title: Xanthohumol, a prenylated chalcone from beer hops, acts as an α-glucosidase inhibitor in vitro.
abstract: Xanthohumol (XN) is a unique prenylated flavonoid in hops (Humulus lupulus L.) and beer. XN alleviates hyperglycemia and has potential usage in the treatment of type 2 diabetes. In the present study, a series of in vitro experiments were performed to investigate whether XN was an effective inhibitor of α-glucosidase. The results showed that XN inhibited α-glucosidase in a reversible and noncompetitive manner, with an IC50 value of 8.8 μM and that XN inhibited the release of glucose from the maltose in the apical side of the Caco-2 cell monolayer. Fluorescence and circular dichroism spectra results indicated that XN directly bound to α-glucosidase and induced minor conformational changes of the enzyme. These results demonstrated that XN is a promising α-glucosidase inhibitor, which therefore could be used as functional food to alleviate postprandial hyperglycemia and as a potential candidate for the development of an antidiabetic agent.
authors.affiliation: Key Laboratory of Marine Drugs, Ministry of Education, School of Medicine and Pharmacy, Ocean University of China , Qingdao 266003, China.
authors.forename: Ming
authors.initials: M
authors.lastname: Liu
authors.forename: Hua
authors.initials: H
authors.lastname: Yin
authors.forename: Ge
authors.initials: G
authors.lastname: Liu
authors.forename: Jianjun
authors.initials: J
authors.lastname: Dong
authors.forename: Zhonghua
authors.initials: Z
authors.lastname: Qian
authors.forename: Jinlai
authors.initials: J
authors.lastname: Miao
mesh_terms: D001515:Beer / Q000032:analysis*; D018938:Caco-2 Cells; D002599:Chalcone / Q000737:chemistry*; D005419:Flavonoids / Q000494:pharmacology*; D005947:Glucose / Q000378:metabolism; D065089:Glycoside Hydrolase Inhibitors / Q000494:pharmacology*; D006801:Humans; D027582:Humulus / Q000737:chemistry*; D006943:Hyperglycemia / Q000188:drug therapy; D007004:Hypoglycemic Agents / Q000494:pharmacology; D054876:Prenylation; D011427:Propiophenones / Q000494:pharmacology*; D000520:alpha-Glucosidases / Q000378:metabolism
chemical_list: D005419:Flavonoids; D065089:Glycoside Hydrolase Inhibitors; D007004:Hypoglycemic Agents; D011427:Propiophenones; D002599:Chalcone; D000520:alpha-Glucosidases; D005947:Glucose; C104536:xanthohumol