MYROSINASE-GENERATED ISOTHIOCYANATE FROM GLUCOSINOLATES - ISOLATION, CHARACTERIZATION AND IN-VITRO ANTIPROLIFERATIVE STUDIES

Epidemiological and pharmacological studies have shown that colorectal cancer development could be reduced by consuming vegetables that cont ain glucosinolates. In view of this the effect of some glucosinolates and their isothiocyanate (ITC)-derived products on in vitro cell growt h was studied. We report the isolation and characterization of ITCs de rived from glucosinolates by using HPLC, GC-MS, and NMR techniques. Th e in vitro activity of ITCs on human erythroleukemic K562 cells has be en investigated by using two alternative approaches: the in situ and p re-mix methods. No differences in antiproliferative activity were foun d comparing the effect of ITCs produced either of these methods. In th e experimental conditions used, the production of ITCs from glucosinol ates is almost quantitative as confirmed by HPLC or GC-MS analysis. Th e ITCs' inhibitory activity on K562 cells growth is particularly evide nt in the cases of ITCs derived from sinigrin, progoitrin, epi-progoit rin, glucotropaeolin and glucocheirolin. Finally, the antiproliferativ e activity of the ITCs obtained from glucoraphenin, taken as an exampl e, was determined on other tumor cell lines with a different origin an d hystotype. Considering the antiproliferative activity found for ITCs these compounds could be considered potentially responsible for the r eduction of colorectal cancer associated with diets rich in cruciferou s vegetables. Further studies will be aimed at the possible applicatio n of glucosinolate-derived products as chemopreventive cancer agents. (C) 1997 Elsevier Science Ltd.