ArticleBMC complementary and alternative medicine2016
Mucosal and blood-brain barrier transport kinetics of the plant N-alkylamide spilanthol using in vitro and in vivo models.
Article in BMC complementary and alternative medicine, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed.
- The Acute and Chronic Cognitive and Cerebral Blood-Flow Effects of Nepalese Pepper (Nutrients · 2019Trial
- Botany, Ethnopharmacology, Phytochemistry, and Biological Activities ofMolecules (Basel, Switzerland) · 2026Review
- Antihypertensive Effect of a Self-Microemulsifying System Obtained from an Ethanolic Extract ofMolecules (Basel, Switzerland) · 2025Article
- Pharmacological Characteristics of the Hydroethanolic Extract ofEvidence-based complementary and alternative medicine : eCAM · 2023Article
- A Review of the Chemistry and Biological Activities ofPlants (Basel, Switzerland) · 2022Review
- Chemical composition of the lipophilic compounds from the rind and pith of papyrus (Frontiers in plant science · 2022Article
- Proangiogenic Effect of Affinin and an Ethanolic Extract fromMolecules (Basel, Switzerland) · 2021Article
- Spilanthol from Traditionally UsedNutrients · 2019Article
- Article
- Interaction of Plant Extracts with Central Nervous System Receptors.Medicines (Basel, Switzerland) · 2017Review
- Affinin (Spilanthol), Isolated from Heliopsis longipes, Induces Vasodilation via Activation of Gasotransmitters and Prostacyclin Signaling Pathways.International journal of molecular sciences · 2017Article
- Quantitative In Vitro and In Vivo Evaluation of Intestinal and Blood-Brain Barrier Transport Kinetics of the Plant N-Alkylamide Pellitorine.BioMed research international · 2016Article
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11 authors.
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Abstract
backgroundN-alkylamides (NAAs) are a large group of secondary metabolites occurring in more than 25 plant families which are often used in traditional medicine. A prominent active NAA is spilanthol. The general goal was to quantitatively investigate the gut mucosa and blood-brain barrier (BBB) permeability pharmacokinetic properties of spilanthol.
methodsSpilanthes acmella (L.) L. extracts, as well as purified spilanthol were used to investigate (1) the permeation of spilanthol through a Caco-2 cell monolayer in vitro, (2) the absorption from the intestinal lumen after oral administration to rats, and (3) the permeation through the BBB in mice after intravenous injection. Quantification of spilanthol was performed using a validated bio-analytical UPLC-MS(2) method.
resultsSpilanthol was able to cross the Caco-2 cell monolayer in vitro from the apical-to-basolateral side and from the basolateral-to-apical side with apparent permeability coefficients Papp between 5.2 · 10(-5) and 10.2 · 10(-5) cm/h. This in vitro permeability was confirmed by the in vivo intestinal absorption in rats after oral administration, where an elimination rate constant ke of 0.6 h(-1) was obtained. Furthermore, once present in the systemic circulation, spilanthol rapidly penetrated the blood-brain barrier: a highly significant influx of spilanthol into the brains was observed with a unidirectional influx rate constant K1 of 796 μl/(g · min).
conclusionsSpilanthol shows a high intestinal absorption from the gut into the systemic circulation, as well as a high BBB permeation rate from the blood into the brain.
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