title: The effect of local anesthetics on arterial lipid metabolism. Inhibition of sterol esterification in vitro.
abstract: The local anesthetics lidocaine, tetracaine, benzocaine and dibucaine were found to inhibit sterol esterification by acylCoA:cholesterol acyltransferase (ACAT, EC 2.3.1.26) in the microsomal fraction isolated from rabbit aortas. In arterial microsomes, the incorporation of [14C]oleoylCoA into [14C]steryl esters was inhibited in a dose-dependent way by the anesthetics over the concentration range 0.25-5.0 mM. The potency of inhibition was dibucaine greater than benzocaine greater than tetracaine greater than lidocaine greater than procaine with inhibition of about 85% occurring with 0.25 mM dibucaine. Sterol esterification to [14C]oleic acid was also inhibited by the anesthetics in intact aortic tissue from the rabbit, dog, and rat. A detailed study of the effects of 5 mM lidocaine on lipid biosynthesis in the rabbit aorta in vitro revealed that lidocaine not only inhibited sterol esterification to [14C]oleate but stimulated [14C]oleate incorporation into glycerides.
mesh_terms: D000777:Anesthetics; D000818:Animals; D001011:Aorta / Q000378:metabolism*; D001566:Benzocaine; D003992:Dibucaine; D004951:Esterification; D008012:Lidocaine; D050356:Lipid Metabolism; D008297:Male; D009829:Oleic Acids / Q000378:metabolism; D011343:Procaine; D011817:Rabbits; D013261:Sterols / Q000378:metabolism*; D013748:Tetracaine
chemical_list: D000777:Anesthetics; D009829:Oleic Acids; D013261:Sterols; D013748:Tetracaine; D011343:Procaine; D008012:Lidocaine; D003992:Dibucaine; D001566:Benzocaine