Monascuspiloin (Monascinol) exhibits anti-androgenic activity with an IC50 of 7 µM. Monascuspiloin inhibits viability of PC-3 and LNCaP with IC50 of 45 and 47 µM. Monascuspiloin induces apoptosis in LNCaP through inhibition of Akt/mTOR signaling pathway, induces autophagy through activation AMPK signaling pathway and arrest cell cycle at G2/M phase in PC-3. Monascuspiloin exhibits antitumor efficacy in mice[1][2].