ArticlePloS one2022
Permeability of dopamine D2 receptor agonist hordenine across the intestinal and blood-brain barrier in vitro.
Article in PloS one, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
5 citing papers in PubMed, 11 citations in OpenAlex.
- Prediction of human exposure and first-pass metabolism of the fungicide trifloxystrobin using an in vitro intestinal pancreatin and Caco-2/HT29-MTX model.Archives of toxicology · 2026Article
- Revamping Parkinson's disease therapy using PLGA-based drug delivery systems.NPJ Parkinson's disease · 2025Review
- Protective Effect of Hordenine on Concanavalin A-Induced Hepatic Injury.Journal of inflammation research · 2025Article
- Beneficial Effects of Hordenine on a Model of Ulcerative Colitis.Molecules (Basel, Switzerland) · 2023Article
- Chemical characterization and metabolic profiling of Xiao-Er-An-Shen Decoction by UPLC-QTOF/MS.Frontiers in pharmacology · 2023Article
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
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.
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Registered trials
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