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Scientific Name:
Echinacea purpurea, E. angustifolia, E. pallida
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Evidence of Activity
Pharmacokinetics (ADME)
Echinacea was among dietary supplements shown to exhibit CYP P450 metabolism along with possible CYP3A4 induction activity, which may affect pharmacogenetic profiles and result in interactions with medications and other supplements. Matura 2021
Combined oral administration of Echinacea angustifolia and Zingiber officinale extracts in softgel capsules resulted in rapid assimilation of the bioactive constituents in healthy human subjects, with tmax detected in plasma from 30?min to 1.40?h. Dall'Acqua 2019
Seven phenolic acids (syringic, ferulic, caffeic, vanillic, p-coumaric, 3,4-dihydroxybenzoic, and 4-hydroxybenzoic acids) were quantified in rat plasma following oral administration of Echinacea purpurea extract, using a newly developed and validated UHPLC-MS/MS method. Du 2017
The pharmacokinetics, tissue distribution, and plasma protein binding of cichoric acid administered at 50 mg/kg via gastric gavage were studied in rats. Wang 2016
A sensitive method for the determination of phenolic compounds from Echinacea purpurea (cichoric acid, chlorogenic acid, quinic acid, and caffeic acid) in rat plasma following oral administration was developed. Gan 2016
Echinacea angustifolia active compounds, dodeca-2E,4E,8Z,10E/Z-tetraenoic acid isobutylamides, were shown to accumulate in the brain and periepididymal fat following oral administration of E. angustifolia root extract, in rats. Jedlinszki 2014
Non-determined constituents in an Echinacea pallida ethanolic extract modulated the metabolism and efflux of its alkamides and ketones in the human intestinal epithelial Caco-2 cell model. Both the extract and several isolated compounds decreased P-glycoprotein-mediated transport in the cells. Qiang 2013
An LC-MS/MS method for the determination of the major alkylamides of Echinacea purpurea in human plasma was developed. Goey 2012
Administration of an Echinacea purpurea extract increased the bioavailability of dodeca-2 E,4 E,8 Z,10 E/ Z-tetraenoic acid isobutylamides (tetraenes), compared to the pure compounds, in rats. Ardjomand-Woelkart 2011
An LC-MS/MS method for the quantitative analysis of the Echinacea purpurea constituent undeca-2-ene-8,10-diynoic acid isobutylamide in human plasma was developed and validated. Goey 2011
Pharmacokinetic pathways of some of the most commonly used herbal medicines, including echinacea, are reviewed. He 2010
Metabolism of one of the major echinacea compounds by human recombinant cytochrome P450 (CYP) enzymes and human liver microsomes was investigated. Metabolites of CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, and CYP2E1 were identified. Toselli 2010
It is demonstrated using split-thickness human skin in a Franz diffusion cell (FDC) system for the first time that spilanthol, a prominent N-alkylamide present in genera Echinacea, Xanthoxylum and Spilanthes permeates the skin. Boonen 2009
The pharmacokinetics of dodeca-2 E,4 E,8 Z,10 E/ Z-tetraenoic acid isobutylamides(tetraenes), the main alkamides in echinacea preparations, was investigated in rats after oral administration and showed that these tetraenes are bioavailable in rats with rapid passage across blood-brain barrier. Woelkart 2009
The relative bioavailability of major alkamides, dodeca-2E,4E,8Z,10E/Z-tetraenoic acid isobutylamides, from Echinacea purpurea lozenges at 3 dose levels (0.07, 0.21 & 0.9 mg) was evaluated in a pharmacokinetic study in humans & the possible effects on immunological system were measured. Guiotto 2008
The pharmacokinetics, bioavailability, the elucidation of metabolic pathways of the main alkamides after administration of three different Echinacea purpurea preparations in humans was determined. Woelkart 2008
The study evaluated the effects of St. John's wort and Echinacea on the pharmacokinetics of digoxin, a recognized P-gp substrate in 18 healthy volunteers which showed that Echinacea supplementation did not affect digoxin pharmacokinetics. Gurley 2008
The in vitro CYP3A4 inhibition profiles of Echinacea purpurea, St. John's wort & ketoconazole were evaluated by 3 different substrates: 7-benzyloxy-trifluoromethylcoumarin, 7-benzyloxyquinoline & testosterone which showed a weak inhibition potential of E. purpurea towards CYP3A4-mediated metabolism. Hansen 2008
