10074-g5 and Carcinoma--Hepatocellular

B-Cell-specific Moloney murine leukemia virus insertion region 1 (BMI1) is a core component of the polycomb repressive complex 1 (PRC1). Abnormal expression of BMI1 is associated with a number of human malignances and cancer stem cells (CSCs), which cause chemotherapy resistance. Therefore, small molecules that inhibit BMI1 expression are potential candidates for cancer therapy. In this study, a cell-based reporter gene assay was developed that allowed BMI1 promoter activity to be measured in 293T human embryonic kidney cells based on luciferase expression levels. Using this screening assay, the methanol-soluble extracts of Beaumontia murtonii and Eugenia operculata were selected as leads. Bioassay-guided fractionation of the extracts led to the isolation of three known cardenolides (1-3) and one new compound (4) from B. murtonii and two known triterpenoids (5 and 6) and one new compound (7) from E. operculata. These seven compounds inhibited BMI1 promoter activity (IC

Topics: Animals; Antineoplastic Agents; Apocynaceae; Blotting, Western; Carcinoma, Hepatocellular; Cardenolides; Cell Line, Tumor; Eugenia; HCT116 Cells; HEK293 Cells; Humans; Inhibitory Concentration 50; Liver Neoplasms; Mice; Molecular Structure; Neoplastic Stem Cells; Plant Leaves; Polycomb Repressive Complex 1; Thailand; Triterpenes