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(Reference retrieved automatically from SciELO through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Biological activity and binding of estradiol to SK-Mel 23 human melanoma cells

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Author(s):
M.S.M.V. Sarti [1] ; M.A. Visconti [2] ; A.M.L. Castrucci [3]
Total Authors: 3
Affiliation:
[1] Universidade de São Paulo. Instituto de Biociências. Departamento de Fisiologia - Brasil
[2] Universidade de São Paulo. Instituto de Biociências. Departamento de Fisiologia - Brasil
[3] Universidade de São Paulo. Instituto de Biociências. Departamento de Fisiologia - Brasil
Total Affiliations: 3
Document type: Journal article
Source: Brazilian Journal of Medical and Biological Research; v. 37, n. 6, p. 901-905, 2004-06-00.
Abstract

Patients expressing estradiol receptors in melanoma cells have been reported to have a better prognosis. We therefore decided to investigate the in vitro effects of ß-estradiol and tamoxifen on the growth and tyrosinase activity of SK-Mel 23 human melanoma cells. Twenty-four-hour treatment with 0.4 nM ß-estradiol inhibited cell proliferation in 30% (0.70 ± 0.03 x 10(5) cells) and increased tyrosinase activity in 50% (7130.5 ± 376.5 cpm/10(5) cells), as compared to untreated cells (1.0 ± 0.05 x 10(5) cells and 4769 ± 25.5 cpm/10(5) cells, respectively). Both responses were completely (100%) blocked by 1 µM tamoxifen. Higher concentrations (up to 1.6 nM) or longer treatments (up to 72 h) did not result in a larger effect of the hormone on proliferation or tyrosinase activity. Competition binding assays demonstrated the presence of binding sites to [2,4,6,7-³H]-ß-estradiol, and that the tritiated analogue was displaced by the unlabeled hormone (1 nM to 100 µM, Kd = 0.14 µM, maximal displacement of 93%) or by 10 µM tamoxifen (displacement of 60%). ß-estradiol also increased the phosphorylated state of two proteins of 16 and 46 kDa, after 4-h treatment, as determined by Western blot. The absorbance of each band was 1.9- and 4-fold the controls, respectively, as determined with Image-Pro Plus software. Shorter incubation periods with ß-estradiol did not enhance phosporylation; after 6-h treatment with the hormone, the two proteins returned to the control phosphorylation levels. The growth inhibition promoted by estradiol may explain the better prognosis of melanoma-bearing women as compared to men, and open new perspectives for drug therapy. (AU)

FAPESP's process: 01/02460-1 - Melanopsin: comparative physiology of the gene and of the transduction of the luminous signal in pigmentary cells of fish, amphibians and mammals
Grantee:Ana Maria de Lauro Castrucci
Support Opportunities: Research Projects - Thematic Grants