Phytochemical Analysis and Evaluation of Genotoxic, Antigenotoxic Effects in Bacterial Models, and Hypoglycemic Activity of Epilobium angustifolium L. with Bioguided Isolation of Active Compounds.

This study examined the effects of methanol extract and its sub-extracts from Epilobium angustifolium on α-glucosidase and α-amylase activity. Secondary metabolites and amino acids were quantified using LC-MS/MS. Dichloromethane sub-extract displayed the highest activity and was chosen for further investigation. Despite the widespread use of E. angustifolium, genotoxicity studies were conducted to assess its safety. Dichloromethane significantly inhibited α-glucosidase (IC50 =17.340 µg/mL), making it approximately 293 times more effective than acarbose. Six known compounds, including gallic acid (1), a mixture of quercetin-3-O-α-galactoside (2a) and quercetin-3-O-α-glucoside (2b), quercetin-3-O-α-glucuronic acid (3), quercetin-3-O-α-rhamnoside (4), and kaempferol-3-O-α-rhamnoside (5) were identified. Quercetin-3-O-α-rhamnoside exhibited the highest inhibition of α-glucosidase (IC50 =1735±85 µM), making it 3.70 times more effective than acarbose. Dichloromethane also showed significant antigenotoxic activity against mutagenesis induced by NaN3, 9-AA, 4-NPD, and MNNG. Gallic acid was found in the highest abundance (13253.6931 ng/mL) in the methanolic extract. Furthermore, L-Aspartic acid was the most concentrated amino acid (363.5620 nmol/mL) in the methanolic extract.

Effect of willow herb (Epilobium angustifolium L.) extract addition to canned meat with reduced amount of nitrite on the antioxidant and other activities of peptides.

The present study aimed to evaluate the effect of the addition of various amounts (50, 100, 150 and 1000 mg kg-1) of E. angustifolium L. extracts on the biological activity of peptides in canned meat with reduced amount of sodium nitrite and their stability during 180 days of storage (4 °C). The initial peptide data were collected by LC/MS. Antioxidant activities of peptide extracts were detected on the basis of ABTS˙*, FRAP, and iron(II) chelating activity in in vitro tests. A computational study (based on the BIOPEP-UWM database and INNOVAGEN, PeptideRanker and PROTPARAM tools) was also performed to assist in the interpretation of results. The addition of E. angustifolium L. extracts has a positive effect on the peptide profile and various biological activities, the results of which depend on the amount of the extract added to the meat product. However, it should be remembered that the differences between in silico and in vitro experimental environments necessitate further research to confirm the antioxidant behavior of canned meat products supplemented with E. angustifolium L. extract under physiological conditions. Other interactions between the peptide and the food matrix should also be considered as these can lead to chemical and structural modifications that can affect the bioavailability of the bioactive peptides.

Biological Activity of an Epilobium angustifolium L. (Fireweed) Infusion after In Vitro Digestion.

The biological activity of an in vitro digested infusion of Epilobium angustifolium (fireweed) was examined in a model system of intestinal epithelial and colon cancer tissues. The content of selected phenolic compounds in the digested aqueous extract of fireweed was determined using HPLC-ESI-QTOF-MS/MS. Biological activity was examined using the human colon adenocarcinoma cell lines HT-29 and CaCo-2 and the human colon epithelial cell line CCD 841 CoTr. Cytotoxicity was assessed by an MTT assay, a Neutral Red uptake assay, May-Grünwald-Giemsa staining, and a label-free Electric Cell-Substrate Impedance Sensing cytotoxicity assay. The effect of the infusion on the growth of selected intestinal bacteria was also examined. The extract inhibited the growth of intestinal cancer cells HT-29. This effect can be attributed to the activity of quercetin and kaempferol, which were the most abundant phenolic compounds found in the extract after in vitro digestion. The cytotoxicity of the fireweed infusion was dose-dependent. The highest decrease in proliferation (by almost 80%) compared to the control was observed in HT-29 line treated with the extract at a concentration of 250 µg/mL. The fireweed infusion did not affect the growth of beneficial intestinal bacteria, but it did significantly inhibit E. coli. The cytotoxic effect of the fireweed extract indicates that it does not lose its biological activity after in vitro digestion. It can be concluded that the fireweed infusion has the potential to be used as a supporting agent in colon cancer therapy.

