Effect of tamoxifen and tamoxifen derivatives on the conversion of estrone sulfate to estradiol in the MCF-7 mammary cancer cell line

Cancer Letters
J R Pasqualini, C Gelly

Abstract

The human mammary cancer cell line MCF-7 in culture was used to study the effect of tamoxifen and its derivatives: 4-hydroxytamoxifen (4-OH-Tam), N-desmethyltamoxifen (Dem-Tam) and cis-tamoxifen (cis-Tam) on the uptake and conversion of [3H]estrone sulfate (3H-E1S) to estradiol (E2). When [3H]-E1S (4 X 10(-9) M) was incubated by itself (control) a great proportion of the radioactivity was found as [3H]E2, predominantly in the nuclear fraction. All of the anti-estrogens (10(-6) M - 10(-5) M) studied decreased the total uptake of radioactivity by the cells by 50-60% and the quantity of E2 formed. The calculated concentrations (in pg/mg DNA +/- S.E.M.) of E2 (cytosol + 0.6 M KCl nuclear extract) with the anti-estrogens at 10(-5) M were as follows: control 56 +/- 3; Tam treated cells 4 +/- 1; + 4-OH-Tam 2 +/- 1; + Dem-Tam 5 +/- 2; + cis-Tam 8 +/- 4. A significant decrease in the concentrations of E2 was also observed in the mitochondria-microsomal fractions after the different treatments. It is suggested that the MCF-7 cells can use estrone-3-sulfate as a source of E2 and that the inhibitory effect of tamoxifen and its derivatives on the conversion of this sulfate to E2 could be involved in the anti-estrogenic process of these trip...Continue Reading

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Citations

Oct 1, 1988·Journal of Steroid Biochemistry·J R PasqualiniN Giambiagi
Jan 1, 1989·Journal of Steroid Biochemistry·J R PasqualiniC Vella
Dec 1, 1989·Journal of Steroid Biochemistry·K NaitohT Nambara
Mar 1, 1995·Steroids·P K LiL Dibbelt
Mar 1, 1992·The Journal of Steroid Biochemistry and Molecular Biology·J R PasqualiniB L Nguyen
May 1, 1993·The Journal of Steroid Biochemistry and Molecular Biology·S J Santner, R J Santen
Mar 1, 1995·The Journal of Steroid Biochemistry and Molecular Biology·K W Selcer, P K Li
May 1, 1995·The Journal of Steroid Biochemistry and Molecular Biology·P E LønningH Adlercreutz
Nov 1, 1995·Critical Reviews in Oncology/hematology·E Lønning, E A Lien
Jun 1, 2001·The Journal of Steroid Biochemistry and Molecular Biology·G S Chetrite, J R Pasqualini
Jul 27, 1999·The Journal of Steroid Biochemistry and Molecular Biology·J R Pasqualini, G S Chetrite
Jun 22, 2000·Gynecological Endocrinology : the Official Journal of the International Society of Gynecological Endocrinology·J R PasqualiniG S Chetrite
Apr 1, 1993·Cancer Treatment Reviews·E Lønning
Jan 1, 1992·European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)·J R Pasqualini
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Jun 3, 2004·Biochimica Et Biophysica Acta·Jorge R Pasqualini
Oct 13, 1998·Cancer Treatment Reviews·G Y Locker

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