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Acarbose (BAY g 5421) sulfate, antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose sulfate can potentiate the hypoglycemic effects of sulfonylureas or insulin[1][2][3]. | [in vivo]
Acarbose (300 mg/60 kg body weight) decreases the fasting blood glucose, and regulates the glucose tolerance of DM rats without body weight loss. Acarbose significantly suppresses serum IL6 and TNF-α in DM rats[1]. Acarbose (2.5 and 5.0?mg/kg) significantly and dose-dependently decreases the intensity of neointimal IL-6, TNF-α, and iNOS staining, and significantly increases the intensity of neointimal p-AMPK staining. Acarbose (2.5 and 5.0?mg/kg) significantly and dose-dependently decreases neointimal Ras and β-galactosidase expression in HCD-fed rabbits without body weight loss[2]. | [References]
[1] Hanefeld M, et al. Acarbose: oral anti-diabetes drug with additional cardiovascular benefits [published correction appears in Expert Rev Cardiovasc Ther. 2009 Mar;7(3):330]. Expert Rev Cardiovasc Ther. 2008;6(2):153-163. DOI:10.1586/14779072.6.2.153
[2] Yee HS, et al. A review of the safety and efficacy of acarbose in diabetes mellitus. Pharmacotherapy. 1996;16(5):792-805. PMID:8888075
[3] Oki T, et al. Evaluation of alpha-glucosidase inhibition by using an immobilized assay system. Biol Pharm Bull. 2000;23(9):1084-1087. DOI:10.1248/bpb.23.1084
[4] Zhang Q, et al. Acarbose Reduces Blood Glucose by Activating miR-10a-5p and miR-664 in Diabetic Rats. PLoS One. 2013 Nov 18;8(11):e79697. DOI:10.1371/journal.pone.0079697
[5] Chan KC, et al. Pleiotropic effects of acarbose on atherosclerosis development in rabbits are mediated via upregulating AMPK signals. Sci Rep. 2016 Dec 7;6:3864 DOI:10.1038/srep38642 |
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