A platform for fast screening potential anti‐breast cancer compounds in traditional Chinese medicines

Several Chinese herbs, namely, Pu‐Gong‐Ying, Gan‐Cao, Chai‐Hu, Mu‐Xiang, Gua‐Lou and Huang‐Yao‐Zi, are frequently used in complex traditional Chinese medicing formulas for breast hyperplasia and breast tumor therapy. The pharmacological effects of these Chinese herbs are all described as ‘clearing heat‐toxin and resolving masses’ in traditional use. However, the chemical profiles of anti‐breast cancer constituents in these herbs has not been investigated so far. In this study, a bioactivity‐oriented screening platform, which was based on a human breast cancer MCF‐7 cellular model, semi‐preparative high performance liquid chromatography coupled with ultraviolet spectrophotometry and ultraperformance liquid chromatography coupled to quadrupole‐time‐of‐flight mass spectrometer, was developed to rapidly screen the six Chinese herbs. Two potential anti‐breast cancer compounds, which were costunolide (Cos) and dehydrocostus lactone (Dehy), were identified in Mu‐Xiang. Combination of the two compounds showed a synergism on inhibiting the proliferation of MCF‐7 cells in vitro, which exhibits a potential application prospect for breast cancer therapy. This bioactivity‐oriented screening strategy is rapid, economical, reliable and specific for screening potential anti‐breast cancer compounds in traditional Chinese medicines. Copyright © 2013 John Wiley & Sons, Ltd.