis were established from shoot explants using Agrobacterium rhizogenes strain A4. The highest frequency of transformation (45%) was achieved when the shoot was inoculated at the node or internode by bacteria cultivated on Yeast/Mannitol/Broth (YMB) medium supplemented with acetosyringone. The transformation of the root clones was confirmed by polymerase chain reaction using aux1, aux2, rolB and rolC primers. Of the five obtained transformed root clones, the highest biomass was achieved for clone K3 (13.63 ± 0.5 g/L after 5 weeks) grown in Woody Plant (WP) medium in darkness. The UPLC-PDA-ESI–MS analysis of hydromethanolic extracts of transformed roots of S. viridis revealed the presence of 10 compounds identified as caffeic acid derivatives. Quantitative analysis showed that rosmarinic acid (RA) was the predominant compound in all clones. The highest RA (35.8 mg/g dry weight) and total polyphenol (41.24 mg/g dry weight) content were evaluated in clone K3 cultured in WP medium. These values were 8-fold higher than those of the non-transformed roots, indicating that hairy root cultivation could be a promising technique for the production of valuable compounds from S. viridis.

Plants belonging to the family Oleaceae have been traditionally used in treatment of various inflammatory skin disorders. One of the most well-known species is Olea europaea L. (olive), cultivated in the Mediterranean countries. Another species is Ligustrum vulgare L. (common privet), occurring particularly in Northern Europe and Asia. The aim of the study was a comparison of the composition of aqueous and ethanolic extracts from leaves of O. europaea and L. vulgare (HPLC-DAD-MS), and determination of the total content of phenolics and flavonoids, as well as the content of the major compound, oleuropein. Secondly, we aimed to study the protective effect of extracts on reactive oxygen species (ROS) production by human fibroblast cells (NHDF), cell viability (MTT assay), and apoptosis rate (Annexin V/propidium iodide staining) after UVA-irradiation. The phytochemical analysis allowed us to identify compounds belonging to the groups of flavonoids, phenylpropanoids and secoiridoids in the extracts. The compounds from the group of lignans (olivil) were identified as being unique to O. europaea extracts. Echinacoside, ligustroflavone and ligustaloside A were identified in L. vulgare extracts in contrast to olive preparations. It was established that the aqueous and ethanolic extracts from leaves of both species, except the privet aqueous extract at a concentration of 5 μg/ml, did not show any significant inhibition of ROS production after UVA-irradiation in the model of NHDF cell line. The aqueous extracts of both species at concentrations of 5 and 25 μg/ml had a protective effect on the viability of UVA-treated cells in contrast to the ethanolic extract. In conclusion, no significant difference in the activity of olive and privet leaf extracts has been observed, which suggests that both plant materials’ extracts, particularly aqueous ones, are effective herbal medicines and photoprotectors, which – to some extent – confirms the use of their preparations in skin disorders.

Ethnopharmacological relevance During the epidemic season, over 90% of acute wheezing disease is associated with bronchial inflammation. Both neutrophil- and eosinophil-mediated inflammation have been involved in the pathophysiology of acute bronchitis, but neutrophil cell recruitment has been shown to be dominant. The ongoing inflammation increases the chemotaxis of neutrophils to inflamed site providing to their overaccumulation. The pharmacological reduction of neutrophil migration can be limited by suppression of major chemo-attractants and cytokines (IL-8, IL-1β and TNF-α) release and downregulation of adhesive molecules. Aim of the study During a screening of plants traditionally used in respiratory tracts diseases (e.g. cough, rhinitis, bronchitis, throat infection, fever, influenza) in Europe, we have selected roots of Inula helenium and aerial parts of Grindelia squarrosa as a potential source of compounds limiting neutrophil migration. Materials and methods The effect on IL-8, IL-1β and TNF-α release by neutrophils and respiratory epithelium cell line (A549) was measured by enzyme-linked immunosorbent assay (ELISA). The surface expression of adhesive molecules was analyzed with flow cytometry, and the neutrophil attachment to the epithelial cells was assessed fluorimetrically. Results We confirmed the ability of selected extracts and compounds to suppress neutrophil binding to the epithelium surface via downregulation of β2 integrin. Alantolactone and grindelic acid have shown significant suppression of IL-8, TNF-α and IL-1β release comparable with budesonide, used as a positive control. Conclusions The present study demonstrated that Inula helenium and Grindelia squarrosa, which have been traditionally used in Europe as medicinal plants, are a valuable source of active compounds with anti-inflammatory activity. Our observations justify the traditional use of I. helenium and G. squarrosa for a treatment of inflammation-based diseases in respiratory tract.

