Abstract

The influence of the common tansy (Tanacetum vulgare) flower polysaccharide complex on P-glycoprotein (Pgp, ABCB1-protein) activity in Caco-2 cell line was studied. The in vitro Pgp activity was assessed by measuring fexofenadine transport in a transwell-system. The ratio of apparent permeability coefficients b–a/a–b for fexofenadine decreased by 57.1, 62.7, and 72.1% as compared to a control series if the transport medium was treated with the polysaccharide complex at concentrations of 7, 10, and 100 μM, respectively. This indicated that the polysaccharide decreased the ABCB1-protein activity. Acomparison of the apparent permeability coefficients of fexofenadine and their ratio for the Pgp inhibitor verapamil and the polysaccharide complex from common tansy flowers showed that the polysaccharide inhibited Pgp more than verapamil. The IC50 of the studied polysaccharide complex was calculated and allowed the dose for in vivo studies to be determined.

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