Overexpression of P-glycoprotein (P-gp) and
multidrug resistance-
associate protein 1 (MRP1) is a major mechanism leading to
multidrug resistance (MDR) of cancer cells. These transporters expel anti-cancer
drugs and greatly impair therapeutic efficacy of chemotherapy. A Chinese herbal plant Yanhusuo (
Corydalis yanhusuo W.T. Wang, YHS) is frequently used in functional food and traditional Chinese medicine to improve the efficacy of chemotherapy. The objective of this work was to study effects of glaucine, an alkaloid component of YHS, on P-gp and MRP1 in resistant cancer cells.
The resistant cancer cell line, MCF-7/ADR and corresponding parental sensitive cells were employed to determine reversal properties of glaucine. Glaucine inhibits P-gp and MRP1-mediated efflux and activates ATPase activities of the transporters, indicating that it is a substrate and inhibits P-gp and MRP1 competitively. Furthermore, glaucine suppresses expression of ABC transporter genes. It reverses the resistance of MCF-7/ADR to adriamycin and mitoxantrone effectively.