Natural phenolic compounds exhibit a lot of beneficial health effects in humans including antioxidant, anti-aging, anti-inflammatory, and antimicrobial activity. Plant family Lamiaceae and its largest genus Salvia are one of the richest sources of antioxidant and antimicrobial phenolics. In the present study the aerial parts and roots of Salvia cadmica Boiss., an underexplored species endemic to Turkey and cultivated in Poland, were investigated for phenolic composition and antioxidant, antibacterial, and antifungal effects, as well as for biological safety. The UPLC-DAD/ESI-MS/MS analysis showed a total of 14 phenols in the hydromethanolic extract of the aerial parts: three flavonoids and 11 phenolic acid derivatives. In the root extract 10 phenolic acid derivatives were identified. Among the detected compounds, rosmarinic acid (RA) and salvianolic acid K (SAK) predominated in the aerial parts and roots, respectively. Both aerial parts and root extracts demonstrated antioxidant potential, indicated by radical scavenging assays towards DPPH and O2•-; they also demonstrated antimicrobial activity against two Candida species and several Gram-positive bacteria, including Bacillus cereus and four strains of Staphylococcus spp. However, the aerial parts demonstrated stronger antioxidant potential, while the roots exhibited stronger antimicrobial activity The tested extracts show low cytotoxicity against mouse L929 fibroblasts in MTT assay. Thus, S. cadmica extracts offer promise as herbal drug, and as a source of bioactive secondary metabolites.

Dracocephalum forrestii, an important plant in Tibetan medicine, was transformed with Agrobacterium rhizogenes strain A4 to obtain hairy root culture. A maximum transformation frequency of 82% after seven weeks was obtained by inoculation of internodal stem segments. Six lines of hairy roots were obtained and cultured in darkness in Woody Plant (WPM) liquid medium. The transgenic nature of the hairy roots was investigated by PCR and RT-PCR. Three main compounds: rosmarinic acid (RA), salvianolic acid B (SAB) and caffeic acid (CA) were identified in extracts of D. forrestii hairy roots by UPLC-PDA-ESI-MS analysis. Quantitative HPLC analysis showed that RA levels were greatly increased in hairy roots (max. 19.97 mg/g DW) compared with the roots of one-year-old field grown plants (4.7 mg/g DW), but SAB levels were significantly lower in transformed roots (max. 11.7 mg/g DW) than in untransformed roots (16.4 mg/g DW). Caffeic acid was detected only in transformed roots. A time course experiment with the most productive hairy root line showed that a culture period of 30 days and a medium supplemented with 3% of sucrose was optimal for biomass and production of analysed phenolic compounds. Production remained stable over at least 3.5 years of continuous subculturing of the hairy roots.

Four new caffeoyl -glucaric and -altraric acid derivatives along with eleven known compounds were isolated from aerial parts of Galinsonga parviflora. Their structures were elucidated by high-resolution spectroscopic studies. The four new compounds were determined as being 2,3,4,5-tetracaffeoylglucaric acid (1), 2,4,5-tricaffeoylglucaric acid (2), 2,3,4- or 3,4,5-tricaffeoylaltraric acid (3) and 2,3(4,5)-dicaffeoylaltraric acid (4). A reliable criterion for the determination of the linkage position of caffeic acids moieties in glucaric acid derivatives has been proposed, on the basis of detailed analysis of the respective J-couplings, including substitution and solvent influence on the observed values. All hexaric acids derivatives appeared as inhibitors of reactive oxygen species production by stimulated neutrophils.

In this study, the flowers of Forsythia × intermedia, Forsythia suspensa and Forsythia ovata are presented as valued raw materials for isolation of rutin, an industrial and pharmacologically active flavonoid. An efficient strategy based on three high-performance chromatographic techniques was established to screen and purify the target compound from the plant matrices. In the first step, an UHPLC-PDA-ESI-MS 3 assay documented the relatively simple phytochemical profiles of the flower extracts and led to the identification of ten polyphenols classified as caffeoyl acid derivatives, flavonoids, phenylethanoids and lignans, with rutin as the major constituent. Significant levels of rutin (20.0–57.6 mg/g dw) were found in the flowers by the validated HPLC-PDA method, with the highest values observed for F. suspensa . Finally, a novel, fast, single-step HPCCC method was developed and successfully applied for the separation of rutin from the plant samples. The ethyl acetate- n -butanol-water (4:1:5, v / v / v) was selected as the optimum two-phase solvent system for both analytical and preparative normal (NP) and reversed-phase (RP) HPCCC separations. Under optimal RP-HPCCC conditions, 155 mg of the crude methanol extract was separated in a single 50 min run, yielding 14.6 mg of rutin with 97.2% HPLC purity and 95.9% recovery. The process efficiency of the HPCCC rutin isolation was demonstrated to be superior to the existing HSCCC methods. The results indicated the usefulness of Forsythia flowers and the developed RP-HPCCC methodology for practical and commercial applications.

