| RRC ID |
42270
|
| Author |
Papoutsi Z, Kassi E, Papaevangeliou D, Pratsinis H, Zoumpourlis V, Halabalaki M, Mitakou S, Kalofoutis A, Moutsatsou P.
|
| Title |
Plant 2-arylobenzofurans demonstrate a selective estrogen receptor modulator profile.
|
| Journal |
Steroids
|
| 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 III 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.
|
| Volume |
69(11-12)
|
| Pages |
727-34
|
| Published |
2004-1-1
|
| DOI |
10.1016/j.steroids.2004.07.005
|
| PII |
S0039-128X(04)00153-9
|
| PMID |
15579325
|
| MeSH |
Adenocarcinoma / metabolism
Alkaline Phosphatase / metabolism
Animals
Anthraquinones / pharmacology
Benzofurans / chemistry*
Calcium / metabolism
Cell Differentiation
Cell Line
Cell Line, Tumor
Chloramphenicol O-Acetyltransferase / metabolism
Dose-Response Relationship, Drug
Estradiol / analogs & derivatives*
Estradiol / pharmacology
Estrogen Receptor Modulators / metabolism*
Estrogens / metabolism
Female
Fulvestrant
Furans / chemistry
HeLa Cells
Humans
Insulin-Like Growth Factor Binding Protein 3 / metabolism
Mice
Osteoblasts / metabolism
Plants / metabolism*
Plants, Medicinal*
Receptors, Estrogen / metabolism
Tetrazolium Salts / pharmacology
Thiazoles / pharmacology
Time Factors
Transfection
Uterine Cervical Neoplasms / drug therapy
|
| IF |
1.948
|
| Times Cited |
13
|
|
WOS Category
|
ENDOCRINOLOGY & METABOLISM
BIOCHEMISTRY & MOLECULAR BIOLOGY
|
| Resource |
| Human and Animal Cells |
MC3T3-E1(RCB1126) |
