An integrative approach for the isolation, screening and analysis of antitumor agents by liquid chromatography combined with mass spectrometry

A rapid approach has been developed for screening trace level compounds with antitumor activities based on their interactions with microtubules. This interaction can be quantified with liquid chromatography (LC) by measuring the difference of bioactive compound's concentration before and after the formation of compound–microtubule complexes in the fast dialyzers. To test the effectiveness of this approach, several antitumor drugs such as colchicine, taxol, daunorubicin, and a non-antitumor reagent ketoprofen were used. Results indicate that the antitumor constituents can be identified without any disturbance, and the inactive components can be excluded. This screening method was then successfully applied to some potential antitumor compound mixtures, and the active compounds could be separated and screened rapidly. The binding activities measured were consistent with their cytotoxicity assays. This integrative approach is rapid and convenient for screening, isolating, and analyzing potential antitumor active compounds from a mixture.