The current study estimates the effect of different cytokinins on shoot proliferation and biosynthesis of caffeic acid derivatives in Dracocephalum forrestii in vitro culture. The shoots were grown on Murashige and Skoog (MS) agar medium with 1 µM indole-3-acetic acid (IAA) and different content of 6-benzyloaminopurine (BAP), zeatin, kinetin (1, 2, 4, 8, 18 µM) or thidiazuron (TDZ) (0.1, 0.2, 0.5, 1, 2 µM). The highest multiplication rate (about seven shoots and/or buds per explant) was obtained after 4 weeks of culture on MS medium with 1 µM IAA and 8 or 16 µM BAP. Optimal biomass of plant material was also received on the same media. The identity of the compounds present in the hydromethanolic extracts from D. forrestii shoots grown on cytokinin-supplemented media was confirmed using UPLC–PDA–ESI–MS method. The analysis revealed the presence of nine metabolites recognized as caffeic acid derivatives. The content of the predominant phenolic acids in the extracts, i.e. rosmarinic acid (RA) and salvianolic acid B (SAB), was determined with UHPLC. The highest yield of RA was found in shoots cultivated in the medium containing 1 µM IAA and 2 µM BAP (18.7 mg/g DW). The highest level of SAB (5.3–5.9 mg/g DW) was identified in multiple shoots grown in the presence of 1 µM IAA and 0.5–1 µM TDZ or 2 µM BAP.

Salvia viridis L. is an annual herb used in Mediterranean medicine. The purpose of this study was to determine the polyphenol profile of aqueous (decoction and infusion) and hydroethanolic extracts of aerial parts of field-grown S.viridis and to evaluate their antioxidant activity. The polyphenol profiling was performed via UPLC-DAD/ESI-MS. Additionally, the total polyphenol content in extracts tested were determined by UV-Vis spectrophotometry using the Folin-Ciocalteu assay. The antioxidant effect was evaluated by the FRAP, DPPH, ABTS, O2&bull, &minus, scavenging and TBARS methods. The hydroethanolic extract gave the highest content of total phenolic compounds, followed by the infusion. The UPLC-DAD/ESI-MS analysis of extracts showed a total of 19 phenolic compounds identified as flavonoids (four compounds), phenylethanoids (eight compounds) and phenolic acids (seven compounds). Rosmarinic acid was the predominant phenolic acid, verbascoside was the predominant phenylethanoid, while apigenin glucuronide or methylluteolin glucuronide, depending on the sample, were the predominant flavonoids in the analyzed extracts. The presence of a high polyphenol level indicated a high antioxidant activity of both the infusion and the hydroalcoholic extract. These results indicate that S. viridis is a rich resource of phenolic compounds and can be used in dietary applications with the potential to reduce oxidative stress.

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.

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.

In an initial screening, the dichloromethane extract from the leaves of Melodorum fruticosum showed distinct inhibitory effects on the release of interleukin‐8 (IL‐8) in human neutrophils. Therefore, the aim of the present study was the phytochemical and pharmacological investigation of this extract, to better understand which compounds might be responsible for the anti‐inflammatory effect. Phytochemical analysis led to the isolation of 12 known compounds and two new natural products, 5‐hydroxy‐6‐(2‐hydroxybenzyl)‐4′,7‐dimethoxyflavanone (13) and 2′,4′‐dihydroxy‐3′‐(2‐hydroxybenzyl)‐4,6′‐dimethoxychalcone (14). The influence of the isolated compounds on the production and release of the pro‐inflammatory factors IL‐8, tumor necrosis factor alpha (TNF‐α), reactive oxygen species (ROS), and adhesion molecules (CD62L and CD11b) in human neutrophils was evaluated. Three constituents, melodamide A, 2′,4′‐dihydroxy‐4,6′‐dimethoxychalcone, and 2′,6′‐dihydroxy‐4′‐methoxychalcone, showed significant inhibition of IL‐8 release (IC50=6.6, 8.6, and 11.6 μm, respectively) and TNF‐α production (IC50=4.5, 13.3, and 6.2 μm, respectively).

Scope Ellagitannin-rich food products and medicinal plant materials were shown to have beneficial effects toward intestinal inflammation. Due to the questionable bioavailability of ellagitannins their gut microbiota metabolites-urolithins have come to be regarded as potential factors responsible for biological activities observed in vivo. The aim of the study was to determine the influence of the three most abundant bioavailable ellagitannin gut microbiota metabolites-urolithins A, B, and C on inflammatory responses in RAW 264.7 murine macrophages, which are involved in the pathogenesis of intestine inflammation. Methods and results Urolithins A, B, and C decreased NO production via inhibition of the iNOS protein and mRNA expression. They decreased the expression of IL-1β, TNF-α, and IL-6 mRNA in LPS challenged RAW 264.7 murine macrophages. A clear inhibition of NF-κB p65 nuclear translocation and p50 DNA-binding activity was associated with the observed anti-inflammatory activities of urolithins. Among the tested compounds urolithin A had the strongest anti-inflammatory activity. Conclusion The anti-inflammatory effects of urolithins at concentrations that are physiologically relevant for gut tissues (≥40 μM), as revealed in this study, support the data from in vivo studies showing the beneficial effects of ellagitannin-rich products toward intestinal inflammation.

