Echinacea angustifolia

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  • Alkamides from Echinacea angustifolia Interact with P-glycoprotein of primary brain capillary endothelial cells isolated from porcine brain blood vessels.
    Planta medica, 2013
    Co-Authors: Anne Mahringer, Rudolf Bauer, Karin Ardjomand-woelkart, Gert Fricker, Thomas Efferth
    Abstract:

    The blood-brain barrier prevents the passage of toxic compounds from blood circulation into brain tissue. Unfortunately, drugs for the treatment of neurodegenerative diseases, brain tumors, and other diseases also do not cross the blood-brain barrier. In the present investigation, we used isolated porcine brain capillary endothelial cells and a flow cytometric calcein-AM assay to analyze inhibition of P-glycoprotein, a major constituent of the blood-brain barrier. We tested 8 alkamides isolated from Echinacea angustifolia and found that four of them inhibited P-glycoprotein-mediated calcein transport in porcine brain capillary endothelial cells.

  • an evaluation of Echinacea angustifolia in experimental rhinovirus infections
    The New England Journal of Medicine, 2005
    Co-Authors: Ronald B. Turner, Rudolf Bauer, Karin Woelkart, Thomas C Hulsey, David J Gangemi
    Abstract:

    background Echinacea has been widely used as an herbal remedy for the common cold, but efficacy studies have produced conflicting results, and there are a variety of Echinacea products on the market with different phytochemical compositions. We evaluated the effect of chemically defined extracts from Echinacea angustifolia roots on rhinovirus infection. methods Three preparations of Echinacea, with distinct phytochemical profiles, were produced by extraction from E. angustifolia roots with supercritical carbon dioxide, 60 percent ethanol, or 20 percent ethanol. A total of 437 volunteers were randomly assigned to receive either prophylaxis (beginning seven days before the virus challenge) or treatment (beginning at the time of the challenge) either with one of these preparations or with placebo. The results for 399 volunteers who were challenged with rhinovirus type 39 and observed in a sequestered setting for five days were included in the data analysis. results There were no statistically significant effects of the three Echinacea extracts on rates of infection or severity of symptoms. Similarly, there were no significant effects of treatment on the volume of nasal secretions, on polymorphonuclear leukocyte or interleukin-8 concentrations in nasal-lavage specimens, or on quantitative-virus titer. conclusions The results of this study indicate that extracts of E. angustifolia root, either alone or in combination, do not have clinically significant effects on infection with a rhinovirus or on the clinical illness that results from it.

  • The endocannabinoid system as a target for alkamides from Echinacea angustifolia roots.
    Planta medica, 2005
    Co-Authors: Karin Woelkart, Ying Pei, Alexandros Makriyannis, Robert P. Picone, Rudolf Bauer
    Abstract:

    Alkamides are the major lipophilic constituents of Echinacea angustifolia roots. Due to their structural similarity with anandamide, we have evaluated their ability to bind to rodent cannabinoid receptors CB1 and CB2 by a standard receptor binding assay using [(3)H]CP-55,940 as a radioligand. The alkamides exhibited selective affinity especially to CB2 receptors and can therefore be considered as CB ligands. Most of the alkamides showed good metabolic stability as indicated by the similarity between affinity to CB1 determined in the presence/absence of the protease inhibitor PMSF. It is suggested that CB2 interactions may be the molecular mode of action of Echinacea alkamides as immunomodulators.

  • Bioavailability and pharmacokinetics of alkamides from the roots of Echinacea angustifolia in humans.
    Journal of clinical pharmacology, 2005
    Co-Authors: Karin Woelkart, J. David Gangemi, Ronald B. Turner, Christoph Koidl, Andrea J. Grisold, Egon Marth, Rudolf Bauer
    Abstract:

    Alkamides are suspected to contribute to the activity of Echinacea preparations. They are mainly derived from undeca- and dodecanoic acid and differ in the degree of unsaturation and the configuration of the double bonds. In total, 6 alkamides have been isolated from the roots of Echinacea angustifolia as major lipophilic constituents and have been investigated regarding their pharmacokinetics. A sensitive and specific method has been developed for the identification and quantification of these alkamides in human plasma using liquid chromatography electrospray ionization ion-trap mass spectrometry. The method was applied to analyze plasma samples obtained from a randomized, open, single-dose, crossover study after oral administration of a 60% ethanolic extract from the roots of E. angustifolia to 11 healthy subjects. The maximum concentration of dodeca-2E,4E,8Z,10E/Z-tetraenoic acid isobutylamides, the main alkamides in the roots of E. angustifolia, appeared already after 30 minutes and was 10.88 ng/mL for the 2.5-mL dose.

  • Enzymatic degradation of echinacoside and cynarine in Echinacea angustifolia root preparations
    Pharmaceutical Biology, 2004
    Co-Authors: Karin Wölkart, J. David Gangemi, Ronald B. Turner, Rudolf Bauer
    Abstract:

    Echinacea preparations are among the bestselling herbal medicinal products in North America and Europe. Echinacoside and cynarine are the major polar constituents in the roots of Echinacea angustifolia DC and therefore are often used as marker compounds for the standardization of corresponding Echinacea preparations. This study demonstrates that echinacoside and cynarine are highly susceptible to enzymatic degradation and oxidation in hydroalcoholic solutions during the extraction process. This makes their use as analytical marker compounds still possible, although care must be taken to avoid error due to this enzymatic degradation. Batch-to-batch consistency and standardization of preparations from E. angustifolia roots require in particular a control of this enzymatic activity. The polyphenol oxidase (PPO), which is responsible for the oxidative degradation of echinacoside and cynarine, was isolated from the roots of E. angustifolia. An Electrospray Ionization-Liquid Chromotography-Mass Spectometry (ESI...

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