Electrochemical lab on a chip for high-throughput analysis of anticancer drugs efficiency.

We describe a new method for rapid, sensitive, and high-throughput detection of colon cancer cells' response to differentiation therapy, using a novel electrochemical lab-on-a-chip system. Differentiation-inducing agents such as butyric acid and its derivatives were introduced to miniature colon cancer samples within the nanovolume chip chambers. The efficacy of each of the differentiation-inducing agents was evaluated by electrochemical detection of the cellular enzymatic activity level, whereas reappearance of normal enzymatic activity denotes effective therapy.

Novel prodrugs of tegafur that display improved anticancer activity and antiangiogenic properties.

New and more potent prodrugs of the 5-fluorouracyl family derived by hydroxymethylation or acyloxymethylation of 5-fluoro-1-(tetrahydro-2-furanyl)-2,4(1H,3H)-pyrimidinedione (tegafur, 1) are described. The anticancer activity of the butyroyloxymethyl-tegafur derivative 3 and not that of tegafur was attenuated by the antioxidant N-acetylcysteine, suggesting that the increased activity of the prodrug is in part mediated by an increase of reactive oxygen species. Compound 3 in an in vitro matrigel assay was found to be a more potent antiangiogenic agent than tegafur.

Mode of interaction between butyroyloxymethyl-diethyl phosphate (AN-7) and doxorubicin in MCF-7 and resistant MCF-7/Dx cell lines.

Purpose: To investigate the anticancer activity and mode of action of butyroyloxymethyl-diethyl phosphate (AN-7), a prodrug of butyric acid and formaldehyde, as a single agent and in combination with doxorubicin in human carcinoma MCF-7 and the multidrug resistant MCF-7 Dx cell lines.

Methods: The anti-cancer activity of AN-7 as a single agent or in combination with doxorubicin was measured by the Hoechst cell viability and colony forming assays as well as by FACS analyses of cells stained with propidium iodide and annexin V-FITC. Modulations of protein expression and acetylation were measured by Western blot analyses.