Evidence mapPaperPMID 40963079Full record

ArticleAnnals of biomedical engineering2025

Cholesterol Depletion with U18666A and Methyl-β Cyclodextrin Increased Small Molecule Permeability Across Brain Microvascular Endothelial Cells.

Bilal Moiz, Viviana Alpizar Vargas, Ken D Brandon, Gurneet Sangha, Callie Weber, Andrew Li, Tristan Pepper, Matthew Walls, Anthony Qin, Sara Hart and 4 more

Abstract read
In one paragraph

Article in Annals of biomedical engineering, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

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.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

4 citing papers in PubMed.

  1. Article
  2. Article
  3. Review
  4. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

14 authors.

Bilal MoizUniversity of Maryland, College Park, MD, 20742, USA.ORCID http://orcid.org/0000-0001-7378-6399
Viviana Alpizar VargasUniversity of Maryland, College Park, MD, 20742, USA.
Ken D BrandonUniversity of Maryland, College Park, MD, 20742, USA.
Gurneet SanghaUniversity of Maryland, College Park, MD, 20742, USA.
Callie WeberUniversity of Maryland, College Park, MD, 20742, USA.
Andrew LiUniversity of Maryland, College Park, MD, 20742, USA.
Tristan PepperUniversity of Maryland, College Park, MD, 20742, USA.
Matthew WallsUniversity of Maryland, College Park, MD, 20742, USA.
Anthony QinUniversity of Maryland, College Park, MD, 20742, USA.
Sara HartUniversity of Maryland, College Park, MD, 20742, USA.
Cristin DavidsonEunice Kennedy Shriver National Institute of Child Health and Human Development, National Institutes of Health, Bethesda, MD, 20892, USA.
Kimberly StrokaUniversity of Maryland, College Park, MD, 20742, USA.
Forbes D PorterEunice Kennedy Shriver National Institute of Child Health and Human Development, National Institutes of Health, Bethesda, MD, 20892, USA.
Alisa Morss ClyneUniversity of Maryland, College Park, MD, 20742, USA. aclyne@umd.edu.ORCID http://orcid.org/0000-0003-2462-2122

Funding

Metabolic interactions in the vascular wall: an integrated experimental and computational approachR01HL165193 · UNIV OF MARYLAND, COLLEGE PARK · 2025 to 2025
$744k
The effect of laminar and disturbed flow on endothelial glucose metabolismR01HL140239 · NHLBI · UNIV OF MARYLAND, COLLEGE PARK · PI Alisa S Morss Clyne · 2022 to 2022
$383k
Exploring mechanisms of aquaporin-mediated cell migrationR35GM142838 · UNIV OF MARYLAND, COLLEGE PARK · 2025 to 2025
$380k
American Heart Association 1030856American Heart Association 916512Eunice Kennedy Shriver National Institute of Child Health and Human Development HD008988National Science Foundation 2211966National Science Foundation DGE 1632976NHLBI NIH HHS R01 HL140239NHLBI NIH HHS R01HL140239-01NHLBI NIH HHS R01 HL165193NHLBI NIH HHS RO1HL165193NIGMS NIH HHS R35 GM142838
6 · The paper itself

Abstract

Cholesterol is a vital component of the cell membrane and plays an essential role in mediating integral membrane protein function. Altered cholesterol regulation has been implicated in neurological diseases that are associated with blood-brain barrier breakdown. However, the role of brain barrier function in inherited disorders of cholesterol metabolism, such as Niemann-Pick disease C1 (NP-C1), remains unclear. In this study, we determined how cholesterol depletion with U18666A, a chemical inhibitor of NPC1 protein, as well as with the cholesterol-depleting agent methyl-β cyclodextrin (MβCD), impacted brain endothelial cell barrier function. We hypothesized that cholesterol depletion would decrease barrier integrity by disrupting tight junction protein continuity. To test this hypothesis, we differentiated human-induced pluripotent stem cells into brain microvascular endothelial cells (hiBMECs). We then assessed barrier integrity by quantifying trans-endothelial electrical resistance (TEER), small fluorescent molecule permeability, and tight junction continuity and protein levels. We now show that U18666A-treated hiBMECs demonstrated a 75% decrease in TEER and 9-fold increase in sodium fluorescein permeability. Similar trends were observed for hiBMECs treated with MβCD, which showed significantly lowered TEER (93% decrease) and increased sodium fluorescein permeability (20-fold higher). We also observed decreased continuity of the tight junction proteins occludin (13% lower) and claudin-5 (8% lower) as well as a 53% decrease in claudin-5 protein with U18666A treatment. Co-treating U18666A-treated hiBMECs with hydroxypropyl-β cyclodextrin (HPβCD), which releases lysosomal cholesterol, prevented these changes. Together, our results demonstrate that cholesterol is vital for hiBMEC barrier function and tight junction continuity. This study highlights the potential of therapeutics targeted to brain endothelium in NP-C1 and other cholesterol metabolism disorders.

Indexed as

Androstenesbeta-CyclodextrinsBlood-Brain BarrierBrainCapillary PermeabilityCholesterolEndothelial CellsMicrovesselsCell LineHumansInduced Pluripotent Stem CellsTight Junctions3-beta-(2-(diethylamino)ethoxy)androst-5-en-17-oneAndrostenesbeta-CyclodextrinsCholesterolmethyl-beta-cyclodextrinBlood–brain barrierBrain endothelialCholesteroliPSC-BMECNiemann-Pick diseaseTight junction

Identifiers

PMID40963079
PMCPMC12575569

What Socratic holds

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LicenceCC BY
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.