Abstract: OBJECTIVE To investigate the antitumor activity of Brucea javanica pieces and the extracted dregs， and to compare the contents of Brusatol and Bruceine A. METHODS The inhibitory effect of Brucea javanica pieces and dregs on A549 cells was investigated by Real-time cell-based assay (RTCA)， and the contents of Brusatol and Bruceine A were determined by HPLC simultaneously. RESULTS The Brucea javanica pieces and dregs both showed certain inhibitory effects on A549 cells and the IC₅₀ values were 4.576-7.256 mg/mL and 4.115-9.766 mg/mL. The total content of Brusatol and Bruceine A in Brucea javanica pieces and the extracted dregs were 0.113 9%-0.143 5% and 0.110 0%-0.135 9%. CONCLUSION The pieces and dregs of Brucea javanica have certain antitumor activity， and there is no significant difference in the contents of anti-tumor components between the dregs and the pieces. The dregs of Brucea javanica can be researched and developed in depth centering on nigakilactone. It also can promote the comprehensive use of Chinese medicinal resources.