Evaluation of anticholinesterase effect of some Epilobium species and quantification of hyperoside by HPLC.

This article presents the evaluation of anticholinesterase effects of aerial parts of Epilobium angustifolium, E. stevenii and E. hirsutum and isolated flavonoids from E. angustifolium, and quantification of the flavonoids by HPLC. Besides, the highest acetylcholinesterase inhibition was seen in the EtOAc sub-extracts of E. angustifolium and E. stevenii (36.51 ± 1.88 and 39.89 ± 3.09%, respectively), whereas EtOAc sub-extract of E. angustifolium had the best butyrylcholinesterase inhibition (62.09 ± 1.98%). Hyperoside showed strong inhibition activity on both enzymes. The active EtOAc sub-extract of E. angustifolium was quantitatively analyzed for their content of hyperoside (quercetin-3-O-ß-D-galactoside) by HPLC. The content of hyperoside in EtOAc sub-extract of E. angustifolium was detected as 3.312%. The anatomical structures of the stem, leaf, sepal, petal, anther, and filament of E. angustifolium were investigated. The anatomical properties given in this study provide a description of E. angustifolium.[Formula: see text].

Epilobium angustifolium L. Essential Oil-Biological Activity and Enhancement of the Skin Penetration of Drugs-In Vitro Study.

Epilobium angustifolium L. is a popular medicinal plant found in many regions of the world. This plant contains small amounts of essential oil whose composition and properties have not been extensively investigated. There are few reports in the literature on the antioxidant and antifungal properties of this essential oil and the possibility of applying it as a potential promoter of the skin penetration of drugs. The essential oil was obtained by distillation using a Clavenger type apparatus. The chemical composition was analyzed by the GC-MS method. The major active compounds of E. angustifolium L. essential oil (EOEa) were terpenes, including α-caryophyllene oxide, eucalyptol, ß-linalool, camphor, (S)-carvone, and ß-caryophyllene. The analyzed essential oil was also characterized by antioxidant activity amounting to 78% RSA (Radical Scavenging Activity). Antifungal activity against the strains Aspergillus niger, A. ochraceus, A. parasiticum, and Penicillium cyclopium was also determined. The largest inhibition zone was observed for strains from the Aspergillus group. The EOEa enhanced the percutaneous penetration of ibuprofen and lidocaine. After a 24 h test, the content of terpene in the skin and the acceptor fluid was examined. It has been shown that the main compounds contained in the essential oil do not penetrate through the skin, but accumulate in it. Additionally, FTIR-ATR analysis showed a disturbance of the stratum corneum (SC) lipids caused by the essential oil application. Due to its rich composition and high biological activity, EOEa may be a potential candidate to be applied, for example, in the pharmaceutical or cosmetic industries. Moreover, due to the reaction of the essential oil components with SC lipids, the EOEa could be an effective permeation enhancer of topically applied hydrophilic and lipophilic drugs.

Isolation, Chemical Characterization and Antioxidant Activity of Pectic Polysaccharides of Fireweed (Epilobium angustifolium L.).

The aim of this study was to isolate pectins with antioxidant activity from the leaves of Epilobium angustifolium L. Two pectins, EA-4.0 and EA-0.8, with galacturonic acid contents of 88 and 91% were isolated from the leaves of E. angustifolium L. by the treatment of plant raw materials with aqueous hydrochloric acid at pH 4.0 and 0.8, respectively. EA-4.0 and EA-0.8 were found to scavenge the DPPH radical in a concentration-dependent manner at 17-133 µg/mL, whereas commercial apple pectin scavenged at 0.5-2 mg/mL. The antioxidant activity of EA-4.0 was the highest and exceeded the activity of EA-0.8 and a commercial apple pectin by 2 and 39 times (IC50-0.050, 0.109 and 1.961 mg/mL), respectively. Pectins EA-4.0 and EA-0.8 were found to possess superoxide radical scavenging activity, with IC50s equal to 0.27 and 0.97 mg/mL, respectively. Correlation analysis of the composition and activity of 32 polysaccharide fractions obtained by enzyme hydrolysis and anionic exchange chromatography revealed that the antioxidant capacity of fireweed pectins is mainly due to phenolics and is partially associated with xylogalacturonan chains. The data obtained demonstrate that pectic polysaccharides appeared to be bioactive components of fireweed leaves with high antioxidant activity, which depend on pH at their extraction.

