In:
PLOS ONE, Public Library of Science (PLoS), Vol. 17, No. 6 ( 2022-6-16), p. e0269486-
Abstract:
Hordenine, a bioactive food compound, has several pharmacological properties and has recently been identified as a dopamine D2 receptor (D2R) agonist. Since the pharmacokinetic profile of hordenine has been described to a limited extent, the present study focused on the transfer and transport of hordenine across the intestinal epithelium and the blood-brain barrier (BBB) in vitro . Hordenine was quickly transferred through the Caco-2 monolayer in only a few hours, indicating a rapid oral uptake. However, the high bioavailability may be reduced by the observed efflux transport of hordenine from the bloodstream back into the intestinal lumen and by first pass metabolism in intestinal epithelial cells. To determine the biotransformation rate of hordenine, the metabolite hordenine sulfate was synthesized as reference standard for analytical purposes. In addition, transfer studies using primary porcine brain capillary endothelial cells (PBCEC) showed that hordenine is able to rapidly penetrate the BBB and potentially accumulate in the brain. Thus, a D2R interaction of hordenine and activation of dopaminergic signaling is conceivable, assuming that the intestinal barrier can be circumvented by a route of administration alternative to oral uptake.
Type of Medium:
Online Resource
ISSN:
1932-6203
DOI:
10.1371/journal.pone.0269486
DOI:
10.1371/journal.pone.0269486.g001
DOI:
10.1371/journal.pone.0269486.g002
DOI:
10.1371/journal.pone.0269486.g003
DOI:
10.1371/journal.pone.0269486.g004
DOI:
10.1371/journal.pone.0269486.g005
DOI:
10.1371/journal.pone.0269486.g006
DOI:
10.1371/journal.pone.0269486.t001
DOI:
10.1371/journal.pone.0269486.t002
DOI:
10.1371/journal.pone.0269486.s001
DOI:
10.1371/journal.pone.0269486.s002
Language:
English
Publisher:
Public Library of Science (PLoS)
Publication Date:
2022
detail.hit.zdb_id:
2267670-3