Planta Med 2014; 80 - PD93
DOI: 10.1055/s-0034-1382514

Isolation and structure elucidation of bioactive leads from terrestrial plants

HR Bokesch 1, 2, CJ Henrich 1, 2, TT Ransom 2, XW Wang 3, JB McMahon 2, KR Gustafson 2
  • 1Basic Research Program, Leidos Biomedical Research, Inc., Frederick National Laboratory, Frederick, Maryland 21702
  • 2Molecular Targets Laboratory, Center for Cancer Research, National Cancer Institute, Frederick National Laboratory, Frederick, Maryland 21702
  • 3Laboratory of Human Carcinogenesis, Center for Cancer Research, National Cancer Institute, Bethesda, MD 20892

Epithelial cell adhesion molecule (EpCAM) has been implicated in tumor development in hepatocellular carcinoma cells (HCC). Studies have shown that EpCAM(+) HCC cells are more efficient at forming highly invasive tumors in mice than EpCAM(-) HCC cells. On this basis, a high-throughput screening assay was developed to identify specific inhibitors of EpCAM-dependent growth of hepatocellular carcinoma (HCC) cells. Investigation of the organic extracts of Mertensia paniculata and Pilostyles thurberi yielded a series of chalcones and diynenes which showed differential growth inhibition between EpCAM(+) and EpCAM(-) HCC's. The isolation, structure determination and biological activity of the compounds will be presented.

Funded by NCI Contract HHSN261200800001E