Effects of pinostrobin on estrogen metabolism and estrogen receptor transactivation.

Abstract

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.

• Authors: J C Le Bail, L Aubourg, G Habrioux
• Journal: Cancer letters (Cancer Lett) Vol. 156 Issue 1 Pg. 37-44 (Aug 01 2000) ISSN: 0304-3835 [Print] Ireland
• PMID: 10840157 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents, Phytogenic
• Aromatase Inhibitors
• Estrogens
• Flavanones
• Flavonoids
• Receptors, Estrogen
• Dehydroepiandrosterone Sulfate
• Hydroxysteroid Dehydrogenases
• pinostrobin

Topics

• Antineoplastic Agents, Phytogenic (pharmacology)
• Aromatase Inhibitors
• Cell Division (drug effects)
• Dehydroepiandrosterone Sulfate (pharmacology)
• Estrogens (metabolism)
• Female
• Flavanones
• Flavonoids (pharmacology)
• Humans
• Hydroxysteroid Dehydrogenases (antagonists & inhibitors)
• Receptors, Estrogen (drug effects, metabolism)
• Transcriptional Activation (drug effects)
• Tumor Cells, Cultured