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Mucosal and blood-brain barrier transport kinetics of the plant N-alkylamide spilanthol using in vitro and in vivo models

Overview of attention for article published in BMC Complementary and Alternative Medicine, June 2016
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Title
Mucosal and blood-brain barrier transport kinetics of the plant N-alkylamide spilanthol using in vitro and in vivo models
Published in
BMC Complementary and Alternative Medicine, June 2016
DOI 10.1186/s12906-016-1159-0
Pubmed ID
Authors

Lieselotte Veryser, Lien Taevernier, Tanmayee Joshi, Pratima Tatke, Evelien Wynendaele, Nathalie Bracke, Sofie Stalmans, Kathelijne Peremans, Christian Burvenich, Martijn Risseeuw, Bart De Spiegeleer

Abstract

N-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. Spilanthes 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. Spilanthol 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). Spilanthol 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.

Twitter Demographics

The data shown below were collected from the profiles of 2 tweeters who shared this research output. Click here to find out more about how the information was compiled.

Mendeley readers

The data shown below were compiled from readership statistics for 42 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 42 100%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 8 19%
Student > Bachelor 7 17%
Researcher 6 14%
Student > Master 6 14%
Student > Doctoral Student 5 12%
Other 4 10%
Unknown 6 14%
Readers by discipline Count As %
Agricultural and Biological Sciences 11 26%
Pharmacology, Toxicology and Pharmaceutical Science 9 21%
Chemistry 4 10%
Biochemistry, Genetics and Molecular Biology 3 7%
Medicine and Dentistry 3 7%
Other 6 14%
Unknown 6 14%

Attention Score in Context

This research output has an Altmetric Attention Score of 2. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 12 August 2016.
All research outputs
#4,120,459
of 8,204,367 outputs
Outputs from BMC Complementary and Alternative Medicine
#1,024
of 2,064 outputs
Outputs of similar age
#133,432
of 270,105 outputs
Outputs of similar age from BMC Complementary and Alternative Medicine
#31
of 76 outputs
Altmetric has tracked 8,204,367 research outputs across all sources so far. This one is in the 47th percentile – i.e., 47% of other outputs scored the same or lower than it.
So far Altmetric has tracked 2,064 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 6.6. This one is in the 44th percentile – i.e., 44% of its peers scored the same or lower than it.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 270,105 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 46th percentile – i.e., 46% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 76 others from the same source and published within six weeks on either side of this one. This one has gotten more attention than average, scoring higher than 53% of its contemporaries.