Wedelolactone induces growth of breast cancer cells by stimulation of estrogen receptor signalling
Jazyk angličtina Země Velká Británie, Anglie Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
25934092
DOI
10.1016/j.jsbmb.2015.04.019
PII: S0960-0760(15)00124-7
Knihovny.cz E-zdroje
- Klíčová slova
- Breast cancer, Estrogen receptor, Phytoestrogen, Wedelolactone,
- MeSH
- aktivace transkripce genetika MeSH
- alfa receptor estrogenů metabolismus MeSH
- antagonisté estrogenového receptoru farmakologie MeSH
- antitumorózní látky farmakologie MeSH
- beta receptor estrogenů metabolismus MeSH
- estradiol analogy a deriváty farmakologie MeSH
- estrogeny farmakologie MeSH
- fulvestrant MeSH
- HEK293 buňky MeSH
- kumariny farmakologie MeSH
- lidé MeSH
- MFC-7 buňky MeSH
- nádorové buněčné linie MeSH
- nádory prsu farmakoterapie MeSH
- proliferace buněk účinky léků MeSH
- responzivní elementy genetika MeSH
- signální transdukce účinky léků MeSH
- simulace molekulového dockingu MeSH
- transkripční faktor AP-1 metabolismus MeSH
- vazebná místa účinky léků MeSH
- Check Tag
- lidé MeSH
- ženské pohlaví MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- alfa receptor estrogenů MeSH
- antagonisté estrogenového receptoru MeSH
- antitumorózní látky MeSH
- beta receptor estrogenů MeSH
- ESR1 protein, human MeSH Prohlížeč
- estradiol MeSH
- estrogen receptor beta isoform M, human MeSH Prohlížeč
- estrogeny MeSH
- fulvestrant MeSH
- kumariny MeSH
- transkripční faktor AP-1 MeSH
- wedelolactone MeSH Prohlížeč
Wedelolactone, a plant coumestan, was shown to act as anti-cancer agent for breast and prostate carcinomas in vitro and in vivo targeting multiple cellular proteins including androgen receptors, 5-lipoxygenase and topoisomerase IIα. It is cytotoxic to breast, prostate, pituitary and myeloma cancer cell lines in vitro at μM concentrations. In this study, however, a novel biological activity of nM dose of wedelolactone was demonstrated. Wedelolactone acts as agonist of estrogen receptors (ER) α and β as demonstrated by transactivation of estrogen response element (ERE) in cells transiently expressing either ERα or ERβ and by molecular docking of this coumestan into ligand binding pocket of both ERα and ERβ. In breast cancer cells, wedelolactone stimulates growth of estrogen receptor-positive cells, expression of estrogen-responsive genes and activates rapid non-genomic estrogen signalling. All these effects can be inhibited by pretreatment with pure ER antagonist ICI 182,780 and they are not observed in ER-negative breast cancer cells. We conclude that wedelolactone acts as phytoestrogen in breast cancer cells by stimulating ER genomic and non-genomic signalling pathways.
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