Antioxidant and Antiinflammatory Effects of Epilobium parviflorum, Melilotus officinalis and Cardiospermum halicacabum Plant Extracts in Macrophage and Microglial Cells.

BACKGROUND: We investigated the phenolic content characterizing different plant extracts from Epilobium parviflorum, Cardiospermum halicacabum, and Melilotus officinalis, their antioxidant, antiinflammatory effects, and their mechanism of action. METHODS: plant samples were macerated in 40% ethanol or hot/ cold glycerate and assessed for polyphenols content. The antioxidant activity was investigated by DPPH radical scavenging assay and H2DCFDA test in LPS-stimulated RAW264.7 macrophages and N9 microglial cells. MTS experiments and antiinflammatory properties verified cellular toxicity through NO assay. Interaction with A2A adenosine receptors was evaluated through binding assays using [3H]ZM241385 radioligand. RESULTS: Polyphenols were present in 40% ethanol plant extract, which at 0.1-10 µg/µL achieved good antioxidant effects, with a DPPH radical scavenging rate of about 90%. In LPS-stimulated cells, these plant extracts, at 1µg/µL, did not affect cell vitality, displayed significant inhibition of H2DCFDA and NO production, and inhibited ZM 241385 binding in CHO cells transfected with A2A receptors. RAW 264.7 and N9 cells presented a density of them quantified in 60 ± 9 and 45 ± 5 fmol/mg of protein, respectively. CONCLUSION: Epilobium parviflorum, Cardiospermum halicacabum, and Melilotus officinalis extracts may be considered a source of agents for treating disorders related to oxidative stress and inflammation.

Epilobium angustifolium L. Extracts as Valuable Ingredients in Cosmetic and Dermatological Products.

Epilobium angustifolium L. is a popular and well-known medicinal plant. In this study, an attempt to evaluate the possibility of using this plant in preparations for the care and treatment of skin diseases was made. The antioxidant, antiaging and anti-inflammatory properties of ethanolic extracts from Epilobium angustifolium (FEE) were assessed. Qualitative and quantitative evaluation of extracts chemically composition was performed by gas chromatography with mass spectrometry (GC-MS) and high-performance liquid chromatography (HPLC). The total polyphenol content (TPC) of biologically active compounds, such as the total content of polyphenols (TPC), flavonoids (TFC), and assimilation pigments, as well as selected phenolic acids, was assessed. FEE was evaluated for their anti-inflammatory and antiaging properties, achieving 68% inhibition of lipoxygenase activity, 60% of collagenase and 49% of elastase. FEE also showed high antioxidant activity, reaching to 87% of free radical scavenging using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 59% using 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS). Additionally, in vitro penetration studies were performed using two vehicles, i.e., a hydrogel and an emulsion containing FEE. These studies showed that the active ingredients contained in FEE penetrate through human skin and accumulate in it. The obtained results indicate that E. angustifolium may be an interesting plant material to be applied as a component of cosmetic and dermatological preparations with antiaging and anti-inflammatory properties.

Bacterial Cellulose Membrane Containing Epilobium angustifolium L. Extract as a Promising Material for the Topical Delivery of Antioxidants to the Skin.

Bacterial cellulose membranes (BCs) are becoming useful as a drug delivery system to the skin. However, there are very few reports on their application of plant substances to the skin. Komagataeibacter xylinus was used for the production of bacterial cellulose (BC). The BC containing 5% and 10% ethanolic extract of Epilobium angustifolium (FEE) (BC-5%FEE and BC-10%FEE, respectively) were prepared. Their mechanical, structural, and antioxidant properties, as well as phenolic acid content, were evaluated. The bioavailability of BC-FESs using mouse L929 fibroblasts as model cells was tested. Moreover, In Vitro penetration through the pigskin of the selected phenolic acids contained in FEE and their accumulation in the skin after topical application of BC-FEEs was examined. The BC-FEEs were characterized by antioxidant activity. The BC-5% FEE showed relatively low toxicity to healthy mouse fibroblasts. Gallic acid (GA), chlorogenic acid (ChA), 3,4-dihydroxybenzoic acid (3,4-DHB), 4-hydroxybenzoic acid (4-HB), 3-hydroxybenzoic acid (3-HB), and caffeic acid (CA) found in FEE were also identified in the membranes. After topical application of the membranes to the pigskin penetration of some phenolic acid and other antioxidants through the skin as well as their accumulation in the skin was observed. The bacterial cellulose membrane loaded by plant extract may be an interesting solution for topical antioxidant delivery to the skin.

