Reference profile correlation reveals estrogen-like trancriptional activity of Curcumin.
BACKGROUND
Several secondary metabolites from herbal nutrient products act as weak estrogens (phytoestrogens), competing with endogenous estrogen for binding to the estrogen receptors and inhibiting steroid converting enzymes. However, it is still unclear whether these compounds elicit estrogen dependent transcription of genes at physiological concentrations.


METHODS
We compare the effects of physiological concentrations (100 nM) of the two phytoestrogens Enterolactone and Quercetin and the suspected phytoestrogen Curcumin on gene expression in the breast cancer cell line MCF7 with the effects elicited by 17-beta-estradiol (E2).


RESULTS
All three phytocompounds have weak effects on gene transcription; most of the E2 genes respond to the phytoestrogens in the same direction though to a much lesser extent and in the order Curcumin > Quercetin > Enterolactone. Gene regulation induced by these compounds was low for genes strongly induced by E2 and similar to the latter for genes only weakly regulated by the classic estrogen. Of interest with regard to the treatment of menopausal symptoms, the survival factor Birc5/survivin and the oncogene MYBL1 are strongly induced by E2 but only marginally by phytoestrogens.


CONCLUSIONS
This approach demonstrates estrogenic effects of putative phytoestrogens at physiological concentrations and shows, for the first time, estrogenic effects of Curcumin.
Bachmeier
Beatrice E
BE
Department of Clinical Chemistry and Clinical Biochemistry, Ludwig-Maximilians-University, Munich, Germany. bachmeier@med.uni-muenchen.de
Mirisola
Valentina
V
Romeo
Francesco
F
Generoso
Luca
L
Esposito
Alessia
A
Dell'eva
Raffaella
R
Blengio
Fabiola
F
Killian
Peter H
PH
Albini
Adriana
A
Pfeffer
Ulrich
U
D015107:4-Butyrolactone / Q000031:analogs & derivatives / Q000494:pharmacology; D045744:Cell Line, Tumor; D003474:Curcumin / Q000494:pharmacology*; D004958:Estradiol / Q000494:pharmacology; D020869:Gene Expression Profiling / Q000592:standards; D006801:Humans; D051034:Inhibitor of Apoptosis Proteins; D017705:Lignans / Q000494:pharmacology; D008869:Microtubule-Associated Proteins / Q000235:genetics / Q000378:metabolism; D048789:Phytoestrogens / Q000494:pharmacology*; D011518:Proto-Oncogene Proteins / Q000235:genetics / Q000378:metabolism; D011794:Quercetin / Q000494:pharmacology; D012016:Reference Values; D000077022:Survivin; D015534:Trans-Activators / Q000235:genetics / Q000378:metabolism; D014158:Transcription, Genetic / Q000187:drug effects*
C107489:BIRC5 protein, human; D051034:Inhibitor of Apoptosis Proteins; D017705:Lignans; C088831:MYBL1 protein, human; D008869:Microtubule-Associated Proteins; D048789:Phytoestrogens; D011518:Proto-Oncogene Proteins; D000077022:Survivin; D015534:Trans-Activators; D004958:Estradiol; D011794:Quercetin; D003474:Curcumin; D015107:4-Butyrolactone; C029497:2,3-bis(3'-hydroxybenzyl)butyrolactone