Antitumor activities of quercetin and quercetin-5',8-disulfonate in human colon and breast cancer cell lines.
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.
College of Food Engineering and Nutritional Science, Key Laboratory of Ministry of Education for Medicinal Resource and Natural Pharmaceutical Chemistry, Shaanxi Normal University, Xi'an 710062, China.
Haisheng
H
Zhang
Min
M
Zhang
Linhong
L
Yu
Yan
Y
Zhao
Nianwu
N
He
Xingbin
X
Yang
D000970:Antineoplastic Agents / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000473:pathology*; D002455:Cell Division / Q000187:drug effects; D045744:Cell Line, Tumor; D003110:Colonic Neoplasms / Q000473:pathology*; D005260:Female; D005434:Flow Cytometry; D006801:Humans; D011794:Quercetin / Q000031:analogs & derivatives* / Q000494:pharmacology*
D000970:Antineoplastic Agents; C574501:quercetin-5',8-disulfonate; D011794:Quercetin