β-Aescin shows potent antiproliferative activity in osteosarcoma cells by inducing autophagy, ROS generation and mitochondrial membrane potential loss.

Purpose: Osteosarcoma is one of the frequent bone tumor affecting mainly children and is associated with considerable mortality. The limited availability of anticancer drugs and less efficacious treatment options have led to poor survival rates of patients with osteosarcoma. Therefore, there is need to look for more viable treatment options and against this backdrop, natural products may prove handy. Therefore the aim of the present study was to evaluate the anticancer activity of a natural product of plant origin, β-aescin, against U2OS human osteosarcoma cells.

Methods: U205 human osteosarcoma cell line was used in this study. Antiproliferative activity was determined by MTT assay. Reactive oxygen species (ROS) and mitochondrial membrane potential (MMP) were evaluated by flow cytometry. Autophagy was detected by monodansylcadaverine (MDC) staining and immunofluorescence. Protein expression was examined by western blotting.

Results: The results indicated that β-aescin showed significant anticancer activity against U2OS human osteosarcoma cells and exhibited an IC50 of 40 μM. β-aescin treatment caused significant increase in ROS and decrease in the MMP. The anticancer effect of β-aescin was found to be due mainly to autophagic cell death as evidenced from MDC staining and immunofluorescence. Moreover, β-aescin caused significant increase in the expression levels of LC3- II protein in U2OS osteosarcoma cells in a time and dosedependent manner.

Conclusion: Taken together we propose that β-aescin may prove a lead molecule in the management of osteosarcoma and deserves further research efforts.