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*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

13 Citations (Scopus)

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 (

Original languageEnglish
Pages (from-to)25-32
Number of pages8
JournalJournal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences
Volume906
DOIs
Publication statusPublished - 1 Oct 2012
Externally publishedYes

Keywords

  • HIV-1 iron chelator
  • HPLC method development
  • Inter-convertible Z and E isomers
  • Caco2 drug permeability
  • INHIBIT HIV-1 TRANSCRIPTION
  • IRON CHELATORS
  • GENE-EXPRESSION
  • CELLS
  • TRANSPORT
  • DESFERRIOXAMINE
  • MECHANISMS
  • SERIES
  • IDENTIFICATION
  • DEFERIPRONE

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