FUNCTIONAL ACTIVITY OF P-GLYCOPROTEIN DURING EXPERIMENTAL MANIPULATIONS

Effect of Honey on CYP3A4 Enzyme and P-Glycoprotein Activity in Healthy Human Volunteers

The activity of cytochrome p450 isozyme 3A4 (CYP3A4) enzyme and P-glycoprotein (P-gp) is modulated by grapefruit juice and herbal drugs. CYP3A4 is the major phase I drug metabolizing enzyme and P-gp is an ATP-dependent drug efflux pump that regulates the intestinal absorption of orally administered drugs. Honey is commonly consumed as a dietary supplement. However, its influence on human CY...

evaluation of the functional role of p-glycoprotein in brain uptake of tramadol in rat

Examination of the functional activity of P-glycoprotein in the rat placental barrier using rhodamine 123.

Rhodamine 123 (Rho123), a model substrate of P-glycoprotein (P-gp), was used to evaluate the functional activity of P-gp efflux transporter in the rat placental barrier. The dually perfused rat-term placenta method was used. In our experiments, the materno-fetal transplacental passage of Rho123 did not meet the criteria of the first-order pharmacokinetics, suggesting an involvement of transport...

Influence of functional MDR1 gene polymorphisms on P-glycoprotein activity in CD34+ hematopoietic stem cells.

BACKGROUND AND OBJECTIVES Expression of the multidrug resistance P-glycoprotein, a transmembrane drug transporter, is influenced by recently described polymorphisms of the human MDR1 gene. Hematopoietic cells, such as lymphocytes, and hematopoietic stem cells, express P-glycoprotein, but the effect of MDR1 gene polymorphisms on P-glycoprotein activity in stem cells is unknown. We investigated w...

Expression and functional activity of P-glycoprotein in cultured hepatocytes from Oncorhynchus mykiss.

P-glycoproteins encoded by multidrug resistance 1 (mdr1) genes are ATP-dependent transporters located in the plasma membrane that mediate the extrusion of hydrophobic compounds from the cell. Using cultured isolated rainbow trout hepatocytes, we characterized an mdr1-like transport mechanism of the teleost liver. Immunoblots with the monoclonal antibody C219, which recognizes a conserved epitop...