A glucosidase inhibitors

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. 

The first member of this class, acarbose, was introduced in the early 1990s. a-Glucosidase inhibitors slow the intestinal process of carbohydrate digestion by competitive inhibition of the activity of a-glucosidase enzymes located in the brush border of the enterocytes... 

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. 

The a-glucosidase inhibitors, acarbose (Precose) and miglitol (Glyset), lower blood sugar by delaying die digestion of carbohydrates and absorption of carbohydrates in the intestine. 

The a-glucosidase inhibitors are contraindicated in patients with a hypersensitivity to the drug, diabetic ketoacidosis, cirrhosis, inflammatory bowel disease, colonic ulceration, partial intestinal obstruction or predisposition to intestinal obstruction, or chronic intestinal diseases. Acarbose and miglitol are used cautiously in patients with renal impairment or pre-existing gastrointestinal (GI) problems such as irritable... 

Acarbose is an intestinal a-glucosidase inhibitor that delays digestion and absorption of starch and sucrose. It is used in diabetes mellitus and is contraindicated in inflammatory bowel disease. 

Takada K, Uehara T, Nakao Y, Matsunaga S, van Soest WM, Fusetani N. (2004) Schulzeines A-C, new a-glucosidase inhibitors from the marine Sponge Penares schulzei. J Am Chem Soc 126 187-193. 

Yoshikawa M, Shimada H, Nishida N, Li Y, Toguchida I, Yamahara J, Matsuda H. (1998) Antidiabetic principles of natural medicines. II. Aldose reductase and a-glucosidase inhibitors from Brazilian natural medicine, the leaves of Myrcia multiflora DC. (Myrtacae) Structures of myrciacitrins I and II and myrciaphenones A and B. Chem Pharm Bull 46 113-119. 

Nishioka T, Kawabata J, Aoyama Y. (1998) Baicalein, an a-glucosidase inhibitor from Scutellaria baicalensis. J Nat Prod 61 1413-1415. 

Toda M, Kawabata J, Kasai T. (2000) a-Glucosidase inhibitors from Clove (Syzgium aromaticum). Biosci Biotechnol Biochem 64 294-298. 

Ozaki S, Oe H, Kitamura S. (2008) a-Glucosidase inhibitor from Kothala-himbutu (Salacia reticulata Wight). J Nat Prod 71 981-984. 

Oe H, Ozaki S. (2008) Hypoglycemic effect of 13-membered ring thiocy-clitol, a novel a-glucosidase inhibitor from Kothala-himbutu Salacia reticulata). Biosci Biotechnol Biochem 72 1962-1964. 

Acarbose (an a-glucosidase inhibitor) delays intestinal formation of glucose from disaccharides. 

Y. Nakao,T. Maki, S. Matsunaga, R. W. M. van Soest, and N. Fusetani, Penarolide sulfates A t andA2, new a-glucosidase inhibitors from a marine sponge Penares sp, Tetrahedron, 56 (2000) 8977-8987. 

K. H. Park, Sulfonamide chalcone as a new class of a-glucosidase inhibitors, Bioorg. Med. Chem. Lett., 15 (2005) 5514-5516. 

---