Evidence for Estrogen Receptor β-Selective Activity of Vitex agnus-castus and Isolated Flavones (original) (raw)
Planta Med 2003; 69(10): 945-947
DOI: 10.1055/s-2003-45105
Letter
© Georg Thieme Verlag Stuttgart · New York
Hubertus Jarry1 , Barbara Spengler2 , Andrea Porzel3 , Juergen Schmidt3 , Wolfgang Wuttke1 , Volker Christoffel2
- 1Klinische und Experimentelle Endokrinologie, Universitätsfrauenklinik Göttingen, Göttingen, Germany
- 2Bionorica AG, Neumarkt/Opf, Germany
- 3Leibnitz-Institut für Pflanzenbiochemie, Abteilung Natur- und Wirkstoffchemie, Halle/Saale, Germany
Further Information
Publication History
Received: March 4, 2003
Accepted: June 19, 2003
Publication Date:
02 December 2003 (online)
Abstract
Recent cell culture experiments indicated that extracts of Vitex agnus-castus (VAC) may contain yet unidentified phytoestrogens. Estrogenic actions are mediated via estrogen receptors (ER). To investigate whether VAC compounds bind to the currently known isoforms ERα or ERß, ligand binding assays (LBA) were performed. Subtype specific ER-LBA revealed a binding of VAC to ERß only. To isolate the ERß-selective compounds, the extract was fractionated by bio-guidance. The flavonoid apigenin was isolated and identified as the most active ERß-selective phytoestrogen in VAC. Other isolated compounds were vitexin and penduletin. These data demonstrate that the phytoestrogens in VAC are ERß-selective.
References
- 1 Hoberg E, Orjala J, Meier B, Sticher O. Diterpenoids from the fruits of Vitex agnus-castus . Phytochemistry. 1999; 52 1555-8
- 2 Dixon-Shanies D, Shaikh N. Growth inhibition of human breast cancer cells by herbs and phytoestrogens. Oncol Rep. 1999; 6 1383-7
- 3 Kuiper G G, Enmark E, Pelto-Huikko M, Nilsson S, Gustafsson J A. Cloning of a novel receptor expressed in rat prostate and ovary. Proc Natl Acad Sci USA. 1996; 93 5925-30
- 4 Roth L. Roth Collection of Natural Product Data. Weinheim; VCH 1995
- 5 Wang Y, Hamburger M, Gueho J, Hostettmann K. Antimicrobial flavonoids from Psiadia trinervia and their methylated and acetylated derivatives. Phytochemistry. 1989; 28 2323-7
- 6 Belic I, Bergant-Dolar J, Morton R A. Constituents of Vitex agnus-castus seeds. Part I. J Chem Soc 1961: 2523-5
- 7 Liu J, Burdette J A, Xu H, Gu C, Van Breemen R B, Bhat K PL, Booth N, Constantinou A I, Pezzuto J M, Fong H HS, Farnsworth N R, Bolton J L. Evaluation of estrogenic activity of plant extracts for the potential treatment of menopausal symptoms. J Agric Food Chem. 2001; 49 2472-9
- 8 Lindenmeyer F, Li H, Menashi S, Soria C, Lu H. Apigenin acts on the tumor cell invasion process and regulates protease production. Nutr Cancer. 2001; 39 139-47
- 9 Knowles L M, Zigrossi D A, Tauber R A, Hightower C, Milner J A. Flavonoids suppress androgen-independent human prostate tumor proliferation. Nutr Cancer. 2000; 38 116-22
- 10 Yin F, Giuliano A E, Law R E, Van Herle A J. Apigenin inhibits growth and induces G2/M arrest by modulating cyclin-CDK regulators and ERK MAP kinase activation in breast carcinoma cells. Anticancer Res. 2001; 21 413-20
Hubertus Jarry
Abteilung für klinische und experimentelle Endokrinologie
Universitätsfrauenklinik Göttingen
Robert Koch-Straβe 40
37075 Göttingen
Germany
Phone: +49-551-396522
Fax: +49-551-396518