The Role of Alpha-Glucosidase Inhibitors (Acarbose)

Synthesis of novel α-glucans with potential health benefits through controlled glucose release in the human gastrointestinal tract

“…Many have hypothesized that postprandial hyperglycemia contributes to diabetes complications through damaging the vasculature tissue, such as retinopathy and nephropathy, which is likely why the cardiovascular disease incidence is so highly correlated to poorly controlled diabetes (Ceriello et al 2004;Meigs et al 2002). Even in non-diabetics, a meal high in rapidly digestible starches allows for some postprandial and post-challenge hyperglycemia that may contribute to cardiovascular damage (Hanefeld and Schaper 2007). Poor insulin secretion and decreased insulin sensitivity are key characterizations of type 2 diabetes, as well as progressive beta cell dysfunction (Wallander et al 2005).…”

“…Currently, acarbose is used as a competitive inhibitor affecting the activities of enzymes in the human digestive tract, i.e. pancreatic a-amylase and various a-glucosidases (Hanefeld and Schaper 2007;Martin and Montgomery 1996). While enzyme inhibition is one method clinically used to slow the glucose release of carbohydrate digestion, as mentioned, this review will examine the potential to modulate glycemic response through the use of a-glucans with structures and glycosidic linkages that do not allow for immediate hydrolysis.…”

“…Acarbose is produced by some Gram-positive bacteria and is a potent selective inhibitor of the C-terminal a-glucosidase subunits (Lee et al 2012). 1-Deoxynojirimycin which is found in the mulberry plant bark and root was shown to be a potent competitive MGAM inhibitor (Breitmeier, G€ unther, and Heymann 1997), but against which subunit has yet to be determined (Breitmeier, G€ unther, and Heymann 1997;Hanefeld and Schaper 2007;Liu et al 2015;Martin and Montgomery 1996). The glucoamylase C-terminal MGAM subunit acts very rapidly on smaller starch units and its inhibition could potentially be used to slow the rate of hydrolysis on longer chain maltooligosaccharides.…”

Effect of Acarbose on Vascular Disease in Patients with Abnormal Glucose Tolerance

“…An appropriate agent of microbial origin (culture filtrates or actinoplanes)-acarbose-was described in 1977 [9,10] and came out on the market in 1990. Two other α-glucosidase inhibitors, miglitol and voglibose developed later, are only used in Japan and a few other countries without study evidence for effects on cardiovascular events [11]. In the last years other 'prandial' oral antidiabetics have been introduced such as short acting insulin secretagogues repaglinide and nateglinide, GLP1 receptor antagonists (exenatide, liraglutide) and incretin enhancers (DPP IV inhibitors) to meet the needs of better postprandial glucose control [7].…”

Medium optimization for acarbose production by Actinoplanes sp. A56 using the response surface methodology

“…Acarbose is a pseudo-oligosaccharide, which acts as a competitive -glucosidase inhibitor. Because it is hardly digestible and generally have no detectable toxicity (Wehmeier and Piepersberg, 2004), acarbose has widely been used in the therapy of type II diabetes (non-insulindependent), which could better control blood sugar contents of patients after meals (Hanefeld et al, 2008;Kihara et al, 1997;Hanefeld, 2007).…”