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  • Flavonoids, cinnamic acid derivatives as inhibitors of 17 ß-hydroxysteroid dehydrogenase type 1
    Brožič, Petra ...
    17ß-Hydroxysteroid dehydrogenase (17ß-HSD) type 1 converts estrone to estradiol, a potent ligand for estrogen receptors. It represents an important target for the development of drugs for treatment ... of estrogen-dependent diseases. In the present study, we have examined the inhibitory activities of some flavonoids, their biosynthetic precursors (cinnamic acids and coumaric acid), and their derivatives. The proliferative activity of flavonoids on the T-47D estrogen-receptor-positive breast cancer cell line was also evaluated. Among 10 flavonoids, 7,4ß-dihydroxyflavone, diosmetin, chrysoeriol, scutellarein, genkwanin and fisetin showed more than 70% inhibition of 17ß-HSDtype 1 at 6 ßM. In a series of 18 derivatives of cinnamic acid, the best inhibitor was 4ß-cyanophenyl 3,4-methylenedioxycinnamate, with more than 70% inhibition of 1717ß-HSD type 1. None of flavonoids affected the proliferation of T-47D breast cancer cells.
    Vrsta gradiva - prispevek na konferenci
    Leto - 2009
    Jezik - angleški
    COBISS.SI-ID - 24720601