INHIBITORY EFFECT OF CURCUMINOIDS ON MCF-7 CELL-PROLIFERATION AND STRUCTURE-ACTIVITY-RELATIONSHIPS

Curcumin, demethoxycurcumin and bisdemethoxycurcumin are the yellow co loring phenolic compounds isolated from the spice turmeric. This study was part of a program correlating the biological activity and molecul ar structure of antitumor agents; the effect of these curcuminoids and cyclocurcumin (Cyclocur) was examined on the proliferation of MCF-7 h uman breast tumor cells. Curcuminoids appeared to be potent inhibitors , whereas Cyclocur was less inhibitory. To contribute to our understan ding of the mechanism of antiproliferative activity of curcumin, cell cycle analysis was performed by propidium iodide staining and a flow c ytometry technique. Curcumin exerts a cytostatic effect at G2/M which explains its antiproliferative activity. The presence of the diketone moiety in the curcumin molecule seems to be essential for the inhibito ry activity. (C) 1998 Elsevier Science Ireland Ltd. All rights reserve d.