Sipholenol A efficiently inhibits the function of P-glycoprotein (Pgp, MDR-1). It is a new reversing agent for the treatment of multidrug resistance (MDR) in Pgp-overexpressing tumors. This has antiproliferative activity, and is cytotoxic. By inhibiting MDR-1, active compounds remain in the cytoplasm longer, allowing them to be more effective within the cell.
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