title: In vitro investigation of 2',4'-dihydroxy-6'-methoxy-3',5'-dimethylchalcone for glycemic control.
abstract: 2',4'-Dihydroxy-6'-methoxy-3',5'-dimethylchalcone (DMC), a compound isolated and purified from the dried flower buds of Cleistocalyx operculatus (Roxb.) Merr. et Perry (Myrtaceae), was investigated for its glucose control benefits using in vitro methods. DMC showed strong noncompetitive (IC(50) of 43 μM) inhibition of pancreatic α-amylase; it was, however, ineffective against intestinal α-glucosidase. In addition, DMC exhibited remarkable glucose transport inhibition effects in both simulated fasting and fed states in Caco-2 cell monolayers (P < 0.05). Besides, exposure of MIN6 cells to 250 μM H(2)O(2) for 1 h caused a significant viability loss and insulin secretion reduction. Pretreatment of MIN6 cells with DMC for 2 h protected against the H(2)O(2)-induced decrease in glucose-stimulated insulin secretion in a dose-dependent manner and also enhanced the impaired basal insulin secretion. Such effects highlight the therapeutic potential of DMC in the management of hyperglycemia.
authors.affiliation: State Key Laboratory of Bioreactor Engineering, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, People's Republic of China.
authors.forename: Ying-Chun
authors.initials: YC
authors.lastname: Hu
authors.forename: Ying-Di
authors.initials: YD
authors.lastname: Luo
authors.forename: Lin
authors.initials: L
authors.lastname: Li
authors.forename: Manoj Kumar
authors.initials: MK
authors.lastname: Joshi
authors.forename: Yan-Hua
authors.initials: YH
authors.lastname: Lu
mesh_terms: D001786:Blood Glucose / Q000032:analysis*; D018938:Caco-2 Cells; D047188:Chalcones / Q000494:pharmacology*; D006801:Humans; D066298:In Vitro Techniques
chemical_list: C501649:2',4'-dihydroxy-6'-methoxy-3',5'-dimethylchalcone; D001786:Blood Glucose; D047188:Chalcones