Baicalein and genistein display differential actions on estrogen receptor (ER) transactivation and apoptosis in MCF-7 cells.
Genistein is a soy isoflavone that has attracted much attention for its chemopreventive properties. Baicalein is a flavone found in Scutellaria species, and its structure is analogous to that of genistein. We examined the two flavones' antiestrogenicity by using a transient transfection model. Our results indicated that baicalein could suppress 17beta-estradiol-induced transactivation in cells expressing estrogen receptor alpha, whereas no antagonistic activity was seen in genistein. Cell death assay and flow cytometry analysis demonstrated that baicalein was a stronger apoptosis inducing agent than genistein. Considering all the criteria tested, baicalein could be a better chemopreventive agent than genistein.
D000970:Antineoplastic Agents / Q000494:pharmacology; D000975:Antioxidants / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D001943:Breast Neoplasms / Q000188:drug therapy / Q000378:metabolism* / Q000473:pathology; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy / Q000378:metabolism* / Q000473:pathology; D002455:Cell Division; D047628:Estrogen Receptor alpha; D005260:Female; D044950:Flavanones; D005419:Flavonoids / Q000494:pharmacology*; D005434:Flow Cytometry; D019833:Genistein / Q000494:pharmacology*; D006801:Humans; D008156:Luciferases / Q000378:metabolism; D011960:Receptors, Estrogen / Q000235:genetics / Q000378:metabolism*; D020218:Response Elements; D059005:Topoisomerase II Inhibitors; D015533:Transcriptional Activation / Q000187:drug effects; D014162:Transfection; D014407:Tumor Cells, Cultured / Q000187:drug effects / Q000378:metabolism
D000970:Antineoplastic Agents; D000975:Antioxidants; D047628:Estrogen Receptor alpha; D044950:Flavanones; D005419:Flavonoids; D011960:Receptors, Estrogen; D059005:Topoisomerase II Inhibitors; C006680:baicalein; D019833:Genistein; D008156:Luciferases