A new anticancer ligustrazine derivative,3-hydroxyolea-12-en-28-oicacid-3, 5, 6-trimethylpyrazin-2-methylester (T-OA,C38H58O3N2), was previously reported.It was synthesized via conjugating hepatoprotective and anticancer ingredients of traditional Chinese medicine.We found T-OA exerted its anticancer activity by preventing the expression of nuclear transcription factor NF-κB/p65 and COX-2 in S180 mice.However, the selective cytotoxicity of T-OA on various kinds of cell lines has not been studied sufficiently.In present study, compared with Cisplatin, T-OA was more toxic to human hepatoma cell line Bel-7402 (IC50 =6.36±1.56 μM) than other three cancer cell lines (HeLa,HT-29, BGC-823), and no toxicity was observed toward Madin-Darby canine kidney cell line MDCK (IC50 > 150 μM).The morphological changes of Bel-7402 cells demonstrated that T-OA had an apoptosis-inducing effect which had been substantiated using DAPI staining, AO/EB staining, flow cytometry and mitochondrial membrane potential assay.Combining the immumohistochemical staining, we found T-OA could prevent the expression of NF-κB/p65 and COX-2 in Bel-7402 cells.Both of the proteins have been known to play roles in apoptosis.The result can indicate that T-OA can induce Bel-7402 cells apoptosis by inhibiting the expression of NF-κB/p65 and COX-2.