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Antitumor activities of quercetin and quercetin-5',8-disulfonate in human colon and breast cancer cell lines.

Abstract
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 IC(50) values of 40.2 and 28.0 μM for LoVo cells and 30.8 and 19.9 μM 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 24h 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 μM 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.
AuthorsHaisheng Zhang, Min Zhang, Linhong Yu, Yan Zhao, Nianwu He, Xingbin Yang
JournalFood and chemical toxicology : an international journal published for the British Industrial Biological Research Association (Food Chem Toxicol) Vol. 50 Issue 5 Pg. 1589-99 (May 2012) ISSN: 1873-6351 [Electronic] England
PMID22310237 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2012 Elsevier Ltd. All rights reserved.
Chemical References
  • Antineoplastic Agents
  • quercetin-5',8-disulfonate
  • Quercetin
Topics
  • Antineoplastic Agents (pharmacology)
  • Breast Neoplasms (pathology)
  • Cell Division (drug effects)
  • Cell Line, Tumor
  • Colonic Neoplasms (pathology)
  • Female
  • Flow Cytometry
  • Humans
  • Quercetin (analogs & derivatives, pharmacology)

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