Acaterin, a novel inhibitor of acyl-CoA: cholesterol acyltransferase produced by Pseudomonas sp. A92.
Acaterin, a novel inhibitor of acyl-CoA: cholesterol acyltransferase (ACAT), was isolated from a culture broth of Pseudomonas sp. A92 by Diaion HP-20 column chromatography, solvent extraction and reverse phase HPLC. Spectroscopic analyses of the compound yielded 3-(1-hydroxyoctyl)-5-methyl-2(5H)-furanone as the proposed structure. In the presence of oxidized low density lipoprotein, acaterin inhibited the synthesis of cholesteryl ester in macrophage J774 by 50% at a concentration of 45 microM. Acaterin also inhibited ACAT activity in the rat liver microsomes by 50% at a concentration of 120 microM. Kinetic studies suggested that inhibition of ACAT by acaterin was noncompetitive with respect to oleoyl-CoA.
Naganuma
S
S
Department of Applied Biological Science, Tokyo Noko University, Japan.
Sakai
K
K
Hasumi
K
K
Endo
A
A
D000818:Animals; D002460:Cell Line; D002788:Cholesterol Esters / Q000378:metabolism; D005285:Fermentation; D005663:Furans / Q000302:isolation & purification* / Q000494:pharmacology; D066298:In Vitro Techniques; D007700:Kinetics; D008264:Macrophages / Q000378:metabolism; D051379:Mice; D011549:Pseudomonas / Q000145:classification / Q000378:metabolism*; D051381:Rats; D002785:Sterol O-Acyltransferase / Q000037:antagonists & inhibitors*
D002788:Cholesterol Esters; D005663:Furans; C077326:acaterin; D002785:Sterol O-Acyltransferase