Metabolism and antiproliferative effects of sulforaphane and broccoli sprouts in human intestinal (Caco-2) and hepatic (HepG2) cells
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The purpose of this work was to study the absorption and metabolism of sulforaphane (SFN) from broccoli sprouts, their major glucosinolate glucoraphanin and its hydrolysis product SFN. This was done by monitoring SFN’s main metabolites, i.e. SFN, SFN-glutathione and SFN-cysteine, in two different cell models of absorption and metabolism (Caco-2 colorectal carcinoma cells and HepG2 hepatocellular carcinoma cells), during 3, 6, and 24 h of treatment, using a selective UHPLC-QqQ-MS/MS procedure. Concentrations ranging 0.5–90 nmol/l were found within the cells and released in the medium, depending on the type of analyte under study. Cells were capable of conjugative metabolism, since the SFN mercapturic derivatives could be identified in the cell medium. The antiproliferative activity of broccoli sprouts, glucoraphanin and sulforaphane was compared in Caco-2 and HT-29 human colorectal carcinoma cells, and HepG2 hepatocellular carcinoma cells, establishing the minimal concentration of a given compound to achieve half inhibition of the maximal cell growth (IC50) for broccoli sprouts extract and sulforaphane. However, glucoraphanin did not show an antiproliferative effect in the cells under study.
KeywordsBrassica oleraceae Metabolism Cytotoxicity UHPLC-QqQ-MS/MS
This work was supported by the Spanish Ministry of Economy and Competitiveness through projects: AGL2012-30803 and AGL2013-46247-P, and the CYTED Program (Ref. 112RT0460) CORNUCOPIA Thematic Network. N. Baenas was funded by a FPU grant from the Spanish Ministry of Education Fellowship Programme. J. M. Silvan wishes to thank CSIC and FSE for a JAE-Doc postdoctoral contract. The glucoraphanin for these studies was a generous gift from Dr. Gina R. de Nicola and Dr. Renato Iori CRA-CIN, Bologna, Italy.
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