Compounds Exhibiting Anti-Proliferative, Apoptosis-Inducing, and Demethylating Effects on Prostate Cancer Cells.

(AS) is distributed in Korea, Japan, China, and Russia and has reported anti-oxidant, anti-inflammatory, and reducing activities on atopic dermatitis-like skin lesions, along with other beneficial health properties. In the present study, we tried to prove the cancer-preventive activity against prostate cancer. The extracted and isolated compounds, oregonin (), hirsutenone (), and hirsutanonol (), which were isolated from AS, were tested for anti-proliferative activity. To do this, we used the MTT assay; NF-κB inhibitory activity, using Western blotting; apoptosis-inducing activity using flow cytometry; DNA methylation activity, using methylation-specific polymerase chain reaction in androgen-dependent (LNCaP) and androgen-independent (PC-3) prostate cancer cell lines. The compounds (-) showed potent anti-proliferative activity against both prostate cancer cell lines. Hirsutenone () exhibited the strongest NF-κB inhibitory and apoptosis-inducing activities compared with oregonin () and hirsutanonol (). DNA methylation activity, which was assessed for hirsutenone (), revealed a concentration-dependent enhancement of the unmethylated DNA content and a reduction in the methylated DNA content in both PC-3 and LNCaP cells. Overall, these findings suggest that hirsutenone (), when isolated from AS, may be a potential agent for preventing the development or progression of prostate cancer.