Evidence map›Paper›PMID 22954966›Full record

ArticleJournal of chromatography. B, Analytical technologies in the biomedical and life sciences2012

Development of a sensitive HPLC method to measure in vitro permeability of E- and Z-isomeric forms of thiosemicarbazones in Caco-2 monolayers.

Zufan Debebe, Sergei Nekhai, Meseret Ashenafi, David B Lovejoy, Danuta S Kalinowski, Victor R Gordeuk, W Malcolm Byrnes, Des R Richardson, Pradeep K Karla

Abstract read
In one paragraph

Article in Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
1.4field-weighted citation impact, top 19% of its field
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

5 citing papers in PubMed, 17 citations in OpenAlex.

  1. Article
  2. Synthesis and Antibacterial Activity of Novel Hydroxy Semicarbazone Derivatives.Iranian journal of pharmaceutical research : IJPR · 2016
    Article
  3. Article
  4. Article
  5. 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

9 authors at 4 institutions in 2 countries.

Zufan DebebeCenter for Sickle Cell Disease, Department of Medicine, Howard University College of Medicine, Washington, DC, United States.
Sergei Nekhai
Meseret Ashenafi
David B Lovejoy
Danuta S Kalinowski
Victor R Gordeuk
W Malcolm Byrnes
Des R Richardson
Pradeep K Karla
Howard University · USUniversity of Sydney · AURobert Bosch (Australia) · AUUniversity of Illinois Chicago · US

Funding

STRUCTURAL/FUNCTIONAL CHARACTERIZATION OF AMINOGLYCOSIDEG12RR003048 · NCRR · HOWARD UNIVERSITY · PI SOUTHERLAND, WILLIAM M. · 1985 to 2011
$19.0M
UVDM01RR010284 · NCRR · HOWARD UNIVERSITY · PI TAYLOR, WILLIAM ROBERT · 1996 to 2010
$17.4M
Georgetown-Howard Universities Center for Clinical and Translational Science (GHUUL1RR031975 · NCRR · GEORGETOWN UNIVERSITY · PI VERBALIS, JOSEPH G · 2010 to 2011
$14.6M
Howard University Research Scientist AwardR25HL003679 · NHLBI · HOWARD UNIVERSITY · PI NEKHAI, SERGEI · 2005 to 2009
$1.7M
Regulation of HIV-1 Transcription by CDK2SC1GM082325 · NIGMS · HOWARD UNIVERSITY · PI NEKHAI, SERGEI · 2008 to 2011
$1.2M
Georgetown-Howard Universities Center for Clinical and Translational Science (GHUKL2RR031974 · NCRR · GEORGETOWN UNIVERSITY · PI VERBALIS, JOSEPH G · 2010 to 2011
$711k
Characterization and Engineering of Fused Chorismate-Utilizing EnzymesSC3GM083752 · NIGMS · HOWARD UNIVERSITY · PI BYRNES, WALTON MALCOLM · 2008 to 2011
$623k
Effect of Iron Chelators on HIV-1 transcriptionF31HL090025 · NHLBI · HOWARD UNIVERSITY · PI DEBEBE, ZUFAN KEREGO · 2008 to 2011
$139k
NCRR NIH HHS 2G12RR003048NCRR NIH HHS 2MO1 RR10284NCRR NIH HHS G12 RR003048NCRR NIH HHS KL2 RR031974NCRR NIH HHS KL2RR031974NCRR NIH HHS M01 RR010284NCRR NIH HHS UL1 RR031975NCRR NIH HHS UL1RR031975NHLBI NIH HHS 2R25 HL003679-08NHLBI NIH HHS F31 HL090025NHLBI NIH HHS R25 HL003679NIGMS NIH HHS 1SC1GM082325NIGMS NIH HHS 1SC3GM083752NIGMS NIH HHS SC1 GM082325NIGMS NIH HHS SC3 GM083752
6 · The paper itself

Abstract

In the current study, we developed a HPLC method to quantitatively measure the permeability of the BpT-based chelators, 2-benzoylpyridine 4-ethyl-3-thiosemicarbazone (Bp4eT) and 2-benzoylpyridine 4-allyl-3-thiosemicarbazone (Bp4aT), across human colorectal adenocarcinoma (Caco-2) monolayers as a model of gut absorption. In aqueous solution, Bp4eT and Bp4aT formed inter-convertible Z and E isomers that were resolved by HPLC. Peak area was linear with respect to chelator concentration. Acceptable within-day and between-day precision (<22%) and accuracy (85-115% of true values) were obtained over a range of 1.0-100μM for Bp4eT and 1.5-300μM for Bp4aT. Limits of detection were 0.3μM and 1μM for Bp4eT and Bp4aT, respectively, while corresponding limits of quantification were 1μM and 5μM. Both chelators showed significant ability to chelate iron in THP-1 cells using a calcein-based assay and no apparent cytotoxicity was observed within 24h. Ratios of the apical to basolateral and basolateral to apical transport for Bp4eT were 1.10 and 0.89 at 100μM and 300μM respectively, indicating equal bi-directional movement of the compounds. Similarly, ratios were 0.77 and 0.92 for Bp4aT, respectively. This study demonstrates that Bp4eT and Bp4aT can be efficiently transported through Caco-2 cells and can potentially be formulated for oral delivery.

Indexed as

Caco-2 CellsCell Line, TumorCell Membrane PermeabilityCell SurvivalChromatography, High Pressure LiquidHumansIronIron Chelating AgentsIsomerismIsoquinolinesLimit of DetectionModels, BiologicalReproducibility of ResultsThiosemicarbazonesIronIron Chelating AgentsIsoquinolineslucifer yellowThiosemicarbazones

Identifiers

PMID22954966
PMCPMC3457786
OpenAlexW2093729543

What OpenQuestion holds

Textmetadata
LicenceTDM
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 OpenQuestion graph.