title: Xanthohumol, a prenylated chalcone from Humulus lupulus L., inhibits cholesteryl ester transfer protein.
abstract: High density lipoprotein (HDL)-cholesterol levels are correlated with a low risk of atherosclerosis. The inhibition of cholesteryl ester transfer protein (CETP), which catalyses cholesterol transfer between lipoproteins, leads to an increase in HDL-cholesterol and is expected to be the next anti-atherogenic target. This study revealed that xanthohumol, a prenylated chalcone, showed the highest inhibition against CETP from screening of natural products in various plants. We investigated the inhibitory activity of some chalcones and flavanones. Naringenin chalcone showed weak CETP inhibition compared with xanthohumol. In addition, isoxanthohumol and naringenin drastically decreased the inhibitory activity. These results suggest that the prenyl group and chalcone structure of xanthohumol were responsible for the CETP inhibitory activity.
authors.affiliation: Frontier Laboratories of Value Creation, Sapporo Breweries Ltd., 10 Okatohme, Yaizu, Shizuoka 425-0013, Japan.
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Hirata
authors.affiliation: Frontier Laboratories of Value Creation, Sapporo Breweries Ltd., 10 Okatohme, Yaizu, Shizuoka 425-0013, Japan.
authors.forename: Koji
authors.initials: K
authors.lastname: Takazumi
authors.affiliation: Frontier Laboratories of Value Creation, Sapporo Breweries Ltd., 10 Okatohme, Yaizu, Shizuoka 425-0013, Japan.
authors.forename: Shuichi
authors.initials: S
authors.lastname: Segawa
authors.affiliation: Frontier Laboratories of Value Creation, Sapporo Breweries Ltd., 10 Okatohme, Yaizu, Shizuoka 425-0013, Japan.
authors.forename: Yukio
authors.initials: Y
authors.lastname: Okada
authors.affiliation: Frontier Laboratories of Value Creation, Sapporo Breweries Ltd., 10 Okatohme, Yaizu, Shizuoka 425-0013, Japan.
authors.forename: Naoyuki
authors.initials: N
authors.lastname: Kobayashi
authors.affiliation: Frontier Laboratories of Value Creation, Sapporo Breweries Ltd., 10 Okatohme, Yaizu, Shizuoka 425-0013, Japan.
authors.forename: Tatsuro
authors.initials: T
authors.lastname: Shigyo
authors.affiliation: Faculty of Health Science, Hokkaido University School of Medicine, Kita 12, Nishi 5, Kita-ku, Sapporo 060-0812, Japan.
authors.forename: Hitoshi
authors.initials: H
authors.lastname: Chiba
mesh_terms: D047188:Chalcones / Q000737:chemistry*; D053480:Cholesterol Ester Transfer Proteins / Q000737:chemistry*; D008076:Cholesterol, HDL / Q000737:chemistry*; D005419:Flavonoids / Q000737:chemistry*; D027582:Humulus / Q000737:chemistry*; D011427:Propiophenones / Q000737:chemistry*
chemical_list: D047188:Chalcones; D053480:Cholesterol Ester Transfer Proteins; D008076:Cholesterol, HDL; D005419:Flavonoids; D011427:Propiophenones; C104536:xanthohumol