Effects of fulvestrant alone or combined with different steroids in human breast cancer cells<i>in vitro</i>

Jansen, Gunther; Franke, H; Wolbers, F.; Brinkhuis, Mariël; Vermes, I.

doi:10.1080/13697130802232500

Cited by 5 publications

(3 citation statements)

References 26 publications

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“…Statistically significant differences ( p < 0.05) between the ER + cell line and the two ER – cell lines are indicated in these graphs by italic letters A and N . In line with previous literature, the pure antiestrogenic drug fulvestrant significantly reduced cell growth of the ER + cells while having little or no impact on the growth of either of the ER – cell lines . 4-Hydroxytamoxifen, the active metabolite of tamoxifen, specifically inhibited only the ER + cell line at 10 –8 M to 10 –6 M, with both ER + and ER – cell lines being affected at higher concentrations.…”

Section: Biological Results and Discussionsupporting

confidence: 90%

Biomimetic Syntheses and Antiproliferative Activities of Racemic, Natural (−), and Unnnatural (+) Glyceollin I

et al. 2011

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A 14-step biomimetic synthetic route to glyceollin I (1.5% overall yield) was developed and deployed to produce the natural enantiomeric form in soy, its unnatural stereoisomer, and a racemic mixture. Enantiomeric excess was assessed by asymmetric NMR shift reagents and chiral HPLC. Antiproliferative effects were measured in human breast, ovarian, and prostate cancer cell lines, with all three chiral forms exhibiting growth inhibition (GI) in the low to mid μM range for all cells. The natural enantiomer, and in some cases the racemate, gave significantly greater GI than the unnatural stereoisomer for estrogen receptor positive (ER(+)) versus ER(-) breast/ovarian cell lines as well as for androgen receptor positive (AR(+)) versus AR(-) prostate cancer cells. Surprisingly, differences between ER(+) and ER(-) cell lines were not altered by media estrogen conditions. These results suggest the antiproliferative mechanism of glyceollin I stereoisomers may be more complicated than strictly ER interactions.

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Section: Biological Results and Discussionsupporting

confidence: 90%

Biomimetic Syntheses and Antiproliferative Activities of Racemic, Natural (−), and Unnnatural (+) Glyceollin I

et al. 2011

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“…As genistein‐mediated PON1 induction was inhibited by the oestrogen‐receptor antagonist fulvestrant, it may be hypothesized that the induction of PON1 because of genistein could be partly be via an oestrogen‐receptor‐dependent signal transduction pathway. However, it needs to be taken into account that the fulvestrant concentration, as used in our Huh7 cell culture studies, was manifold higher than those previously reported in the literature . Furthermore, we found putative AhR binding sites in the PON1 promoter in silico .…”

Section: Discussionmentioning

confidence: 99%

Genistein as a potential inducer of the anti‐atherogenic enzyme paraoxonase‐1: studies in cultured hepatocytes in vitro and in rat liver in vivo

Schrader

Ernst

Sinnecker

et al. 2012

J Cellular Molecular Medi

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A number of cardioprotective effects, including the reduced oxidation of the low-density lipoprotein (LDL) particles, have been attributed to dietary soy isoflavones. Paraoxonase 1 (PON1), an enzyme mainly synthesized in the liver, may exhibit anti-atherogenic activity by protecting LDL from oxidation. Thus, dietary and pharmacological inducers of PON1 may decrease cardiovascular disease risk. Using a luciferase reporter gene assay we screened different flavonoids for their ability to induce PON1 in Huh7 hepatocytes in culture. Genistein was the most potent flavonoid with regard to its PON1-inducing activity, followed by daidzein, luteolin, isorhamnetin and quercetin. Other flavonoids such as naringenin, cyanidin, malvidin and catechin showed only little or no PON1-inducing activity. Genistein-mediated PON1 transactivation was partly inhibited by the oestrogen-receptor antagonist fulvestrant as well as by the aryl hydrocarbon receptor antagonist 7-ketocholesterol. In contrast to genistein, the conjugated genistein metabolites genistein-7-glucuronide, genistein-7-sulfate and genistein-7,4′-disulfate were only weak inducers of PON1 transactivation. Accordingly, dietary genistein supplementation (2 g/kg diet over three weeks) in growing rats did not increase hepatic PON1 mRNA and protein levels as well as plasma PON1 activity. Thus, genistein may be a PON1 inducer in cultured hepatocytes in vitro, but not in rats in vivo.

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“…To answer the research questions, an epidemiological study and in vitro research were carried out. 26,27 …”

mentioning

confidence: 98%

Cancer prevalence in osteoporotic women with low serum vitamin D levels

et al. 2011

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Effects of fulvestrant alone or combined with different steroids in human breast cancer cellsin vitro

Abstract: Our study demonstrated that fulvestrant, an ER antagonist used in the treatment of ER-positive breast cancer, combined with E2 and DHD or in combination with tibolone, is not compromised in its efficacy in inducing apoptosis in ER-positive breast cancer cell lines in vitro.

Cited by 5 publications

References 26 publications

Biomimetic Syntheses and Antiproliferative Activities of Racemic, Natural (−), and Unnnatural (+) Glyceollin I

Biomimetic Syntheses and Antiproliferative Activities of Racemic, Natural (−), and Unnnatural (+) Glyceollin I

Genistein as a potential inducer of the anti‐atherogenic enzyme paraoxonase‐1: studies in cultured hepatocytes in vitro and in rat liver in vivo

Cancer prevalence in osteoporotic women with low serum vitamin D levels

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