Abstract
Emeriamine [(R)-3-amino-4-trimethylaminobutyric acid], derived from a novel fungal metabolite "emericedin" [(R)-3-acetylamino-4-trimethylaminobutyric acid], was proved to be a strong and specific inhibitor of carnitine-dependent oxidation of long chain fatty acid (IC50; 3.2 X 10(-6)M) and its main inhibition site was shown to be carnitine palmitoyltransferase I located on the outer-surface of the mitochondrial inner membrane. Emeriamine also showed hypoglycemic and antiketogenic activities in a dose-dependent manner (1 - 10 mg/kg) when administered orally to fasted normal and diabetic animals.
MeSH terms
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Acyltransferases / antagonists & inhibitors*
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Animals
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Betaine / analogs & derivatives*
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Betaine / pharmacology
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Biological Transport, Active
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Blood Glucose / analysis
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Carnitine / metabolism
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Carnitine O-Palmitoyltransferase / antagonists & inhibitors*
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Dose-Response Relationship, Drug
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Fatty Acids / metabolism
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Hypoglycemic Agents / pharmacology*
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Intracellular Membranes / enzymology
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Ketone Bodies / blood
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Male
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Membrane Proteins / antagonists & inhibitors
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Mitochondria, Liver / enzymology
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Oxidation-Reduction
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Rats
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Rats, Inbred Strains
Substances
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Blood Glucose
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Fatty Acids
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Hypoglycemic Agents
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Ketone Bodies
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Membrane Proteins
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Betaine
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emeriamine
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Acyltransferases
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Carnitine O-Palmitoyltransferase
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Carnitine