Antiketogenic and hypoglycemic effects of aminocarnitine and acylaminocarnitines

Journal Article · Wed Jan 01 04:00:00 EST 1986 · Proc. Natl. Acad. Sci. U.S.A.; (United States)

DOI:https://doi.org/10.1073/pnas.83.2.290· OSTI ID:6470155

Jenkins, D L; Griffith, O W

DL-Aminocarnitine (DL-3-amino-4-trimethyl-aminobutyrate) is a potent, noncovalent inhibitor of carnitine palmitoyltransferase (palmitoyl-CoA:L-carinite O-palmitoyltransferase, EC 2.3.1.21). Here the authors show that decanoyl-DL-aminocarnitine and palmitoyl-DL-aminocarnitine inhibit carnitine palmitoyltransferase in vitro about 7-fold and 100-fold more effectively than does aminocarnitine. Aminocarnitine and its decanoyl and palmitoyl derivatives are active in vivo following oral or parenteral administration and, at doses of 0.3 mmol/kg or less, inhibit the oxidation of (/sup 14/C)palmitate to /sup 14/CO/sup 2/ by 45-70% in mice. Larger doses do not significantly increase the extent of inhibition, a finding suggesting that substantial carnitine palmitoyltransferase-independent long-chain fatty acid oxidation may occur in vivo. Small doses of aminocarnitine and palmitoylaminocarnitine prevent the development of ketoacidemia in fasted, normal mice and reverse the ketoacidemia observed in diabetic mice. Aminocarnitine has a strong hypoglycemic effect in fasted diabetic mice; a single dose (0.3 mmol/kg) normalizes plasma glucose levels within 4-8 hr and remains effective for at least 12 hr.

• Research Organization: Cornell Univ. Medical College, New York, NY
• OSTI ID: 6470155
• Journal Information: Proc. Natl. Acad. Sci. U.S.A.; (United States), Journal Name: Proc. Natl. Acad. Sci. U.S.A.; (United States) Vol. 83:2; ISSN PNASA
• Country of Publication: United States
• Language: English

Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ACYLATION
AMINO ACIDS
ANIMALS
BIOLOGICAL EFFECTS
CARBON 14 COMPOUNDS
CARBON COMPOUNDS
CARBON DIOXIDE
CARBON OXIDES
CARBOXYLIC ACIDS
CARNITINE
CHALCOGENIDES
CHEMICAL REACTIONS
ENZYME INHIBITORS
ENZYMES
FASTING
HEXADECANOIC ACID
HYDROXY ACIDS
LABELLED COMPOUNDS
MAMMALS
MICE
MONOCARBOXYLIC ACIDS
ORGANIC ACIDS
ORGANIC COMPOUNDS
OXIDATION
OXIDES
OXYGEN COMPOUNDS
RODENTS
TRANSFERASES
VERTEBRATES
VITAMIN B GROUP
VITAMINS