Abstract
A novel α-glucosidase inhibitor, vomifoliol 9-O-α-arabinofuranosyl (1→6)-β-D-glucopyranoside, was isolated for the first time from leaves of Diospyros Kaki and its bioactivity analyzed. This inhibitor exhibited strong anti-α-glucosidase activity with an IC50 value of 170.62nM and stimulated a dose-dependent increase in the uptake of a fluorescent d-glucose analog, 2-[N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino]-2-deoxy-D-glucose (2-NBDG), in HepG2 cells at a rate higher than that of insulin controls. It was also found to be associated with adipocyte differentiation and moderate increases in 2-NBDG uptake by 3T3-L1 cells. These findings suggest that vomifoliol 9-O-α-arabinofuranosyl (1→6)-β-D-glucopyranoside could augment peripheral glucose as an insulin-sensitizing agent against Type 2 diabetes mellitus.
Crown Copyright © 2011. Published by Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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3T3-L1 Cells
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4-Chloro-7-nitrobenzofurazan / analogs & derivatives
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4-Chloro-7-nitrobenzofurazan / metabolism
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Animals
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Butanols / chemistry
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Butanols / pharmacology*
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Cell Differentiation / drug effects*
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Cyclohexanols / chemistry
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Cyclohexanols / isolation & purification
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Cyclohexanols / pharmacology*
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Cyclohexanones / chemistry
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Cyclohexanones / pharmacology*
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Deoxyglucose / analogs & derivatives
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Deoxyglucose / metabolism
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Diabetes Mellitus, Type 2 / metabolism
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Diabetes Mellitus, Type 2 / pathology
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Diospyros / metabolism*
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Disaccharides / chemistry
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Disaccharides / isolation & purification
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Disaccharides / pharmacology*
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Dose-Response Relationship, Drug
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / isolation & purification
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Enzyme Inhibitors / pharmacology*
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Glycoside Hydrolase Inhibitors*
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Hep G2 Cells
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Humans
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Hypoglycemic Agents / chemistry
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Hypoglycemic Agents / isolation & purification
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Hypoglycemic Agents / pharmacology*
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Mice
Substances
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Butanols
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Cyclohexanols
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Cyclohexanones
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Disaccharides
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Enzyme Inhibitors
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Glycoside Hydrolase Inhibitors
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Hypoglycemic Agents
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vomifoliol 9-O-arabinofuranosyl-(1-6)-glucopyranoside
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Deoxyglucose
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4-Chloro-7-nitrobenzofurazan
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2-(N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino)-2-deoxyglucose
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vomifoliol