Plant 2-arylobenzofurans demonstrate a selective estrogen receptor modulator profile

Papoutsi, Z; Kassi, E; Papaevangeliou, D; Pratsinis, H; Zoumpourlis, V; Halabalaki, M; Mitakou, S; Kalofoutis, A; Moutsatsou, P

dc.contributor.author	Papoutsi, Z	en
dc.contributor.author	Kassi, E	en
dc.contributor.author	Papaevangeliou, D	en
dc.contributor.author	Pratsinis, H	en
dc.contributor.author	Zoumpourlis, V	en
dc.contributor.author	Halabalaki, M	en
dc.contributor.author	Mitakou, S	en
dc.contributor.author	Kalofoutis, A	en
dc.contributor.author	Moutsatsou, P	en
dc.date.accessioned	2014-03-01T01:54:01Z
dc.date.available	2014-03-01T01:54:01Z
dc.date.issued	2004	en
dc.identifier.issn	0039-128X	en
dc.identifier.uri	https://dspace.lib.ntua.gr/xmlui/handle/123456789/27166
dc.subject	arylobenzofurans	en
dc.subject	selective estrogen receptor modulators	en
dc.subject	antiestrogen	en
dc.subject	breast cancer	en
dc.subject	osteoblast	en
dc.subject	mineralization	en
dc.subject.classification	Biochemistry & Molecular Biology	en
dc.subject.classification	Endocrinology & Metabolism	en
dc.subject.other	BREAST-CANCER CELLS	en
dc.subject.other	MC3T3-E1 CELLS	en
dc.subject.other	BINDING-SITES	en
dc.subject.other	II ESTROGEN	en
dc.subject.other	GROWTH	en
dc.subject.other	DIFFERENTIATION	en
dc.subject.other	PHYTOESTROGENS	en
dc.subject.other	PROLIFERATION	en
dc.subject.other	ANTIESTROGENS	en
dc.subject.other	ESTRADIOL	en
dc.title	Plant 2-arylobenzofurans demonstrate a selective estrogen receptor modulator profile	en
heal.type	journalArticle	en
heal.language	English	en
heal.publicationDate	2004	en
heal.abstract	We have isolated from the plant Onobrychis ebenoides three novel arylobenzofurans with binding affinity for the estrogen receptor. In this study, we evaluated these arylobenzofurans, namely ebenfuran I, ebenfuran II and ebenfuran HI for their potential selective estrogen receptor modulator (SERM)-like properties. We examined their ability, (1) to induce the insulin growth factor binding protein-3 (IGFBP-3) in MCF-7 breast cancer cells, (2) to stimulate differentiation and mineralization of osteoblastic cell culture by histochemical staining for alkaline phosphatase, Alizarin Red-S staining and calcium levels in the supernatants and (3) to inhibit cell proliferation of cervical adenocarcinoma (Hela) cells by use of the MTT assay. An estrogen receptor mediated effect was investigated by carrying out chloramphenicol acetyl transferase (CAT) assay on transient MCF-7 transfectants. Estradiol and the "pure" antiestrogen ICI 182780 were included to serve as control samples of the estrogenic and antiestrogenic effect respectively. Our data reveal that ebenfuran II is a highly potent SERM, exhibiting antiestrogenic activity in breast cancer cells via the estrogen receptor, estrogenic effect on osteoblasts and no stimulatory effect on cervix adenocarcinoma cells. In conclusion, our study is the first to demonstrate that plant derived arylobenzofurans show a SERM profile and may be considered for the prevention and treatment of diseases such as breast cancer, cervical cancer and osteoporosis. (C) 2004 Elsevier Inc. All rights reserved.	en
heal.publisher	ELSEVIER SCIENCE INC	en
heal.journalName	STEROIDS	en
dc.identifier.isi	ISI:000226189800003	en
dc.identifier.volume	69	en
dc.identifier.issue	11-12	en
dc.identifier.spage	727	en
dc.identifier.epage	734	en