Glucose 3-glucosidase

Acarbose is a nonabsorbable a-glucosidase inhibitor which blocks the digestion of starch, sucrose, and maltose. The digestion of complex carbohydrates is delayed and occurs throughout the small intestine rather than in the upper part of the jejunum. Absorption of glucose and other monosaccharides is not affected. Acarbose is adrninistered orally three times a day and chewed with the first mouthful of food. 

Amygdalin Glucosidase Glucose, Benzaldehyde, CN- NaH2P04 pH 6.4 Cyanide 10 2 10"5 M... 

When a-glucosidase activity is inhibited, carbohydrate digestion is prolonged and takes place further along the intestinal tract. This in turn delays and spreads the period of glucose absorption, which reduces the extent of the postprandial rise in blood glucose concentrations. The effectiveness of a-glucosidase inhibitors is dq en-dent on the consumption of a meal rich in complex carbohydrate. 

Acarbose and Miglitol These agents are specific inhibitors of intestinal glucosidases and reduce the conversion of sucrose and starch to glucose. Their main effect is a delay, not a complete inhibition, of the absorption of carbohydrates. Postprandial blood sugar excursions are effectively reduced. Because a small portion of the carbohydrates enters the colon, their microbial degradation frequently causes flatulence or... 

Inhibition of o-Glucosidase Aj from Aspergillus wentii and / D-Gluco idase B (Ref. 51) from Bitter Almonds by Basic and Non-Basic Derivatives of D-Glucose... 

A different type of reactive bromo compound having a moderate resemblance to hexoses is represented by the bromoconduritols B (40) and F (41), named after the respective parent tetrahydroxycyclohexene. Even thou their hydroxylation pattern resembles that of D-glucose, only a few examples of D-glucosidase inhibition have been reported. The first was a-D-glucosi-dase from yeast, which is inhibited by bromoconduritol B (formerly called bromoconduritol A), having ki(max)/Kj 69,000 M" min", by alkylation of a histidine residue at the active site. 

As a matter of fact, the second cycle increases the conformational rigidity of the molecule sometime increasing the activity and selectivity of the inhibitor. In the case of castanospermine for example, it has been postulated that the increase of inhibitory activity on a-glucosidase with respect to nojirimicin, is due to the orientation of the hydroxyl group at C-6 (referred to glucose) that in the case of castanospermine is restricted (Fig. 45).76... 

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