Ethnopharmacological relevance Purple loosestrife -Lythrum salicaria L. is a herbaceous perennial plant belonging to the Lythraceae family. It has been used for centuries in European traditional medicine. Despite Lythri herba being a pharmacopoeial plant material (Ph. Eur.), L. salicaria popularity as a medicinal plant has recently declined. The aim of the paper is to recall a traditional and historical use of L. salicaria and juxtapose it with comprehensive view on the current knowledge about its chemical composition and documented biological activities in order to bring back the interest into this valuable plant and indicate reasonable directions of future research and possible applications. Materials and methods Systematic survey of historical and ethnopharmacological literature was carried out using sources of European and American libraries. Pharmacological and phytochemical literature research was performed using Scopus, PubMed, Web of Science and Reaxys databases. Results The review of historical sources from ancient times till 20th century revealed an outstanding position of L. salicaria in traditional medicine. The main applications indicated were gastrointestinal tract ailments (mainly dysentery and diarrhea) as well as different skin and mucosa affections. The current phytochemical studies have shown that polyphenols ( C -glucosidic ellagitannins and C -glucosidic flavonoids) as well as heteropolysaccharides are dominating constituents, which probably determine the observed pharmacological effects. The extracts and some isolated compounds were shown to possess antidiarrheal, antimicrobial, anti-oxidant, anti-inflammatory and anti-diabetic activities. Conclusions The intrinsic literature overview conclusively demonstrates that L. salicaria L. used to be considered as an exceptionally effective remedy in European traditional medicine. Despite its unquestionable important position from unknown reasons its popularity has been weakened during the past few decades. Unfortunately the contemporary pharmacological research is still insufficient to support its thoroughly described traditional uses. The necessity of complex studies regarding modes of action, which would directly refer to L. salicaria main traditional applications—gastrointestinal tract ailments, is strongly underlined.

Galinsoga ciliata Raf. Blake like Galinsoga parviflora Cav., comes from the Andes region. The chemical composition, activity and use are similar for both species. Galinsoga species are used in folk medicine as anti-inflammatory agents and accelerators for wound healing. Extracts are applied topically onto the skin to treat dermatological diseases, eczemas, lichens and hard-healing-wounds, and also to treat snakebites. Orally they used to cure flu and colds. In the studies using HPTLC method, different stationary phases, including unmodified silica gel, silica gels modified with CN, NH2, DIOL and RP18 groups were tried. The best separation of the tested compounds was achieved on silica gel plates, when as mobile phases mixtures – ethyl acetate–acetic acid–formic acid–water (100:11:11:26, v/v/v/v), ethyl acetate–methanol–formic acid–water (50:3:4:6, v/v/v/v) and ethyl acetate–methyl ethyl ketone–formic acid–water (30:9:3:3, v/v/v/v) – were used. Using reference substances, in the examined extracts the presence of flavonoids: patulitrin, quercimeritrin, quercitagetrin, and phenolic acids – caffeic and chlorogenic acids was found. HPLC analyses of extracts were carried out on a reversed-phase Zorbax SB column (150 mm × 2.1 mm, 1.9 μm). The mobile phase (A) was water/acetonitrile/formic acid (95:5:0.1, v/v/v) and the mobile phase (B) was acetonitrile/formic acid (100:0.1, v/v). A linear gradient system was used: 0–30 min, 1–30% B. Application of HPLC-DAD-MS method confirmed the results obtained by HPTLC method. Moreover, in the tested extracts the presence of caffeoylglucaric acids as dominating compounds was detected.

Introduction The genus Ligustrum (Oleaceae) is distributed in Europe and Asia (south China and Korea), where it is used to prevent hypertension, sore throats, inflammation and diabetes. The main groups of compounds in extracts of Ligustrum vulgare are biologically active secoiridoids and phenylpropanoids. Objectives The aim of the study was primarily the development and validation of a HPTLC–photodensitometry method for separation and determination of secoiridoids (oleacein, oleuropein) and phenylpropanoids (echinacoside) in different extracts prepared from leaves of L. vulgare. A secondary issue was the quantitative screening of oleacein, oleuropein and echinacoside in extracts from leaves collected at different stages of plant growth (from May to September). Methods A HPTLC–photodensitometry method was developed and validated for quantification of oleuropein, oleacein and echinacoside in plant extracts (aqueous and ethanolic extract, decoction, infusion). Silica gel was used as the stationary phase and dichloromethane:methanol:formic acid:water (80:25:1.5:4, v/v/v/v) as the mobile phase. Results The HPTLC–photodensitometry method developed for quantification of oleacein, oleuropein and echinacoside was specific, accurate and precise. The presence of oleacein was detected in aqueous extracts, whereas oleuropein was present, in particular, in ethanolic extracts, decoctions and infusions. Echinacoside was detected in all the extracts prepared. The content of secoiridoids was variable from May to September, whereas the amount of echinacoside increased in this term. Conclusion The developed and validated HPTLC–photodensitometry method allowed performing fast screening of quantitative profiles of oleacein, oleuropein and echinacoside in preparations of privet leaves. Copyright © 2015 John Wiley & Sons, Ltd.

