Inhibitory effects of polyphenols on p-glycoprotein-mediated transport.
Overexpression of P-glycoprotein (P-gp), a plasma membrane transporter which extrudes chemotherapeutic agents out of cells, has been associated with the multidrug resistance ( MDR) of cancer cells. It has been revealed that flavonoids and other polyphenols inhibit P-gp activity. Due to their inhibitory activities of polyphenols on P-gp function and their physiological safety, they are possible candidates for modulators of MDR. To determine suitable candidates, it is important to clarify the structure-activity relationships of their inhibitory activities on P-gp function. Determining the structure-activity relationships is also meaningful because the intake of dietary polyphenols may also alter drug pharmacokinetics and pharmacodynamics via inhibition of P-gp-mediated drug efflux in tissues such as the intestinal epithelium, blood-brain barrier, hepatocytes and renal tubular cells. This is a review of our recent investigations using multidrug-resistant P-gp overexpressing KB-C2 cells.[1]References
- Inhibitory effects of polyphenols on p-glycoprotein-mediated transport. Kitagawa, S. Biol. Pharm. Bull. (2006) [Pubmed]
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