Abstract: Object To isolate the active compounds on reversing multidrug resistance (MDR) of tumor cell from the ethanol extract in the seeds of Cnidium monnieri (L.) Cuss. Methods The fractionation directed by bioactivity was carried out with silica gel chromatography and RP-HPLC. Results Three active coumarins were obtained: imperatorin ( Ⅰ ), edultin ( Ⅱ ) and 3′-isobutyryloxy-O-acetyl columbionetin ( Ⅲ ). Their sturctures were identified by spectroscopic analysis. Conclusion These three compounds have a medium reversing MDR of KBV200 in vitro.