Synthesis, characterization, biological activities and molecular docking of Epilobium parviflorum aqueous extract loaded chitosan nanoparticles.

Epilobium is a medicinal plant; its extracts are widely used traditional medicine due to their broad range of pharmacological and therapeutic properties. Its most prominent feature is its therapeutic effects on prostatic diseases. The aim of this study is preparation of controlled release system of Epilobium parviflorum, and determination of its potential of anticancer applications. For this purpose, Epilobium parviflorum extract (EPE) loaded chitosan nanoparticles were prepared with ionic gelation method to increase the bioavailability of the extract. The nanoparticles were investigated in terms of size, zeta potential, polydispersity index, encapsulation efficiency, loading capacity and release profile. Besides, scanning electron microscopy (SEM) was used to observe the morphology of the nanoparticles. Moreover, Ames/Salmonella test was used to determine the mutagenicity of EPE, and it was shown that it had no mutagenic effect. It was found that EPE loaded chitosan nanoparticles were with 64.47 nm in average size, 0.168 PdI and 15.2 mV zeta potential. Encapsulation efficiency and loading capacity were found as 92.46% and 8%, respectively. Finally, DNA binding assay and in silico molecular docking studies were performed between EPE and DNA in order to contribute to design of plant based controlled release system for use in cancer therapy.

Inventing a herbal tradition: The complex roots of the current popularity of Epilobium angustifolium in Eastern Europe.

ETHNOPHARMACOLOGICAL RELEVANCE: Currently various scientific and popular sources provide a wide spectrum of ethnopharmacological information on many plants, yet the sources of that information, as well as the information itself, are often not clear, potentially resulting in the erroneous use of plants among lay people or even in official medicine. Our field studies in seven countries on the Eastern edge of Europe have revealed an unusual increase in the medicinal use of Epilobium angustifolium L., especially in Estonia, where the majority of uses were specifically related to "men's problems". THE AIM OF THE CURRENT WORK IS: to understand the recent and sudden increase in the interest in the use of E. angustifolium in Estonia; to evaluate the extent of documented traditional use of E. angustifolium among sources of knowledge considered traditional; to track different sources describing (or attributed as describing) the benefits of E. angustifolium; and to detect direct and indirect influences of the written sources on the currently documented local uses of E. angustifolium on the Eastern edge of Europe. MATERIALS AND METHODS: In this study we used a variety of methods: semi-structured interviews with 599 people in 7 countries, historical data analysis and historical ethnopharmacological source analysis. We researched historical and archival sources, and academic and popular literature published on the medicinal use of E. angustifolium in the regions of our field sites as well as internationally, paying close attention to the literature that might have directly or indirectly contributed to the popularity of E. angustifolium at different times in history. RESULTS: Our results show that the sudden and recent popularity in the medical use of E. angustifolium in Estonia has been caused by local popular authors with academic medical backgrounds, relying simultaneously on "western" and Russian sources. While Russian sources have propagated (partially unpublished) results from the 1930s, "western" sources are scientific insights derived from the popularization of other Epilobium species by Austrian herbalist Maria Treben. The information Treben disseminated could have been originated from a previous peak in popularity of E. angustifolium in USA in the second half of the 19th century, caused in turn by misinterpretation of ancient herbals. The traditional uses of E. angustifolium were related to wounds and skin diseases, fever, pain (headache, sore throat, childbirth), and abdominal-related problems (constipation, stomach ache) and intestinal bleeding. Few more uses were based on the similarity principle. The main theme, however, is the fragmentation of use and its lack of consistency apart from wounds and skin diseases. CONCLUSIONS: Historical ethnobotanical investigations could help to avoid creating repeating waves of popularity of plants that have already been tried for certain diseases and later abandoned as not fully effective. There is, of course, a chance that E. angustifolium could also finally be proven to be clinically safe and cost-effective for treating benign prostatic hyperplasia, but this has not yet happened despite recent intensive research. Documented traditional use would suggest investigating the dermatological, intestinal anti-hemorrhagic and pain inhibiting properties of this plant, if any.

