The inhibitory effect of diarylpropionitrile, a selective agonist of estrogen receptor beta, on the growth of MC38 colon cancer line

Motylewska, Ewelina; Stasikowska, Olga; Mełeń-Mucha, Gabriela

doi:10.1016/j.canlet.2008.10.050

Cited by 32 publications

(20 citation statements)

References 21 publications

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“…This phenomenon motivates us to investigative the potential role of ER as a protein with tumor suppressive function. Although earlier reported studies have shown eVects of ER on proliferation in other colon cancer cell lines (Motylewska et al 2009;Hartman et al 2009), these studies focused on scientiWc researches, not clinically therapeutic strategies. Using adenovirus as a vector to carry ER gene to investigate the antitumor eVect of ER in colon cancer in vitro and in vivo is lacking.…”

Section: Discussionmentioning

confidence: 98%

“…Ewelina Motylewska groups reported that diarylpropionitrile (DPN), a selective agonist of ER , induced a growth inhibition of MC38 colon cancer cell line (Motylewska et al 2009), suggesting a possibility of using a selective estrogen receptor agonist in the treatment of colon cancer. Hartman et al (2009) reported that stably introducing ER into colon cancer cell line SW480 leads to inhibited proliferation by repressing components of the cell cycle gene transcription, which are associated with proliferation, such as c-myc, cyclin D 1 , and cyclin A and by increasing the expression of Cdk inhibitor p21 Cip1 and p27 Kip1 , which leads to a G2 cell cycle arrest.…”

Section: Introductionmentioning

confidence: 98%

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Estrogen receptor β potentiates the antiproliferative effect of raloxifene and affects the cell migration and invasion in HCT-116 colon cancer cells

Tian

et al. 2012

J Cancer Res Clin Oncol

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Section: Discussionmentioning

confidence: 98%

Section: Introductionmentioning

confidence: 98%

Estrogen receptor β potentiates the antiproliferative effect of raloxifene and affects the cell migration and invasion in HCT-116 colon cancer cells

Tian

et al. 2012

J Cancer Res Clin Oncol

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“…In particular, we assessed the effects of DPN [23] and 8beta-VE2 [5] in comparison to the natural ligand 3beta-Adiol [11]; DPN and 8beta-VE2 are two known synthetic selective ERbeta agonists, the biological activity of which have been tested in other mammalian cell models [25, 26], in comparison to the natural ligand 3beta-Adiol [11]. Rv1 cells were chosen as a model of primary androgen-responsive human PC; these cells have also the advantage to maintain an exponential growth up to 15 days in vitro and to display a steady doubling time for a long period [31].…”

Section: Discussionmentioning

confidence: 99%

In VitroChronic Administration of ERbeta Selective Ligands and Prostate Cancer Cell Growth: Hypotheses on the Selective Role of 3beta-Adiol in AR-Positive RV1 Cells

Colciago

Ruscica

Mornati

et al. 2014

BioMed Research International

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Prostate cancer (PC) progression from androgen-dependent (AD) to castration-resistant (CR) disease is a process caused by modifications of different signal transduction pathways within tumor microenvironment. Reducing cell proliferation, estrogen receptor beta (ERbeta) is emerging as a potential target in PC chemoprevention. Among the known selective ERbeta ligands, 3beta-Adiol, the endogenous ligand in the prostate, has been proved to counteract PC progression. This study compares the effects of chronic exposure (1–12 weeks) to different ERbeta selective ligands (DPN, 8beta-VE2, 3beta-Adiol) on proliferation of human androgen-responsive CWR22Rv1 cells, representing an intermediate phenotype between the AD- and CR-PC. 3beta-Adiol (10 nM) is the sole ligand decreasing cell proliferation and increasing p21 levels. In vitro transcriptional activity assays were performed to elucidate different behavior between 3beta-Adiol and the other ligands; in these experiments the endogenous and the main ERbeta subtype activation were considered. It is concluded that ERbeta activation has positive effects also in androgen-responsive PC. The underlying mechanisms are still to be clarified and may include the interplay among different ERbeta subtypes and the specific PC microenvironment. ERbeta agonists might be useful in counteracting PC progression, although the final outcome may depend upon the molecular pattern specific to each PC lesion.

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“…Generally, ERα agonists are pro‐proliferative while ERβ agonists are anti‐proliferative (Thomas and Gustafsson ). For example, DPN inhibits growth in the colon cancer cell line MC38 (Motylewska et al ., ). DPN administered to Apc(Min/+) mice significantly reduces the incidence of intestinal tumours compared to untreated controls (Giroux et al .…”

Section: Discussionmentioning

confidence: 97%

Multiple Phytoestrogens Inhibit Cell Growth and Confer Cytoprotection By Inducing Manganese Superoxide Dismutase Expression

Robb

Stuart

2013

Phytotherapy Research

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Phytoestrogens are of interest because of their reported beneficial effects on many human maladies including cancer, neurodegeneration, cardiovascular disease and diabetes. As data on phytoestrogens continues to accumulate, it is clear that there is significant overlap in the cellular effects elicited by these various compounds. Here, we show that one mechanism by which a number of phytoestrogens achieve their growth inhibitory and cytoprotective effects is via induction of the mitochondrial manganese superoxide dismutase (MnSOD). Eight phytoestrogens, including resveratrol, coumestrol, kaempferol, genistein, daidzein, apigenin, isoliquirtigenin and glycitin, were tested for their ability to induce MnSOD expression in mouse C2C12 and primary myoblasts. Five of these, resveratrol, coumestrol, kaempferol, genistein and daidzein, significantly increased MnSOD expression, slowed proliferative growth and enhanced stress resistance (hydrogen peroxide LD50) . When siRNA was used to prevent the MnSOD induction by genistein, coumestrol or daidzein, none of these compounds exerted any effect on proliferative growth, and only the effect of coumestrol on stress resistance persisted. The estrogen antagonist ICI182780 prevented the increased MnSOD expression and also the changes in cell growth and stress resistance, indicating that these effects are mediated by estrogen receptors (ER). The absence of effects of resveratrol or coumestrol, but not genistein, in ERβ-null cells further indicated that this ER in particular is important in mediating these effects. Thus, an ER-mediated induction of MnSOD expression appears to underlie the growth inhibitory and cytoprotective activities of multiple phytoestrogens.

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The inhibitory effect of diarylpropionitrile, a selective agonist of estrogen receptor beta, on the growth of MC38 colon cancer line

Cited by 32 publications

References 21 publications

Estrogen receptor β potentiates the antiproliferative effect of raloxifene and affects the cell migration and invasion in HCT-116 colon cancer cells

Estrogen receptor β potentiates the antiproliferative effect of raloxifene and affects the cell migration and invasion in HCT-116 colon cancer cells

In VitroChronic Administration of ERbeta Selective Ligands and Prostate Cancer Cell Growth: Hypotheses on the Selective Role of 3beta-Adiol in AR-Positive RV1 Cells

Multiple Phytoestrogens Inhibit Cell Growth and Confer Cytoprotection By Inducing Manganese Superoxide Dismutase Expression

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