In vitro growth inhibition of human cancer cells by novel honokiol analogs

Bioorg Med Chem. 2012 May 15;20(10):3202-11. doi: 10.1016/j.bmc.2012.03.062. Epub 2012 Apr 3.

Abstract

Honokiol possesses many pharmacological activities including anti-cancer properties. Here in, we designed and synthesized honokiol analogs that block major honokiol metabolic pathway which may enhance their effectiveness. We studied their cytotoxicity in human cancer cells and evaluated possible mechanism of cell cycle arrest. Two analogs, namely 2 and 4, showed much higher growth inhibitory activity in A549 human lung cancer cells and significant increase of cell population in the G0-G1 phase. Further elucidation of the inhibition mechanism on cell cycle showed that analogs 2 and 4 inhibit both CDK1 and cyclin B1 protien levels in A549 cells.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents, Phytogenic / chemical synthesis
  • Antineoplastic Agents, Phytogenic / chemistry
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Biphenyl Compounds / chemistry*
  • Biphenyl Compounds / pharmacology*
  • Blotting, Western
  • Cell Cycle / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Humans
  • Inhibitory Concentration 50
  • Lignans / chemistry*
  • Lignans / pharmacology*
  • Lung Neoplasms / pathology
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents, Phytogenic
  • Biphenyl Compounds
  • Lignans
  • honokiol