Effects of pinostrobin on estrogen metabolism and estrogen receptor transactivation.
The interaction between the estrogen receptor and 5-hydroxy-7-methoxyflavanone (pinostrobin) was studied in the presence or absence of estradiol or dehydroepiandrosterone sulfate (DHEAS), respectively, using a stably transfected human breast cancer cell line (MVLN). We also evaluated its action on the proliferation in estrogen-dependent (MCF-7) human breast cancer cells in the same conditions than the estrogen receptor assay. On the other hand pinostrobin was evaluated for their effects on the human placental aromatase, 3beta-hydroxysteroid dehydrogenase Delta(4)/Delta(5) isomerase and 17beta-hydroxysteroid dehydrogenase activities. Pinostrobin did not possess antiestrogenic activity but presented anti-aromatase activity and decreased the growth of MCF-7 cells induced by DHEAS and E(2). This study provides particularly evidence of the potential biological interest of pinostrobin among the flavonoids.
Le Bail
J C
JC
UPRES EA 1085, Laboratoire de Biochimie, Faculté de Pharmacie, 2 Rue du Dr Marcland, 87025, Limoges Cédex, France.
Aubourg
L
L
Habrioux
G
G
D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology*; D047072:Aromatase Inhibitors; D002455:Cell Division / Q000187:drug effects; D019314:Dehydroepiandrosterone Sulfate / Q000494:pharmacology; D004967:Estrogens / Q000378:metabolism*; D005260:Female; D044950:Flavanones; D005419:Flavonoids / Q000494:pharmacology*; D006801:Humans; D006913:Hydroxysteroid Dehydrogenases / Q000037:antagonists & inhibitors; D011960:Receptors, Estrogen / Q000187:drug effects* / Q000378:metabolism; D015533:Transcriptional Activation / Q000187:drug effects*; D014407:Tumor Cells, Cultured
D000972:Antineoplastic Agents, Phytogenic; D047072:Aromatase Inhibitors; D004967:Estrogens; D044950:Flavanones; D005419:Flavonoids; D011960:Receptors, Estrogen; D019314:Dehydroepiandrosterone Sulfate; D006913:Hydroxysteroid Dehydrogenases; C411294:pinostrobin