Objective: To explore the apoptosis of human
gastric cancer MGC-803 cells induced by
toosendanin(TSN) and its mechanism. Methods: The human
gastric cancer MGC-803 cells were divided into 5 groups, each group was set with 3 replicate.
Fluorouracil (5-FU) and 0 nmol/L
toosendanin (TSN) were used as positive control and negative control, respectively. The other three groups were treated with
toosendanin at the final concentrations of 30, 50, and 70 nmol/L, respectively. After 48 h of treatment with
toosendanin, the morphology of the cells were observed under
laser confocal microscopy. Flow cytometry was used to detect the mitochondrial membrane potential, and
enzyme-labeled assays were used to detect the activities of
Caspase-3 and
Caspase-9. The
mRNA and
protein levels of Bcl-2, Bax, Cyt c and APAF-1 were measured by qRT-PCR and Western blot. Results: Compared with the 0 nmol/L TSN group, after the human
gastric cancer MGC-803 cells were treated with
toosendanin at the concentrations of 30, 50, and 70 nmol/L for 48 h, the cell volume shrinkage, nucleus cleavage and
chromatin morphological changes were observed under the microscope. The activities of
Caspase-3 and
Caspase-9 were increased significantly (P<0.05), while the mitochondrial membrane potential was decreased significantly (P<0.05). In addition, the
mRNA and
protein expression levels of Bax, Cyt c and APAF-1 were increased significantly (P<0.05), while the
mRNA and
protein expression levels of Bcl-2 were decreased significantly (P<0.05). Conclusion:
Toosendanin up-regulates the expressions of Bax, Cyt c and APAF-1, down-regulates the expression of Bcl-2 gene, enhances the activities of
caspase-3 and
caspase-9, and induces the apoptosis of human
gastric cancer MGC-803 cells.