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Updated: Feb 10, 2026

Efficient Mammalian Cell Expression and Single-step Purification of Extracellular Glycoproteins for Crystallization
Published on: December 23, 2015
[INFLUENCE OF ETHINYLESTRADIOL - GESTODENE COMBINATION ON THE FUNCTIONAL ACTIVITY AND EXPRESSION OF P-GLYCOPROTEIN.]
Abstract:
The influence of a combination of ethinylestradiol (6.5 mg/kg) and gestodene (16.5 mg/kg) on the functional activity of P-glycoprotein efflux transporter and its expression in the liver and small intestine was studied on 20 Chinchilla rabbits. P-glycoprotein functional activity was characterized by the pharmacokinetics of its marker substrate - fexofenadine upon single peroral administration. P-glycoprotein expression was investigated by the immunohistochemical method. It was established that 14-day administration of ethinylestradiol - gestodene combination did not influence the functional activity of P-glycoprotein. After 21-day administration of this combination, the maximum concentration of fexofenadine and its area under concentration - time curve were increased and its clearance was decreased. These data are indicative of the inhibition of P-glycoprotein functional activity in the organism. Immunohistochemical analysis showed a reduction in the total expression of P-glycoprotein in the liver and small intestine after joint administration of ethinylestradiol and gestodene for 21 days, which confirmed a decrease in P-glycoprotein synthesis. Correlations between P-glycoprotein activity, its expression in the liver, and estradiol level were revealed.
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