The Effects Of Benzotriazole Derivatives On Tumour Cells

Benzotriazole compounds have been found to show extensive biological activities.many of them have been developed and used as fungicides, plant growth regulatorsand medicine,and also have been shown to be able to induce growth inhibition incancer cells.In present study, we synthesized eight bioactive benzotriazole derivatives and theirstructures were confirmed by means of ~1HNMR, IR determination, of which onecompound Benzoic acid 1-benzotriazol-1-ylmethyl-2-(4-methoxy-phenyl)-2-oxo- ethylester (C8) was selected. It was demonstrated that C8 could significantly inhibitproliferation of cultured hepatocarcinoma BEL-7402 cancer cells in a dose- andtime-dependent manner. Treatment with C8 resulted in generation of reactive oxygenspecies (ROS), disruption of mitochondrial membrane potential (Δψm), DNAfragmentation, and apoptosis in BEL -7402 cells. The results suggested thatC8-induces cells growth inhibition and apoptosis of BEL -7402 cells may be throughmodulation of mitochondrial functions regulated by ROS. It seems that collapse ofΔψm prior to intracellular ROS arise during the apoptotic process in our experimentalsystem. However, disruption of mitochondrial membrane potential can further augmentROS production and amplify an apoptotic stimulus.C8 also induce obvious growth inhibition in human breast cancer cells MCF-7and rat breast cancer cells 4T-1. Treatment with C8 resulted in generation of reactiveoxygen species (ROS), disruption of mitochondrial membrane potential in these cells,But no DNA-Ladder.It form specifically length DNA fragmentation.Significantly, C8 could induce obvious growth inhibition and apoptosis in cancer cells,which may be a forceful evidence for anti-cancer of benzotriazole compounds.