Planta Med 2016; 82 - PB48
DOI: 10.1055/s-0036-1578696

A Phyllanthusmin Derivative Exhibiting Intracellular Effects On Reactive Oxygen Species

Z Tang 1, JL Woodard 1, AC Huntsman 1, Y Ren 1, JR Fuchs 1, AD Kinghorn 1, EJ Carcache de Blanco 1
  • 1College of Pharmacy, The Ohio State University Columbus, Ohio 43210

Natural products always are a major source for cancer drug research and development. Several phyllanthusmin analogues isolated from Phyllanthus poilanei, collected in Vietnam, exhibited significant cytotoxic activity in HT-29 colon cancer cells, particularly phyllanthusmin D (0.17µM). Twelve new derivatives were synthesized to optimize cytotoxic activity and anticancer drug-like properties. After testing the new derivatives against a panel of cancer cells, derivative Phy-14 exhibited a high cytotoxic potential against DU145 prostate cancer cell (ED50 0.27µM). Phy-14 also exhibited dose-dependent Reactive Oxygen Species (ROS) intracellular amplification in DU145 cells. H2O2 and Vitamin C were used as control [1]. Additional studies on the potential mechanism of action are ongoing, and will include a thorough analysis of the oxidative pathway.

Reference: [1] Kim J-A, Lau EK, et al. (2010) Anticancer Research, 30: 3295 – 3000.