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DNA Polymerase β Inhibitors from Tetracera Boiviniana

1999; American Chemical Society; Volume: 62; Issue: 12 Linguagem: Inglês

10.1021/np990326p

1520-6025

Ji Ma, Shelley Starck, Sidney M. Hecht,

Bioactive Compounds and Antitumor Agents

Bioassay-guided fractionation of an active methyl ethyl ketone extract of Tetracera boiviniana, using a sensitive assay to monitor DNA polymerase β inhibition, resulted in the isolation of three known triterpenoids, betulinic acid (1), 3-cis-p-coumaroyl maslinic acid (2), and 3-trans-p-coumaroyl maslinic acid (3). Compounds 1−3 inhibited DNA polymerase β with IC50 values of 14, 15, and 4.2 μM in the presence of bovine serum albumin (BSA) and 6.5, 7.5, and 2.0 μM in the absence of BSA, respectively. Further, compounds 1−3 potentiated the effects of bleomycin in cultured P-388D1 cells.