Author/Editor		Brožič, Petra; Kocbek, Petra; Sova, Matej; Kristl, Julijana; Martens, Stefan; Adamski, Jerzy; Gobec, Stanislav; Lanišnik-Rižner, Tea
Title		Flavonoids, cinnamic acid derivatives as inhibitors of 17 beta-hydroxysteroid dehydrogenase type 1
Type		članek
Source		Mol Cell Endocrinol
Vol. and No.		Letnik 301, št. 1-2
Publication year		2009
Volume		str. 229-34
Language		eng
Abstract		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.
Descriptors		FLAVONES CINNAMATES 17-HYDROXYSTEROID DEHYDROGENASES