Royleanone diterpenoid exhibits potent anticancer effects in LNCaP human prostate carcinoma cells by inducing mitochondrial mediated apoptosis, cell cycle arrest, suppression of cell migration and downregulation of mTOR/PI3K/AKT signalling pathway.

PURPOSE

Prostate cancer is a deadly malignancy and is responsible for significant cancer-related mortality in men. The incidence of prostate cancer is continuously increasing across the globe and the existing treatment options for this disease are limited and associated with a lot of side effects. Therefore there is an urgent need to identify novel and efficient therapeutic agents for the management of prostate cancer. In the current study we evaluated the anticancer activity of royleanone diterpenoid against prostate cancer LNCaP cell line.

METHODS

The anticancer activity of royleanone was determined by CCK8 assay. Apoptosis was detected by acridine orange and ethidium bromide as well as by annexin V/ propidium iodide (PI) staining. Mitochondrial membrane potential (MMP) and cell cycle analysis were investigated by flow cytometry and protein expression by western blotting.

RESULTS

The results showed that royleanone exerts potent anticancer activity on LNCaP prostate cancer cells with an IC50 of 12.5 μM at 48 hrs of incubation. The anticancer activity of royleanone was due to induction of cell cycle arrest and mitochondrial-mediated apoptosis. Moreover, royleanone could also suppress the cell migration potential and inhibited the mTOR/ PI3/AKT signalling pathway in LNCaP prostate cancer cells.

CONCLUSIONS

Taken together, we propose that royleanone could prove to be an important anticancer lead molecule for the treatment and overall management of prostate cancer, provided further in vivo studies are carried out.