Evaluation of the therapeutic effect against benign prostatic hyperplasia and the active constituents from Epilobium angustifolium L.

ETHNOPHARMACOLOGICAL RELEVANCE: Plants of Epilobium angustifolium are popular in China to treatment of traumatic injury, subduing inflammation and menstrual disorders. In European, the preparations or extracts containing E. angustifolium are popular to treat prostate diseases. Recent research suggested that E. angustifolium showed therapeutic effects in early stage of BPH, inflammation of urethra and prostate, as well as micturition problems. And the related researches were focus on aqueous extract and its main constituent of oenothein B. AIM OF THE STUDY: This study aims to evaluate the therapeutic effect against BPH of the ethyl acetate extracts (EAE) and n-butanol extracts (BUE) from E. angustifolium and to chemical investigation of the active constituents. MATERIALS AND METHODS: The in vitro anti-BPH activity was assessed by determining the benign prostatic hyperplasia epithelial-1 (BPH-1) cell viability using MTT assay as well as suppressing of prostate specific antigen (PSA) secretion in prostate epithelial cancer hormone-dependent (LNCaP) cells measured by ELISA method. The in vivo anti-BPH was evaluated by testosterone propionate induced BPH SD rats. After oral administration of BUE at 100, 200 and 400 mg/kg B.W. for 28 days, the prostate weight and index, plasma androgen level, histopathological alteration, oxidative and inflammatory-related factors in prostate were assessed. Phytochemical investigation on active extracts was carried by chromatographic and spectroscopic techniques. Anti-BPH activities of the isolates were evaluated in vitro. RESULTS: BUE and EAE from E. angustifolium exhibited significant anti-BPH effect in vitro. Further in vivo study demonstrated that BUE exhibited therapeutic effects against TP-induced BPH in SD rats via down-regulating of the androgen level, suppressing the expression of NF-κB and eventually alleviating the inflammatory responses and oxidative stress. Phytochemical research on BUE and EAE extracts led to the isolation and identification of 50 compounds. In vitro anti-BPH screening revealed that 26 compounds exhibited anti-proliferation in BHP-1 cell and 36 compounds showed PSA inhibition in LNCap cell, in which 7 compounds exhibited very significant anti-BPH activities in both two cell lines (P < 0.01), 5 compounds with extremely significant activities in one of the cell lines (P < 0.001), and compound 25 exhibited the most potent anti-BPH activity (P < 0.001). CONCLUSIONS: E. angustifolium exhibited the therapeutic potential against BPH, and its active compounds may be used as candidate for treatment of BPH.

Epilobium spp: Pharmacology and Phytochemistry.

The Epilobium species and their extracts are very popular in folk medicine, for a wide range of applications. The purpose of this review is the analysis of the pharmacological properties of Epilobium spp, considering whether their effects (e.g., anti-inflammatory, antioxidant, antitumor, antimicrobial, analgesic, and antiandrogenic) could rationally justify the use of Epilobium as a treatment of numerous diseases. Even if numerous preclinical studies have been reported, randomized controlled clinical trials (for the evaluation of safety and efficacy), and eventually cost-effectiveness studies (to estimate the long-term cumulative costs), are still needed to confirm the usefulness of these medicinal plants in human diseases.

HPLC-ESI-MS/MS analysis of phenolics and in vitro antioxidant activity of Epilobium angustifolium L.

The aerial parts of Epilobium plants are widely used as folk medicine and food around the world. The present study was aimed to investigate the antioxidant activities and active chemical constituents from Epilobium angustifolium L. The results revealed that the EtOAc extract, rich in phenolic compounds and flavonoids (16.81 ± 0.67 g GAE/100 g extract and 4.95 ± 0.21 g QE/100 g extract, respectively), possessed significantly antioxidant activities in reducing power, DPPH radical scavenging activity, ABTS radical scavenging activity and highly in inhibiting lipid peroxidation activity. Simultaneously, active fractions F to H from EtOAc extracts showing potent in vitro antioxidant activities also contained high content of total phenolic and flavonoid. Twenty-eight compounds were identified as phenolic compounds and flavonoids by LC-MS/MS. The results illustrate that the E. angustifolium L., which is rich in phenolics, could be used as a natural resource of antioxidant ingredient.

