Avtor/Urednik		Brožič, Petra; Kocbek, Petra; Sova, Matej; Kristl, Julijana; Martens, Stefan; Adamski, Jerzy; Gobec, Stanislav; Lanišnik-Rižner, Tea
Naslov		Flavonoids, cinnamic acid derivatives as inhibitors of 17 beta-hydroxysteroid dehydrogenase type 1
Tip		članek
Vir		Mol Cell Endocrinol
Vol. in št.		Letnik 301, št. 1-2
Leto izdaje		2009
Obseg		str. 229-34
Jezik		eng
Abstrakt		17β-Hydroxysteroid dehydrogenase (17β-HSD) type 1 converts estrone to estradiol, a potent ligand forestrogen 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 linewas also evaluated. Among 10 flavonoids, 7,4'-dihydroxyflavone, diosmetin, chrysoeriol, scutellarein, genkwanin and fisetin showed more than 70% inhibition of 17β-HSD type 1 at 6-M. In a series of 18 derivatives of cinnamic acid, the best inhibitor was 4-cyanophenyl 3,4-methylenedioxycinnamate, with more than 70% inhibition of 17β-HSD type 1. None of flavonoids affected the proliferation of T-47D breast cancer cells.
Deskriptorji		FLAVONES CINNAMATES 17-HYDROXYSTEROID DEHYDROGENASES