Estrogenic/antiestrogenic activity of selected selective serotonin reuptake inhibitors

Authors

  • Anca Pop
  • Diana Ioana Lupu
  • Julien Cherfan
  • Bela Kiss
  • Felicia Loghin

DOI:

https://doi.org/10.15386/cjmed-474

Keywords:

fluoxetine, sertraline, paroxetine, luciferase assay

Abstract

Backround & Aims: Selective serotonin reuptake inhibitors (SSRIs) are one of the most prescribed classes of psychotropics. Even though the SSRI class consists of 6 molecules (citalopram, escitalopram, fluoxetine, fluvoxamine, paroxetine and sertraline), only fluoxetine was intensively studied for endocrine disruptive effects, while the other SSRIs received less attention. This study was designed to evaluate the estrogenic/antiestrogenic effect of fluoxetine, sertraline and paroxetine.

Materials and methods: The in vitro (anti)estrogenic activity was assessed using a firefly luciferase reporter construct in the T47D-KBluc breast cancer cell line. These cells express nuclear estrogen receptors that can activate the transcription of the luciferase reporter gene upon binding of estrogen receptor agonists.  

Results: All three compounds were found to interact with the estrogen receptor. Fluoxetine had dual properties, weak estrogenic at lower concentrations and antiestrogenic effect at higher concentrations. Sertraline shared the same properties with fluoxetine, but also increased the estradiol-mediated transcriptional activity. Paroxetine presented only one type of effect, the ability to increase the estradiol-mediated transcriptional activity.

 Conclusions: Overall, our results indicate a possible interaction of SSRIs with the estrogen receptor. As SSRIs are being used by all categories of population, including pregnant women or children, establishing whether they can affect the endocrine mediated mechanisms should be a priority.

Author Biographies

Anca Pop, "Iuliu Hatieganu" University of Medicine and Pharmacy, Faculty of Pharmacy

Toxicology

Diana Ioana Lupu, "Iuliu Hatieganu" University of Medicine and Pharmacy, Faculty of Pharmacy

Toxicology

Julien Cherfan, "Iuliu Hatieganu" University of Medicine and Pharmacy, Faculty of Pharmacy

Toxicology

Felicia Loghin, "Iuliu Hatieganu" University of Medicine and Pharmacy, Faculty of Pharmacy

Toxicology

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Published

2015-07-22

How to Cite

1.
Pop A, Lupu DI, Cherfan J, Kiss B, Loghin F. Estrogenic/antiestrogenic activity of selected selective serotonin reuptake inhibitors. Med Pharm Rep [Internet]. 2015 Jul. 22 [cited 2025 Oct. 5];88(3):381-5. Available from: https://medpharmareports.com/index.php/mpr/article/view/474

Issue

Section

Original Research