ArticleCellular and molecular neurobiology2008
Endothelin-1 reduces p-glycoprotein transport activity in an in vitro model of human adult blood-brain barrier.
Article in Cellular and molecular neurobiology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed, 23 citations in OpenAlex.
- Uptake of DU145 and LNCaP prostate cancer cell line derived extracellular vesicles is inversely correlated with blood-brain barrier integrity in vitro.Fluids and barriers of the CNS · 2025Article
- The role of reactive oxygen species in the regulation of the blood-brain barrier.Tissue barriers · 2025Review
- The multidrug resistance 1 gene Abcb1 in brain and placenta: comparative analysis in human and guinea pig.PloS one · 2014Article
- Minimally invasive procedures reduce perihematomal endothelin-1 levels and the permeability of the BBB in a rabbit model of intracerebral hematoma.Neurological sciences : official journal of the Italian Neurological Society and of the Italian Society of Clinical Neurophysiology · 2013Article
- Susceptibility of juvenile and adult blood-brain barrier to endothelin-1: regulation of P-glycoprotein and breast cancer resistance protein expression and transport activity.Journal of neuroinflammation · 2012Article
- Drug transport into the central nervous system: using newer findings about the blood-brain barriers.Drug delivery and translational research · 2012Article
- Lipopolysaccharide impairs blood-brain barrier P-glycoprotein function in mice through prostaglandin- and nitric oxide-independent pathways.Journal of neuroimmune pharmacology : the official journal of the Society on NeuroImmune Pharmacology · 2009Article
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimsIt is a huge challenge to understand the blood-brain barrier (BBB), which is a key element in neuroinflammation associated with many brain diseases. The BBB also regulates the passage of xenobiotics into the central nervous system (CNS), and therefore influences drug efficacy. This may be due to the presence of ATP binding cassette transporters such as P-glycoprotein (Pgp) on the BBB, which are efflux pumps known to transport many drugs. The peptide endothelin 1 (ET-1) is involved in different kinds of CNS diseases and neuroinflammation, and is known to modulate Pgp transport activity. Although there are data from animal models, data from human models are scarce. We evaluated Pgp expression and transport activity in adult human brain microvascular endothelial cells (HBMECs) when exposing an adult human in vitro BBB model to ET-1.
methodsAdult HBMECs were cocultured with human adult glial cells on a Transwells to mimic blood and CNS compartments. These human in vitro BBBs were exposed for 24 h to 100 nM and 10 nM ET-1. Pgp expression was assessed by flow cytometry and its transport activity by measuring radiolabelled digoxin passage.
resultsAfter exposure to ET-1, flow cytometry showed no shift of fluorescence intensity for a Pgp specific antibody. The passage of digoxin increased with a significant decrease of Q ratio for 10 nM ET-1.
conclusionOur results show that ET-1 has no effect on Pgp expression of adult HBMECs, but does modulate Pgp transport activity.
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