Lecithin-cholesterol acyltransferase: inhibition by local anesthetics in plasma from man and experimental animals in vitro.

Lecithin-cholesterol acyltransferase (LCAT, EC 2.3.1.43) was assayed in vitro in plasma from normal man, rat, rabbit and dog by following the formation of 14C-cholesteryl esters subsequent to labeling the plasma with 14C-cholesterol in vitro. In all species examined, various local anesthetics were found to inhibit LCAT when studied over the concentration range of 1 to 5 mM. The order of inhibition was dibucaine>benzocaine>tetracaine>lidocaine>procaine. Since LCAT activity represents the combined effect of a deacylation step and an esterification step, inhibition of LCAT by local anesthetics could theoretically involve either or both steps.