title: Pharmacokinetics and immunomodulatory effect of lipophilic Echinacea extract formulated in softgel capsules.
abstract: An attractive herbal product, softgel capsules containing 10 mg of Echinacea angustifolia lipophilic extract, was given in a single oral administration to 10 human volunteers to perform a pharmacokinetic and immunological study. The plasma concentration of the major constituent was monitored, quantifying at predetermined time points the dodeca-2E,4E,8Z,10E/Z-tetraenoic isobutylamides (tetraene). The plasmatic levels of IL-2, IL-6, IL-8, IL-10 and TNF-a in samples collected before and 24 h after drug administration were analyzed by cytokine assay. The total RNA was extracted from limpho-monocyte isolated from the same blood samples and the same cytokines in terms of gene expression were evaluated. With the help of proper statistical tests the differences between the values obtained at 0 and 24 h were evaluated. Results of pharmacokinetic studies attest an approximately 3.5-fold improvement of tetraene oral bioavailability compared with previously published studies. Dodeca-2E,4E-dienoic acid isobutylamide exerts immunomodulatory effects down-regulating the gene expression and reducing the protein plasmatic levels of pro-inflammatory cytokines such as IL-6, TNF-α and IL-8, and up-regulating the expression of anti-inflammatory molecules as IL-10. Student's two-sided paired t-test and non-parametric Wilcoxon-Mann-Whitney signed rank test agree in the conclusions about the differences between the ln values at 24 h and corresponding ln values at 0 h.
authors.affiliation: Department of Pharmaceutical Sciences, University of Padova, Via F. Marzolo 5, 35131 Padova, Italy.
authors.forename: Stefano
authors.initials: S
authors.lastname: Dall'Acqua
authors.affiliation: Department of Chemical and Pharmaceutical Sciences, University of Trieste, P.le Europa 1, 34127 Trieste, Italy.
authors.forename: Beatrice
authors.initials: B
authors.lastname: Perissutti
authors.affiliation: Faculty of Pharmacy, University of Ljubljana, Askerceva 7, SI-1000 Ljubljana, Slovenia.
authors.forename: Iztok
authors.initials: I
authors.lastname: Grabnar
authors.affiliation: Department of Life Sciences, University of Trieste, Cattinara Hospital, P.le Europa 1, 34127 Trieste, Italy.
authors.forename: Rossella
authors.initials: R
authors.lastname: Farra
authors.affiliation: Institute for Maternal and Child Health IRCCS Burlo Garofolo, Via dell'Istria 65/1, 34100 Trieste, Italy; Department of Medicine, Surgery and Health Sciences, University of Trieste, Trieste, Italy.
authors.forename: Manola
authors.initials: M
authors.lastname: Comar
authors.affiliation: Institute for Maternal and Child Health IRCCS Burlo Garofolo, Via dell'Istria 65/1, 34100 Trieste, Italy.
authors.forename: Chiara
authors.initials: C
authors.lastname: Agostinis
authors.affiliation: Department of Mathematics and Geosciences, University of Trieste, Via A. Valerio 12/1, 34127 Trieste, Italy.
authors.forename: Gabriella
authors.initials: G
authors.lastname: Caristi
authors.affiliation: Department of Chemical and Pharmaceutical Sciences, University of Trieste, P.le Europa 1, 34127 Trieste, Italy.
authors.forename: Samuel
authors.initials: S
authors.lastname: Golob
authors.affiliation: Department of Chemical and Pharmaceutical Sciences, University of Trieste, P.le Europa 1, 34127 Trieste, Italy. Electronic address: vojnovic@units.it.
authors.forename: Dario
authors.initials: D
authors.lastname: Voinovich
mesh_terms: D000328:Adult; D001682:Biological Availability; D002214:Capsules; D016207:Cytokines / Q000097:blood* / Q000235:genetics; D020900:Echinacea / Q000737:chemistry*; D005260:Female; D005786:Gene Expression Regulation; D006801:Humans; D007155:Immunologic Factors / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D007378:Interleukins / Q000097:blood / Q000235:genetics; D008297:Male; D008875:Middle Aged; D010936:Plant Extracts / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D016037:Single-Blind Method; D018709:Statistics, Nonparametric; D013997:Time Factors; D014409:Tumor Necrosis Factor-alpha / Q000097:blood / Q000235:genetics
chemical_list: D002214:Capsules; D016207:Cytokines; D007155:Immunologic Factors; D007378:Interleukins; D010936:Plant Extracts; D014409:Tumor Necrosis Factor-alpha
keywords: Echinacea angustifolia lipophilic extract; Pharmacokinetics; Pro-inflammatory cytokines; Softgel capsules; Tetraene