ObjectiveTo investigate the effects of celastrol on the growth and apoptosis of huamn hepatoma SMMC-7721 cells, and investigate its preliminary action mechansim. MethodsSMMC-7721 cells were cultured in vitro, CCK-8 assay and Annexin V-FITC/PI staining method were conducted to investigate the effects of celastrol on the growth and apoptosis of huamn hepatoma SMMC-7721 cells after the cells were treated with drugs, and then the Caspase-3 activity and NF-κB protein expression were determined by Caspase-3 activity determination kit and Western blot. Huamn hepatoma SMMC-7721 cells transplantation tumor models in nude mice were established and the effect of celastrol on the growth of transplantation tumor were observed. ResultsCelastrol could inhibit the SMMC-7721 cells growth in a dose and time dependent manner. Annexin-V/PI staining showed that SMMC-7721 cells were induced to death with the concentration increasing of celastrol. Caspase-3 activity was measured after treatment with celastrol and the results indicated that the activity of caspase-3 was significantly enhanced. Western blot experiments showed that the expression of NF-κB protein decreased in a time-dependent manner after treatment with celastrol. Celastrol could inhibit SMMC-7721 cells transplantation tumor growth in nude mice. ConclusionsCelastrol could inhibit the proliferation of human hepatoma SMMC-7721 cells and induces apoptosis, and inhibit SMMC-7721 cell transplantation tumor growth in nude mice. Celastrol induce apoptosis of SMMC-7721 cells might through activating Caspase-3 pathway and NF-κB pathway.