bakuchicin and bakuchiol

Bioassay-guided fractionation of the H(2)O extract of the seeds of Psoralea corylifolia furnished one hepatoprotective compound, bakuchiol (1), together with two moderately active compounds, bakuchicin (2) and psoralen (3), on tacrine-induced cytotoxicity in human liver-derived Hep G2 cells. The EC(50) values of compounds 1 - 3 are 1.0, 47.0, 50.0 microg/ml, respectively. Silymarin as a positive control showed the EC(50) value with 5.0 microg/ml.

Topics: Antineoplastic Agents, Phytogenic; Carcinoma, Hepatocellular; Ficusin; Heterocyclic Compounds, 3-Ring; Humans; Phenols; Protective Agents; Psoralea; Seeds; Silymarin; Tacrine; Tumor Cells, Cultured

An ethanol extract of Psoralea corylifolia caused strong DNA polymerase inhibition in a whole cell bioassay specific for inhibitors of DNA replication enzymes. Bioassay-directed purification of the active compounds led to the isolation of the new compound corylifolin (1) and the known compound bakuchiol (2) as DNA polymerase inhibitors. On the basis of the structures of 1 and 2, resveratrol (3) was tested and found to be active as a DNA polymerase inhibitor in this bioassay. Neobavaisoflavone (4) was isolated as a DNA polymerase inhibitor, daidzein (5) as a DNA polymerase and topoisomerase II inhibitor, and bakuchicin (6) as a topoisomerase II inhibitor.

Topics: China; Enzyme Inhibitors; Flavonoids; Magnetic Resonance Spectroscopy; Nucleic Acid Synthesis Inhibitors; Plants, Medicinal; Simian virus 40; Topoisomerase II Inhibitors; Virus Replication