Article
Systematic analysis of anti-estrogen effects in pituitary adenoma cells
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Published: | June 9, 2017 |
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Objective: Interfering with the estrogen receptor alpha pathway appears an attractive way to eliminate tumor cells in pituitary adenomas. Here we attempted to assess the potency of several anti-estrogens on cell viability in rodent pituitary adenoma cells.
Methods: TtT-GF and GH3 cells were incubated with Bazedoxifene, Clomiphen, Fulvestrant, Raloxifene, and Tamoxifen in a submicromolar to high micromolar concentration range for up to five days. Cell viability was assessed using either a water soluble tetrazolium (WST)-1 assay or 4',6-diamidino-2-phenylindole (DAPI) staining. Half-maximal inhibitory concentrations (IC50) of anti-estrogens were calculated based on three independent experiments performed in triplicates.
Results: After five days, viability of TtT-GF cells was significantly decreased by Bazedoxifene (IC50=35µM, p=0.0044), Clomiphen (IC50=5µM, p<0.0001), and Raloxifene (IC50=20µM, p=0.013), while Fulvestrant did not show a significant effect on TtT-GF cell viability even at high micromolar concentrations. Similarly, after five days, viability of GH3 cells was significantly decreased by Bazedoxifene (IC50=20µM, p=0.013), Clomiphen (IC50=15µM, p=0038), Fulvestrant (IC50=1µM, p<0.022), and Raloxifene (IC50=35µM, p=0.031).
Conclusion: Viability of TtT-GF and GH3 cells was selectively decreased by anti-estrogens, of which Clomiphen had the highest potency in both cell lines. Further investigation of anti-estrogens in human cell lines is warranted to evaluate the clinical potential of anti-estrogens in pituitary adenomas.