The In Vitro Anti-tumor Efficiency Of Curcumin Analogues And Their Abilities To Induce Tumor Cell Apoptosis

The rhizome of turmeric (Curcuma longa Linn.) has long been used in traditional Asian medicine to treat gastrointestinal upset, arthritic pain and "low energy." Laboratory and animal research has demonstrated anti-inflammatory, antioxidant and anti-cancer properties of its constituent curcumin. However, due to its water insolubility and low bioavailability in vivo, the application of curcumin as a potential anti-tumor drug has been strongly impeded.In order to find more active compounds with improved physicalchemical properties, we synthesized four curcumin analogues using curcumin as the lead compound, i.e., curcumin acid derivative, curcumin glycol derivative, eurcumin glycerol derivative, and sodium curcuminate derivative. Additionally, their in vitro anti-tumor activities, their influence on cell cycle and their ability to induce apoptosis have been evaluated on six tumor cell lines, such as HepG2, SMMC-7721, Hela, CT26, A549 and Skov3.Our study revealed that: the synthesized curcumin analogues had tumor inhibition effects and induced the apoptosis of the above tumor cell strains, with varied degrees; their tumor inhibition rates were both concentration- and time- dependent. However, their tumor inhibition effects and the ability to induce cell apoptosis proved relatively poorer than curcumin itself, probably due to the blockage of active group - phenolic hydroxide.Since the synthesized analogues showed improved physical and chemical properties, with certain in vitro anti-tumor efficiencies, our study actually provided a new way for the development of novel anticancer compound with high efficiency and low toxicity.