Alpha-amylase inhibitors: the montbretins and uses thereof

C - Chemistry – Metallurgy – 07 – H

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C07H 15/26 (2006.01) A23G 4/12 (2006.01) A23L 1/30 (2006.01) A23L 2/52 (2006.01) A61K 31/704 (2006.01) A61K 31/7042 (2006.01)

Patent

CA 2738834

Particular naturally occurring glycosylated acyl-flavonols, e.g. montbretm A (of the formula below wherein R1, R2, R3, R5, R5', and R7 is OH each, X is .beta.-D-glucopyranosyl), are now shown to be effective mammalian .alpha.-amylase inhibitors Such compounds can be obtained from plants of the genus Crocosmia The compounds and their analogs of the formula below are useful in controlling starch digestion such as for management of glycermia in pre- diabetic or diabetic subjects, for management of obesity or for inhibiting oral caries or plaque formation R1, R2, R3, R5, R5' and R7 are independently H, OH or OR, wherein R is C1-C6 alkyl, X is H, OH, or glucopyranosyl moiety each

La présente invention concerne des acyles-flavonols glycosylés naturels particuliers, par ex. une montbrétine A (présentant la formule ci-dessous dans laquelle R1, R2, R3, R5, R5' et R7 représentent chacun OH, X représente ß-D-glucopyranosyle), qui constituent des inhibiteurs efficaces de l'a-amylase de mammifères. De tels composés peuvent être obtenus à partir de plantes du genreCrocosmia. Les composés et leurs analogues présentant la formule ci-dessous sont utilisés pour réguler la digestion de l'amidon, par exemple pour maîtriser la glycémie chez des sujets prédiabétiques ou diabétiques, pour maîtriser une obésité ou pour inhiber la formation de caries ou de plaque dans la bouche. R1, R2, R3, R5, R5' et R7 représentent indépendamment H, OH ou OR, avec R représentant alkyle C1-C6, X représente H, OH ou un groupe glucopyranosyle.

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