Psoralea corylifolia L. (Fabaceae) is a widely used medical plant in China. This study was designed to screen and identify bioactive compounds with anticancer activity from the seeds of Psoralea corylifolia L. One volatile fraction (fraction I) and three other fractions (fraction II, III, IV) from
methanol extraction of P. corylifolia L. were obtained. Bioactivities of these fractions were evaluated by the cytotoxicity on KB, KBv200, K562, K562/ADM
cancer cells with MTT assay. Major components in the active fraction were identified by HPLC/MS(n). Fraction IV significantly inhibits the growth of
cancer cells in a dose-dependent manner. The IC(50) values were 21.6, 24.4, 10.0 and 26.9, respectively.
Psoralen and
isopsoralen, isolated from fraction IV, were subject to bioactive assay and presented a dose-dependent anticancer activity in four
cancer cell lines (KB, KBv200, K562 and K562/ADM). The IC(50) values of
psoralen were 88.1, 86.6, 24.4 and 62.6, which of
isopsoralen were 61.9, 49.4, 49.6 and 72.0, respectively. Apoptosis of
tumor cell significantly increased after treated with
psoralen and
isopsoralen. Induction of apoptotic activity was confirmed by flow cytometry after staining with
Annexin V/PI. These results suggested
psoralen and
isopsoralen contribute to anticancer effect of P. corylifolia L.