title: A platform for fast screening potential anti-breast cancer compounds in traditional Chinese medicines.
abstract: 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.
authors.affiliation: School of Pharmacy, Shanghai Jiao Tong University, Shanghai, 200240, China.
authors.forename: Zhang-xiao
authors.initials: ZX
authors.lastname: Peng
authors.forename: Yan
authors.initials: Y
authors.lastname: Wang
authors.forename: Xue
authors.initials: X
authors.lastname: Gu
authors.forename: Yuan-yuan
authors.initials: YY
authors.lastname: Wen
authors.forename: Chao
authors.initials: C
authors.lastname: Yan
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D004354:Drug Screening Assays, Antitumor / Q000379:methods*; D004357:Drug Synergism; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000494:pharmacology*; D005260:Female; D006801:Humans; D010946:Plants, Medicinal / Q000737:chemistry*; D021241:Spectrometry, Mass, Electrospray Ionization / Q000379:methods
chemical_list: D000970:Antineoplastic Agents; D004365:Drugs, Chinese Herbal
keywords: LC-MS; bioactivity-oriented screening; breast cancer; costunolide; dehydrocostus lactone