Synthesis of Cantharidin Derivatives as Photo-Initiated DNA Cleavage Agents

Abstract

Previous studies indicated that cantharidin (exo-2,3-dimethy-7-oxabicyclo [2,2,1] heptane-2,3-dicarboxylic anhydride) could inhibit the proliferation of cancer cells via p53 dependent mechanism. It could also inhibit protein phosphatases 1(PP1) and protein phosphatases 2A (PP2A). When cantharidin was treated with cancer cell, it could induce to produce oxidative stress.Oxidative stress would cause damage the single and double stand DNA increasingly. But the mechanism of anticancer is still not clear. Here, cantharidin and cantharidin derivatives were served as photo-initiated DNA cleavage agents. We combined them with irradiation (λ=352nm) to see if they have the ability to cleavage the supercoiled DNA. The results displayed that the cantharidin derivatives could cleavage DNA at acidic condition with irradiation. Then, we used high-resolution gel electrophoresis to analyze the results and the experiment of Maxma-Gilbert was served as standard. The results indicated that cantharidin derivatives have better ability of cleavage at the guanine site.