Differential effects of baicalein and its sulfated derivatives in inhibiting proliferation of human breast cancer MCF-7 cells

Chem Biol Interact. 2014 Sep 25:221:99-108. doi: 10.1016/j.cbi.2014.08.003. Epub 2014 Aug 14.

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.

Keywords: Anti-proliferation; Apoptosis; Baicalein-8-sodium sulfonate; Cell cycle; Cytotoxicity; MCF-7 cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apoptosis / drug effects
  • Breast Neoplasms / drug therapy
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Female
  • Flavanones / chemistry
  • Flavanones / pharmacology*
  • Flow Cytometry
  • Humans
  • MCF-7 Cells
  • Reactive Oxygen Species

Substances

  • Flavanones
  • Reactive Oxygen Species
  • baicalein