Potent genistein derivatives as inhibitors of estrogen receptor alpha-positive breast cancer

Marik, Radharani; Allu, Madhan; Anchoori, Ravi; Stearns, Vered; Umbricht, Christopher B.; Khan, Saeed R.

doi:10.4161/cbt.11.10.15184

Cited by 53 publications

(26 citation statements)

References 31 publications

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“…In this view, the discovery of derivatives of genistein able to exert an inhibitory effect on breast cancer growth at low doses, as shown by Marik and colleagues in the current issue of Cancer Biology & Therapy, 10 is noteworthy. The authors …”

Section: ©2 0 1 1 L a N D E S B I O S C I E N C E D O N O T D I S Tmentioning

confidence: 99%

“…10 The relationship between genistein and ERβ expression and activity has been previously investigated. Whereas E2 binds to ERα and ERβ with similar affinity, genistein selectively binds to ERβ, 17 inducing an association with coactivators and activation of downstream gene transcription.…”

Section: ©2 0 1 1 L a N D E S B I O S C I E N C E D O N O T D I S Tmentioning

confidence: 99%

“…Marik and colleagues 10 report the modified expression of the PSN gene (psoriasin), a member of the S100 gene family implicated in breast cancer cell survival and associated with aggressive behaviour, as one possible effect. Recently, a decrease in phosphorylated p90RSK has demonstrated that genistein derivatives (MA-8, MA-9, MA-19) had anti-proliferative activity, induced apoptosis, reduced ERα mRNA expression, and increased ERβ expression at much lower doses than parental genistein.…”

Section: ©2 0 1 1 L a N D E S B I O S C I E N C E D O N O T D I S Tmentioning

confidence: 99%

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Genistein: The future of prevention and treatment of breast cancer?

Orlando

Schiavone²,

Cinieri³

2011

Cancer Biology & Therapy

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Section: ©2 0 1 1 L a N D E S B I O S C I E N C E D O N O T D I S Tmentioning

confidence: 99%

Section: ©2 0 1 1 L a N D E S B I O S C I E N C E D O N O T D I S Tmentioning

confidence: 99%

Section: ©2 0 1 1 L a N D E S B I O S C I E N C E D O N O T D I S Tmentioning

confidence: 99%

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Genistein: The future of prevention and treatment of breast cancer?

Orlando

Schiavone²,

Cinieri³

2011

Cancer Biology & Therapy

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“…Phyto- and xenoestrogens apparently also influence the expression levels of ERα and ERβ [167, 169]. Pennie et al showed that the activation of the vitellogenin and luteinizing hormone beta promoters differs for the two receptor subtypes and also depends on the specific ligand [170].…”

Section: Molecular Mechanismsmentioning

confidence: 99%

Combating Malaria with Plant Molecules: A Brief Update

Negi¹,

Gupta²,

Hamid

2013

CMC

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Observations on the role of ovarian hormones in breast cancer growth, as well as interest in contraception, stimulated research into the biology of estrogens. The identification of the classical receptors ERα and ERβ and the transmembrane receptor GPER and the resolution of the structure of the ligand bound to its receptor established the principal molecular mechanisms of estrogen action. The presence of estrogen-like compounds in many plants used in traditional medicine or ingested as food ingredients, phytoestrogens, as well as the estrogenic activities of many industrial pollutants and pesticides, xenoestrogens, have prompted investigations into their role in human health. Phyto- and xenoestrogens bind to the estrogen receptors with a lower affinity than the endogenous estrogens and can compete or substitute the hormone. Xenoestrogens, which accumulate in the body throughout life, are believed to increase breast cancer risk, especially in cases of prenatal and prepuberal exposure whereas the role of phytoestrogens is still a matter of debate. At present, the application of phytoestrogens appears to be limited to the treatment of post-menopausal symptoms in women where the production of endogenous estrogens has ceased. In this review we discuss chemistry, structure and classification, estrogen signaling and the consequences of the interactions of estrogens, phytoestrogens and xenoestrogens with their receptors, the complex interactions of endogenous and exogenous ligands, the evaluation of the health risks related to xenoestrogens, and the perspectives toward the synthesis of potent third generation selective estrogen receptor modulators (SERMs).

