Xanthohumol, a prenylated chalcone from Humulus lupulus L., inhibits cholesteryl ester transfer protein

► Inhibition of CETP is expected to alleviate atherosclerosis by its affect on HDL-cholesterol. ► We demonstrated that hop-derived xanthohumol had a potent CTEP inhibitory property. ► Its IC50 value was approximately 31.2 μg/ml (88.0 μM). ► Its inhibitory mechanism for the CETP reaction was mixed, non competitive. ► Its chalcone structure and prenyl group were essential for its CETP inhibitory action.