Anti-proliferative properties of prenylated flavonoids from hops (Humulus lupulus L.) in human prostate cancer cell lines

Abstract 

Chalcones xanthohumol (X) and desmethylxanthohumol (DMX), present in hops (Humulus lupulus L.), and the corresponding flavanones isoxanthohumol (IX, from X), 8-prenylnaringenin (8-PN, from DMX), and 6-prenylnaringenin (6-PN, from DMX), have been examined in vitro for their anti-proliferative activity on human prostate cancer cells PC-3 and DU145. X proved to be the most active compound in inhibiting the growth of the cell lines with IC₅₀ values of 12.3±1.1μM for DU145 and 13.2±1.1μM for PC-3. 6-PN was the second most active growth inhibitor, particularly in PC-3 cells (IC₅₀ of 18.4±1.2μM). 8-PN, a highly potent phytoestrogen, exhibited pronounced anti-proliferative effects on PC-3 and DU145 (IC₅₀ of 33.5±1.0 and 43.1±1.2μM, respectively), and IX gave comparable activities (IC₅₀ of 45.2±1.1μM for PC-3 and 47.4±1.1μM for DU145). DMX was the least active compound. It was evidenced for the first time that this family of prenylated flavonoids from hops effectively inhibits proliferation of prostate cancer cells in vitro.

Keywords: Prenylflavonoids, Humulus lupulus L., Prostate cancer cells, Antiproliferative activity