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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

DNA polymerase beta lyase inhibitors from Maytenus putterlickoides.

During a survey of plant secondary metabolites for DNA polymerase beta lyase inhibitors, we found that a crude methyl ethyl ketone extract prepared from Maytenus putterlickoides showed strong inhibition of the lyase activity of DNA polymerase beta in an in vitro assay. Bioassay-guided fractionation of the extract, using an in vitro assay, resulted in the discovery of a new active principle, 30-(4'-hydroxybenzoyloxy)-11alpha-hydroxylupane-20(29)-en-3-one (1), as well as a known compound, (-)-epicatechin (2). Compounds 1 and 2 exhibited DNA polymerase beta lyase inhibitory activity with IC50 values of 62.8 and 18.5 microM, respectively. Compound 2 was capable of potentiating the action of the monofunctional methylating agent methyl methanesulfonate in cultured human cancer cells, consistent with the possible utility of inhibitors of this type in vivo.[1]


  1. DNA polymerase beta lyase inhibitors from Maytenus putterlickoides. Feng, X., Gao, Z., Li, S., Jones, S.H., Hecht, S.M. J. Nat. Prod. (2004) [Pubmed]
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