title: The antihyperglycaemic activity of berberine arises from a decrease of glucose absorption.
abstract: The mechanism of action of berberine as an antihyperglycaemic agent was investigated in the Caco-2 cell line. Berberine was found to effectively inhibit the activity of disaccharidases in Caco-2 cells. It also decreased sucrase activity after preincubation with Caco-2 cells for 72 hours. However gluconeogenesis and glucose consumption of Caco-2 cells were not influenced. 2-Deoxyglucose transporting through Caco-2 cell monolayers was decreased by berberine but the effect was not statistically significant. These results suggest that the antihyperglycaemic activity of berberine is at least partly due to its ability to inhibit alpha-glucosidase and decrease glucose transport through the intestinal epithelium.
authors.affiliation: Center of Pharmacokinetics, China Pharmaceutical University, Nanjing, China.
authors.forename: Guo-Yu
authors.initials: GY
authors.lastname: Pan
authors.forename: Zhi-Jiang
authors.initials: ZJ
authors.lastname: Huang
authors.forename: Guang-Ji
authors.initials: GJ
authors.lastname: Wang
authors.forename: J Paul
authors.initials: JP
authors.lastname: Fawcett
authors.forename: Xiao-Dong
authors.initials: XD
authors.lastname: Liu
authors.forename: Xiao-Chen
authors.initials: XC
authors.lastname: Zhao
authors.forename: Jian-Guo
authors.initials: JG
authors.lastname: Sun
authors.forename: Yuan-Yuan
authors.initials: YY
authors.lastname: Xie
mesh_terms: D001599:Berberine / Q000494:pharmacology*; D018938:Caco-2 Cells; D004789:Enzyme Activation; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005943:Gluconeogenesis; D005947:Glucose / Q000096:biosynthesis / Q000378:metabolism*; D065089:Glycoside Hydrolase Inhibitors; D006801:Humans; D006943:Hyperglycemia / Q000517:prevention & control*; D007004:Hypoglycemic Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D007408:Intestinal Absorption; D013393:Sucrase / Q000378:metabolism; D000520:alpha-Glucosidases / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D065089:Glycoside Hydrolase Inhibitors; D007004:Hypoglycemic Agents; D001599:Berberine; D000520:alpha-Glucosidases; D013393:Sucrase; D005947:Glucose