Inhibitory effect of clemastine on P-glycoprotein expression and function: an in vitro and in situ study

Authors

  • Hadi Valizadeh Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, Iran
  • Hamed Hamishekar Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, Iran
  • Leila Mohammadnejad Immunology Research Center, Tabriz University of Medical Sciences, Tabriz, Iran
  • Mehran Mesgari Abbasi Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, Iran|Students Research Committee, Tabriz University of Medical Sciences, Tabriz, Iran
  • Parvin Zakeri-Milani Liver and Gastrointestinal Diseases Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran
Abstract:

Objective(s):Transporters have an important role in pharmacokinetics of drugs. Inhibition or induction of drug transporters activity can affect drug absorption, safety, and efficacy. P-glycoprotein (P-gp) is the most important membrane transporter that is responsible for active efflux of drugs. It is important to understand which drugs are substrates, inhibitors, or inducers of P-gp to minimize or avoid unwanted interactions. The aim of this study was to investigate the effects of clemastine on the expression and function of P-gp. Materials and Methods: The effect of clemastine on P-gp function and expression was evaluated in vitro byrhodamine-123 (Rho123) efflux assay in Caco-2 cells and Western blot analysis. Rat in situ single pass intestinal permeability model was used to investigate the clemastine effect on digoxin Peff, as a known P-gp substrate. Digoxin levels in intestinal perfusates were assayed by high performance liquid chromatography (HPLC) method. Results:The Caco-2 intracellular accumulation of Rho123 in clemastine and verapamil treated cells was 90.8 ± 9.8 and 420.6±25.4 pg/mg protein, respectively which was significantly higher than that in control cells (50.2±6.0; P

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Journal title

volume 19  issue 4

pages  423- 429

publication date 2016-04-01

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