Evaluation of the Effect of Epilobium angustifolium Aqueous Extract on LNCaP Cell Proliferation in In Vitro and In Vivo Models.

Epilobium sp. are commonly used in traditional medicine in the treatment of early stages of benign prostatic hyperplasia and inflammation. It is suggested that a dominating constituent, oenothein B, is responsible for the extracts therapeutic effects. Several bioactivities were established for extracts and oenothein B in various in vitro models, but due to the questionable bioavailability of this dimeric macrocyclic ellagitannin, their significance in the in vivo effects remains unresolved. We have thus focused our attention on a complex comparative investigation of the in vitro and in vivo activities of phytochemically characterized Epilobium angustifolium aqueous extract and oenothein B on prostate cancer cells proliferation.Incubation of different cell lines with E. angustifolium aqueous extract resulted in a significant reduction of proliferation of PZ-HPV-7 and LNCaP cells, which was partly associated with antiandrogenic activity. These effects were fully congruent with oenothein B, examined in parallel. Oral supplementation of rats implanted with LNCaP cells with E. angustifolium aqueous extract 50-200 mg/kg b. w. resulted in a reduction of the occurrence of prostatic adenoma up to 13 %. Oenothein B was not detected in the urine and feces of the E. angustifolium aqueous extract-treated group, however, conjugates of nasutins gut microbiota metabolites of ellagitannins were detected in the urine, while in human volunteers supplemented with Epilobium tea, only urolithin conjugates were present.Despite observing significant and consistent effects in vitro and in vivo, we were unable to point out unequivocally the factors contributing to the observed E. angustifolium aqueous extract activity, facing the problems of an unknown metabolic fate of oenothein B and interspecies differences in E. angustifolium aqueous extract gut microbiota metabolism.

Evaluation of iron chelating and antioxidant potential of Epilobium hirsutum for the management of iron overload disease.

The present study deals with the investigation of iron chelating and antioxidant potential of Epilobium hirsutum in iron-overloaded rats. Iron overload was induced by 6 IP injections of Iron dextran (12.5mg/100g) administered uniformly over a period of 30 days. Different fractions of E. hirsutum were given orally and deferoxamine (DFO) subcutaneously for 30 days. The extent of iron chelation and various biochemical parameters were estimated on 15th and 30th day of treatment. In-vitro study was assessed by EDTA and DFO method; the results exhibited a dose-dependant iron chelation. The methanolic fraction of methanolic extract (MFME) and methanolic fraction of aqueous extract (MFAE) of E. hirsutum showed significant (p<0.01) iron chelating and antioxidant potential as compared to disease control (DC) rats. The animals treated with MFME and MFAE of E. hirsutum showed significant (p<0.01) vital organ protection as compared to DC rats. The animals treated for longer duration (30th day) reveals better iron chelation potential than shorter ones (15th day). Superior iron chelation was seen at higher dose (300mg/kg) as compared to lower dose (150mg/kg). Taken into an account, our result reveals the reversible iron chelating and antioxidant ability of E. hirsutum and gives some evidence for its possible mechanism via excretion of iron in urine and feces.

Inter-population and inter-organ distribution of the main polyphenolic compounds of Epilobium angustifolium.

Rosebay willowherb (Epilobium angustifolium) contains large amounts of polyphenolic compounds, including tellimagrandin I-based oligomeric ellagitannins (ETs). The aim of this study was to assess the interpopulational and inter-organ variability of the polyphenol fingerprint of E. angustifolium. Seven ETs, 11 flavonol glycosides and neochlorogenic acid were quantified by UHPLC-DAD-ESI-QqQ-MS in the leaves, flowers and stem parts of plants from 10 populations. Total polyphenol content of leaves and flowers ranged from 150 to 200 mg/g dry wt, of which 90% was constituted by dimeric to heptameric ETs. Flowers contained, on average, 10% more oenothein B (dimeric ET) and 2 times less oenothein A (trimeric ET) than leaves. Tetrameric and pentameric ETs exhibited rather similar levels in leaves and flowers whereas hexameric and heptameric were 3-4 times more abundant in flowers than in leaves. Quercetin-3-O-rhamnoside, myricetin-3-O-rhamnoside and kaempferol-3-O-rhamnoside were specific to flower tissue and were absent from leaves. The inflorescence stem showed the highest content in total polyphenols with an average of 250 mg/g dry wt and contained remarkably large amounts of oenothein B and A. Polyphenol content steadily decreased along the inflorescence stem and reached its lowest level in the vegetative part of the stem. The interpopulational variability of most polyphenols was within a two- to threefold range across the 10 sampled populations. Myricetin-3-O-glucoside and myricetin-3-O-glucuronide, however, showed a more population-specific distribution with concentrations varying from 0 to 2.3 mg/g dry wt. Finally, this study showed that the levels of oenothein B and A in the plant are not interdependent but that their relative abundance is constant within a population.

