Abstract
Glucoraphasatin (GRH), a glucosinolate present abundantly in the plants of the Brassicaceae family, is hydrolyzed by myrosinase to raphasatin, which is considered responsible for its cancer chemopreventive activity; however, the underlying mechanisms of action have not been investigated, particularly in human cell lines. The aims of this study are to determine the cytotoxicity of raphasatin, and to evaluate its potential to cause apoptosis and modulate cell cycle arrest in human breast adenocarcinoma MCF-7 cells. The cytotoxicity was determined following incubation of the cells with glucoraphasatin or raphasatin (0–100 µM), for 24, 48, and 72 h. GRH displayed no cytotoxicity as exemplified by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. When myrosinase was added to the incubation system to convert GRH to raphasatin, cytotoxicity was evident. Exposure of the cells to raphasatin stimulated apoptosis, as was exemplified by cell shrinkage, membrane blebbing, chromatin condensation, and nuclear fragmentation. Moreover, using Annexin V-FITC assay, raphasatin induced apoptosis, as witnessed by changes in cellular distribution of cells, at different stages of apoptosis; in addition, raphasatin caused the arrest of the MCF-7 cells at the G2 + M phase. In conclusion, raphasatin demonstrated cancer chemopreventive potential against human breast adenocarcinoma (MCF-7) cells, through induction of apoptosis and cell cycle arrest.
Highlights
Cancer is a failure of the mechanisms that regulate cell growth and division, and remains a leading cause of death worldwide
Data are expressed as mean ± standard deviation (SD) of three independent experiments
Extensive experimental studies have established that isothiocyanates, both aliphatic and aromatic, such as sulforaphane, erucin, and phenethyl isothiocyanate, owe their potent cancer chemopreventive activity to the fact that they act through a number of mechanisms, modulating favorably the initiation and promotion stages of carcinogenesis [18,22,23,24,25,26,27,28,29,30]
Summary
Cancer is a failure of the mechanisms that regulate cell growth and division, and remains a leading cause of death worldwide. Chemo- and radio-therapies are currently used routinely in cancer. Molecules 2018, 23, 3092 therapy [1], these are accompanied by serious side-effects, as a result of damage to normal tissues surrounding the tumors [2]. Tumors may demonstrate resistance to these treatments [3]. Breast cancer is a very common disease among Malaysian women and worldwide, with about 150–200 new cases being diagnosed, annually, in the Breast Clinic in Kuala Lumpur Hospital, alone.
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