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Brozic, P.* ; Kocbek, P.* ; Sova, M.* ; Kristl, J.* ; Martens, S.* ; Adamski, J. ; Gobec, S.* ; Rizner, T.L.*

Flavonoids and cinnamic acid derivatives as inhibitors of 17beta-hydroxysteroid dehydrogenase type 1.

Mol. Cell. Endocrinol. 301, 229-234 (2009)
DOI
Open Access Green as soon as Postprint is submitted to ZB.
17beta-Hydroxysteroid dehydrogenase (17beta-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, 7,4'-dihydroxyflavone, diosmetin, chrysoeriol, scutellarein, genkwanin and fisetin showed more than 70% inhibition of 17beta-HSD type 1 at 6muM. In a series of 18 derivatives of cinnamic acid, the best inhibitor was 4'-cyanophenyl 3,4-methylenedioxycinnamate, with more than 70% inhibition of 17beta-HSD type 1. None of flavonoids affected the proliferation of T-47D breast cancer cells.
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Publication type Article: Journal article
Document type Scientific Article
Keywords 17beta-Hydroxysteroid dehydrogenase type 1; Inhibitors; Flavonoids; Cinnamic acid derivatives
Language english
Publication Year 2009
Prepublished in Year 2008
HGF-reported in Year 2008
ISSN (print) / ISBN 0303-7207
e-ISSN 1872-8057
Journal Molecular and Cellular Endocrinology
Quellenangaben Volume: 301, Issue: 1-2, Pages: 229-234 Article Number: , Supplement: ,
Publisher Elsevier
Publishing Place Shannon
Reviewing status Peer reviewed
Institute(s) Institute of Experimental Genetics (IEG)
Research field(s) Genetics and Epidemiology
PSP Element(s) FE 70691
DOI 10.1016/j.mce.2008.09.004
Scopus ID 60249103689
Erfassungsdatum 2008-12-31
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