Abstract
<p>Twenty eight xanthone derivatives were designed and docked into the N-terminal catalytic domain of maltase-glucoamylase (ntMGAM) by considering Miglitol as standard drug. Most of the molecules showed excellent docking scores and docking interaction as compared to the binding cavity of the standard molecule. The five best scoring ligands were synthesized and characterized by a number of analytical and spectroscopic techniques. The molecules were screened for the <em>in vivo</em> antidiabetic activity in streptozotocin (STZ) induced diabetic animal model in Wistar rats. Compound P4 showed the most prominent inhibition among others. The synthesized compounds reported significant (p&lt; 0.01) effect of lowering glucose levels in the blood compared to miglitol as a standard α-glucosidase inhibitor.</p><p><strong>Video clip</strong></p><p>Induction of diabetes: </p>
Highlights
Glucosidase catalyzes especially hydrolyses the carbohydrates to free glucose unit in blood in the final step of carbohydrate metabolism
Type 2 diabetes mellitus is major health problem. In this manuscript we present an approach to control blood glucose levels in individuals with type 2 diabetes by targeting maltase-glucoamylase and intestinal glucosidases using some novel xanthone alpha-glucosidase inhibitors
One of the intestinal glucosidases targeted the N-terminal catalytic domain of maltase-glucoamylase which is responsible for the hydrolysis of terminal starch products into glucose (Sim et al, 2010)
Summary
Glucosidase catalyzes especially hydrolyses the carbohydrates to free glucose unit in blood in the final step of carbohydrate metabolism. Glucosidase causes hydrolysis of and glycosidic linkages of carbohydrates, they are -glucosidase and -glucosidase (Heightman et al, 1999). Since the discovery of acarbose, first -glucosidase inhibitor lots of synthetic (Xu et al, 2007; Tanabe et al, 2007; Liu et al, 2007) and natural molecules (Luo et al, 2007; Saludes et al, 2007; Du et al, 2006) reported for the management of type 2 diabetes, but continuous administration of these agents causing adverse effects like diarrhea, abdominal discomfort, flatulence (Campbell et al, 2000), and hepatotoxicity (Hsiao et al, 2006)
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