The aim of the study was to obtain transformed roots ofRhaponticum carthamoidesand evaluate their phytochemical profile. Hairy roots were induced from leaf explants by the transformation ofAgrobacterium rhizogenesstrains A4 and ATCC 15834. The best response (43%) was achieved by infection with A4 strain. The effects of different liquid media (WPM, B5, SH) with full and half-strength concentrations of macro- and micronutrients on biomass accumulation of the best grown hairy root line (RC3) at two different lighting conditions (light or dark) were investigated. The highest biomass (93 g L−1of the fresh weight after 35 days) was obtained in WPM medium under periodic light. UPLC-PDA-ESI-MS3and HPLC-PDA analyses of 80% aqueous methanol extracts from the obtained hairy roots revealed the presence of eleven caffeoylquinic acids and their derivatives and five flavonoid glycosides. The production of caffeoylquinic acids and their derivatives was elevated in hairy roots grown in the light. Only light-grown hairy roots demonstrated the capability for the biosynthesis of such flavonoid glycosides as quercetagetin, quercetin, luteolin, and patuletin hexosides. Chlorogenic acid, 3,5-di-O-caffeoylquinic acid and a tentatively identified tricaffeoylquinic acid derivative were detected as the major compounds present in the transformed roots.

The aim of our study was to investigate the presence and quantitative contents of lignans in the tissues of Taxus ×media. The presence of the lignans: pinoresinol, matairesinol and secoisolariciresinol was assessed in needles, shoots cultures and suspension culture. Pinoresinol was the only lignan found in the tissue of T. ×media. The total pinoresinol content in the needles and in the shoots was 1.24 mg/g dry weight (dw) and 0.69 mg/g dw, respectively. Most of the pinoresinol identified was appeared glycosidically bound. In needles, the amount of glycosidically bound pinoresinol (0.81 mg/g dw) was about twice as high as that of free pinoresinol (0.43 mg/g dw). The content of free and glycosidically bound pinoresinol showed the level of 0.18 mg/g dw and 0.51 mg/g dw, respectively in the in vitro shoot cultures. In the cell culture, no pinoresinol was found.

Background Chronic hyperalgesia and allodynia associated with progressive damage of peripheral neurons are the most prevalent complications of diabetes mellitus. Plants belonging to the family of Oleaceae were traditionally used in folk medicine for the management of diabetes. Hypothesis/Purpose The aim of this study was to investigate whether an aqueous extract from the leaves of Ligustrum vulgare (common privet) could be useful to target neuropathic pain in a rat streptozotocin (STZ) model of diabetes. Methods The chemical composition of the aqueous extract from privet leaf was characterized with the UHPLC-DAD-MS method and the analytical quantification of its constituents was performed with HPLC-DAD. Mechanical hyperalgesia and allodynia were evaluated with the Randall–Selitto and von Frey tests. Results Our investigation revealed the presence of secoiridoids: oleacein (23.48 ± 0.87 mg/g), oleocanthal (8.44 ± 0.08 mg/g), oleuropein (1.50 ± 0.01 mg/g), as well as phenylpropanoids: echinacoside (6.46 ± 0.07 mg/g), verbascoside (4.03 ± 0.04 mg/g) and p-coumaroyl glucarates in the dried aqueous extract of privet leaves. Behavioral data indicated that chronic intraperitoneal administration of the extract (50–200 mg/kg) for 21 days resulted in a decrease in diabetes-induced hyperalgesia and allodynia. Blood glucose levels remained unaltered, while body weight and water intake decreased significantly. Conclusion The aqueous privet leaf extract could serve useful in facilitating treatment of painful diabetic neuropathy. Additionally, the study showed that the antihyperalgesic activity of Ligustrum vulgare leaf extract is not likely related to its antihyperglycemic properties.

Thirteen new compounds including caffeoyl-glucaric and p-coumaroyl-altraric acid derivatives, one monoterpenoid glucoside, four secoiridoid glycosides, and three hydroxycinnamoyl phenylpropanoid glycosides esterified with an oleoside 11-methyl ester along with fifteen known compounds were isolated from flowers of Syringa vulgaris L. (Oleaceae). Their structures were elucidated by high-resolution spectroscopic methods. The tested compounds were able to decrease the production of reactive oxygen species. Moreover, oleoechinacoside (13), demethylhydroxyoleonuezhenide (14), demethyloleonuezhenide (15), syringaoleoacteoside (25) and oleoacteoside (26) at the concentration of 50μM, moderately suppressed the LPS-stimulated release of pro-inflammatory chemokine IL-8 and TNF-α from human neutrophils. Moreover, oleonuezhenide (12), oleoside 11-methyl ester (16) and oleoacteoside (26) at the concentration of 50μM were able to induce the surface expression of interleukin 10 receptor, which is suppressed by the incubation of monocyte/macrophage cells with LPS.