Extracts of six commonly used herbal products, St. John's wort, common valerian, common sage, Ginkgo biloba, Echinacea purpurea & horse chestnut were investigated for their in vitro inhibitory potential of CYP3A4 mediated metabolism & P-glycoprotein efflux transport activity. Hellum 2008
Comparison of relative oral bioavailability of alkylamides from 2 different Echinacea dosage forms (liquid & tablet) in a small two-way crossover study in humans shows that there was no significant difference in the bioavailability of alkylamides from the liquid and tablet Echinacea formulations. Matthias 2007
The absorption, tissue distribution, and metabolism of trans-Caftaric acid which occurs in chicory and which is one of the bioactive components of Echinacea purpurea was investigated in the ligated stomach of anaesthetized rats. Vanzo 2007
In order to compare the bioavailability of alkamides from liquid and tablet preparations of Echinacea purpurea (Echinaforce) in humans and to study the effects on ex vivo stimulated blood cells, a randomized, single-dose, crossover study with 10 (8 test, 2 placebo) volunteers was performed. Woelkart 2006
The intake of milk thistle, Echinacea species, and goldenseal inhibits cytochrome P450 enzymes in vitro and may increase antiretroviral drugs concentrations, but by clinically unimportant amounts. Lee 2006
The potential bioavailability of alkyl- amides and caffeic acid conjugates using Caco-2 monolayers was assessed and compared with their actual bioavailability in a Phase I clinical trial in healthy volunteers. Matthias 2005
Plasma samples obtained from a randomized, open, single-dose, crossover study after oral administration of a 60% E-OH extract from the roots of E. angustifolia to 11 healthy subjects were analysed by liquid chromatography electrospray ionization ion-trap mass spectrometry. Woelkart 2005
Examination of serial plasma samples from 9 healthy volunteers who ingested echinacea(E) tablets manufactured from Echinacea & E. purpurea provides evidence that alkamides are orally available & their pharmacokinetics are in agreement with the 1 dose 3 times daily regimen recommended for E. Matthias 2005a
Investigation of the metabolism of alkylamide components from an Echinacea preparation as well as that of pure synthetic alkylamides by human liver microsomes suggests they may affect the P450-mediated metabolism of other concurrently ingested pharmaceuticals. Matthias 2005
The alkylamides from Echinacea found to diffuse through Caco-2 monolayers, which are a model of the intestinal epithelial barrier with an apparent permeability of 1 x 10(-4) cm/s but caffeic acid conjugates permeated poorly through the Caco-2 monolayers. Matthias 2004
Oral and intravenous midazolam administration before and after a short course of echinacea (400 mg 4 times a day for 8 days) in 12 healthy subjects in vivo selectively modulated the catalytic activity of cytochrome P450 probed midazolam. Gorski 2004
The earlier findings on Hypericum (St. John's wort) & Echinacea purpurea activities have been confirmed and reported that extracts of Valeriana as well as a fish oil preparation were potent inhibitors of all human cytochrome P-450 enzymes. Strandell 2004
Herbs with the potential to modulate the activity of drug-metabolizing enzymes and/or the drug transporter P-glycoprotein include garlic, ginkgo, echinacea (E. purpurea), ginseng, St John' s wort and kava. Sparreboom 2004
Alkamides from Echinacea species can be easily transported from the intestinum through Caco-2 monolayers and hence may contribute to the in vivo effects of Echinacea preparations. Jager 2002
A quantification method by which it is possible to detect dodeca-2E,4E,8Z,10E/Z-tetraenoic acid isobutylamides in human blood has been developed after oral application of Echinacea purpurea mother tincture. Dietz 2001
Among 21 commercial herbal extracts, Echinacea angustifolia roots, wild cherry, chamomile and licorice, which had IC50 values ranging from 1%-2% of full strength showed significant inhibition of CYP3A4 metabolite formation. Budzinski 2000
History of Record
May 1999
MAJOR REVISION BY: J. Mohanasundarum, MD, PhD
January 2010
December 2022