New targets in the battle against dandruff.

Dandruff is a scalp disorder characterized by flaking skin and itch of an excessive oily scalp skin. It affects 55% of the global youth and adult population. Seborrheic dermatitis is a similar scalp skin disorder with aggravated itchy rashes and flaking. Different factors are identified in the dandruff development: increased sebum production, uncontrolled fungal growth of Malassezia strains and individual reaction to pro-inflammatory environment, and the susceptibility to trigger an immunological response. Using in vitro and ex vivo models, we show that an Epilobium angustifolium extract dose dependently reduces lipid synthesis in sebocytes to a maximum of -43% (1% extract), and protects the epidermis from Malassezia-induced morphological changes. Epilobium angustifolium extract also acts through innovative mechanisms involving regulations of defensins (human beta-defensins [hBD2] and hBD3) and toll-like receptor 2 involved in the immunological response of the skin. The anti-dandruff and sebum-regulating efficacy of E. angustifolium extract (1.5%) was confirmed in a clinical study that mobilized 24 volunteers with dandruff and greasy scalp for 30 days. At the end of the study, nonadherent and adherent dandruffs were significantly (p < 0.0001) reduced in average by -54% and -48%, respectively. Using Sebumeter® measurements, scalp sebum production was inhibited by -67% (p < 0.0001) in average over baseline. In conclusion, E. angustifolium extract offers a new innovative approach to dandruff reduction through immunomodulation of the skin response to Malassezia invasion.

Therapeutic Potential of Polyphenols from Epilobium Angustifolium (Fireweed).

Epilobium angustifolium is a medicinal plant used around the world in traditional medicine for the treatment of many disorders and ailments. Experimental studies have demonstrated that Epilobium extracts possess a broad range of pharmacological and therapeutic effects, including antioxidant, anti-proliferative, anti-inflammatory, antibacterial, and anti-aging properties. Flavonoids and ellagitannins, such as oenothein B, are among the compounds considered to be the primary biologically active components in Epilobium extracts. In this review, we focus on the biological properties and the potential clinical usefulness of oenothein B, flavonoids, and other polyphenols derived from E. angustifolium. Understanding the biochemical properties and therapeutic effects of polyphenols present in E. angustifolium extracts will benefit further development of therapeutic treatments from this plant. Copyright © 2016 John Wiley & Sons, Ltd.

Isolation, characterisation and quantification of the main oligomeric macrocyclic ellagitannins in Epilobium angustifolium by ultra-high performance chromatography with diode array detection and electrospray tandem mass spectrometry.

Tannins have beneficial effects in animal nutrition as they are able to decrease methane emission in ruminants and exert anthelminthic activity against intestinal nematodes. However, tannins can have very diverse structures and therefore, different activities. In order to enhance the research in tannin-rich forages we need tools which are able to quantify tannins individually. In this study we isolated and characterised the main tellimagrandin I (TI)-based oligomeric ellagitannins (ETs) from Epilobium angustifolium (willowherb) and developed a UHPLC-DAD-ESI-MS/MS method to quantify them in plant extracts. The mass spectrometer was operated in Multiple Reaction Monitoring mode to enable the selective detection of dimeric to heptameric ETs from the plant extract. The method proved to be sensitive, with limits of detection ranging from 0.1 to 1.3µgmL(-1). The stability test showed a good repeatability with an inter-run deviation of the results from 0.1 to 5%, except for the pentamer and hexamer where it reached 8%. The method was then successfully applied to evaluate the distribution of those ETs in the plant. This work also provides the first time evidence of the presence of tetrameric to heptameric TI in willowherb.