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“…Ce sont des perturbateurs endocriniens et ne présentent donc pas d'intérêt en clinique. Cependant, l'apigénine (Mak et al, 2006) et la ginestéine (Marik et al, 2011 ;Orlando et al, 2011) inhiberaient la croissance de cellules cancéreuses mammaires in vitro via leur interaction respectivement avec le REβ ou le REα.…”

Section: Les Ligands Des Resunclassified

The DHEA metabolite 7β-hydroxy-epiandrosterone exerts anti-estrogenic effects on breast cancer cell lines

et al. 2012

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Titre : La 7β-hydroxy-épiandrostérone dans des modèles in vitro de cancer du sein : effets anti-estrogéniques et rôle des récepteurs des estrogènes. La 7β-hydroxy-épiandrostérone, stéroïde endogène dérivant de la DHEA, présente des propriétés antiinflammatoires. En effet, elle module la voie des prostaglandines (PGs) en inhibant la production de la PGE2 pro-inflammatoires et en augmentant la production de la 15-Deoxy-∆ 12,14 -PGJ2 cyto-protectrice in vivo et in vitro. Les faibles doses de 7β-hydroxy-épiandrostérone (1nM, 10nM, 100nM) pour lesquelles ces effets sont observés, suggèrent une liaison à un récepteur spécifique. L'inflammation et la production des PGs jouent un rôle important dans le développement et la prolifération des tumeurs mammaires estrogéno-dépendantes. Le 17β-estradiol (E2), en se fixant sur les récepteurs des estrogènes (REs), induit la production de PGE2 et la prolifération cellulaire dans ces cellules tumorales. De ce fait, notre objectif était de tester les effets de la 7β-hydroxy-épiandrostérone sur la prolifération (comptage avec exclusion au bleu trypan), le cycle cellulaire et l'apoptose (cytométrie de flux) dans les lignées cellulaires de cancer du sein MCF-7 (REα+, REβ+, GPR30+) et MDA-MB-231 (REα-, REβ+, GPR30+) et d'identifier une(des) cible(s) potentielle(s) dans ces cellules (transactivation) et dans des cellules négatives pour les REs nucléaires SKBr3 (GPR30+) (études de prolifération). Cette étude a montré que la 7β-hydroxy-épiandrostérone exerce des effets anti-estrogéniques dans les cellules MCF-7 et MDA-MB-231 associés à une inhibition de la prolifération et un arrêt du cycle cellulaire. Les études de transactivation et de prolifération avec les agonistes spécifiques des REs ont montré une interaction avec le REβ. De plus, les résultats des études de proliférations sur les trois lignées cellulaires suggèrent que la 7β-hydroxy-épiandrostérone pourrait également interagir avec le GPR30. Ces résultats indiquent que ce stéroïde androgène agit comme un anti-estrogène. De plus, c'est la première fois qu'un stéroïde androgène à faible dose montre une action anti-proliférative dans des lignées de cancers du sein. De études ultérieures restent à réaliser afin de mieux comprendre ces effets observés. Mots clés : 7β-hydroxy-épiandrostérone, récepteurs des estrogènes, lignées de carcinomes mammaires, prolifération, transactivationThe DHEA metabolite 7β-hydroxy-epiandrosterone exerts anti-estrogenic effects on breast cancer cell lines 7β-hydroxy-epiandrosterone, an endogenous androgenic derivative of DHEA, has previously been shown to exert anti-inflammatory action in vitro and in vivo via a shift from prostaglandin E2 (PGE2) to 15-deoxy-∆ 12,14 -PGJ2 production. This modulation in prostaglandin production was obtained with low concentrations of 7β-hydroxy-epiandrosterone (1-100 nM) and suggested that it might act through a specific receptor. Inflammation and prostaglandin synthesis is important in the development and survival of estrogendependent mammary cancers. Estrogen induced PGE2 ...

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Potent genistein derivatives as inhibitors of estrogen receptor alpha-positive breast cancer

Cited by 53 publications

References 31 publications

Genistein: The future of prevention and treatment of breast cancer?

Genistein: The future of prevention and treatment of breast cancer?

Combating Malaria with Plant Molecules: A Brief Update

The DHEA metabolite 7β-hydroxy-epiandrosterone exerts anti-estrogenic effects on breast cancer cell lines

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