Next Article in Journal
USP Reference Standard Monoclonal Antibodies: Tools to Verify Glycan Structure
Previous Article in Journal
The Inhibition of the Small-Conductance Ca2+-Activated Potassium Channels Decreases the Sinus Node Pacemaking during Beta-Adrenergic Activation
 
 
Search for Articles:
Title / Keyword
Author / Affiliation / Email
Journal
Article Type
 
 
Advanced Search
 
Section
Special Issue
Volume
Issue
Number
Page
 
Journals
Pharmaceuticals
Volume 15
Issue 3
10.3390/ph15030314
pharmaceuticals-logo
Submit to this Journal Review for this Journal Propose a Special Issue
► Article Menu

Article Menu

share Share announcement Help format_quote Cite question_answer Discuss in SciProfiles
first_page
settings
Order Article Reprints
Font Type:
Arial Georgia Verdana
Font Size:
Aa Aa Aa
Line Spacing:
Column Width:
Background:
Article

Investigation of the Antitumor Effects of Tamoxifen and Its Ferrocene-Linked Derivatives on Pancreatic and Breast Cancer Cell Lines

by
Márton Kalabay
1,
Zsófia Szász
1,
Orsolya Láng
1,
Eszter Lajkó
1,
Éva Pállinger
1,
Cintia Duró
2,
Tamás Jernei
2,
Antal Csámpai
2,
Angéla Takács
1 and
László Kőhidai
1,*
1
Department of Genetics, Cell and Immunobiology, Faculty of Medicine, Semmelweis University, 1085 Budapest, Hungary
2
Department of Inorganic Chemistry, Faculty of Chemistry, Eötvös Loránd University, 1053 Budapest, Hungary
*
Author to whom correspondence should be addressed.
Pharmaceuticals 2022, 15(3), 314; https://doi.org/10.3390/ph15030314
Submission received: 28 January 2022 / Revised: 26 February 2022 / Accepted: 2 March 2022 / Published: 5 March 2022
(This article belongs to the Section Pharmacology)
Browse Figures
Review Reports Versions Notes

Abstract

Tamoxifen is a long-known anti-tumor drug, which is the gold standard therapy in estrogen receptor (ER) positive breast cancer patients. According to previous studies, the conjugation of the original tamoxifen molecule with different functional groups can significantly improve its antitumor effect. The purpose of this research was to uncover the molecular mechanisms behind the cytotoxicity of different ferrocene-linked tamoxifen derivates. Tamoxifen and its ferrocene-linked derivatives, T5 and T15 were tested in PANC1, MCF7, and MDA-MB-231 cells, where the incorporation of the ferrocene group improved the cytotoxicity on all cell lines. PANC1, MCF7, and MDA-MB-231 express ERα and GPER1 (G-protein coupled ER 1). However, ERβ is only expressed by MCF7 and MDA-MB-231 cells. Tamoxifen is a known agonist of GPER1, a receptor that can promote tumor progression. Analysis of the protein expression profile showed that while being cytotoxic, tamoxifen elevated the levels of different tumor growth-promoting factors (e.g., Bcl-XL, Survivin, EGFR, Cathepsins, chemokines). On the other hand, the ferrocene-linked derivates were able to lower these proteins. Further analysis showed that the ferrocene-linked derivatives significantly elevated the cellular oxidative stress compared to tamoxifen treatment. In conclusion, we were able to find two molecules possessing better cytotoxicity compared to their unmodified parent molecule while also being able to counter the negative effects of the presence of the GPER1 through the ER-independent mechanism of oxidative stress induction.
Keywords: tamoxifen; GPER1; ferrocene; oxidative stress; cytotoxicity tamoxifen; GPER1; ferrocene; oxidative stress; cytotoxicity
Graphical Abstract

Share and Cite

MDPI and ACS Style

Kalabay, M.; Szász, Z.; Láng, O.; Lajkó, E.; Pállinger, É.; Duró, C.; Jernei, T.; Csámpai, A.; Takács, A.; Kőhidai, L. Investigation of the Antitumor Effects of Tamoxifen and Its Ferrocene-Linked Derivatives on Pancreatic and Breast Cancer Cell Lines. Pharmaceuticals 2022, 15, 314. https://doi.org/10.3390/ph15030314

AMA Style

Kalabay M, Szász Z, Láng O, Lajkó E, Pállinger É, Duró C, Jernei T, Csámpai A, Takács A, Kőhidai L. Investigation of the Antitumor Effects of Tamoxifen and Its Ferrocene-Linked Derivatives on Pancreatic and Breast Cancer Cell Lines. Pharmaceuticals. 2022; 15(3):314. https://doi.org/10.3390/ph15030314

Chicago/Turabian Style

Kalabay, Márton, Zsófia Szász, Orsolya Láng, Eszter Lajkó, Éva Pállinger, Cintia Duró, Tamás Jernei, Antal Csámpai, Angéla Takács, and László Kőhidai. 2022. "Investigation of the Antitumor Effects of Tamoxifen and Its Ferrocene-Linked Derivatives on Pancreatic and Breast Cancer Cell Lines" Pharmaceuticals 15, no. 3: 314. https://doi.org/10.3390/ph15030314

APA Style

Kalabay, M., Szász, Z., Láng, O., Lajkó, E., Pállinger, É., Duró, C., Jernei, T., Csámpai, A., Takács, A., & Kőhidai, L. (2022). Investigation of the Antitumor Effects of Tamoxifen and Its Ferrocene-Linked Derivatives on Pancreatic and Breast Cancer Cell Lines. Pharmaceuticals, 15(3), 314. https://doi.org/10.3390/ph15030314

Note that from the first issue of 2016, this journal uses article numbers instead of page numbers. See further details here.

Article Metrics

Back to TopTop