In vitro anti-tumor activity of 2',4'-dihydroxy-6'-methoxy-3',5'-dimethylchalcone against six established human cancer cell lines.

摘要

2',4'-Dihydroxy-6'-methoxy-3',5'-dimethylchalcone (DMC), isolated from the buds of Cleistocalyx operculatus, was investigated in its cytotoxicity and its influence on six human cancer cell lines. Among SMMC-7721, 8898, HeLa, SPC-A-1, 95-D and GBC-SD cell lines, SMMC-7721 cells was the most sensitive one in these tested cell lines, with IC(50) equal to 32.3 +/- 1.13microM, EC(50) equal to 9.00 +/- 0.36microM and the therapeutic index equal to 3.59. Staining with Hoechst 33258 showed fragmentation and condensation of chromatin in the cells treated with 9microM DMC for 48h. Flow cytometric analysis was performed to determine hypodiploid cells. The results of flow cytometry assay indicated that the percentage of hypodiploid SMMC-7721 cells were 49.44 +/- 1.06% after 48h treatment with 18.0microM DMC. The treatment resulted in the appearance of a hypodiploid peak (A(0) region), probably due to the presence of apoptosing cells and/or apoptotic bodies with DNA content less than 2n. To our knowledge, this is the first report on anti-tumor activity by DMC.