Emeriamine, an antidiabetic beta-aminobetaine derived from a novel fungal metabolite.
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.
D000217:Acyltransferases / Q000037:antagonists & inhibitors*; D000818:Animals; D001622:Betaine / Q000031:analogs & derivatives* / Q000494:pharmacology; D001693:Biological Transport, Active; D001786:Blood Glucose / Q000032:analysis; D002331:Carnitine / Q000378:metabolism; D002334:Carnitine O-Palmitoyltransferase / Q000037:antagonists & inhibitors*; D004305:Dose-Response Relationship, Drug; D005227:Fatty Acids / Q000378:metabolism; D007004:Hypoglycemic Agents / Q000494:pharmacology*; D007425:Intracellular Membranes / Q000201:enzymology; D007657:Ketone Bodies / Q000097:blood; D008297:Male; D008565:Membrane Proteins / Q000037:antagonists & inhibitors; D008930:Mitochondria, Liver / Q000201:enzymology; D010084:Oxidation-Reduction; D051381:Rats; D011919:Rats, Inbred Strains
D001786:Blood Glucose; D005227:Fatty Acids; D007004:Hypoglycemic Agents; D007657:Ketone Bodies; D008565:Membrane Proteins; D001622:Betaine; C045761:emeriamine; D000217:Acyltransferases; D002334:Carnitine O-Palmitoyltransferase; D002331:Carnitine