Journal
FOOD AND CHEMICAL TOXICOLOGY
Volume 50, Issue 5, Pages 1589-1599Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.fct.2012.01.025
Keywords
Quercetin; Quercetin-5 ',8-disulfonate; Antiproliferation; Cell cycle; Apoptosis; ROS
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Funding
- National Natural Science Foundation of China [C30972054, C20802091, C31171678]
- China Agriculture Research System [CARS-28]
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This study is designed to compare the anticancer effects of quercetin and its water-soluble sulfated derivative, quercetin-5',8-disulfonate (QS), in human colon cancer LoVo cells and breast cancer MCF-7 cells. It was found that both quercetin and QS can inhibit the growth of cancer cells in a dose-dependent manner, with the IC50 values of 40.2 and 28.0 mu M for LoVo cells and 30.8 and 19.9 mu M for MCF-7 cells, respectively, suggesting QS was more effective against the cancer cells than quercetin. Moreover, flow cytometric assay revealed that quercetin and QS could mediate the cell-cycle arrest principally in the S phase after 24 h of treatment with the two tumor cells. It was also found that 69.6% of LoVo cells and 90.6% of MCF-7 cells entered the early phase of apoptosis when treated with 100 mu M QS for 48 h. Furthermore, we firstly found the generation of ROS is a critical mediator in QS-induced cell growth inhibition. Taken together, the novel sulfated derivative of quercetin possesses strong antitumor activity via a ROS-dependent apoptosis pathway, and has the excellent potential to be developed into an antitumor precursor compound. (C) 2012 Elsevier Ltd. All rights reserved.
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