2,2′-Methoxyl Mono-Carbonyl Curcumin Promotes HEPG2 Cell Apoptosis and ROS Generation.

Cancer, characterized by uncontrolled tumor cells growth, is a highly fatal disease worldwide. Molecular simplification of natural compounds is a modern and less costly strategy in drug discovery. Mono-carbonyl analogs of curcumin (MACs) are curcumin-originated anticancer agents possessing potent bioactivity in vitro. In this work, the cytotoxicity of methoxyl-substituted MACs toward HepG2 cells was evaluated by MTT assay. Among these, 2,2′-methoxyl MAC exhibited the most potent anti-proliferation activity, and it could promote the ROS production, redox imbalance, lipid peroxidation, the loss of mitochondrial membrane potential, and ultimately lead to cell cycle arrest and apoptosis of HepG2 cells. These results suggest that enhancing ROS generation may be a potent strategy for the expansion of new anti-hepatocellular carcinoma agents. [ABSTRACT FROM AUTHOR]