Ethnopharmacological relevance Ellagitannin-rich plant materials are widely used in traditional medicine as effective, internally used anti-inflammatory agents. Due to the not well-established bioavailability of ellagitannins, the mechanisms of observed therapeutic effects following oral administration still remain unclear. The aim of the study was to evaluate if selected ellagitannin-rich plant materials could be the source of bioavailable gut microbiota metabolites, i.e. urolithins, together with determination of the anti-inflammatory activity of the metabolites produced on the THP-1 cell line derived macrophages model. Materials and Methods The formation of urolithins was determined by ex vivo incubation of human fecal samples with aqueous extracts from selected plant materials. The anti-inflammatory activity study of metabolites was determined on PMA differentiated, IFN-γ and LPS stimulated, human THP-1 cell line-derived macrophages. Results The formation of urolithin A, B and C by human gut microbiota was established for aqueous extracts from Filipendula ulmaria (L.) Maxim. herb (Ph. Eur.), Geranium pratense L. herb, Geranium robertianum L. herb, Geum urbanum L. root and rhizome, Lythrum salicaria L. herb (Ph. Eur.), Potentilla anserina L. herb, Potentilla erecta (L.) Raeusch rhizome (Ph. Eur.), Quercus robur L. bark (Ph. Eur.), Rubus idaeus L. leaf, Rubus fruticosus L. and pure ellagitannin vescalagin. Significant inhibition of TNF-α production was determined for all urolithins, while for the most potent urolithin A inhibition was observed at nanomolar concentrations (at 0.625 μM 29.2±6.4% of inhibition). Urolithin C was the only compound inhibiting IL-6 production (at 0.625 μM 13.9±2.2% of inhibition). Conclusions The data obtained clearly indicate that in the case of peroral use of the examined ellagitannin-rich plant materials the bioactivity of gut microbiota metabolites, i.e. urolithins, has to be taken under consideration.

Geum urbanum L. commonly known as wood avens or St. Benedict’s herb is an herbaceous perennial plant with characteristic pinnate leaves with a very large and lobed terminal leaflet. G. urbanum belongs to the family of Rosaceae and is native to humid woods of Europe and Asia (Wichtl, 2004). Infusions from the roots and rhizomes of wood avens have been traditionally used in folk medicine in the treatment of acute diarrhea and as astringent agent for inflammations of the mucosa and gums and for treatment of hemorrhoids (Wichtl, 2004; Popovic et al., 2012). This study investigates the roots of G. urbanum collected from flowering plants growing in their natural state in Umer ( Swietokrzyskie district, Poland) in September 2011. Plant material was authenticated by Izabella Kirpluk (Botanical Garden, University of Warsaw, Poland). Voucher specimen (no. GU092011) has been deposited in the Plant Collection, Department of Pharmacognosy and Molecular Basis of Phytotherapy, Medical University of Warsaw, Poland.

The aim of our study was to determine antioxidant activity of aqueous and hydroethanolic extracts obtained from both freeze-drying leaves and flowers, as well as juice squeezed from the fresh herb of Tropaeolum majus L. In cell-free systems the scavenging of synthetic radical (DPPH) and two radicals (O 2 − , H 2 O 2 ) was evaluated. In in vitro experiments, the effect on reactive oxygen species (ROS) production by f-MLP-stimulated neutrophils, as well as the effect on ROS generation by human skin fibroblasts after UV irradiation were determined. In studies on fibroblasts, the protective effect of the extracts/juice against cell membrane damage caused by UV irradiation was also tested. The tested extracts/juice were chemically characterized by the determination of the content of flavonoids, total phenols and ascorbic acid. Scavenging activity of the tested extracts/juice against synthetic radical-DPPH was low. Against H 2 O 2 and O 2 − the extracts showed stronger antioxidant activity, while the juice was significantly active only against O 2 − . In the human neutrophils model the hydroethanolic extract most strongly inhibited production of ROS. The weakest activity was shown by the juice. Studies on human skin fibroblasts showed no cytotoxic activity of the tested extracts/juice. We also observed inhibition of ROS production by tested extracts/juice induced by UVA as well as by UVB irradiation. The strongest inhibition of ROS production after UVA irradiation was shown by the juice, while after UVB irradiation the most potent was the hydroethanolic extract. Our results partly explain the use of extracts from nasturtium in skin diseases, such as sunburns.

Ellagitannin-rich plant materials are used as popular remedies in the treatment of various inflammatory diseases. Urolithins are gut microbiota metabolites of ellagitannins and are considered responsible for in vivo health effects. Various natural products have been studied that are known sources of urolithins. However, few studies have focused on the metabolism of ellagitannin molecules. The aim of the study was to examine the metabolic fate of select ellagitannins using ex vivo cultures of human gut microbiota. Fifteen monomeric and dimeric ellagitannins, 1-O-galloyl-4,6-(S)-HHDP-β-d-glucose (2), pedunculagin (3), potentillin (4), casuarictin (5), coriariin B (6), vescalagin (7), castalagin (8), stachyurin (9), casuarinin (10), stenophyllinin A (11), stenophyllanin A (12), salicarinin A (13), gemin A (14), agrimoniin (15), and oenothein B (16), and ellagic acid (1) were studied. The formation of the metabolites in ex vivo human microbiota cultures was monitored using UHPLC-DAD-MS/MS. Ellagitannins possessing hexahydroxydiphenoyl moieties were metabolized to 6H-dibenzo[b,d]pyran-6-one derivatives, i.e., urolithins. The observed differences in amounts of produced urolithins indicated that the individual microbiota composition and type of ingested ellagitannins could determine the rate of urolithin production. When the oral ingestion of natural products containing ellagitannins with hexahydroxydiphenoyl groups is considered, the formation of urolithins and their bioactivity should be addressed.

