Abstract
The natural product mangiferin (compound 7) has been identified as a potential glucokinase activator by structure-based virtual ligand screening. It was proved by enzyme activation experiment and cell-based assays in vitro, with potency in micromolar range. Meanwhile, this compound showed good antihyperglycemic activity in db/db mice without obvious side effects such as excessive hypoglycaemia.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Blood Glucose / metabolism
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Body Weight / drug effects
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Diabetes Mellitus, Experimental / drug therapy
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Diabetes Mellitus, Experimental / pathology
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Drug Evaluation, Preclinical*
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Enzyme Activation / drug effects
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Enzyme Activators / chemistry*
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Enzyme Activators / pharmacology*
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Enzyme Activators / therapeutic use
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Glucokinase / chemistry
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Glucokinase / metabolism*
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Glucose / metabolism
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Glucose Tolerance Test
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Hep G2 Cells
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Humans
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Insulin / blood
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Islets of Langerhans / drug effects
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Islets of Langerhans / pathology
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Ligands
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Male
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Mice
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Molecular Conformation
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Molecular Docking Simulation
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Myoblasts / drug effects
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Myoblasts / metabolism
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Structure-Activity Relationship
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User-Computer Interface*
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Xanthones / chemistry*
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Xanthones / pharmacology*
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Xanthones / therapeutic use
Substances
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Blood Glucose
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Enzyme Activators
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Insulin
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Ligands
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Xanthones
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mangiferin
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Glucokinase
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Glucose