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DOI: 10.1055/s-0036-1578696
A Phyllanthusmin Derivative Exhibiting Intracellular Effects On Reactive Oxygen Species
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.