title: Bioassay-guided Separation of Anti-tumor Components from Euphorbia kansui by Means of Two-dimensional Preparative High Performance Liquid Chromatography and Real-time Cell Analysis.
abstract: A new strategy for the convergence of two-dimensional preparative high performance liquid chromatography (HPLC) and real-time cell analysis (RTCA) was developed for rapidly separating and screening anti-tumor components from the ethyl acetate extract of the traditional Chinese medicine (TCM), Euphorbia kansui. Eight compounds: esulone A (1), kansuinin A (2), (3β,11β)-3,11-dihydroxylanosta-8,24-dien-7-one (3), kansuinin E (4), kansuinin B (5), isoscopoletin (6), kansuinin D (7) and kansuinin G (8) were efficiently isolated with purity above 97%. Of all the compounds, esulone A has been isolated from this plant for the first time. The structures were identified by NMR spectroscopy and comparisons were made with the data in previous literature. The anti-tumor bioassay was performed on A549 (human lung cancer cells) and Hep-G2 (human liver cancer cells) with a newly developed RTCA system. The result revealed that compounds 1, 3, 7 and 8 almost entirely inhibited the proliferation of A549 cells and that compound 8 was also thought to be the most active compound against Hep-G2 cells. The method provided considerable assistance for the efficient separation of different polar compounds and rapid screening of anti-tumor active compounds.
authors.affiliation: School of Pharmaceutical Science and Technology, Tianjin University.
authors.forename: Hong
authors.initials: H
authors.lastname: Ma
authors.forename: Shanshan
authors.initials: S
authors.lastname: Yang
authors.forename: Hong
authors.initials: H
authors.lastname: Lu
authors.forename: Yaozhou
authors.initials: Y
authors.lastname: Zhang
mesh_terms: D000072283:A549 Cells; D000970:Antineoplastic Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D001681:Biological Assay / Q000379:methods*; D049109:Cell Proliferation / Q000187:drug effects; D002851:Chromatography, High Pressure Liquid; D028481:Euphorbia / Q000737:chemistry*; D056945:Hep G2 Cells; D006801:Humans; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy; D010936:Plant Extracts / Q000302:isolation & purification* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D010936:Plant Extracts