Cytotoxic and antiproliferative effects of heptaacetyltiliroside on human leukemic cell lines

The peracetylated derivative of kaempferol-3-O-beta-D-(6 "-E-p-coumaroyl) g lycopyranoside (tiliroside) (1a) was tested for its cytotoxic and cytostati c activity against several human leukemic cell lines. The significant cytot oxic activity of this derivative, prompted to an additional examination on some of the cell lines used. The effect on the uptake of [H-3]thymidine as a marker of DNA synthesis and on the cell proliferation, was investigated a s well as the morphology of the cells and the kind of death induced, using the Wright-Giemsa dye and horizontal agarose-gel electrophoresis. Flow cyto metric experiments of 1a on some leukemic cell lines was also performed. Co mpound 1a showed a significant antiproliferative effect as soon as 1 h of c ontinuous incubation at all cell lines tested. Cells were killed, through t he process of apoptosis and the appearance of the apoptotic signs was time and dose-dependent, while from the flow cytometric experiments, a synchroni sation (through a delay probably in the G(0/1) phase) of the cells seems to take place. (C) 1999 Published by Elsevier Science Ltd. All rights reserve d.