We have isolated two novel a-glucosidase inhibitors, O-[4-deoxy-4-(2,3-epoxy-3-hydroxymethyl-4,5,6-trihydroxycyclohexane-1-yl-amino)-alpha-D-glucopyranosyl]-(1-->4)-O-alpha-D-glucopyranosyl-(1-->4)-alpha-D-glucopyranose (named CKD-711) and its hexameric analog CKD-711a, from the fermentation broth of Streptomyces sp. CK-4416. HRFAB-MS and NMR analyses reveal that molecular formulae of CKD-711 a...

Previous studies of alpha-glucosidase inhibitors derived from thalidomide revealed that 4,5,6,7-tetrachloro-N-alkylphthalimide derivatives are superior lead compounds. Structure-activity relationship studies indicated that a hydrophobic group at the N(2) position is mandatory for potent activity. Accordingly, we have designed and synthesized some 4,5,6,7-tetrachloro-N-cycloalkylphthalimide and ...

Intestinal adaptation (small intestinal weight and length, weight of the caecum and of the residual colon) to feeding different doses (0-5-50-500 mg/kg bw) of the absorbable, competitive alpha-glucosidase inhibitors BAY m 1099 and BAY o 1248 for three, seven, or 28 days was studied in rats. With the highest dose of either inhibitor, a significant and time dependent growth of the caecum was obse...

The alpha-glucosidase inhibitors acarbose and miglitol have been successfully used to control postprandial hyperglycaemia in diabetics. They probably work by slowing carbohydrate digestion and absorption, but their effect on mouth to caecum transit time has not been studied. The effect acarbose (100 mg), miglitol (100 mg), and placebo on mouth to caecum transit time (380 kcal breakfast with 20 ...

BACKGROUND Pleiotropic effects on cardiovascular protection have been suggested in several oral antidiabetic drugs (OAD). The impacts of OADs on aortic aneurysm (AA) growth have been found in animal studies, but the evidence of their beneficial effects for AA protection in human are lacking. We investigated the relationship between OAD therapy and the risk of developing AA. METHODS We conduct...

Background: Diabetes mellitus is a chronic disease. Decreasing postprandial hyperglycemia by retarding glucose absorption through inhibiting carbohydrates digesting enzymes (α-amylase and α-glucosidase) is one of many approaches used for the management of this disease. This study was aimed at evaluating the normoglycaemic potential of Helianthus annuus leaf. Methods: The effect o...

Alpha-glucosidase inhibitors currently form an important basis for developing novel drugs for diabetes treatment. In our preliminary tests, the ethyl acetate fraction of Phlomis tuberosa extracts showed significant α-glucosidase inhibitory activity (IC₅₀ = 100 μg/mL). In the present study, a combined method using Sepbox chromatography and thin-layer chromatography (TLC) bioautography was develo...

background: the mechanism of hypoglycemic and hypolipidemic activities of pyrus biossieriana buhse leaf extract (pbble) and its phytochemical component arbutin, have not been well determined. the present study was performed to understand the hypoglycemic activity mechanisms of pbble and arbutin more clearly.methods: in vitro enzymatic carbohydrate digestion with pbble and arbutin was assessed u...

bilberry [vaccinium myrtillus linn. (ericaceae)] fruit (vmf) has been traditionally used for treatment of bladder stones, biliary disorders, scurvy, coughs, and lung tuberculosis. vmf may have some pharmaceutical properties owing to these uses, but in vivo and in vitro studies are limited for clarification of medicinal activity and its antidiabetic and antioxidant properties are not investigate...