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Article

In Vitro Evaluation of Sulforaphane and a Natural Analog as Potent Inducers of 5-Fluorouracil Anticancer Activity

1
Department of Drug Biotechnology and Bioinformatics, National Medicines Institute, 30/34 Chełmska St, 00-725 Warsaw, Poland
2
Chair and Department of Synthesis and Chemical Technology of Pharmaceutical Substances, Medical University of Lublin, 1 Aleje Racławickie St, 20-059 Lublin, Poland
*
Author to whom correspondence should be addressed.
Received: 26 October 2018 / Revised: 13 November 2018 / Accepted: 19 November 2018 / Published: 21 November 2018
(This article belongs to the Special Issue Focusing on Sulfur in Medicinal Chemistry)
Isothiocyanates (R-NCS) are sulphur-containing phytochemicals. The main source are plants of the Brassicaceae family. The best known plant-derived isothiocyanate is sulforaphane that has exhibited anticancer activity in both in vivo and in vitro studies. Recent attempts to expand their use in cancer therapy involve combining them with standard chemotherapeutics in order to increase their therapeutic efficacy. The aim of this paper is to determine the impact of sulforaphane and its natural analog alyssin on the anticancer activity of the well-known anticancer drug 5-fluorouracil. The type of drug-drug interactions was determined in prostate and colon cancer cell lines. Confocal microscopy, western blot and flow cytometry methods were employed to determine the mechanism of cytotoxic and cytostatic action of the combinations. The study revealed that additive or synergistic interactions were observed between 5-fluorouracil and both isothiocyanates, which enhanced the anticancer activity of 5-fluorouracil, particularly in colon cancer cell lines. An increased cytostatic effect was observed in case of alyssin while for sulforaphane the synergistic interaction with 5-fluorouracil involved an intensification of apoptotic cell death. View Full-Text
Keywords: sulforaphane; 5-fluorouracil; drug interactions; apoptosis; cell cycle sulforaphane; 5-fluorouracil; drug interactions; apoptosis; cell cycle
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MDPI and ACS Style

Milczarek, M.; Mielczarek, L.; Lubelska, K.; Dąbrowska, A.; Chilmonczyk, Z.; Matosiuk, D.; Wiktorska, K. In Vitro Evaluation of Sulforaphane and a Natural Analog as Potent Inducers of 5-Fluorouracil Anticancer Activity. Molecules 2018, 23, 3040. https://0-doi-org.brum.beds.ac.uk/10.3390/molecules23113040

AMA Style

Milczarek M, Mielczarek L, Lubelska K, Dąbrowska A, Chilmonczyk Z, Matosiuk D, Wiktorska K. In Vitro Evaluation of Sulforaphane and a Natural Analog as Potent Inducers of 5-Fluorouracil Anticancer Activity. Molecules. 2018; 23(11):3040. https://0-doi-org.brum.beds.ac.uk/10.3390/molecules23113040

Chicago/Turabian Style

Milczarek, Małgorzata, Lidia Mielczarek, Katarzyna Lubelska, Aleksandra Dąbrowska, Zdzisław Chilmonczyk, Dariusz Matosiuk, and Katarzyna Wiktorska. 2018. "In Vitro Evaluation of Sulforaphane and a Natural Analog as Potent Inducers of 5-Fluorouracil Anticancer Activity" Molecules 23, no. 11: 3040. https://0-doi-org.brum.beds.ac.uk/10.3390/molecules23113040

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