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Comparison of antiproliferative activity of the natural isothiocyanates and their mercapturic derivatives.

Mateusz Psurski 1Patrycja Gawora 1Joanna Wietrzyk 2Józef Oleksyszyn 1

1. Wroclaw University of Technology, Division of Medicinal Chemistry and Microbiology (PWR), Wybrzeże Wyspiańskiego 27, Wrocław 50-370, Poland
2. Polish Academy of Sciences, Institute of Immunology and Experimental Therapy (IITD), Rudolfa Weigla 12, Wrocław 53-114, Poland


A number of natural compounds with the antitumor activity have been found in our diet. Among them there is a large group of compounds known as isothiocyanates (ITC), the majority of which occur in plants, especially in Cruciferous vegetables like broccoli, cauliflower, cabbage and others. Highly reactive isothiocyanate (-NCS) group have an ability to simultaneously modulate multiple cellular targets involved in cancer development and its main targets are cysteine residues. The main metabolic pathway involved in isothiocyanates elimination from cells is the mercapturic acids pathway. The process starts from glutathione, an important redox state guardian, and leads to cysteine and N-acetylocysteine (NAC) conjugates. Interestingly, this metabolic products also exhibits antitumor activity.
We compared the antiproliferative activity of a group of natural isothiocyanates and their metabolites. In vitro studies on several lung and breast cancer cells lines were performed. We have showed that isothiocyanates can be strong antiproliferative agents with relatively low cytotoxicity towards normal cells. Moreover, our studies showed that the isothiocyanates metabolites not only posses the antiproliferative activity, but in many cases this activity is greater than activity of ITCs.  Because of that, and because of some other reasons (discussed in the paper), we believe that isothiocyanates metabolites could by both anticancer drugs and element of chemopreventive diet.


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Submitted: 2010-03-13 15:47
Revised:   2010-03-13 15:47