The invention provides an extraction method of an anticancer active monomer in Curcuma zedoaria. The method includes: taking Curcuma zedoaria tuber as the raw material, grinding the Curcuma zedoaria tuber into powder, then conducting ethanol extraction, concentrating the filtrate, then dissolving the product in a n-hexane-ethanol mixed solvent; conducting one-dimensional liquid chromatography separation: employing a normal phase silica gel chromatographic column, adopting a binary mobile phase with n-hexane as the phase A and ethanol as the phase B, carrying out elution with the phase B at a concentration of 0-50%, and collecting the 15.5-17min eluent; performing dissolving with the n-hexane-ethanol mixed solvent; conducting two-dimensional liquid chromatography separation: employing an Acchrom X-Amide chromatographic column, adopting a binary mobile phase with n-hexane as the phase A and ethanol as the phase B, carrying out elution with the phase B at a concentration of 0-30%, and collecting the 17-18min eluent so as to obtain a target product. The invention provides a new compound never reported before, the process has the characteristics of simplicity, low cost, large preparation capacity and good repeatability, and the obtained monomer compound has high purity, good biological activity and anticancer drug development potential.