Bioavailability and pharmacokinetics of Echinacea purpurea preparations and their interaction with the immune system

Cannabinoids and the immune system: An overview

“…have structural similarities with AEA and affinity for CB2R (Raduner et al, 2006). In low nanomolar concentrations, they can exert effects on cytokine and chemokine expression in human blood (Woelkart et al, 2006). It was shown that IL-6 produced by B cells or macrophages can be increased by alkamides and AEA in a CB2R-dependent manner (Jones, 2005;Woelkart et al, 2008).…”

Synergistic immunomopharmacological effects of N-alkylamides in Echinacea purpurea herbal extracts

“…2). Based on data showing that certain Echinacea N-isobutylamides and N-methylbutylamides bind to and partially activate the CB 2 receptor in vitro [5,14], the E. purpurea radix and herba tinctures were dried under N 2 and dissolved in DMSO to determine whether they displace the high-affinity cannabinoid receptor ligand [ 3 H]CP-55940 (hCB 2 K i = 0.39 nM) from the hCB 2 receptor. In addition, the extracts were tested for their ability to activate the CB 2 receptor in HL60 cells as a function of the intracellular calcium [Ca 2+ ] i release that can be blocked by the selective CB 2 receptor antagonist SR144528.…”

“…Based on the fact that the phytochemical profiles of distinct Echinacea products are highly variable and strictly depend on the harvested plant material and extraction protocols [12] an understanding of the bioavailability and immunopharmacology of potentially bioactive compounds is important. N-alkylamides have been shown to reach nM plasma concentrations in humans despite their relatively moderate bioavailability, and depending on the initial dose, potentially bioactive concentrations can be reached [13,14]. Moreover, there is good evidence that the major bioavailable Echinacea N-alkylamides in part mimic the action of endocannabinoids [4][5][6]15].…”

Alkamide production from hairy root cultures of Echinacea

“…More than 20 different alkamides have been identified in Echinacea species (Barnes et al 2005). Alkamides trigger enhanced anti-inflammatory activity and immunostimulatory responses (Chen et al 2005;Woelkart et al 2006). Alkamides from Echinacea modulated a therapeutic response via the CB 2 -specific cannabinoid receptor and inhibited lipopolysaccharide-induced inflammation in human whole blood (Raduner et al 2006;Woelkart and Bauer 2007).…”