Inhibitory effect of curcuminoids on MCF-7 cell proliferation and structure-activity relationships.
Curcumin, demethoxycurcumin and bisdemethoxycurcumin are the yellow coloring phenolic compounds isolated from the spice turmeric. This study was part of a program correlating the biological activity and molecular structure of antitumor agents; the effect of these curcuminoids and cyclocurcumin (Cyclocur) was examined on the proliferation of MCF-7 human breast tumor cells. Curcuminoids appeared to be potent inhibitors, whereas Cyclocur was less inhibitory. To contribute to our understanding of the mechanism of antiproliferative activity of curcumin, cell cycle analysis was performed by propidium iodide staining and a flow cytometry 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 inhibitory activity.
Laboratoire de Chimie Physique et Minérale, Faculté de Pharmacie, Limoges, France.
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A
Simon
D P
DP
Allais
J L
JL
Duroux
J P
JP
Basly
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Durand-Fontanier
C
C
Delage
D016588:Anticarcinogenic Agents / Q000737:chemistry / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000473:pathology; D002453:Cell Cycle / Q000187:drug effects; D002455:Cell Division / Q000187:drug effects*; D003373:Coumaric Acids / Q000737:chemistry / Q000494:pharmacology*; D003474:Curcumin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D036381:Diarylheptanoids; D006801:Humans; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D016588:Anticarcinogenic Agents; D003373:Coumaric Acids; D036381:Diarylheptanoids; C034786:bisdemethoxycurcumin; D003474:Curcumin; C050229:demethoxycurcumin