Antiproliferative Effects of Curcumin Analogues;Comparative antiproliferative activities of curcumin, tetrahydrocurcumin, dimethoxycurcumin and bis-demethoxycurcumin in human leukemia HL-60 cells

Abstract

Curcumin and its analogues(Tetrahydrocurcumin THC, demethoxycurcumin ; BDMC and dimethoxycurcumin DiMC) were compared for their ability to inhibit the growth of human leukemia HL-60 cells. The growth of HL-60 cells was inhibited by curcumin, DeMC and DiMC, but not by THC lacking ${\alpha},{\beta}-unsaturated$ carbonyl groups thus suggesting that ${\alpha},{\beta}-unsaturated$ carbonyl groups are crucial for antiproliferative activity. The order of antiproliferative activity was DiMC, curcumin and BDMC indicating that the number of methoxy groups on the aromatic rings of the active compounds plays an important role in enhancing anti-proliferating activity. In comparison with cellular uptake of the active compounds, uptake capacity was found to be highest with DiMC, followed by curcumin and BDMC. Therefore, it is most likely that the differential antiproliferative activities of DiMC, curcumin and BDMC are associated with their capacities of cellular uptake resulting in building up of enough concentration inside the cells.

Keywords

• curcumin;
• dimethoxycurcumin;
• bis-demethoxycurcumin;
• tetrahydrocurcumin;
• antiproliferation