title: Differential effects of baicalein and its sulfated derivatives in inhibiting proliferation of human breast cancer MCF-7 cells.
abstract: This study was to investigate the anticancer effects of baicalein (Bai) and its two sulfated derivatives, namely baicalein-7-O-sulfate (BoS) and baicalein-8-sodium sulfonate (BcS). BcS was shown to exhibit stronger growth inhibition against human breast cancer MCF-7 cells, compared with structurally related Bai and BoS, where IC50 values of BoS, Bai and BcS were 97.7, 68.3 and 30.4μM, respectively. BoS, Bai and BcS were further shown to mediate the cell-cycle arrest principally in G0/G1-phase within 12h of treatment with MCF-7 cells, and after 12h, they arrested principally in S-phase. It was also found that 17.7%, 44.9% and 70.5% of MCF-7 cells entered the early phase of apoptosis when treated with 200μM BoS, Bai and BcS for 24h, followed by an intracellular ROS generation. BcS displays strong antitumor effect through ROS-dependent apoptosis pathway in MCF-7 cells, and has promising potential to be developed as an antitumor compound.
authors.affiliation: Key Laboratory of Ministry of Education for Medicinal Resource and Natural Pharmaceutical Chemistry, College of Food Engineering and Nutritional Science, Shaanxi Normal University, Xi'an 710062, China.
authors.forename: Ning
authors.initials: N
authors.lastname: Wang
authors.affiliation: Key Laboratory of Ministry of Education for Medicinal Resource and Natural Pharmaceutical Chemistry, College of Food Engineering and Nutritional Science, Shaanxi Normal University, Xi'an 710062, China.
authors.forename: Daoyuan
authors.initials: D
authors.lastname: Ren
authors.affiliation: Key Laboratory of Ministry of Education for Medicinal Resource and Natural Pharmaceutical Chemistry, College of Food Engineering and Nutritional Science, Shaanxi Normal University, Xi'an 710062, China.
authors.forename: Shan
authors.initials: S
authors.lastname: Deng
authors.affiliation: Key Laboratory of Ministry of Education for Medicinal Resource and Natural Pharmaceutical Chemistry, College of Food Engineering and Nutritional Science, Shaanxi Normal University, Xi'an 710062, China. Electronic address: xbyang@snnu.edu.cn.
authors.forename: Xingbin
authors.initials: X
authors.lastname: Yang
mesh_terms: D017209:Apoptosis / Q000187:drug effects; D001943:Breast Neoplasms / Q000188:drug therapy; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D005260:Female; D044950:Flavanones / Q000737:chemistry / Q000494:pharmacology*; D005434:Flow Cytometry; D006801:Humans; D061986:MCF-7 Cells; D017382:Reactive Oxygen Species
chemical_list: D044950:Flavanones; D017382:Reactive Oxygen Species; C006680:baicalein
keywords: Anti-proliferation; Apoptosis; Baicalein-8-sodium sulfonate; Cell cycle; Cytotoxicity; MCF-7 cells