Acarbose (BAY g 5421) is a hypoglycemic agent that is an inhibitor of orally active alpha-glucosidase (IC50=11 nM). Acarbose enhances the hypoglycemic effect of sulfonylureas or insulin.

sucrose (4 g/l):3.2 μg/ml, Caco-2 cells:5 μM, maltose (1 g/l):36 μg/ml, maltose (2 g/l):57 μg/ml, alpha-glucosidase:11 nM, α-glucosidase:2.154 µg/mL

METHODS: A7r5 cells pretreated with TNF-α were treated with Acarbose (1, 2, and 3 μM) and the expression levels of target proteins were detected by Western Blot.
RESULTS: Acarbose decreased the expression of β-galactosidase and Ras and increased the expression of p-AMPK in a dose-dependent manner. [1]

METHODS: To study the hypoglycemic effect of Acarbose, rats were treated with Acarbose (30, 60 mg/kg) by gavage once daily for 8 weeks.
RESULTS: Acarbose reduced fasting glucose and modulated glucose tolerance without weight loss in DM rats. Acarbose significantly inhibited serum IL6 and TNF-α in DM rats. [2]
METHODS: To study the effect of Acarbose on atherosclerosis, rabbits were fed Acarbose (2.5-5.0 mg/kg) for 25 weeks.
RESULTS: Acarbose significantly and dose-dependent reduced the intensity of IL-6, TNF-α and iNOS staining, and significantly increased the intensity of p-AMPK staining in the neointima. Acarbose significantly and dose-dependent reduced neointimal Ras and β-galactosidase expression in HCD-fed rabbits without weight loss. [1]

Cell viability is determined using the MTT assay. Cells are seeded in 24-well culture plates at a density of 2×104 cells/well, incubated for 48 h, treated with acarbose at varying concentrations (0.5, 1.0, 2.0, 3.0, and 5.0 μM) for 24 h; or pre-treated with TNF-α (20 ng/mL) for either 24 h or 48 h to evaluate the dose-dependent effects of acarbose on VSMC growth and viability, cultured with 0.5 mg/mL MTT at 37°C in a humidified atmosphere of 5% CO2 for another 4 h, and solubilized with isopropanol. The viable cell number varies directly with the concentration of formazan product measured spectrophotometrically at 563 nm.