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.

In this study, we synthesized several imperatorin analogs using imperatorin and xanthotoxin as substrates. The anti-cholinesterase activities of all compounds were evaluated in in vitro experiments according to the modified Ellman's method. For each synthesized compound, IC50 values for both enzymes were established. Galantamine hydrobromide was used as a positive control in the enzymatic experiments. All active compounds showed selectivity toward butyrylcholinesterase (BuChE) rather than acetylcholinesterase. The most active ones were 8-(3-methylbutoxy)-psoralen and 8-hexoxypsoralen with IC50 values for BuChE of around 16.5 and 16.4 µM, respectively. The results of our study may be considered as the beginning of a search for potential anti-Alzheimer's disease drugs based on the structure of natural furocoumarins.

The aim of this study was comparison of antioxidant, anti-inflammatory, and antimicrobial activity, as well as chemical composition of extracts of Tropaeolum majus L. herb. Aqueous and hydroethanolic extracts derived from dried and freeze-dried nasturtium herb, prepared both at room temperature and at 90 °C, were studied. In the studies there were no significant differences between antioxidant activity of the extracts. All extracts showed scavenging activity against all the examined reactive species in a concentration-dependent manner. The strongest scavenging activity they showed against reactive nitrogen species, NO (SC50 4.54 ± 0.26–10.90 ± 1.39 μg/mL) and ONOO − (SC50 2.49 ± 1.50–6.37 ± 1.86 μg/mL). Among reactive oxygen species, they showed strong scavenging activity against H 2 O 2 (SC50 14.90 ± 3.91–38.63 ± 9.28 μg/mL). Scavenging activity against O 2 − was weaker, while against HClO the extracts showed very weak activity, practically at the level of statistical error. Against synthetic radical – DPPH scavenging activity of the tested extracts was negligible. The extracts demonstrated stronger antioxidant activity in ex vivo experiment on human neutrophils. The extracts showed no inhibitory activity on hyaluronidase, but at a concentration of 50 μg/mL they inhibited the activity of COX1 by approximately 60%. Lack of antimicrobial activity of the extracts seems to be associated with a low content of benzyl isothiocyanate. The aqueous extracts were characterized by the presence of esters of quinic acid with cinnamic acids (chlorogenic acids, p-coumaroylquinic acids) and the presence of flavonoids. Meanwhile the hydroethanolic extracts were mainly rich in the above mentioned acid esters.

Leaves of Ligustrum vulgare (common privet) have been used for treatment of oropharyngeal inflammations or as antirheumatic, diuretic, and hypotensive agents in folk medicine in southern Europe. Taking into account that neutrophils are involved in the inflammation, the aim of the study was to determine the effect of an aqueous extract prepared from leaves of Ligustrum vulgare on neutrophil functions. The extract was characterized by the HPLC-DAD-MSn method. The inhibition of reactive oxygen species production by formyl-met-leu-phenylalanine- or phorbol 12-myristate 13-acetate-stimulated neutrophils was determined using luminol- or lucigenin-dependent chemiluminescence. The effect on myeloperoxidase, metalloproteinase 9, and interleukin 8 production by neutrophils was measured by an enzyme-linked immunosorbent assay. Neutrophil elastase release was established spectrophotometrically. The expression of adhesion molecules on neutrophils was analyzed with flow cytometry. The main compounds detected were flavonoids, phenylpropanoids, hydroxycinnamates, and secoiridoids. The inhibition of oxidative burst by the extract was comparable in both stimuli models (formyl-met-leu-phenylalanine: IC50 = 18.2 ± 4.0 µg/mL; phorbol 12-myristate 13-acetate: IC50 = 19.8 ± 3.0 µg/mL). The extract in the concentration range of 5–50 µg/mL inhibited neutrophil elastase release by 23.9–34.1 % and myeloperoxidase release by 24.2–37.4 %. The inhibitory effect on metalloproteinase 9 and interleukin 8 production was around 20 %. The extract in the highest concentration modulated the expression of L-selectin and β 2 integrin. Our results partly support the traditional use of common privet leaves as an anti-inflammatory agent.

