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?-Glucosidase Inhibitors from Vauquelinia corymbosa.


ABSTRACT: The ?-glucosidase inhibitory activity of an aqueous extract and compounds from the aerial parts of V. corymbosa was demonstrated with yeast and rat small intestinal ?-glucosidases. The aqueous extract inhibited yeast ?-glucosidase with a half maximal inhibitory concentration (IC50) of 28.6 ?g/mL. Bioassay-guided fractionation of the extract led to the isolation of several compounds, including one cyanogenic glycoside [prunasin (1)], five flavonoids [(-)-epi-catechin (2), hyperoside (3), isoquercetin (4), quercitrin (5) and quercetin-3-O-(6''-benzoyl)-?-galactoside (6)] and two simple aromatic compounds [picein (7) and methylarbutin (8)]. The most active compound was 6 with IC50 values of 30 ?M in the case of yeast ?-glucosidase, and 437 ?M in the case of the mammalian enzyme. According to the kinetic analyses performed with rat and yeast enzymes, this compound behaved as mixed-type inhibitor; the calculated inhibition constants (Ki) were 212 and 50 ?M, respectively. Molecular docking analyses with yeast and mammalian ?-glucosidases revealed that compound 6 bind differently to these enzymes. Altogether, the results of this work suggest that preparations of V. corymbosa might delay glucose absorption in vivo.

SUBMITTER: Flores-Bocanegra L 

PROVIDER: S-EPMC6332183 | biostudies-literature | 2015 Aug

REPOSITORIES: biostudies-literature

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α-Glucosidase Inhibitors from Vauquelinia corymbosa.

Flores-Bocanegra Laura L   Pérez-Vásquez Araceli A   Torres-Piedra Mariana M   Bye Robert R   Linares Edelmira E   Mata Rachel R  

Molecules (Basel, Switzerland) 20150821 8


The α-glucosidase inhibitory activity of an aqueous extract and compounds from the aerial parts of V. corymbosa was demonstrated with yeast and rat small intestinal α-glucosidases. The aqueous extract inhibited yeast α-glucosidase with a half maximal inhibitory concentration (IC50) of 28.6 μg/mL. Bioassay-guided fractionation of the extract led to the isolation of several compounds, including one cyanogenic glycoside [prunasin (1)], five flavonoids [(-)-epi-catechin (2), hyperoside (3), isoquerc  ...[more]

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