Acarbose

Acarbose is an oligosaccharide and inhibitor of α-glucosidases (IC₅₀s = 0.16 and 2.9 µM for maltase and sucrase, respectively).¹ It also activates phosphorylase kinase in a cell-free assay when used at a concentration of 250 µM.² Acarbose (40 mg/kg in the diet) decreases urine levels of glucose and glycosylated hemoglobin, as well as glomerular mesangial thickening in a db/db mouse model of diabetic nephropathy.³ It reduces sucrose-induced increases in infarct size as a percentage of the area at risk and serum malondialdehyde (MDA) levels in a mouse model of cardiac ischemia-reperfusion injury induced by coronary artery ligation when administered at a dose of 10 mg/kg.⁴

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1. Natori, Y., Imahori, T., Murakami, K., et al. The synthesis and biological evaluation of 1-C-alkyl-ʟ-arabinoiminofuranoses, a novel class of α-glucosidase inhibitors. Bioorg. Med. Chem. Lett. 21(2), 738-741 (2011).

2. Nadeau, O.W., Liu, W., Boulatnikov, I.G., et al. The glucoamylase inhibitor acarbose is a direct activator of phosphorylase kinase. Biochemistry 49(31), 6505-6507 (2010).

3. Lee, S.M. The effect of chronic α-glycosidase inhibition on diabetic nephropathy in the db/db mouse. Diabetes 31(3), 249-254 (1982).

4. Frantz, S., Calvillo, L., Tillmanns, J., et al. Repetitive postprandial hyperglycemia increases cardiac ischemia/reperfusion injury: Prevention by the α-glucosidase inhibitor acarbose. The FASEB Journal 19(6), 591-593 (2005).