Extracts from Epilobium sp. herbs have been traditionally used in the treatment of prostate-associated ailments. Our studies demonstrated that the extracts from Epilobium angustifolium, Epilobium parviflorum and Epilobium hirsutum herbs are potent prostate cancer cells (LNCaP) proliferation inhibitors with IC50 values around 35 mg/ml. The tested extracts reduced prostate specific antigen (PSA) secretion (from 325.625.3 ng/ml to ~90 ng/ml) and inhibited arginase activity (from 65.21.1 mUnits of urea/mg of protein to ~40 mUnits of urea/mg protein). Selected constituents of extracts (oenothein B, quercetin-3-O-glucuronide, myricetin-3-O-rhamnoside) were proventobeactiveinrelationtoLNCaPcells.However,oenotheinBwasthestrongestinhibitorofcellsproliferation (IC50=7.80.8 mM), PSA secretion (IC50=21.93.2 mM) and arginase activity (IC50=19.22.0 mM). Additionally, ellagitannins from E. hirustum extract were proven to be transformed by human gut microbiota into urolithins. Urolithin C showed the strongest activity in the inhibition of cell proliferation (IC50=35.23.7 mM), PSA secretion (reduced PSA secretion to the level of 100.731.0 ng/ml) and arginase activity (reduced to the level of 27.93.3 mUnits of urea/mg of protein). Results of the work offer an explanation of the activity of Epilobium extractsand supporttheuseof Epilobium preparationsin thetreatment of prostate diseases. Copyright © 2013 John Wiley & Sons, Ltd.

Circaea lutetiana L. is a perennial herbaceous plant belonging to the family of Oenotheraceae (Onagraceae). It occurs as a common herb in forests of North America, Europe and Asia. Native Americans have used infusions of Circaea as a remedy for wounds and as a wash on injured parts of the body (Moerman, 1998). This study investigates the aerial parts of C. lutetiana L., which were collected from natural state in Bremen (Germany) in the period of blooming in August 2011. Plant material was authenticated by Dr. Anna Kiss and Dr. Wojciech Szypu1a (Department of Pharmaceutical Botany, Medical University of Warsaw) based on morphological characters. Voucher specimen (no. CL082011) has been deposited in the Plant Collection, Department of Pharmacognosy and Molecular Basis of Phytotherapy, Medical University of Warsaw, Poland.

Polygonum aviculare L. (Common Knotrgrass) ( Polygonaceae Juss.) is an annual from which pharmacopoeial (Ph. Eur.) plant material Polygoni avicularis herba is obtained. Although its main active constituents are flavonoids and its standardization is based on their total content, no profound qualitative analysis has been performed, yet. The use of hyphenated analytical methods: UHPLC–DAD coupled with ion trap or time of flight mass detectors together with acidic hydrolysis products analysis allowed for a comprehensive determination of flavonoid composition. Among dominating compounds, myricetin, kaempferol, isorhamnetin and kaempferide glucuronides, which were not previously reported in P . avicularis herba , were discovered. The developed method can be used as a suitable tool for a more insightful, metabolome-based standardization of flavonoid rich pharmacopoeial plant material – P . avicularis herba .

The popularity of food products and medicinal plant materials containing hydrolysable tannins (HT) is nowadays rapidly increasing. Among various health effects attributable to the products of plant origin rich in gallotannins and/or ellagitannins the most often underlined is the beneficial influence on diseases possessing inflammatory background. Results of clinical, interventional and animal in vivo studies clearly indicate the antiinflammatory potential of HT-containing products, as well as pure ellagitannins and gallotannins. In recent years a great emphasis has been put on the consideration of metabolism and bioavailability of natural products during examination of their biological effects. Conducted in vivo and in vitro studies of polyphenols metabolism put a new light on this issue and indicate the gut microbiota to play a crucial role in the health effects following their oral administration. The aim of the review is to summarize the knowledge about HT-containing products’ phytochemistry and their anti-inflammatory effects together with discussion of the data about observed biological activities with regards to the current concepts on the HTs’ bioavailability and metabolism. Orally administered HT-containing products due to the limited bioavailability of ellagitannins and gallotannins can influence immune response at the level of gastrointestinal tract as well as express modulating effects on the gut microbiota composition. However, due to the chemical changes being a result of their transit through gastrointestinal tract, comprising of hydrolysis and gut microbiota metabolism, the activity of produced metabolites has to be taken into consideration. Studies regarding biological effects of the HTs’ metabolites, in particular urolithins, indicate their strong and structure-dependent anti-inflammatory activities, being observed at the concentrations, which fit the range of their established bioavailability. The impact of HTs on inflammatory processes has been well established on various in vivo and in vitro models, while influence of microbiota metabolites on silencing the immune response gives a new perspective on understanding anti-inflammatory effects attributed to HT containing products, especially their postulated effectiveness in inflammatory bowel diseases (IBD) and cardiovascular diseases.

Hydroalcoholic extract from Inula helenium callus tissue showed remarkable reducing capacity. An HPLC/DAD analysis revealed the presence of numerous hydroxycinnamic acid derivatives, including chlorogenic acid (5-O-CQA, 0.1 % dry weight) and 3,5-dicaffeoylquinic acid (3,5-DCQA, 0.3 % dry weight), which were among major constituents of the examined extract. Application of a hyphenated chromatographic method—UHPLC/DAD/MSn—allowed identification of sixteen compounds, derivatives of caffeic acid. Apart from the compounds commonly found in Inula sp., the plant material contained eight conjugates of caffeic acid with aldaric acid. The aldarates constituted over 50 % of the hydroxycinnamate fraction in the examined tissue. This is the first report on the occurrence of the caffeoylaldaric acids in Inula sp. and in a plant tissue culture.