The class
Hop-derived xanthohumol prevents atherosclerosis in CETP-transgenic mice by inhibiting CETP and enriching HDL with apoE (PLoS One 2012)
Original title: Xanthohumol prevents atherosclerosis by reducing arterial cholesterol content via CETP and apolipoprotein E in CETP-transgenic mice
Xanthohumol, a compound from hops thought to inhibit CETP, was tested for anti-atherosclerotic effects in CETP-transgenic and wild-type C57BL/6N mice fed a high-cholesterol diet with or without 0.05 percent xanthohumol for 18 weeks. In CETP-transgenic mice, xanthohumol significantly decreased accumulated cholesterol in the aortic arch and increased HDL cholesterol compared with controls, with no significant effect in wild-type mice. CETP activity was significantly decreased by xanthohumol in the transgenic mice and inversely correlated with HDL-C (P less than 0.05), and serum and HDL-fraction apolipoprotein E was enriched after xanthohumol treatment. The authors conclude xanthohumol prevents cholesterol accumulation in atherogenic arterial regions through CETP inhibition, which enhances apoE-rich HDL and reverse cholesterol transport.
Original abstract
Background: Xanthohumol is expected to be a potent anti-atherosclerotic agent due to its inhibition of cholesteryl ester transfer protein (CETP). In this study, we hypothesized that xanthohumol prevents atherosclerosis in vivo and used CETP-transgenic mice (CETP-Tg mice) to evaluate xanthohumol as a functional agent.
Methodology/Principal Findings: Two strains of mice, CETP-Tg and C57BL/6N (wild-type), were fed a high cholesterol diet with or without 0.05% (w/w) xanthohumol ad libitum for 18 weeks. In CETP-Tg mice, xanthohumol significantly decreased accumulated cholesterol in the aortic arch and increased HDL cholesterol (HDL-C) when compared to the control group (without xanthohumol). Xanthohumol had no significant effect in wild-type mice. CETP activity was significantly decreased after xanthohumol addition in CETP-Tg mice compared with the control group and it inversely correlated with HDL-C (%) (P<0.05). Furthermore, apolipoprotein E (apoE) was enriched in serum and the HDL-fraction in CETP-Tg mice after xanthohumol addition, suggesting that xanthohumol ameliorates reverse cholesterol transport via apoE-rich HDL resulting from CETP inhibition.
Conclusions: Our results suggest xanthohumol prevents cholesterol accumulation in atherogenic regions by HDL-C metabolism via CETP inhibition leading to apoE enhancement.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.